PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
34652582-11	2022	These effects were partially ameliorated by inhibiting hypoxia-inducible factor 1alpha (HIF-1alpha) degradation via roxadustat administration in hypoxia-stimulated cardiomyocytes.	roxadustat	116-126	hypoxia inducible factor 1, alpha subunit	Mus musculus	55-86
27094610-1	2016	BACKGROUND AND OBJECTIVES: Roxadustat (FG-4592), an oral hypoxia-inducible factor prolyl hydroxylase inhibitor that stimulates erythropoiesis, regulates iron metabolism, and reduces hepcidin, was evaluated in this phase 2b study for safety, efficacy, optimal dose, and dose frequency in patients with nondialysis CKD.	roxadustat	27-37	hepcidin antimicrobial peptide	Homo sapiens	182-190
27094610-15	2016	CONCLUSIONS: In patients with nondialysis CKD who were anemic, various starting dose regimens of roxadustat were well tolerated and achieved anemia correction with reduced serum hepcidin levels.	roxadustat	97-107	hepcidin antimicrobial peptide	Homo sapiens	178-186
26846333-1	2016	BACKGROUND: Roxadustat (FG-4592) is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.	roxadustat	12-22	erythropoietin	Homo sapiens	157-171
26846333-1	2016	BACKGROUND: Roxadustat (FG-4592) is an oral hypoxia-inducible factor prolyl-hydroxylase inhibitor that promotes erythropoiesis through increasing endogenous erythropoietin, improving iron regulation, and reducing hepcidin.	roxadustat	12-22	hepcidin antimicrobial peptide	Homo sapiens	213-221
26846333-11	2016	Hepcidin level reduction was greater at roxadustat 2.0mg/kg versus epoetin alfa (P<0.05).	roxadustat	40-50	hepcidin antimicrobial peptide	Homo sapiens	0-8
26494833-11	2016	In summary, roxadustat was well tolerated and corrected anemia in incident HD and PD patients, regardless of baseline iron repletion status or C-reactive protein level and with oral or IV iron supplementation; it also reduced serum hepcidin levels.	roxadustat	12-22	C-reactive protein	Homo sapiens	143-161
26494833-11	2016	In summary, roxadustat was well tolerated and corrected anemia in incident HD and PD patients, regardless of baseline iron repletion status or C-reactive protein level and with oral or IV iron supplementation; it also reduced serum hepcidin levels.	roxadustat	12-22	hepcidin antimicrobial peptide	Homo sapiens	232-240
26238121-12	2015	CONCLUSIONS: Roxadustat transiently and moderately increased endogenous erythropoietin and reduced hepcidin.	roxadustat	13-23	erythropoietin	Homo sapiens	72-86
26238121-12	2015	CONCLUSIONS: Roxadustat transiently and moderately increased endogenous erythropoietin and reduced hepcidin.	roxadustat	13-23	hepcidin antimicrobial peptide	Homo sapiens	99-107
34167878-10	2022	Roxadustat decreased hepcidin levels and increased total iron-binding capacity.	roxadustat	0-10	hepcidin antimicrobial peptide	Homo sapiens	21-29
34550341-5	2021	Methods: In a pilot study, we tested the required dose of roxadustat to stabilize liver HIF1alpha.	roxadustat	58-68	hypoxia inducible factor 1 subunit alpha	Homo sapiens	88-97
34550341-10	2021	Results: Roxadustat effectively increased early HIF1alpha transactivity.	roxadustat	9-19	hypoxia inducible factor 1 subunit alpha	Homo sapiens	48-57
34569654-3	2021	Treatment with Roxadustat led to significantly accelerated compensatory lung growth (CLG) through downregulation of pigment epithelium-derived factor (PEDF), an anti-angiogenic factor, rather than upregulation of vascular endothelial growth factor (VEGF).	roxadustat	15-25	serpin family F member 1	Homo sapiens	116-149
34569654-3	2021	Treatment with Roxadustat led to significantly accelerated compensatory lung growth (CLG) through downregulation of pigment epithelium-derived factor (PEDF), an anti-angiogenic factor, rather than upregulation of vascular endothelial growth factor (VEGF).	roxadustat	15-25	serpin family F member 1	Homo sapiens	151-155
34569654-3	2021	Treatment with Roxadustat led to significantly accelerated compensatory lung growth (CLG) through downregulation of pigment epithelium-derived factor (PEDF), an anti-angiogenic factor, rather than upregulation of vascular endothelial growth factor (VEGF).	roxadustat	15-25	vascular endothelial growth factor A	Homo sapiens	213-247
34569654-3	2021	Treatment with Roxadustat led to significantly accelerated compensatory lung growth (CLG) through downregulation of pigment epithelium-derived factor (PEDF), an anti-angiogenic factor, rather than upregulation of vascular endothelial growth factor (VEGF).	roxadustat	15-25	vascular endothelial growth factor A	Homo sapiens	249-253
34569654-8	2021	Human microvascular endothelial lung cells (HMVEC-L) and human pulmonary alveolar epithelial cells (HPAEC) similarly demonstrated decreased PEDF expression with Roxadustat administration.	roxadustat	161-171	serpin family F member 1	Homo sapiens	140-144
34569654-9	2021	Additionally, downregulation of PEDF in Roxadustat-treated HMVEC-L and HPAEC, a previously unreported finding, speaks to the potential translatability of Roxadustat from small animal studies.	roxadustat	40-50	serpin family F member 1	Homo sapiens	32-36
26947173-12	2016	Roxadustat increased the geometric mean (GM) prothrombin (PT) and international normalized ratio (INR) AUC from time zero to last measurable sample (AUCPT,last and AUCINR,last) by 24.4%.	roxadustat	0-10	coagulation factor II, thrombin	Homo sapiens	45-56
34500449-0	2022	Roxadustat Improves Erythropoietin Antibody-Mediated Pure Red Cell Aplasia in a Patient with Hemodialysis.	roxadustat	0-10	erythropoietin	Homo sapiens	20-34
34500449-7	2022	After 6 months of roxadustat treatment, the anti-EPO antibody was disappeared, and hemoglobin recovered normal range.	roxadustat	18-28	erythropoietin	Homo sapiens	49-52
34500449-8	2022	The results suggest that roxadustat can be used to treat patients with anti-EPO antibody-mediated PRCA without immunosuppressive therapy.	roxadustat	25-35	erythropoietin	Homo sapiens	76-79
34724959-10	2021	However, TGF-beta1 repressed HIF2alpha-encoding Epas1 promptly through activating activin receptor-like kinase-5 (ALK5), thereby decreasing Epo induction by hypoxia and prolyl hydroxylase domain inhibitor roxadustat.	roxadustat	205-215	transforming growth factor, beta 1	Mus musculus	9-18
34724959-10	2021	However, TGF-beta1 repressed HIF2alpha-encoding Epas1 promptly through activating activin receptor-like kinase-5 (ALK5), thereby decreasing Epo induction by hypoxia and prolyl hydroxylase domain inhibitor roxadustat.	roxadustat	205-215	endothelial PAS domain protein 1	Mus musculus	29-38
34724959-10	2021	However, TGF-beta1 repressed HIF2alpha-encoding Epas1 promptly through activating activin receptor-like kinase-5 (ALK5), thereby decreasing Epo induction by hypoxia and prolyl hydroxylase domain inhibitor roxadustat.	roxadustat	205-215	endothelial PAS domain protein 1	Mus musculus	48-53
34724959-10	2021	However, TGF-beta1 repressed HIF2alpha-encoding Epas1 promptly through activating activin receptor-like kinase-5 (ALK5), thereby decreasing Epo induction by hypoxia and prolyl hydroxylase domain inhibitor roxadustat.	roxadustat	205-215	transforming growth factor, beta receptor I	Mus musculus	82-112
34724959-10	2021	However, TGF-beta1 repressed HIF2alpha-encoding Epas1 promptly through activating activin receptor-like kinase-5 (ALK5), thereby decreasing Epo induction by hypoxia and prolyl hydroxylase domain inhibitor roxadustat.	roxadustat	205-215	erythropoietin	Mus musculus	140-143
