PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 23444281-0 2013 Evaluation of the impact of UGT polymorphism on the pharmacokinetics and pharmacodynamics of the novel PPAR agonist sipoglitazar. sipoglitazar 116-128 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 28-31 24214217-0 2014 A model-based approach to analyze the influence of UGT2B15 polymorphism driven pharmacokinetic differences on the pharmacodynamic response of the PPAR agonist sipoglitazar. sipoglitazar 159-171 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 51-58 24214217-0 2014 A model-based approach to analyze the influence of UGT2B15 polymorphism driven pharmacokinetic differences on the pharmacodynamic response of the PPAR agonist sipoglitazar. sipoglitazar 159-171 peroxisome proliferator activated receptor alpha Homo sapiens 146-150 24214217-1 2014 The pharmacokinetics of sipoglitazar, a peroxisome proliferator activated receptor agonist, are subject to high inter-individual variability resulting from a polymorphism of the UGT2B15 genotype. sipoglitazar 24-36 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 178-185 24214217-5 2014 The effects on FPG and HbA1c could successfully be described for placebo, rosiglitazone, and sipoglitazar treated groups in all three UGT2B15 genotypes. sipoglitazar 93-105 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 134-141 24214217-7 2014 The current PK-PD analysis confirms that UGT2B15 genotype is a major determinant for differences in FPG and HbA1c response to sipoglitazar treatment between Type 2 Diabetes mellitus patients, due to related differences in drug exposure. sipoglitazar 126-138 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 41-48 22960998-0 2013 The effect of genetic polymorphisms in UGT2B15 on the pharmacokinetic profile of sipoglitazar, a novel anti-diabetic agent. sipoglitazar 81-93 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 39-46 22960998-1 2013 PURPOSE: Sipoglitazar was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARgamma, PPARalpha, and PPARdelta. sipoglitazar 9-21 peroxisome proliferator activated receptor alpha Homo sapiens 107-150 22960998-1 2013 PURPOSE: Sipoglitazar was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARgamma, PPARalpha, and PPARdelta. sipoglitazar 9-21 peroxisome proliferator activated receptor alpha Homo sapiens 152-156 22960998-1 2013 PURPOSE: Sipoglitazar was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARgamma, PPARalpha, and PPARdelta. sipoglitazar 9-21 peroxisome proliferator activated receptor gamma Homo sapiens 158-167 22960998-1 2013 PURPOSE: Sipoglitazar was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARgamma, PPARalpha, and PPARdelta. sipoglitazar 9-21 peroxisome proliferator activated receptor alpha Homo sapiens 169-178 22960998-1 2013 PURPOSE: Sipoglitazar was a novel, azolealkanoic acid derivative that possesses selective activity for the peroxisome proliferator-activated receptors (PPAR) PPARgamma, PPARalpha, and PPARdelta. sipoglitazar 9-21 peroxisome proliferator activated receptor delta Homo sapiens 184-193 22960998-3 2013 The aim of this analysis was to explore the influence of genetic polymorphism in UGT on the pharmacokinetics of sipoglitazar. sipoglitazar 112-124 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 81-84 22960998-9 2013 Subjects homozygous for the UGT2B15 D85Y variant (UGT2B15*2/*2) were exposed to greater plasma concentrations of sipoglitazar than subjects homozygous for the wild-type allele UGT2B15*1/*1 (3.26-fold higher) or heterozygous allele UGT2B15*1/*2 (2.16-fold higher). sipoglitazar 113-125 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 28-35 22960998-9 2013 Subjects homozygous for the UGT2B15 D85Y variant (UGT2B15*2/*2) were exposed to greater plasma concentrations of sipoglitazar than subjects homozygous for the wild-type allele UGT2B15*1/*1 (3.26-fold higher) or heterozygous allele UGT2B15*1/*2 (2.16-fold higher). sipoglitazar 113-125 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 50-57 22960998-9 2013 Subjects homozygous for the UGT2B15 D85Y variant (UGT2B15*2/*2) were exposed to greater plasma concentrations of sipoglitazar than subjects homozygous for the wild-type allele UGT2B15*1/*1 (3.26-fold higher) or heterozygous allele UGT2B15*1/*2 (2.16-fold higher). sipoglitazar 113-125 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 50-57 22960998-9 2013 Subjects homozygous for the UGT2B15 D85Y variant (UGT2B15*2/*2) were exposed to greater plasma concentrations of sipoglitazar than subjects homozygous for the wild-type allele UGT2B15*1/*1 (3.26-fold higher) or heterozygous allele UGT2B15*1/*2 (2.16-fold higher). sipoglitazar 113-125 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 50-57 22960998-10 2013 CONCLUSIONS: These results indicate that sipoglitazar clearance is substantially modified by UGT2B15 enzyme variants, with higher exposure observed in the UGT2B15*2/*2 genotype group. sipoglitazar 41-53 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 93-100 22960998-10 2013 CONCLUSIONS: These results indicate that sipoglitazar clearance is substantially modified by UGT2B15 enzyme variants, with higher exposure observed in the UGT2B15*2/*2 genotype group. sipoglitazar 41-53 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 155-162 23444281-0 2013 Evaluation of the impact of UGT polymorphism on the pharmacokinetics and pharmacodynamics of the novel PPAR agonist sipoglitazar. sipoglitazar 116-128 peroxisome proliferator activated receptor alpha Homo sapiens 103-107 23444281-5 2013 Model analysis demonstrated UGT2B15 genotype accounted significantly for the variability in sipoglitazar clearance; however, a small fraction of subjects had a clearance that could not be explained entirely by genotype. sipoglitazar 92-104 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 