PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 35267027-6 2022 For most joint groups, peficitinib demonstrated reduced change from baseline at Week 28/ET in erosion and JSN scores versus placebo; a numerically greater effect was observed with peficitinib 150mg versus 100mg. peficitinib 23-34 major facilitator superfamily domain containing 11 Homo sapiens 88-90 35253941-7 2022 Filgotinib 100 mg was ranked highest for induction of endoscopic remission (SUCRA, 0.67) whereas peficitinib 75 mg BID was ranked highest for induction of clinical response (SUCRA, 0.72). peficitinib 97-108 BH3 interacting domain death agonist Homo sapiens 115-118 35267027-9 2022 Higher baseline CRP and/or prednisolone dose were associated with reduced peficitinib efficacy. peficitinib 74-85 C-reactive protein Homo sapiens 16-19 35253941-11 2022 WHAT IS NEW AND CONCLUSION: Based on indirect comparisons, peficitinib 75 mg/75 mg BID/150 mg, tofacitinib 3 mg and filgotinib 100mg were the most efficacious JAK inhibitor interventions in patients with UC. peficitinib 59-70 BH3 interacting domain death agonist Homo sapiens 83-86 32561292-6 2020 Peficitinib inhibited STAT3 phosphorylation in RA-FLS following induction by interferon (IFN)-alpha2b, IFN-gamma, interleukin (IL)-6, oncostatin M, and leukemia inhibitory factor in a concentration-related manner, and was comparable to approved JAK inhibitors, tofacitinib and baricitinib. peficitinib 0-11 signal transducer and activator of transcription 3 Homo sapiens 22-27 33929089-1 2021 The aim was to analyze the relationship between peficitinib exposure and efficacy response according to American College of Rheumatology (ACR) 20 criteria and 28-joint disease activity score based on C-reactive protein (DAS28-CRP) in rheumatoid arthritis (RA) patients, and to identify relevant covariates by developing exposure-response models. peficitinib 48-59 C-reactive protein Homo sapiens 226-229 33929089-6 2021 The exposure-response models of effect of peficitinib on duration-dependent increase in ACR20 response rate and decrease in DAS28-CRP were adequately described by a continuous time Markov model and an indirect response model, respectively, with a sigmoidal Emax saturable of drug exposure in RA patients. peficitinib 42-53 C-reactive protein Homo sapiens 130-133 33929089-9 2021 Our exposure-response models of peficitinib in RA patients satisfactorily described duration-dependent improvements in ACR20 response rates and DAS28-CRP measurements, and provided consistent covariate effects. peficitinib 32-43 C-reactive protein Homo sapiens 150-153 32561292-6 2020 Peficitinib inhibited STAT3 phosphorylation in RA-FLS following induction by interferon (IFN)-alpha2b, IFN-gamma, interleukin (IL)-6, oncostatin M, and leukemia inhibitory factor in a concentration-related manner, and was comparable to approved JAK inhibitors, tofacitinib and baricitinib. peficitinib 0-11 interferon alpha 2 Homo sapiens 77-101 32561292-6 2020 Peficitinib inhibited STAT3 phosphorylation in RA-FLS following induction by interferon (IFN)-alpha2b, IFN-gamma, interleukin (IL)-6, oncostatin M, and leukemia inhibitory factor in a concentration-related manner, and was comparable to approved JAK inhibitors, tofacitinib and baricitinib. peficitinib 0-11 interferon gamma Homo sapiens 103-112 32561292-6 2020 Peficitinib inhibited STAT3 phosphorylation in RA-FLS following induction by interferon (IFN)-alpha2b, IFN-gamma, interleukin (IL)-6, oncostatin M, and leukemia inhibitory factor in a concentration-related manner, and was comparable to approved JAK inhibitors, tofacitinib and baricitinib. peficitinib 0-11 interleukin 6 Homo sapiens 114-132 32561292-6 2020 Peficitinib inhibited STAT3 phosphorylation in RA-FLS following induction by interferon (IFN)-alpha2b, IFN-gamma, interleukin (IL)-6, oncostatin M, and leukemia inhibitory factor in a concentration-related manner, and was comparable to approved JAK inhibitors, tofacitinib and baricitinib. peficitinib 0-11 oncostatin M Homo sapiens 134-146 32561292-6 2020 Peficitinib inhibited STAT3 phosphorylation in RA-FLS following induction by