PMID-sentid	Pub_year	Sent_text	compound_name	comp_offset	prot_official_name	organism	prot_offset
24519575-5	2014	By following similar synthetic routes, 580.0 mg of (13)CD2-labeled saxagliptin and 153.1 mg of (13)CD2-labeled 5-hydroxysaxagliptin metabolite were prepared.	5-hydroxysaxagliptin	111-131	CD2 molecule	Homo sapiens	99-102
22475049-3	2012	RESULTS: Saxagliptin and its active metabolite (5-hydroxysaxagliptin) are potent inhibitors of human DPP4 with prolonged dissociation from its active site (Ki = 1.3 nM and 2.6 nM, t1/2 = 50 and 23 minutes respectively at 37 C).	5-hydroxysaxagliptin	48-68	dipeptidyl peptidase 4	Homo sapiens	101-105
22475049-4	2012	In comparison, both vildagliptin (3.5 minutes) and sitagliptin ( < 2 minutes) rapidly dissociated from DPP4 at 37 C. Saxagliptin and 5-hydroxysaxagliptin are selective for inhibition of DPP4 versus other DPP family members and a large panel of other proteases, and have similar potency and efficacy across multiple species.Inhibition of plasma DPP activity is used as a biomarker in animal models and clinical trials.	5-hydroxysaxagliptin	136-156	dipeptidyl peptidase 4	Homo sapiens	106-110
22475049-4	2012	In comparison, both vildagliptin (3.5 minutes) and sitagliptin ( < 2 minutes) rapidly dissociated from DPP4 at 37 C. Saxagliptin and 5-hydroxysaxagliptin are selective for inhibition of DPP4 versus other DPP family members and a large panel of other proteases, and have similar potency and efficacy across multiple species.Inhibition of plasma DPP activity is used as a biomarker in animal models and clinical trials.	5-hydroxysaxagliptin	136-156	dipeptidyl peptidase 4	Homo sapiens	189-193
22475049-9	2012	They also demonstrate prolonged inhibition of plasma DPP4 ex vivo in animal models, which implies that saxagliptin and 5-hydroxysaxagliptin would continue to inhibit DPP4 during rapid increases in substrates in vivo.	5-hydroxysaxagliptin	119-139	dipeptidyl peptidase 4	Homo sapiens	53-57
22475049-9	2012	They also demonstrate prolonged inhibition of plasma DPP4 ex vivo in animal models, which implies that saxagliptin and 5-hydroxysaxagliptin would continue to inhibit DPP4 during rapid increases in substrates in vivo.	5-hydroxysaxagliptin	119-139	dipeptidyl peptidase 4	Homo sapiens	166-170
27282159-4	2017	Both saxagliptin and its major active metabolite, 5-hydroxy saxagliptin, demonstrate high degrees of selectivity for DPP-4 compared with other DPP enzymes.	5-hydroxysaxagliptin	50-71	dipeptidyl peptidase 4	Homo sapiens	117-122
21651615-2	2011	Saxagliptin is metabolized by CYP3A4/3A5 to 5-hydroxy saxagliptin, its major pharmacologically active metabolite.	5-hydroxysaxagliptin	44-65	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	30-36
22287853-6	2011	Mean exposure (AUC) of the CYP3A4-generated active metabolite of saxagliptin, 5-hydroxy saxagliptin, decreased with coadministration of simvastatin, diltiazem, and ketoconazole by 2%, 34%, and 88%, respectively.	5-hydroxysaxagliptin	78-99	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	27-33
35247279-1	2022	We characterized the impact of chronic kidney disease (CKD) on the cytochrome P450 3A4 (CYP3A4)-mediated metabolism of saxagliptin to its metabolite, 5-hydroxysaxagliptin, using a physiologically based pharmacokinetic (PBPK) model.	5-hydroxysaxagliptin	150-170	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	67-86
35247279-1	2022	We characterized the impact of chronic kidney disease (CKD) on the cytochrome P450 3A4 (CYP3A4)-mediated metabolism of saxagliptin to its metabolite, 5-hydroxysaxagliptin, using a physiologically based pharmacokinetic (PBPK) model.	5-hydroxysaxagliptin	150-170	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	88-94
35247279-2	2022	A PBPK model of saxagliptin and its CYP3A4 metabolite, 5-hydroxysaxagliptin, was constructed and validated for oral doses ranging from 5 mg-100 mg.	5-hydroxysaxagliptin	55-75	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	36-42
35247279-6	2022	Similarly, simulations using decreased CYP3A4 activity underpredicted the ratio of 5-hydroxysaxagliptin AUC in moderate and severe CKD compared with simulations using preserved CYP3A4 activity.	5-hydroxysaxagliptin	83-103	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	39-45
35247279-6	2022	Similarly, simulations using decreased CYP3A4 activity underpredicted the ratio of 5-hydroxysaxagliptin AUC in moderate and severe CKD compared with simulations using preserved CYP3A4 activity.	5-hydroxysaxagliptin	83-103	cytochrome P450 family 3 subfamily A member 4	Homo sapiens	177-183