34756787-1	2021	OBJECTIVES: The present study aimed to explore the efficacy and safety of roxadustat in patients with renal anemia and erythropoietin (EPO) hyporesponsive who are receiving continuous ambulatory peritoneal dialysis (CAPD).	roxadustat	74-84	erythropoietin	Homo sapiens	119-133
34756787-1	2021	OBJECTIVES: The present study aimed to explore the efficacy and safety of roxadustat in patients with renal anemia and erythropoietin (EPO) hyporesponsive who are receiving continuous ambulatory peritoneal dialysis (CAPD).	roxadustat	74-84	erythropoietin	Homo sapiens	135-138
34756787-18	2021	CONCLUSIONS: In patients with EPO hyporesponsiveness on CAPD, roxadustat can efficiently and safely improve anemia and nutritional status without promoting inflammation.	roxadustat	62-72	erythropoietin	Homo sapiens	30-33
34652582-11	2022	These effects were partially ameliorated by inhibiting hypoxia-inducible factor 1alpha (HIF-1alpha) degradation via roxadustat administration in hypoxia-stimulated cardiomyocytes.	roxadustat	116-126	hypoxia inducible factor 1, alpha subunit	Mus musculus	88-98
34652582-15	2022	Administration of roxadustat can partially reverse these harmful effects by stabilizing HIF-1alpha and inducing a metabolic shift toward glycolysis for energy production.	roxadustat	18-28	hypoxia inducible factor 1, alpha subunit	Mus musculus	88-98
34403364-0	2021	Roxadustat (FG-4592) prevents Ang II hypertension by targeting angiotensin receptors and eNOS.	roxadustat	0-10	angiotensinogen (serpin peptidase inhibitor, clade A, member 8)	Mus musculus	30-36
34403364-0	2021	Roxadustat (FG-4592) prevents Ang II hypertension by targeting angiotensin receptors and eNOS.	roxadustat	0-10	nitric oxide synthase 3, endothelial cell	Mus musculus	89-93
34754441-0	2021	Roxadustat in the treatment of a hemodialysis patient with anti-erythropoietin antibody-mediated pure red cell aplasia.	roxadustat	0-10	erythropoietin	Homo sapiens	64-78
34428860-6	2022	The meta-analysis showed that roxadustat increased haemoglobin (Hb) level by 0.91 g/dL (95% confidence interval (CI): 0.47-1.34, P<0.05), transferrin level by 0.50 mg/dL (95% CI: 0.34-0.65, P<0.05), and total iron-binding capacity by 50.64 mug/dL (95% CI: 36.21-65.07, P<0.05) in CKD patients.	roxadustat	30-40	transferrin	Homo sapiens	138-149
34569654-9	2021	Additionally, downregulation of PEDF in Roxadustat-treated HMVEC-L and HPAEC, a previously unreported finding, speaks to the potential translatability of Roxadustat from small animal studies.	roxadustat	154-164	serpin family F member 1	Homo sapiens	32-36
34569654-10	2021	Taken together, these findings further suggest that PEDF downregulation is the primary mechanism by which Roxadustat accelerates CLG.	roxadustat	106-116	serpin family F member 1	Homo sapiens	52-56
34255035-6	2021	The results showed that FG4592, given to mice 3 days after UIR, markedly alleviated kidney fibrosis and enhanced renal vascular regeneration, possibly via activating the HIF-1alpha/vascular endothelial growth factor A (VEGFA)/VEGF receptor 1 (VEGFR1) signaling pathway and driving the expression of the endogenous antioxidant superoxide dismutase 2 (SOD2).	roxadustat	24-30	vascular endothelial growth factor A	Mus musculus	219-224
34255035-6	2021	The results showed that FG4592, given to mice 3 days after UIR, markedly alleviated kidney fibrosis and enhanced renal vascular regeneration, possibly via activating the HIF-1alpha/vascular endothelial growth factor A (VEGFA)/VEGF receptor 1 (VEGFR1) signaling pathway and driving the expression of the endogenous antioxidant superoxide dismutase 2 (SOD2).	roxadustat	24-30	FMS-like tyrosine kinase 1	Mus musculus	243-249
34255035-6	2021	The results showed that FG4592, given to mice 3 days after UIR, markedly alleviated kidney fibrosis and enhanced renal vascular regeneration, possibly via activating the HIF-1alpha/vascular endothelial growth factor A (VEGFA)/VEGF receptor 1 (VEGFR1) signaling pathway and driving the expression of the endogenous antioxidant superoxide dismutase 2 (SOD2).	roxadustat	24-30	superoxide dismutase 2, mitochondrial	Mus musculus	326-348
34255035-6	2021	The results showed that FG4592, given to mice 3 days after UIR, markedly alleviated kidney fibrosis and enhanced renal vascular regeneration, possibly via activating the HIF-1alpha/vascular endothelial growth factor A (VEGFA)/VEGF receptor 1 (VEGFR1) signaling pathway and driving the expression of the endogenous antioxidant superoxide dismutase 2 (SOD2).	roxadustat	24-30	superoxide dismutase 2, mitochondrial	Mus musculus	350-354
34128578-0	2021	Roxadustat on anti-erythropoietin antibody-related pure red cell aplasia in the patient with end-stage renal disease.	roxadustat	0-10	erythropoietin	Homo sapiens	19-33
34497233-7	2021	Sirolimus and roxadustat may be effective for relapsed/refractory PRCA with renal insufficiency and anti-erythropoietin antibody-mediated PRCA, respectively.	roxadustat	14-24	erythropoietin	Homo sapiens	105-119
35460897-7	2022	RNA-Seq analysis of mRNA expression in rat hepatocytes showed that roxadustat treatment decreased the expression of genes related to inflammation, and genes in the NF-kappaB signaling pathway were induced by IL-1beta.	roxadustat	67-77	interleukin 1 alpha	Rattus norvegicus	208-216
35460897-8	2022	Moreover, roxadustat suppressed IL-1beta-activated signaling pathways in an HIF-dependent manner.	roxadustat	10-20	interleukin 1 alpha	Rattus norvegicus	32-40
35460897-9	2022	GalN/LPS-treated rats were used as in vivo models of hepatic injury, and roxadustat treatment showed a tendency to suppress the death of rats.	roxadustat	73-83	galanin and GMAP prepropeptide	Rattus norvegicus	0-4
34128578-3	2021	Here, we present successful treatment of anti-EPO PRCA with roxadustat, a hypoxia-inducible factor prolyl hydroxylase inhibitor.	roxadustat	60-70	erythropoietin	Homo sapiens	46-49
34128578-11	2021	All in all, this case reveals the potential effect of roxadustat on anti-EPO PRCA.	roxadustat	54-64	erythropoietin	Homo sapiens	73-76
35597989-0	2022	Roxadustat promotes osteoblast differentiation and prevents estrogen deficiency-induced bone loss by stabilizing HIF-1alpha and activating the Wnt/beta-catenin signaling pathway.	roxadustat	0-10	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	113-123
35597989-0	2022	Roxadustat promotes osteoblast differentiation and prevents estrogen deficiency-induced bone loss by stabilizing HIF-1alpha and activating the Wnt/beta-catenin signaling pathway.	roxadustat	0-10	catenin beta 1	Rattus norvegicus	147-159
35597989-9	2022	The effects of roxadustat on the HIF-1alpha and Wnt/beta-catenin pathways were evaluated.	roxadustat	15-25	hypoxia inducible factor 1, alpha subunit	Mus musculus	33-43
35597989-9	2022	The effects of roxadustat on the HIF-1alpha and Wnt/beta-catenin pathways were evaluated.	roxadustat	15-25	catenin (cadherin associated protein), beta 1	Mus musculus	52-64
35597989-15	2022	Roxadustat activated the HIF-1alpha and Wnt/beta-catenin pathways.	roxadustat	0-10	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	25-35
35597989-15	2022	Roxadustat activated the HIF-1alpha and Wnt/beta-catenin pathways.	roxadustat	0-10	catenin beta 1	Rattus norvegicus	44-56