interferon (IFN)-alpha2b, IFN-gamma, interleukin (IL)-6, oncostatin M, and leukemia inhibitory factor in a concentration-related manner, and was comparable to approved JAK inhibitors, tofacitinib and baricitinib. peficitinib 0-11 LIF interleukin 6 family cytokine Homo sapiens 152-178 32561292-7 2020 Peficitinib and tofacitinib suppressed autocrine phosphorylation of STAT3 and expression of apoptosis-resistant genes, and promoted cell death. peficitinib 0-11 signal transducer and activator of transcription 3 Homo sapiens 68-73 32472157-0 2020 A drug-drug interaction study to evaluate the impact of peficitinib on OCT1- and MATE1-mediated transport of metformin in healthy volunteers. peficitinib 56-67 solute carrier family 22 member 1 Homo sapiens 71-75 32472157-0 2020 A drug-drug interaction study to evaluate the impact of peficitinib on OCT1- and MATE1-mediated transport of metformin in healthy volunteers. peficitinib 56-67 solute carrier family 47 member 1 Homo sapiens 81-86 32472157-5 2020 METHODS: Inhibitory effects of peficitinib and its metabolite H2 on metformin uptake into human OCT1/2- and MATE1/2-K-expressing cells were assessed in vitro. peficitinib 31-42 solute carrier family 22 member 1 Homo sapiens 96-102 32472157-9 2020 RESULTS: Peficitinib, but not H2, inhibited metformin uptake into OCT1- and MATE1/2-K-expressing cells. peficitinib 9-20 solute carrier family 22 member 1 Homo sapiens 66-70 32472157-9 2020 RESULTS: Peficitinib, but not H2, inhibited metformin uptake into OCT1- and MATE1/2-K-expressing cells. peficitinib 9-20 solute carrier family 47 member 1 Homo sapiens 76-81 30984167-14 2019 In contrast, only peficitinib and filgotinib decreased the IL-6 release of RASF activated with IL-1beta. peficitinib 18-29 interleukin 6 Homo sapiens 59-63 31350270-9 2019 Changes from baseline in DAS28-C-reactive protein/erythrocyte sedimentation rate and the ACR core set were significantly greater for both peficitinib doses versus placebo at week 12/ET (p<0.001). peficitinib 138-149 C-reactive protein Homo sapiens 31-49 31350270-9 2019 Changes from baseline in DAS28-C-reactive protein/erythrocyte sedimentation rate and the ACR core set were significantly greater for both peficitinib doses versus placebo at week 12/ET (p<0.001). peficitinib 138-149 acrosin Homo sapiens 89-92 31059310-0 2019 JAK3-selective inhibitor peficitinib for the treatment of rheumatoid arthritis. peficitinib 25-36 Janus kinase 3 Homo sapiens 0-4 31059310-6 2019 Expert opinion: Peficitinib is a novel JAK3 inhibitor potently inhibiting JAK3 enzymatic activity and JAK1/3-mediated cell proliferation. peficitinib 16-27 Janus kinase 3 Homo sapiens 39-43 31059310-6 2019 Expert opinion: Peficitinib is a novel JAK3 inhibitor potently inhibiting JAK3 enzymatic activity and JAK1/3-mediated cell proliferation. peficitinib 16-27 Janus kinase 3 Homo sapiens 74-78 31059310-6 2019 Expert opinion: Peficitinib is a novel JAK3 inhibitor potently inhibiting JAK3 enzymatic activity and JAK1/3-mediated cell proliferation. peficitinib 16-27 Janus kinase 1 Homo sapiens 102-106 32274653-8 2020 Mean peak inhibition of STAT5 phosphorylation was higher in Japanese than Caucasian subjects for a given peficitinib dose, but inhibition was comparable across ethnicities for a given plasma peficitinib concentration. peficitinib 105-116 signal transducer and activator of transcription 5A Homo sapiens 24-29 31181818-8 2019 Phosphorylation of STAT1, STAT3, and STAT5 in RA FLS was suppressed by peficitinib in a concentration-dependent manner. peficitinib 71-82 signal transducer and activator of transcription 1 Homo sapiens 19-24 31181818-8 2019 Phosphorylation of STAT1, STAT3, and STAT5 in RA FLS was suppressed by peficitinib in a concentration-dependent manner. peficitinib 71-82 signal transducer and activator of transcription 3 Homo sapiens 26-31 31181818-8 2019 Phosphorylation of STAT1, STAT3, and STAT5 in RA FLS was suppressed by peficitinib in a concentration-dependent manner. peficitinib 71-82 signal transducer and activator of transcription 5A Homo sapiens 37-42 31181818-10 2019 Peficitinib suppressed the secretion