Search Results - "Yang, Tian J"
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Dose optimization of TBI-223 for enhanced therapeutic benefit compared to linezolid in antituberculosis regimen
Published in Nature communications (25-08-2024)“…TBI-223, a novel oxazolidinone for tuberculosis, is designed to provide improved efficacy and safety compared to linezolid in combination with bedaquiline and…”
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2
The Conduct of in Vitro Studies to Address Time-Dependent Inhibition of Drug-Metabolizing Enzymes: A Perspective of the Pharmaceutical Research and Manufacturers of America
Published in Drug metabolism and disposition (01-07-2009)“…Time-dependent inhibition (TDI) of cytochrome P450 (P450) enzymes caused by new molecular entities (NMEs) is of concern because such compounds can be…”
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3
Toxicity and toxicokinetic assessment of an anti-tubercular drug pretomanid in cynomolgus monkeys
Published in Toxicology reports (01-01-2022)“…Pretomanid is a nitroimidazooxazine antimycobacterial drug that was approved in more than 10 countries as part of a three-drug, all oral regimen, consisting of…”
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4
Role of Biotransformation Studies in Minimizing Metabolism-Related Liabilities in Drug Discovery
Published in The AAPS journal (01-03-2008)“…Metabolism-related liabilities continue to be a major cause of attrition for drug candidates in clinical development. Such problems may arise from the…”
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Single Ascending-Dose Study To Evaluate the Safety, Tolerability, and Pharmacokinetics of Sutezolid in Healthy Adult Subjects
Published in Antimicrobial agents and chemotherapy (19-04-2022)“…The primary objective of the study was to evaluate the safety and tolerability of single oral doses of sutezolid tablets administered under fasting conditions…”
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Effective Dosing Regimen of 1-Aminobenzotriazole for Inhibition of Antipyrine Clearance in Rats, Dogs, and Monkeys
Published in Drug metabolism and disposition (01-10-2002)“…1-Aminobenzotriazole (ABT) has been extensively used as a nonspecific inhibitor of cytochromes P450 (P450s) in animals for mechanistic studies, and antipyrine…”
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Advancing the Therapeutic Potential of Indoleamides for Tuberculosis
Published in Antimicrobial agents and chemotherapy (01-07-2019)“…Indole-2-carboxamide derivatives are inhibitors of MmpL3, the cell wall-associated mycolic acid transporter of In the present study, we characterized…”
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CONCURRENT INDUCTION AND MECHANISM-BASED INACTIVATION OF CYP3A4 BY AN l-VALINAMIDE DERIVATIVE
Published in Drug metabolism and disposition (01-09-2003)“…DPC 681 ( N -[(3-fluorophenyl)methyl]glycyl- N -{3-[((3-aminophenyl) sulfonyl)-2-(aminophenyl)amino]-(1 S ,2 S )-2-hydroxy-1-(phenyl-methyl)propyl}-3-methyl- l…”
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9
Phase 1 Study of the Effects of the Tuberculosis Treatment Pretomanid, Alone and in Combination With Moxifloxacin, on the QTc Interval in Healthy Volunteers
Published in Clinical pharmacology in drug development (01-06-2021)“…Tuberculosis (TB) continues to be a serious threat to public health throughout the world. Newer treatments are needed that could offer simplified regimens with…”
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Monoclonal Antibodies Specific and Inhibitory to Human Cytochromes P450 2C8, 2C9, and 2C19
Published in Drug metabolism and disposition (01-11-2001)“…Hybridomas were isolated that produce 13 monoclonal antibodies (mAbs) that are specific and highly inhibitory to members of the human P450 2C subfamily, 2C8,…”
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11
Role of cDNA-Expressed Human Cytochromes P450 in the Metabolism of Diazepam
Published in Biochemical pharmacology (15-03-1998)“…The metabolic conversion of diazepam (DZ) to temazepam (TMZ, a C3-hydroxylation product of DZ) and N-desmethyldiazepam (NDZ, an N1-demethylation product of DZ)…”
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Interaction of Ritonavir on Tissue Distribution of a [14C]L-Valinamide, a Potent Human Immunodeficiency Virus-1 Protease Inhibitor, in Rats Using Quantitative Whole-Body Autoradiography
Published in Drug metabolism and disposition (01-11-2002)“…N -[(3-fluorophenyl)methyl]glycyl- N -{3-[((3-aminophenyl)sulfonyl)- 2-(aminophenyl)amino]-(1 S ,2 S )-2-hydroxy-1-(phenylmethyl)propyl}- 3-methyl- l…”
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13
Effect of Phenobarbital on Hepatic CYP1A1 and CYP1A2 in the Ahr-Null Mouse
Published in Biochemical pharmacology (15-01-1998)“…Studies have suggested that phenobarbital (PB) induces members of the CYP1A subfamily by both transcriptional and post-transcriptional mechanisms. Using the…”
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Further characterization of the expression in liver and catalytic activity of CYP2B6
Published in The Journal of pharmacology and experimental therapeutics (01-09-1998)“…Previous studies in this laboratory have determined the lack of specificity of several antibody and substrate probes of CYP2B6. The goals of the current study…”
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Inhibitory monoclonal antibodies to human cytochrome P450 enzymes: a new avenue for drug discovery
Published in Trends in pharmacological sciences (Regular ed.) (01-11-1999)Get full text
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Eight Inhibitory Monoclonal Antibodies Define the Role of Individual P-450s in Human Liver Microsomal Diazepam, 7-Ethoxycoumarin, and Imipramine Metabolism
Published in Drug metabolism and disposition (01-01-1999)“…Eight inhibitory monoclonal antibodies (MAbs) individually specific to human cytochrome P-450 (P-450) 1A1, 1A2, 2A6, 2B6, 2C subfamily (2C8, 2C9, 2C18 and…”
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Inhibitory Monoclonal Antibody to Human Cytochrome P450 2B6
Published in Biochemical pharmacology (15-05-1998)“…The human cytochrome P450 2B6 metabolizes, among numerous other substrates, diazepam, 7-ethoxycoumarin, testosterone, and phenanthrene. A recombinant…”
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Targeted Disruption of the Microsomal Epoxide Hydrolase Gene
Published in The Journal of biological chemistry (20-08-1999)“…Microsomal epoxide hydrolase (mEH) is a conserved enzyme that is known to hydrolyze many drugs and carcinogens, and a few endogenous steroids and bile acids…”
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Targeted disruption of the microsomal epoxide hydrolase gene. Microsomal epoxide hydrolase is required for the carcinogenic activity of 7,12-dimethylbenz[a]anthracene
Published in The Journal of biological chemistry (20-08-1999)“…Microsomal epoxide hydrolase (mEH) is a conserved enzyme that is known to hydrolyze many drugs and carcinogens, and a few endogenous steroids and bile acids…”
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20
Application of 2D-ultrasonography in prenatal assessment of fetal thymus development
Published in Zhenduanxue Lilun yu Shijian (01-10-2021)“…Objective: To investigate the value of prenatal ultrasound measurement of thymus size and to determine whether maternal administration of euthyrox affects…”
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