35597989-16	2022	HIF-1alpha knockdown or Wnt/beta-catenin pathway inhibition significantly attenuated roxadustat-promoted osteoblast differentiation.	roxadustat	85-95	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	0-10
35597989-16	2022	HIF-1alpha knockdown or Wnt/beta-catenin pathway inhibition significantly attenuated roxadustat-promoted osteoblast differentiation.	roxadustat	85-95	catenin beta 1	Rattus norvegicus	28-40
35597989-18	2022	Roxadustat upregulated the protein expression levels of the osteogenic markers, HIF-1alpha and beta-catenin in the bone tissue of OVX rats.	roxadustat	0-10	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	80-90
35597989-18	2022	Roxadustat upregulated the protein expression levels of the osteogenic markers, HIF-1alpha and beta-catenin in the bone tissue of OVX rats.	roxadustat	0-10	catenin beta 1	Rattus norvegicus	95-107
35114188-2	2022	Roxadustat is one of the first oral medicines inducing EPO production in patients with renal anemia by activating hypoxia-inducible factors (HIFs), which are activators of EPO gene expression.	roxadustat	0-10	erythropoietin	Homo sapiens	55-58
35304594-0	2022	The hypoxia-inducible factor prolyl hydroxylase inhibitor FG4592 promotes natriuresis through upregulation of COX2 in the renal medulla.	roxadustat	58-64	prostaglandin-endoperoxide synthase 2	Mus musculus	110-114
35304594-7	2022	In addition, FG4592 upregulated the expression of COX2 in the renal medulla.	roxadustat	13-19	prostaglandin-endoperoxide synthase 2	Mus musculus	50-54
35304594-9	2022	In addition, the COX2 inhibitor celecoxib diminished the natriuretic effect of FG4592.	roxadustat	79-85	prostaglandin-endoperoxide synthase 2	Mus musculus	17-21
35559232-5	2022	Methods: We searched CBM, CNKI, VIP, Wanfang Database, PubMed, Cochrane Library, Embase, and Web of Science for randomized controlled trials of roxadustat for the treatment of anemia in CKD patients.	roxadustat	144-154	vasoactive intestinal peptide	Homo sapiens	32-35
35492370-0	2022	Roxadustat Attenuates the Disruption of Epithelial Tight Junction in Caco2 Cells and a Rat Model of CKD Through MicroRNA-223.	roxadustat	0-10	microRNA 223	Rattus norvegicus	112-124
35492370-2	2022	Since the decrease of hypoxia inducible factor-1alpha (HIF-1alpha) is reported to be involved in Hcy-induced cell injury, and the upregulation of microRNA-223 (miR-223) plays a vital protective role in the impairment of IBF in the experimental colitis, we investigated the effect of HIF-1alpha stabilizer roxadustat on the disruption of TJPs induced by Hcy and CKD and the underlying mechanism.	roxadustat	305-315	hypoxia inducible factor 1 subunit alpha	Homo sapiens	22-53
35492370-2	2022	Since the decrease of hypoxia inducible factor-1alpha (HIF-1alpha) is reported to be involved in Hcy-induced cell injury, and the upregulation of microRNA-223 (miR-223) plays a vital protective role in the impairment of IBF in the experimental colitis, we investigated the effect of HIF-1alpha stabilizer roxadustat on the disruption of TJPs induced by Hcy and CKD and the underlying mechanism.	roxadustat	305-315	hypoxia inducible factor 1 subunit alpha	Homo sapiens	55-65
35492370-2	2022	Since the decrease of hypoxia inducible factor-1alpha (HIF-1alpha) is reported to be involved in Hcy-induced cell injury, and the upregulation of microRNA-223 (miR-223) plays a vital protective role in the impairment of IBF in the experimental colitis, we investigated the effect of HIF-1alpha stabilizer roxadustat on the disruption of TJPs induced by Hcy and CKD and the underlying mechanism.	roxadustat	305-315	microRNA 223	Homo sapiens	146-158
35492370-2	2022	Since the decrease of hypoxia inducible factor-1alpha (HIF-1alpha) is reported to be involved in Hcy-induced cell injury, and the upregulation of microRNA-223 (miR-223) plays a vital protective role in the impairment of IBF in the experimental colitis, we investigated the effect of HIF-1alpha stabilizer roxadustat on the disruption of TJPs induced by Hcy and CKD and the underlying mechanism.	roxadustat	305-315	microRNA 223	Homo sapiens	160-167
35492370-8	2022	The reduction of HIF-1alpha and miR-223 was reversed by roxadustat and the decrease of TJPs expression was attenuated in both Caco2 cells induced by Hcy and colon tissue of CKD rats.	roxadustat	56-66	hypoxia inducible factor 1 subunit alpha	Homo sapiens	17-27
35492370-8	2022	The reduction of HIF-1alpha and miR-223 was reversed by roxadustat and the decrease of TJPs expression was attenuated in both Caco2 cells induced by Hcy and colon tissue of CKD rats.	roxadustat	56-66	microRNA 223	Homo sapiens	32-39
35620283-0	2022	Roxadustat, a Hypoxia-Inducible Factor 1alpha Activator, Attenuates Both Long- and Short-Term Alcohol-Induced Alcoholic Liver Disease.	roxadustat	0-10	hypoxia inducible factor 1, alpha subunit	Mus musculus	14-45
35620283-7	2022	Roxadustat-reduced fatty liver was mainly contributed by the reducing sterol-responsive element-binding protein 1c (SREBP1c) pathway, and enhancing beta-oxidation through inducing peroxisome proliferator-activated receptor alpha (PPARalpha) and carnitine palmitoyltransferase 1A (CPT1A) expression.	roxadustat	0-10	sterol regulatory element binding transcription factor 1	Mus musculus	70-114
35620283-7	2022	Roxadustat-reduced fatty liver was mainly contributed by the reducing sterol-responsive element-binding protein 1c (SREBP1c) pathway, and enhancing beta-oxidation through inducing peroxisome proliferator-activated receptor alpha (PPARalpha) and carnitine palmitoyltransferase 1A (CPT1A) expression.	roxadustat	0-10	sterol regulatory element binding transcription factor 1	Mus musculus	116-123
35620283-7	2022	Roxadustat-reduced fatty liver was mainly contributed by the reducing sterol-responsive element-binding protein 1c (SREBP1c) pathway, and enhancing beta-oxidation through inducing peroxisome proliferator-activated receptor alpha (PPARalpha) and carnitine palmitoyltransferase 1A (CPT1A) expression.	roxadustat	0-10	peroxisome proliferator activated receptor alpha	Mus musculus	180-228
35620283-7	2022	Roxadustat-reduced fatty liver was mainly contributed by the reducing sterol-responsive element-binding protein 1c (SREBP1c) pathway, and enhancing beta-oxidation through inducing peroxisome proliferator-activated receptor alpha (PPARalpha) and carnitine palmitoyltransferase 1A (CPT1A) expression.	roxadustat	0-10	peroxisome proliferator activated receptor alpha	Mus musculus	230-239
35620283-7	2022	Roxadustat-reduced fatty liver was mainly contributed by the reducing sterol-responsive element-binding protein 1c (SREBP1c) pathway, and enhancing beta-oxidation through inducing peroxisome proliferator-activated receptor alpha (PPARalpha) and carnitine palmitoyltransferase 1A (CPT1A) expression.	roxadustat	0-10	carnitine palmitoyltransferase 1a, liver	Mus musculus	245-278
35620283-7	2022	Roxadustat-reduced fatty liver was mainly contributed by the reducing sterol-responsive element-binding protein 1c (SREBP1c) pathway, and enhancing beta-oxidation through inducing peroxisome proliferator-activated receptor alpha (PPARalpha) and carnitine palmitoyltransferase 1A (CPT1A) expression.	roxadustat	0-10	carnitine palmitoyltransferase 1a, liver	Mus musculus	280-285