of MCP-1/CCL2 in the RA FLS supernatant (p < 0.05). peficitinib 0-11 C-C motif chemokine ligand 2 Homo sapiens 40-45 31181818-10 2019 Peficitinib suppressed the secretion of MCP-1/CCL2 in the RA FLS supernatant (p < 0.05). peficitinib 0-11 C-C motif chemokine ligand 2 Homo sapiens 46-50 31093950-1 2019 Peficitinib [Smyraf (Astellas Pharma)] is a Janus kinase (JAK)1, JAK2, JAK3 and tyrosine kinase (Tyk)2 (pan-JAK) inhibitor recently approved in Japan for the treatment of rheumatoid arthritis. peficitinib 0-11 Janus kinase 1 Homo sapiens 45-64 31093950-1 2019 Peficitinib [Smyraf (Astellas Pharma)] is a Janus kinase (JAK)1, JAK2, JAK3 and tyrosine kinase (Tyk)2 (pan-JAK) inhibitor recently approved in Japan for the treatment of rheumatoid arthritis. peficitinib 0-11 Janus kinase 2 Homo sapiens 66-70 31093950-1 2019 Peficitinib [Smyraf (Astellas Pharma)] is a Janus kinase (JAK)1, JAK2, JAK3 and tyrosine kinase (Tyk)2 (pan-JAK) inhibitor recently approved in Japan for the treatment of rheumatoid arthritis. peficitinib 0-11 Janus kinase 3 Homo sapiens 72-76 31093950-1 2019 Peficitinib [Smyraf (Astellas Pharma)] is a Janus kinase (JAK)1, JAK2, JAK3 and tyrosine kinase (Tyk)2 (pan-JAK) inhibitor recently approved in Japan for the treatment of rheumatoid arthritis. peficitinib 0-11 tyrosine kinase 2 Homo sapiens 81-103 30984167-14 2019 In contrast, only peficitinib and filgotinib decreased the IL-6 release of RASF activated with IL-1beta. peficitinib 18-29 interleukin 1 beta Homo sapiens 95-103 30984167-15 2019 Peficitinib decreased also the MMP-3, CXCL8, and CXCL1 release at 5 muM. peficitinib 0-11 matrix metallopeptidase 3 Homo sapiens 31-36 30984167-15 2019 Peficitinib decreased also the MMP-3, CXCL8, and CXCL1 release at 5 muM. peficitinib 0-11 C-X-C motif chemokine ligand 8 Homo sapiens 38-43 30984167-15 2019 Peficitinib decreased also the MMP-3, CXCL8, and CXCL1 release at 5 muM. peficitinib 0-11 C-X-C motif chemokine ligand 1 Homo sapiens 49-54 30984167-19 2019 Only peficitinib modulated the IL-1beta-induced response of RASF and their proliferation in vitro at concentrations close to reported Cmax values of well tolerated doses in vivo. peficitinib 5-16 interleukin 1 beta Homo sapiens 31-39 28117214-5 2017 We found that peficitinib inhibited JAK1 and JAK3 with 50% inhibitory concentrations of 3.9 and 0.7 nM, respectively. peficitinib 14-25 Janus kinase 1 Rattus norvegicus 36-40 30643464-12 2019 Furthermore, the roles of apoptosis inhibition and viability, invasion, and tumorigenesis promotions induced by OCT4 in NSP cells were all abolished when adding peficitinib. peficitinib 161-172 POU class 5 homeobox 1 Homo sapiens 112-116 30145050-3 2018 Here, we describe the identification of the novel orally bioavailable JAK inhibitor 18, peficitinib (also known as ASP015K), which showed moderate selectivity for JAK3 over JAK1, JAK2, and TYK2 in enzyme assays. peficitinib 88-99 Janus kinase 3 Homo sapiens 163-167 27748083-5 2017 Significant decreases from baseline in the Disease Activity Score in 28 joints using the C-reactive protein level were seen in the peficitinib 50 mg (P < 0.05) and 150 mg (P < 0.01) groups compared with placebo at week 12. peficitinib 131-142 C-reactive protein Homo sapiens 89-107 30145050-3 2018 Here, we describe the identification of the novel orally bioavailable JAK inhibitor 18, peficitinib (also known as ASP015K), which showed moderate selectivity for JAK3 over JAK1, JAK2, and TYK2 in enzyme assays. peficitinib 88-99 Janus kinase 1 Homo sapiens 173-177 30145050-3 2018 Here, we describe the identification of the novel orally bioavailable JAK inhibitor 18, peficitinib (also known as ASP015K), which showed moderate selectivity for JAK3 over JAK1, JAK2, and TYK2 in enzyme assays. peficitinib 88-99 Janus kinase 2 Homo sapiens 179-183 30145050-3 2018 Here, we describe the identification of the novel orally bioavailable JAK inhibitor 18, peficitinib (also known as ASP015K), which showed moderate selectivity for JAK3 over JAK1, JAK2, and TYK2 in enzyme assays. peficitinib 88-99 tyrosine kinase 2 Homo sapiens 189-193 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 