28-35 23444281-8 2013 In summary, UGT2B15 genotype is a strong predictor for sipoglitazar clearance; a greater clinical response observed in the UGT2B15*2/*2 genotype appears to confirm this. sipoglitazar 55-67 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 12-19 23444281-8 2013 In summary, UGT2B15 genotype is a strong predictor for sipoglitazar clearance; a greater clinical response observed in the UGT2B15*2/*2 genotype appears to confirm this. sipoglitazar 55-67 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 123-130 22028317-8 2012 From these results, it is shown that the metabolic pathway from sipoglitazar to M-I is an unusual one, in which sipoglitazar is initially metabolized to sipoglitazar-G1 by UDP-glucuronosyltransferase and then sipoglitazar-G1 is metabolized to M-I by O-dealkylation by CYP2C8 and deconjugation. sipoglitazar 64-76 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 268-274 23648677-1 2013 Recently, genotyping in clinical studies has revealed that UGT2B15 genetic polymorphism has an influence on the clinical pharmacokinetics of sipoglitazar. sipoglitazar 141-153 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 59-66 23648677-3 2013 A study using UGT-expressing supersomes revealed that sipoglitazar glucuronidation was more extensively catalyzed by UGT1A1, 1A3, 1A6, 2B4, and 2B15 than by other UGTs. sipoglitazar 54-66 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 14-17 23648677-3 2013 A study using UGT-expressing supersomes revealed that sipoglitazar glucuronidation was more extensively catalyzed by UGT1A1, 1A3, 1A6, 2B4, and 2B15 than by other UGTs. sipoglitazar 54-66 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 117-123 23648677-5 2013 In a correlation study between sipoglitazar glucuronidation and UGT isoform-specific activities, the glucuronidation of S-oxazepam, a specific substrate for UGT2B15, strongly correlated with that of sipoglitazar, as compared with that of beta-estradiol, a representative UGT1A1 substrate. sipoglitazar 31-43 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 64-67 23648677-5 2013 In a correlation study between sipoglitazar glucuronidation and UGT isoform-specific activities, the glucuronidation of S-oxazepam, a specific substrate for UGT2B15, strongly correlated with that of sipoglitazar, as compared with that of beta-estradiol, a representative UGT1A1 substrate. sipoglitazar 31-43 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 157-164 23648677-5 2013 In a correlation study between sipoglitazar glucuronidation and UGT isoform-specific activities, the glucuronidation of S-oxazepam, a specific substrate for UGT2B15, strongly correlated with that of sipoglitazar, as compared with that of beta-estradiol, a representative UGT1A1 substrate. sipoglitazar 31-43 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 271-277 23648677-5 2013 In a correlation study between sipoglitazar glucuronidation and UGT isoform-specific activities, the glucuronidation of S-oxazepam, a specific substrate for UGT2B15, strongly correlated with that of sipoglitazar, as compared with that of beta-estradiol, a representative UGT1A1 substrate. sipoglitazar 199-211 UDP glucuronosyltransferase family 1 member A complex locus Homo sapiens 64-67 23648677-5 2013 In a correlation study between sipoglitazar glucuronidation and UGT isoform-specific activities, the glucuronidation of S-oxazepam, a specific substrate for UGT2B15, strongly correlated with that of sipoglitazar, as compared with that of beta-estradiol, a representative UGT1A1 substrate. sipoglitazar 199-211 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 157-164 23648677-5 2013 In a correlation study between sipoglitazar glucuronidation and UGT isoform-specific activities, the glucuronidation of S-oxazepam, a specific substrate for UGT2B15, strongly correlated with that of sipoglitazar, as compared with that of beta-estradiol, a representative UGT1A1 substrate. sipoglitazar 199-211 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 271-277 23648677-7 2013 These in vitro findings indicate that UGT2B15 is principally responsible for sipoglitazar glucuronidation. sipoglitazar 77-89 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 38-45 23648677-8 2013 Moreover, the UGT2B15*2 mutation significantly increased the Km value of sipoglitazar in the kinetic analysis using recombinant His-tag UGT2B15*1- or *2-membrane fractions. sipoglitazar 73-85 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 14-21 23648677-8 2013 Moreover, the UGT2B15*2 mutation significantly increased the Km value of sipoglitazar in the kinetic analysis using recombinant His-tag UGT2B15*1- or *2-membrane fractions. sipoglitazar 73-85 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 136-143 23648677-9 2013 These results show that sipoglitazar is a good example to elucidate the relationship between phenotype and genotype for UGT2B15 from in vitro analysis. sipoglitazar 24-36 UDP glucuronosyltransferase family 2 member B15 Homo sapiens 120-127 22123126-0 2012 Metabolic fate of sipoglitazar, a novel oral PPAR agonist with activities for PPAR-gamma, -alpha and -delta, in rats and monkeys and comparison with humans in vitro. sipoglitazar 18-30 peroxisome proliferator activated receptor alpha Rattus norvegicus 45-49 22123126-0 2012 Metabolic fate of sipoglitazar, a novel oral PPAR agonist with activities for PPAR-gamma, -alpha and -delta, in rats and monkeys and comparison with humans in vitro. sipoglitazar 18-30 peroxisome proliferator-activated receptor gamma Rattus norvegicus 78-107 22123126-1 2012 Sipoglitazar is a novel anti-diabetic agent with triple agonistic activities on the human peroxisome proliferator-activated receptors, hPPAR-gamma, -alpha, and -delta. sipoglitazar 0-12 peroxisome proliferator activated receptor gamma Homo sapiens 135-166