35620283-9	2022	Moreover, roxadustat attenuated alcohol caused ROS generation in the liver of those two mouse models mainly by reducing cytochrome P450 2E1 (CYP2E1) and enhancing superoxidase dismutase 1 (SOD1) expression.	roxadustat	10-20	cytochrome P450, family 2, subfamily e, polypeptide 1	Mus musculus	120-139
35620283-9	2022	Moreover, roxadustat attenuated alcohol caused ROS generation in the liver of those two mouse models mainly by reducing cytochrome P450 2E1 (CYP2E1) and enhancing superoxidase dismutase 1 (SOD1) expression.	roxadustat	10-20	cytochrome P450, family 2, subfamily e, polypeptide 1	Mus musculus	141-147
35620283-9	2022	Moreover, roxadustat attenuated alcohol caused ROS generation in the liver of those two mouse models mainly by reducing cytochrome P450 2E1 (CYP2E1) and enhancing superoxidase dismutase 1 (SOD1) expression.	roxadustat	10-20	superoxide dismutase 1, soluble	Mus musculus	163-187
35620283-9	2022	Moreover, roxadustat attenuated alcohol caused ROS generation in the liver of those two mouse models mainly by reducing cytochrome P450 2E1 (CYP2E1) and enhancing superoxidase dismutase 1 (SOD1) expression.	roxadustat	10-20	superoxide dismutase 1, soluble	Mus musculus	189-193
35620283-10	2022	In vitro, we found roxadustat reduced inflammation and lipid accumulation mainly via HIF-1alpha regulation.	roxadustat	19-29	hypoxia inducible factor 1, alpha subunit	Mus musculus	85-95
35492370-11	2022	Conclusion: These results indicated that roxadustat attenuated the disruption of epithelial TJPs induced by Hcy in Caco2 cells and the damage of colonic epithelium in CKD rats through the upregulation of miR-223 induced by HIF-1alpha.	roxadustat	41-51	microRNA 223	Rattus norvegicus	204-211
35492370-11	2022	Conclusion: These results indicated that roxadustat attenuated the disruption of epithelial TJPs induced by Hcy in Caco2 cells and the damage of colonic epithelium in CKD rats through the upregulation of miR-223 induced by HIF-1alpha.	roxadustat	41-51	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	223-233
35361724-2	2022	Roxadustat, an oral hypoxia-inducible factor prolyl hydroxylase inhibitor, stimulates erythropoiesis by increasing endogenous erythropoietin and iron availability.	roxadustat	0-10	erythropoietin	Homo sapiens	126-140
35114188-2	2022	Roxadustat is one of the first oral medicines inducing EPO production in patients with renal anemia by activating hypoxia-inducible factors (HIFs), which are activators of EPO gene expression.	roxadustat	0-10	erythropoietin	Homo sapiens	172-175
35114188-3	2022	In this study, to develop prodrugs of roxadustat with improved permeability through cell membrane, we investigated the effects of 8 types of esterification on the pharmacokinetics and bioactivity of roxadustat using Hep3B hepatoma cells that HIF-dependently produce EPO.	roxadustat	199-209	erythropoietin	Homo sapiens	266-269
35114188-5	2022	Esterification prolonged the effective duration of roxadustat with respect to EPO gene induction and HIF activation in cells transiently exposed to the compounds.	roxadustat	51-61	erythropoietin	Homo sapiens	78-81
35114188-6	2022	In the kidneys and livers of mice, both of which are unique sites of EPO production, a majority of the methyl-esterified roxadustat was deesterified within 6 hours after drug administration.	roxadustat	121-131	erythropoietin	Mus musculus	69-72
35114188-8	2022	Additionally, we confirmed that methyl-esterified roxadustat activated erythropoiesis in mice by inducing EPO mRNA expression exclusively in renal interstitial cells, which have intrinsic EPO-producing potential.	roxadustat	50-60	erythropoietin	Mus musculus	106-109
35114188-8	2022	Additionally, we confirmed that methyl-esterified roxadustat activated erythropoiesis in mice by inducing EPO mRNA expression exclusively in renal interstitial cells, which have intrinsic EPO-producing potential.	roxadustat	50-60	erythropoietin	Mus musculus	188-191
35280255-7	2021	Specifically, FG-4592 pretreatment inhibited hypoxia inducible factor-1alpha activation on the 7th day after folic acid injection, which ameliorated ultrastructural abnormalities, promoted ATP production, and attenuated excessive reactive oxygen species production both in renal tissue and mitochondria.	roxadustat	14-21	hypoxia inducible factor 1 subunit alpha	Homo sapiens	45-76
35280255-10	2021	In vitro, TNF-alpha-induced HK-2 cells injury could be ameliorated by FG-4592 pretreatment.	roxadustat	70-77	tumor necrosis factor	Homo sapiens	10-19
35164384-0	2022	Effects of Roxadustat on Erythropoietin Production in the Rat Body.	roxadustat	11-21	erythropoietin	Rattus norvegicus	25-39
35203399-0	2022	The HIFalpha-Stabilizing Drug Roxadustat Increases the Number of Renal Epo-Producing Sca-1+ Cells.	roxadustat	30-40	erythropoietin	Mus musculus	71-74
35203399-0	2022	The HIFalpha-Stabilizing Drug Roxadustat Increases the Number of Renal Epo-Producing Sca-1+ Cells.	roxadustat	30-40	ataxin 1	Mus musculus	85-90
35203399-1	2022	Inhibition of the prolyl-4-hydroxylase domain (PHD) enzymes, leading to the stabilization of hypoxia-inducible factor (HIF) alpha as well as to the stimulation of erythropoietin (Epo) synthesis, is the functional mechanism of the new anti-anemia drug roxadustat.	roxadustat	251-261	erythropoietin	Mus musculus	163-177
35203399-1	2022	Inhibition of the prolyl-4-hydroxylase domain (PHD) enzymes, leading to the stabilization of hypoxia-inducible factor (HIF) alpha as well as to the stimulation of erythropoietin (Epo) synthesis, is the functional mechanism of the new anti-anemia drug roxadustat.	roxadustat	251-261	erythropoietin	Mus musculus	179-182
35203399-4	2022	The number of Sca-1+ mesenchymal cells following roxadustat treatment increased exclusively in the kidneys.	roxadustat	49-59	ataxin 1	Mus musculus	14-19
35203399-8	2022	In summary, we have identified a Sca-1+ MSC-like cell population that is involved in renal Epo production and might contribute to the strong anti-anemic effect of the PHD inhibitor roxadustat.	roxadustat	181-191	ataxin 1	Mus musculus	33-38
35203399-8	2022	In summary, we have identified a Sca-1+ MSC-like cell population that is involved in renal Epo production and might contribute to the strong anti-anemic effect of the PHD inhibitor roxadustat.	roxadustat	181-191	erythropoietin	Mus musculus	91-94
35164384-6	2022	Using this method, we examined the effects of the PHD inhibitor, Roxadustat (ROX), and severe hypoxia on Epo production in various tissues in rats.	roxadustat	65-75	erythropoietin	Rattus norvegicus	105-108
35164384-6	2022	Using this method, we examined the effects of the PHD inhibitor, Roxadustat (ROX), and severe hypoxia on Epo production in various tissues in rats.	roxadustat	77-80	erythropoietin	Rattus norvegicus	105-108
34021853-0	2021	Roxadustat for dialysis patients with erythropoietin hypo-responsiveness: a single-center, prospective investigation.	roxadustat	0-10	erythropoietin	Homo sapiens	38-52
35010112-8	2022	This method also enabled two clinically used inhibitors-vadadustat and roxadustat-to be loaded into liposomes with a high encapsulation efficiency, indicating its generality to load other heterocyclic glycinamide PHD2 inhibitors.	roxadustat	71-81	egl-9 family hypoxia inducible factor 1	Homo sapiens	213-217