98-109 Janus kinase 1 Homo sapiens 53-57 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 98-109 Janus kinase 2 Homo sapiens 59-63 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 98-109 Janus kinase 3 Homo sapiens 65-69 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 98-109 tyrosine kinase 2 Homo sapiens 75-79 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 185-196 Janus kinase 1 Homo sapiens 53-57 30145050-5 2018 Furthermore, we determined the crystal structures of JAK1, JAK2, JAK3, and TYK2 in a complex with peficitinib, and revealed that the 1H-pyrrolo[2,3-b]pyridine-5-carboxamide scaffold of peficitinib forms triple hydrogen bonds with the hinge region. peficitinib 185-196 tyrosine kinase 2 Homo sapiens 75-79 30145050-6 2018 Interestingly, the binding modes of peficitinib in the ATP-binding pockets differed among JAK1, JAK2, JAK3, and TYK2. peficitinib 36-47 Janus kinase 1 Homo sapiens 90-94 30145050-6 2018 Interestingly, the binding modes of peficitinib in the ATP-binding pockets differed among JAK1, JAK2, JAK3, and TYK2. peficitinib 36-47 Janus kinase 2 Homo sapiens 96-100 30145050-6 2018 Interestingly, the binding modes of peficitinib in the ATP-binding pockets differed among JAK1, JAK2, JAK3, and TYK2. peficitinib 36-47 Janus kinase 3 Homo sapiens 102-106 30145050-6 2018 Interestingly, the binding modes of peficitinib in the ATP-binding pockets differed among JAK1, JAK2, JAK3, and TYK2. peficitinib 36-47 tyrosine kinase 2 Homo sapiens 112-116 28301084-0 2017 The Effect of Verapamil, a P-Glycoprotein Inhibitor, on the Pharmacokinetics of Peficitinib, an Orally Administered, Once-Daily JAK Inhibitor. peficitinib 80-91 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 28301084-3 2017 The effects of verapamil, an inhibitor of the efflux pump P-gp, on the pharmacokinetic profile of peficitinib were assessed in this open-label, single-center, single-sequence, crossover drug-interaction study. peficitinib 98-109 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 27878567-2 2017 Peficitinib and its major metabolite H2 inhibit the hepatic uptake transporter organic anion transporting polypeptide 1B1 (OATP1B1) in vitro. peficitinib 0-11 solute carrier organic anion transporter family member 1B1 Homo sapiens 79-121 27878567-2 2017 Peficitinib and its major metabolite H2 inhibit the hepatic uptake transporter organic anion transporting polypeptide 1B1 (OATP1B1) in vitro. peficitinib 0-11 solute carrier organic anion transporter family member 1B1 Homo sapiens 123-130 27878567-3 2017 This article reports a clinical study evaluating the effects of peficitinib on the pharmacokinetics of rosuvastatin, a substrate for the OATP1B1 transporter, and vice versa. peficitinib 64-75 solute carrier organic anion transporter family member 1B1 Homo sapiens 137-144 27878567-11 2017 Therefore, it is unlikely that peficitinib will have a clinically significant effect on the exposure of other substrates for OATP1B1. peficitinib 31-42 solute carrier organic anion transporter family member 1B1 Homo sapiens 125-132 28117214-5 2017 We found that peficitinib inhibited JAK1 and JAK3 with 50% inhibitory concentrations of 3.9 and 0.7 nM, respectively. peficitinib 14-25 Janus kinase 3 Rattus norvegicus 45-49 28117214-6 2017 Peficitinib also inhibited IL-2-dependent T cell proliferation in vitro and STAT5 phosphorylation in vitro and ex vivo. peficitinib 0-11 interleukin 2 Rattus norvegicus 27-31 28117214-6 2017 Peficitinib also inhibited IL-2-dependent T cell proliferation in vitro and STAT5 phosphorylation in vitro and ex vivo. peficitinib 0-11 signal transducer and activator of transcription 5A Rattus norvegicus 76-81 34924117-8 2022 Furthermore, production of RANKL by human osteoblasts was suppressed by peficitinib but enhanced by etanercept. peficitinib 72-83 TNF superfamily member 11 Homo sapiens 27-32 34248953-13 2021 PsAFLS cell invasion, migratory capacity and MMP1, 3, and 9 were suppressed following JAKi treatment, with Peficitinib showing the greatest effect. peficitinib 107-118 matrix metallopeptidase 1 Homo sapiens 45-49