33475252-10	2021	Phase 3 trials of small molecule inhibitors of the PHD enzymes (hypoxia inducible factor-prolyl hydroxylase inhibitors [HIF-PHIs]), such as Roxadustat, have shown improved iron metabolism and increased circulating Epo levels in a titratable manner, avoiding the supraphysiologic increases that often accompany intravenous EPO therapy.	roxadustat	140-150	erythropoietin	Homo sapiens	214-217
33475252-10	2021	Phase 3 trials of small molecule inhibitors of the PHD enzymes (hypoxia inducible factor-prolyl hydroxylase inhibitors [HIF-PHIs]), such as Roxadustat, have shown improved iron metabolism and increased circulating Epo levels in a titratable manner, avoiding the supraphysiologic increases that often accompany intravenous EPO therapy.	roxadustat	140-150	erythropoietin	Homo sapiens	322-325
34653291-6	2022	Furthermore, these results suggest that pretreatment with FG-4592 significantly reduced the tubular cells apoptosis (decreased TUNEL-positive cells, Bax, caspase12 levels), attenuated mitochondrial damage (increased ATPbeta, PPARgamma, mitochondrial DNA copy number, and decreased cytoplasmic cytochrome C), and alleviated DNA damage after IRI.	roxadustat	58-65	BCL2-associated X protein	Mus musculus	149-152
34653291-6	2022	Furthermore, these results suggest that pretreatment with FG-4592 significantly reduced the tubular cells apoptosis (decreased TUNEL-positive cells, Bax, caspase12 levels), attenuated mitochondrial damage (increased ATPbeta, PPARgamma, mitochondrial DNA copy number, and decreased cytoplasmic cytochrome C), and alleviated DNA damage after IRI.	roxadustat	58-65	caspase 12	Mus musculus	154-163
34653291-6	2022	Furthermore, these results suggest that pretreatment with FG-4592 significantly reduced the tubular cells apoptosis (decreased TUNEL-positive cells, Bax, caspase12 levels), attenuated mitochondrial damage (increased ATPbeta, PPARgamma, mitochondrial DNA copy number, and decreased cytoplasmic cytochrome C), and alleviated DNA damage after IRI.	roxadustat	58-65	peroxisome proliferator activated receptor gamma	Mus musculus	225-234
34021853-2	2021	Roxadustat reversibly binds and inhibits hypoxia-inducible factor-prolyl hydroxylase (HIF-PHD), resulting in increased endogenous EPO which stimulates erythropoiesis, theoretically has an advantage over exogenous EPO in anti-anemia therapy.	roxadustat	0-10	erythropoietin	Homo sapiens	130-133
34021853-2	2021	Roxadustat reversibly binds and inhibits hypoxia-inducible factor-prolyl hydroxylase (HIF-PHD), resulting in increased endogenous EPO which stimulates erythropoiesis, theoretically has an advantage over exogenous EPO in anti-anemia therapy.	roxadustat	0-10	erythropoietin	Homo sapiens	213-216
34021853-14	2021	Significant anti-anemia effects could be achieved in most patients with erythropoietin hypo-responsiveness after treatment with roxadustat, accompanied by relatively mild and rare adverse reactions.	roxadustat	128-138	erythropoietin	Homo sapiens	72-86
33792658-8	2021	EC exposure to FG-4592, a prolyl hydroxylase inhibitor that increases hypoxia-inducible factor expression (HIFs), increased nmMYLK promoter activity, confirmed by HIF1alpha/HIF2alpha silencing.	roxadustat	15-22	hypoxia inducible factor 1, alpha subunit	Mus musculus	163-172
33389461-9	2021	In addition, our result showed that a significant reduction in hepcidin level (- 31.96 ng/mL, 95% CI [- 35.05 ng/mL, - 28.87 ng/mL], p < 0.00001), ferritin (- 44.82 ng/mL, 95% CI [- 64.42 ng/mL, - 25.23 ng/mL], p < 0.00001) was associated with roxadustat.	roxadustat	244-254	hepcidin antimicrobial peptide	Homo sapiens	63-71
33913468-18	2022	Broad spectrum-PHD inhibitors, e.g. Roxadustat, are currently being prescribed to chronic kidney disease patients, who are already at risk for cardiovascular disease.	roxadustat	36-46	phosducin	Mus musculus	15-18
33852916-4	2021	We demonstrate that hypoxia and the HIF prolyl hydroxylase inhibitor Roxadustat reduce ACE2 expression and inhibit SARS-CoV-2 entry and replication in lung epithelial cells via an HIF-1alpha-dependent pathway.	roxadustat	69-79	angiotensin converting enzyme 2	Homo sapiens	87-91
33852916-4	2021	We demonstrate that hypoxia and the HIF prolyl hydroxylase inhibitor Roxadustat reduce ACE2 expression and inhibit SARS-CoV-2 entry and replication in lung epithelial cells via an HIF-1alpha-dependent pathway.	roxadustat	69-79	hypoxia inducible factor 1 subunit alpha	Homo sapiens	180-190
33792658-8	2021	EC exposure to FG-4592, a prolyl hydroxylase inhibitor that increases hypoxia-inducible factor expression (HIFs), increased nmMYLK promoter activity, confirmed by HIF1alpha/HIF2alpha silencing.	roxadustat	15-22	endothelial PAS domain protein 1	Mus musculus	173-182
33596451-7	2021	A monocarboxylate transporter-4 (MCT4) inhibitor, syrosingopine, inhibited lactate release from roxadustat-treated cells and reduced the elution of Ni ions by the cells at 10 microM.	roxadustat	96-106	solute carrier family 16 member 3	Homo sapiens	2-31
33853432-0	2021	Successful application of roxadustat in the treatment of patients with anti-erythropoietin antibody-mediated renal anaemia: a case report and literature review.	roxadustat	26-36	erythropoietin	Homo sapiens	76-90
33853432-8	2021	This current case report demonstrates that roxadustat can be used to successfully treat anti-EPO antibody-mediated renal anaemia without the use of steroid-based immunosuppressants.	roxadustat	43-53	erythropoietin	Homo sapiens	93-96
33865748-12	2021	Roxadustat promoted pulmonary angiogenesis on hyperoxia exposure by stabilizing HIF-1alpha and upregulating the expression of proangiogenic factors, indicating its potential in clinical and therapeutic applications.	roxadustat	0-10	hypoxia inducible factor 1 subunit alpha	Homo sapiens	80-90
33743638-2	2021	Roxadustat has high affinity to thyroid hormone receptor beta, which may affect thyroid hormone homeostasis.	roxadustat	0-10	thyroid hormone receptor beta	Homo sapiens	32-61
33596451-7	2021	A monocarboxylate transporter-4 (MCT4) inhibitor, syrosingopine, inhibited lactate release from roxadustat-treated cells and reduced the elution of Ni ions by the cells at 10 microM.	roxadustat	96-106	solute carrier family 16 member 3	Homo sapiens	33-37
33649100-0	2021	Roxadustat for Renal Anemia in ESRD from PKD Patients: Is It Safe Enough?	roxadustat	0-10	protein kinase D1	Homo sapiens	41-44
33427060-8	2021	FG4592, a PHD inhibitor, increased HIF-1alpha and AQP2 protein abundance in association with decreased NFkappaB p65 protein expression in IMCD cells with H/R.	roxadustat	0-6	hypoxia inducible factor 1, alpha subunit	Mus musculus	35-45
33427060-8	2021	FG4592, a PHD inhibitor, increased HIF-1alpha and AQP2 protein abundance in association with decreased NFkappaB p65 protein expression in IMCD cells with H/R.	roxadustat	0-6	aquaporin 2	Mus musculus	50-54
33063127-0	2021	Correction to: Remarkable response to roxadustat in a case of anti-erythropoietin antibody-mediated pure red cell aplasia.	roxadustat	38-48	erythropoietin	Homo sapiens	67-81
32940725-0	2021	Remarkable response to roxadustat in a case of anti-erythropoietin antibody-mediated pure red cell aplasia.	roxadustat	23-33	erythropoietin	Homo sapiens	52-66
33959275-5	2021	Roxadustat has structural similarity with T3 and is a selective activating ligand for thyroid hormone receptor-beta possibly suppressing TSH release.	roxadustat	0-10	thyroid hormone receptor beta	Homo sapiens	86-115
32603526-7	2020	Roxadustat induced transient elevations of endogenous erythropoietin that peaked between 7 and 14 hours after dosing and returned to baseline by 48 hours after dosing.	roxadustat	0-10	erythropoietin	Homo sapiens	54-68
33129877-8	2021	Gene silencing of HIF-1alpha resulted in the opposite phenomenon in BMSCs with the treatment of FG4592.	roxadustat	96-102	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	18-28
33344604-0	2020	Roxadustat for treatment of erythropoietin-hyporesponsive anemia in a hemodialysis patient: A case report.	roxadustat	0-10	erythropoietin	Homo sapiens	28-42
32666268-4	2020	In this study, we evaluated the potential for Roxadustat (FG-4592), a prolyl hydroxylase inhibitor known to increase endogenous VEGF, in accelerating compensatory lung growth.	roxadustat	46-56	vascular endothelial growth factor A	Homo sapiens	128-132
32666268-4	2020	In this study, we evaluated the potential for Roxadustat (FG-4592), a prolyl hydroxylase inhibitor known to increase endogenous VEGF, in accelerating compensatory lung growth.	roxadustat	58-65	vascular endothelial growth factor A	Homo sapiens	128-132
33345685-6	2021	Additionally, roxadustat, a HIF prolyl-hydroxylase inhibitor, protected the renal tubular epithelial cells against iohexol-induced injury through stabilization of HIF1A and activation of downstream BNIP3-mediated mitophagy in vivo and in vitro.	roxadustat	14-24	hypoxia inducible factor 1, alpha subunit	Mus musculus	163-168
33345685-6	2021	Additionally, roxadustat, a HIF prolyl-hydroxylase inhibitor, protected the renal tubular epithelial cells against iohexol-induced injury through stabilization of HIF1A and activation of downstream BNIP3-mediated mitophagy in vivo and in vitro.	roxadustat	14-24	BCL2/adenovirus E1B interacting protein 3	Mus musculus	198-203
32856389-6	2020	Roxadustat is a new type of drug for the treatment of anaemia, and it can stimulate endogenous EPO within or near the physiologic range and increase haemoglobin levels.	roxadustat	0-10	erythropoietin	Homo sapiens	95-98
33051677-8	2021	Hepcidin levels were reduced significantly in the roxadustat group versus those in the placebo [SMD -1.72 (95% CI -3.03 to -0.41), very low-quality evidence] or epoetin alfa group [SMD -0.23 (95% CI -0.43 to -0.02), low-quality evidence].	roxadustat	50-60	hepcidin antimicrobial peptide	Homo sapiens	0-8
32726645-5	2020	FG-4592 treatment significantly upregulated HIF-1alpha and HO-1 and strikingly attenuated inflammation in vivo and in vitro.	roxadustat	0-7	heme oxygenase 1	Mus musculus	59-63
33011826-4	2020	In CD4+ T cells isolated from the two-way MLRs, western blotting was performed to detect the impact of roxadustat on HIF-1alpha and HIF-2alpha, the apoptotic marker cleaved caspase-3, and the master transcription factors of CD4+ T cells differentiation towards Th1, Th2, Th17, Treg and Tfh subsets.	roxadustat	103-113	hypoxia inducible factor 1 subunit alpha	Homo sapiens	117-127
33011826-7	2020	Roxadustat stabilized HIF-1alpha and HIF-2alpha, suppressed cell proliferation, inhibited CD4+ T-cell differentiation into Th1 and Th17 subsets, while it favored differentiation towards Th2, Treg and Tfh.	roxadustat	0-10	hypoxia inducible factor 1 subunit alpha	Homo sapiens	22-32
33011826-7	2020	Roxadustat stabilized HIF-1alpha and HIF-2alpha, suppressed cell proliferation, inhibited CD4+ T-cell differentiation into Th1 and Th17 subsets, while it favored differentiation towards Th2, Treg and Tfh.	roxadustat	0-10	endothelial PAS domain protein 1	Homo sapiens	37-47
33011826-7	2020	Roxadustat stabilized HIF-1alpha and HIF-2alpha, suppressed cell proliferation, inhibited CD4+ T-cell differentiation into Th1 and Th17 subsets, while it favored differentiation towards Th2, Treg and Tfh.	roxadustat	0-10	CD4 molecule	Homo sapiens	90-93
32446740-8	2020	Furthermore, we demonstrate that activation of the HIF-1 signaling pathway with the chemical compound FG-4592 or DMOG ameliorates liver steatosis and reduces accumulated Cu levels in zebrafish atp7b deficiency models.	roxadustat	102-109	hypoxia inducible factor 1 subunit alpha	Homo sapiens	51-56
32446740-8	2020	Furthermore, we demonstrate that activation of the HIF-1 signaling pathway with the chemical compound FG-4592 or DMOG ameliorates liver steatosis and reduces accumulated Cu levels in zebrafish atp7b deficiency models.	roxadustat	102-109	ATPase copper transporting beta	Danio rerio	193-198
32726645-5	2020	FG-4592 treatment significantly upregulated HIF-1alpha and HO-1 and strikingly attenuated inflammation in vivo and in vitro.	roxadustat	0-7	hypoxia inducible factor 1, alpha subunit	Mus musculus	44-54
32726645-8	2020	FG-4592 treatment remarkably ameliorated the LPS-induced lung injury through the stabilization of HIF-1alpha.	roxadustat	0-7	hypoxia inducible factor 1, alpha subunit	Mus musculus	98-108
32142369-9	2020	The PHD2 (prolyl hydroxylase domain-containing protein 2) inhibitor FG-4592 significantly increased NAMPT promoter activity and protein expression in an HIF-2alpha-dependent manner.	roxadustat	68-75	egl-9 family hypoxia inducible factor 1	Homo sapiens	4-8
33015417-6	2020	Selective activation of HIF-2alpha can be achieved with drugs that: 1) inhibit isoform-selective prolyl hydroxylases (e.g., cobalt chloride and roxadustat); or 2) promote the actions of the redox sensor, sirtuin-1 (e.g., sodium-glucose cotransporter 2 inhibitors).	roxadustat	144-154	endothelial PAS domain protein 1	Homo sapiens	24-34
32534005-5	2020	Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1alpha, alpha-SMA, CTGF, TGF-beta1 and p-Smad3/Smad3.	roxadustat	0-10	egl-9 family hypoxia-inducible factor 1	Mus musculus	164-168
32534005-5	2020	Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1alpha, alpha-SMA, CTGF, TGF-beta1 and p-Smad3/Smad3.	roxadustat	0-10	hypoxia inducible factor 1, alpha subunit	Mus musculus	170-180
32534005-5	2020	Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1alpha, alpha-SMA, CTGF, TGF-beta1 and p-Smad3/Smad3.	roxadustat	0-10	actin alpha 2, smooth muscle, aorta	Mus musculus	182-191
32534005-5	2020	Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1alpha, alpha-SMA, CTGF, TGF-beta1 and p-Smad3/Smad3.	roxadustat	0-10	cellular communication network factor 2	Mus musculus	193-197
32534005-5	2020	Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1alpha, alpha-SMA, CTGF, TGF-beta1 and p-Smad3/Smad3.	roxadustat	0-10	transforming growth factor, beta 1	Mus musculus	199-208
32534005-5	2020	Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1alpha, alpha-SMA, CTGF, TGF-beta1 and p-Smad3/Smad3.	roxadustat	0-10	SMAD family member 3	Mus musculus	215-220
32534005-5	2020	Roxadustat ameliorated pulmonary fibrosis by reducing the pathology score and collagen deposition as well as decreasing the expression of collagen I, collagen III, PHD2, HIF-1alpha, alpha-SMA, CTGF, TGF-beta1 and p-Smad3/Smad3.	roxadustat	0-10	SMAD family member 3	Mus musculus	221-226
32534005-6	2020	Our cumulative results demonstrate that roxadustat administration can attenuate experimental pulmonary fibrosis via the inhibition of TGF-beta1/Smad activation.	roxadustat	40-50	transforming growth factor, beta 1	Mus musculus	134-143
32142369-9	2020	The PHD2 (prolyl hydroxylase domain-containing protein 2) inhibitor FG-4592 significantly increased NAMPT promoter activity and protein expression in an HIF-2alpha-dependent manner.	roxadustat	68-75	egl-9 family hypoxia inducible factor 1	Homo sapiens	10-56
32142369-9	2020	The PHD2 (prolyl hydroxylase domain-containing protein 2) inhibitor FG-4592 significantly increased NAMPT promoter activity and protein expression in an HIF-2alpha-dependent manner.	roxadustat	68-75	nicotinamide phosphoribosyltransferase	Homo sapiens	100-105
32142369-9	2020	The PHD2 (prolyl hydroxylase domain-containing protein 2) inhibitor FG-4592 significantly increased NAMPT promoter activity and protein expression in an HIF-2alpha-dependent manner.	roxadustat	68-75	endothelial PAS domain protein 1	Homo sapiens	153-163
32380083-2	2020	Prolyl hydroxylase (PHD) inhibitors, such as roxadustat, can stabilize hypoxia-inducible factor (HIF)-2alpha and induce erythropoietin (EPO) production under normal conditions.	roxadustat	45-55	endothelial PAS domain protein 1	Homo sapiens	71-108
32380083-2	2020	Prolyl hydroxylase (PHD) inhibitors, such as roxadustat, can stabilize hypoxia-inducible factor (HIF)-2alpha and induce erythropoietin (EPO) production under normal conditions.	roxadustat	45-55	erythropoietin	Homo sapiens	120-134
32380083-2	2020	Prolyl hydroxylase (PHD) inhibitors, such as roxadustat, can stabilize hypoxia-inducible factor (HIF)-2alpha and induce erythropoietin (EPO) production under normal conditions.	roxadustat	45-55	erythropoietin	Homo sapiens	136-139
32150252-9	2020	Our findings also demonstrate that exposure to 1% O2 or to Roxa increases the expression of HIF1alpha, the number of lipid-containing vesicles, the content of neutral lipids, and the activity of DNase II and decreases the pH in IHMGECs in vitro.	roxadustat	59-63	hypoxia inducible factor 1 subunit alpha	Homo sapiens	92-101
32666021-6	2020	The PHD enzyme inhibitor FG-4592 stabilized HIF protein and stimulated osteoclast-mediated bone resorption, but inhibited differentiation of human CD14+ monocytes into osteoclasts.	roxadustat	25-32	CD14 molecule	Homo sapiens	147-151
32487538-4	2020	We hypothesized that roxadustat, an orally available small-molecule inhibitor of HIF-PH, would increase EPO production and promote erythropoiesis in animal models of anemia.	roxadustat	21-31	erythropoietin	Rattus norvegicus	104-107
32487538-5	2020	In cells, roxadustat increased both HIF-1alpha and HIF-2alpha proteins, leading to an increase in EPO production, even in the presence of EPO-suppressing inflammatory cytokines.	roxadustat	10-20	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	36-46
32487538-5	2020	In cells, roxadustat increased both HIF-1alpha and HIF-2alpha proteins, leading to an increase in EPO production, even in the presence of EPO-suppressing inflammatory cytokines.	roxadustat	10-20	endothelial PAS domain protein 1	Rattus norvegicus	51-61
32487538-5	2020	In cells, roxadustat increased both HIF-1alpha and HIF-2alpha proteins, leading to an increase in EPO production, even in the presence of EPO-suppressing inflammatory cytokines.	roxadustat	10-20	erythropoietin	Rattus norvegicus	98-101
32487538-6	2020	Roxadustat administered intermittently to healthy rats and cynomolgus monkeys increased circulating EPO levels, reticulocytes, blood Hb, and hematocrit in a dose-dependent manner.	roxadustat	0-10	erythropoietin	Macaca fascicularis	100-103
32487538-8	2020	In the PG-PS model, roxadustat significantly decreased hepatic expression of hepcidin, a hormone responsible for iron sequestration and functional iron deficiency, and increased expression of two genes involved in duodenal iron absorption: divalent metal transporter 1 and duodenal cytochrome b.	roxadustat	20-30	hepcidin antimicrobial peptide	Rattus norvegicus	77-85
32487538-8	2020	In the PG-PS model, roxadustat significantly decreased hepatic expression of hepcidin, a hormone responsible for iron sequestration and functional iron deficiency, and increased expression of two genes involved in duodenal iron absorption: divalent metal transporter 1 and duodenal cytochrome b.	roxadustat	20-30	solute carrier family 11 member 2	Rattus norvegicus	240-268
32487538-8	2020	In the PG-PS model, roxadustat significantly decreased hepatic expression of hepcidin, a hormone responsible for iron sequestration and functional iron deficiency, and increased expression of two genes involved in duodenal iron absorption: divalent metal transporter 1 and duodenal cytochrome b.	roxadustat	20-30	cytochrome b reductase 1	Rattus norvegicus	273-294
32487538-9	2020	In conclusion, by activating the HIF pathway, roxadustat increased EPO production, elevated Hb, corrected anemia, and improved iron homeostasis.	roxadustat	46-56	erythropoietin	Rattus norvegicus	67-70
32487538-10	2020	The coordinated erythropoietic response stimulated by roxadustat, involving both EPO production and mobilization of iron stores, makes this compound a promising treatment of anemia of CKD and anemia associated with functional iron deficiency.	roxadustat	54-64	erythropoietin	Rattus norvegicus	81-84
32487538-11	2020	SIGNIFICANCE STATEMENT: Roxadustat is a novel orally available small-molecule inhibitor of HIF prolyl hydroxylase enzymes that reversibly stabilizes HIF-alpha, thus activating transcription of HIF-dependent genes, including EPO and regulators of iron homeostasis.	roxadustat	24-34	erythropoietin	Rattus norvegicus	224-227
32487538-13	2020	The coordinated erythropoietic response that increases EPO production and mobilizes iron stores makes roxadustat a promising treatment for anemia of chronic kidney disease and anemia associated with functional iron deficiency.	roxadustat	102-112	erythropoietin	Rattus norvegicus	55-58
31866051-7	2020	At 3 days after UUO, higher dose of FG-4592 potentiated the increased mRNA expression of profibrogenic molecules, plasminogen activator inhibitor 1 (Pai-1) and connective tissue growth factor (Ctgf) but such potentiation disappeared at 7 days after UUO.	roxadustat	36-43	serine (or cysteine) peptidase inhibitor, clade E, member 1	Mus musculus	114-147
31866051-7	2020	At 3 days after UUO, higher dose of FG-4592 potentiated the increased mRNA expression of profibrogenic molecules, plasminogen activator inhibitor 1 (Pai-1) and connective tissue growth factor (Ctgf) but such potentiation disappeared at 7 days after UUO.	roxadustat	36-43	serine (or cysteine) peptidase inhibitor, clade E, member 1	Mus musculus	149-154
31866051-7	2020	At 3 days after UUO, higher dose of FG-4592 potentiated the increased mRNA expression of profibrogenic molecules, plasminogen activator inhibitor 1 (Pai-1) and connective tissue growth factor (Ctgf) but such potentiation disappeared at 7 days after UUO.	roxadustat	36-43	cellular communication network factor 2	Mus musculus	160-191
31866051-7	2020	At 3 days after UUO, higher dose of FG-4592 potentiated the increased mRNA expression of profibrogenic molecules, plasminogen activator inhibitor 1 (Pai-1) and connective tissue growth factor (Ctgf) but such potentiation disappeared at 7 days after UUO.	roxadustat	36-43	cellular communication network factor 2	Mus musculus	193-197
32309288-8	2020	On the one hand, roxadustat could increase endogenous erythropoietin (EPO) levels within or near physiological range in a titratable manner by inducing HIF pathway activation transiently.	roxadustat	17-27	erythropoietin	Homo sapiens	54-68
32309288-8	2020	On the one hand, roxadustat could increase endogenous erythropoietin (EPO) levels within or near physiological range in a titratable manner by inducing HIF pathway activation transiently.	roxadustat	17-27	erythropoietin	Homo sapiens	70-73
32309288-9	2020	On the other hand, roxadustat also improves iron metabolism by decreasing serum hepcidin and increasing intestinal iron absorption, which is beneficial to functional iron deficiency and absolute iron deficiency.	roxadustat	19-29	hepcidin antimicrobial peptide	Homo sapiens	80-88
32309288-13	2020	Roxadustat corrects anemia of CKD patients through multiple pathways, beyond elevating EPO levels within physiological range, and also by handling iron metabolism (particularly decreasing the hepcidin levels).	roxadustat	0-10	erythropoietin	Homo sapiens	87-90
32309288-13	2020	Roxadustat corrects anemia of CKD patients through multiple pathways, beyond elevating EPO levels within physiological range, and also by handling iron metabolism (particularly decreasing the hepcidin levels).	roxadustat	0-10	hepcidin antimicrobial peptide	Homo sapiens	192-200
32051732-0	2020	Pretreatment with Roxadustat (FG-4592) Attenuates Folic Acid-Induced Kidney Injury through Antiferroptosis via Akt/GSK-3beta/Nrf2 Pathway.	roxadustat	18-28	thymoma viral proto-oncogene 1	Mus musculus	111-114
32051732-0	2020	Pretreatment with Roxadustat (FG-4592) Attenuates Folic Acid-Induced Kidney Injury through Antiferroptosis via Akt/GSK-3beta/Nrf2 Pathway.	roxadustat	18-28	glycogen synthase kinase 3 alpha	Mus musculus	115-124
32051732-0	2020	Pretreatment with Roxadustat (FG-4592) Attenuates Folic Acid-Induced Kidney Injury through Antiferroptosis via Akt/GSK-3beta/Nrf2 Pathway.	roxadustat	18-28	nuclear factor, erythroid derived 2, like 2	Mus musculus	125-129
32051732-0	2020	Pretreatment with Roxadustat (FG-4592) Attenuates Folic Acid-Induced Kidney Injury through Antiferroptosis via Akt/GSK-3beta/Nrf2 Pathway.	roxadustat	30-37	thymoma viral proto-oncogene 1	Mus musculus	111-114
32051732-0	2020	Pretreatment with Roxadustat (FG-4592) Attenuates Folic Acid-Induced Kidney Injury through Antiferroptosis via Akt/GSK-3beta/Nrf2 Pathway.	roxadustat	30-37	glycogen synthase kinase 3 alpha	Mus musculus	115-124
32051732-0	2020	Pretreatment with Roxadustat (FG-4592) Attenuates Folic Acid-Induced Kidney Injury through Antiferroptosis via Akt/GSK-3beta/Nrf2 Pathway.	roxadustat	30-37	nuclear factor, erythroid derived 2, like 2	Mus musculus	125-129
31340089-9	2019	The mean reduction from baseline in the hepcidin level (associated with greater iron availability) was 56.14+-63.40 ng per milliliter in the roxadustat group and 15.10+-48.06 ng per milliliter in the placebo group.	roxadustat	141-151	hepcidin antimicrobial peptide	Homo sapiens	40-48
31340116-12	2019	As compared with epoetin alfa, roxadustat increased the transferrin level (difference, 0.43 g per liter; 95% CI, 0.32 to 0.53), maintained the serum iron level (difference, 25 mug per deciliter; 95% CI, 17 to 33), and attenuated decreases in the transferrin saturation (difference, 4.2 percentage points; 95% CI, 1.5 to 6.9).	roxadustat	31-41	transferrin	Homo sapiens	56-67
31340116-12	2019	As compared with epoetin alfa, roxadustat increased the transferrin level (difference, 0.43 g per liter; 95% CI, 0.32 to 0.53), maintained the serum iron level (difference, 25 mug per deciliter; 95% CI, 17 to 33), and attenuated decreases in the transferrin saturation (difference, 4.2 percentage points; 95% CI, 1.5 to 6.9).	roxadustat	31-41	transferrin	Homo sapiens	246-257
31340116-14	2019	Roxadustat was associated with a mean reduction in hepcidin of 30.2 ng per milliliter (95% CI, -64.8 to -13.6), as compared with 2.3 ng per milliliter (95% CI, -51.6 to 6.2) in the epoetin alfa group.	roxadustat	0-10	erythropoietin	Homo sapiens	181-188
30817065-0	2019	Roxadustat promotes angiogenesis through HIF-1alpha/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats.	roxadustat	0-10	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	41-51
30817065-0	2019	Roxadustat promotes angiogenesis through HIF-1alpha/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats.	roxadustat	0-10	vascular endothelial growth factor A	Rattus norvegicus	52-56
30817065-0	2019	Roxadustat promotes angiogenesis through HIF-1alpha/VEGF/VEGFR2 signaling and accelerates cutaneous wound healing in diabetic rats.	roxadustat	0-10	kinase insert domain receptor	Rattus norvegicus	57-63
30817065-4	2019	In vitro, we found that roxadustat could promote the angiogenic activity of human umbilical vein endothelial cells, accompanied by up-regulation of HIF-1alpha/VEGF/VEGFR2 signaling.	roxadustat	24-34	hypoxia inducible factor 1 subunit alpha	Homo sapiens	148-158
30817065-4	2019	In vitro, we found that roxadustat could promote the angiogenic activity of human umbilical vein endothelial cells, accompanied by up-regulation of HIF-1alpha/VEGF/VEGFR2 signaling.	roxadustat	24-34	vascular endothelial growth factor A	Homo sapiens	159-163
30817065-4	2019	In vitro, we found that roxadustat could promote the angiogenic activity of human umbilical vein endothelial cells, accompanied by up-regulation of HIF-1alpha/VEGF/VEGFR2 signaling.	roxadustat	24-34	kinase insert domain receptor	Homo sapiens	164-170
30817065-8	2019	In conclusion, roxadustat promotes angiogenesis via activation of the HIF-1alpha/VEGF/VEGFR2 pathway and exhibits therapeutic effects on diabetic wound healing by increasing angiogenesis.	roxadustat	15-25	hypoxia inducible factor 1 subunit alpha	Rattus norvegicus	70-80
30817065-8	2019	In conclusion, roxadustat promotes angiogenesis via activation of the HIF-1alpha/VEGF/VEGFR2 pathway and exhibits therapeutic effects on diabetic wound healing by increasing angiogenesis.	roxadustat	15-25	vascular endothelial growth factor A	Rattus norvegicus	81-85
30817065-8	2019	In conclusion, roxadustat promotes angiogenesis via activation of the HIF-1alpha/VEGF/VEGFR2 pathway and exhibits therapeutic effects on diabetic wound healing by increasing angiogenesis.	roxadustat	15-25	kinase insert domain receptor	Rattus norvegicus	86-92
29254377-8	2018	Given that the peaks of endogenous EPO are much lower than those observed with traditional ESA, it is possible to speculate the roxadustat (and more in general PHD inhibitors) will be safer than ESA on cardiovascular safety end-points.	roxadustat	128-138	erythropoietin	Homo sapiens	35-38
29153032-2	2017	Inhibition of HIF-PH by roxadustat leads to a rapid increase in cytoplasmic HIF-alpha concentrations, followed by translocation of HIF-alpha to the nucleus and upregulation of HIF-responsive genes, including erythropoietin.	roxadustat	24-34	erythropoietin	Rattus norvegicus	208-222
30898838-4	2019	EGLN1-dependent cells exhibited sensitivity to the pan-EGLN inhibitor FG-4592.	roxadustat	70-77	egl-9 family hypoxia inducible factor 1	Homo sapiens	0-5
29438490-1	2018	Roxadustat (FG-4592, Rox) is a stabilizer for hypoxia-inducible transcription factors (HIFs), which induce production of the erythroid growth factor erythropoietin, and has been listed by the World Anti-Doping Agency as a prohibited substance for athletes since 2011.	roxadustat	0-10	erythropoietin	Mus musculus	149-163