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Abbreviation : TDI
Long Form : time-dependent inhibition
No. Year Title Co-occurring Abbreviation
2020 A Physiologically Based Pharmacokinetic Model of Voriconazole Integrating Time-Dependent Inhibition of CYP3A4, Genetic Polymorphisms of CYP2C19 and Predictions of Drug-Drug Interactions. AUC, DDIs, PBPK, PK
2020 Critical Impact of Drug-Drug Interactions via Intestinal CYP3A in the Risk Assessment of Weak Perpetrators Using Physiologically Based Pharmacokinetic Models. AUC, DDI, DDIs, PBPK
2020 In Vitro Assessment of the Interaction Potential of Ocimum basilicum (L.) Extracts on CYP2B6, 3A4, and Rifampicin Metabolism. 25ODESRIF, GIT, HDI, HLM
2020 Mechanisms of Herb-Drug Interactions Involving Cinnamon and CYP2A6: Focus on Time-Dependent Inhibition by Cinnamaldehyde and 2-Methoxycinnamaldehyde. CA, HDI, MCA
2020 Metabolite Profiling and Reaction Phenotyping for the in Vitro Assessment of the Bioactivation of Bromfenac †. BI, HLM, UGT
2020 NADPH-Independent Inactivation of CYP2B6 and NADPH-Dependent Inactivation of CYP3A4/5 by PBD: Potential Implication for Assessing Covalent Modulators for Time-Dependent Inhibition. PBD
2020 Numerical analysis of time-dependent inhibition kinetics: comparison between rat liver microsomes and rat hepatocyte data for mechanistic model fitting. DEX, MBI, MIC, RLM, SCRH, SRH
2020 Predicting the Potential for Cannabinoids to Precipitate Pharmacokinetic Drug Interactions via Reversible Inhibition or Inactivation of Major Cytochromes P450. CBD, THC
2020 Time-dependent enzyme inactivation: Numerical analyses of in vitro data and prediction of drug-drug interactions. DDIs
10  2019 Critical Differences between Enzyme Sources in Sensitivity to Detect Time-Dependent Inactivation of CYP2C8. HLMs, KI
11  2019 Discovery of 2,4-diamino-5-cyanopyrimidine derivatives as protein kinase C theta inhibitors with mitigated time-dependent drug-drug interactions. PKCtheta
12  2019 In Vitro Assessment of Potential for CYP-Inhibition-Based Drug-Drug Interaction Between Vonoprazan and Clopidogrel. DDIs, HLMs
13  2019 Time-dependent inhibition (TDI) of CYP1A2 by a CYP3A4-mediated reactive metabolite: proposal for a novel mechanism of irreversible TDI by a non-suicide substrate. MBI
14  2018 2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety. MAP4K4
15  2018 A strategy for early-risk predictions of clinical drug-drug interactions involving the GastroPlusTM DDI module for time-dependent CYP inhibitors. ---
16  2018 An Assessment of the In Vitro Inhibition of Cytochrome P450 Enzymes, UDP-Glucuronosyltransferases, and Transporters by Phosphodiester- or Phosphorothioate-Linked Oligonucleotides. CHHs, DDIs, HLMs, UGTs
17  2018 Bush mint (Hyptis suaveolens) and spreading hogweed (Boerhavia diffusa) medicinal plant extracts differentially affect activities of CYP1A2, CYP2D6 and CYP3A4 enzymes. BD, HS
18  2018 Improved Predictions of Drug-Drug Interactions Mediated by Time-Dependent Inhibition of CYP3A. DDIs, DTZ, ERY, IVIVC, NDD, NDE, NV, TAO, VER
19  2018 Kinetic mechanism of time-dependent inhibition of CYP2D6 by 3,4-methylenedioxymethamphetamine (MDMA): Functional heterogeneity of the enzyme and the reversibility of its inactivation. CYP2D6, MDMA, MIC
20  2018 Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety. CYP3A4, MetID, SAR
21  2017 Apigenin, a novel candidate involving herb-drug interaction (HDI), interacts with organic anion transporter 1 (OAT1). HDI, OAT, OAT1
22  2017 Establishment of a novel hepatocyte model that expresses four cytochrome P450 genes stably via mammalian-derived artificial chromosome for pharmacokinetics and toxicity studies. TC-HepG2
23  2017 Preclinical evaluation of the potential for cytochrome P450 inhibition and induction of the selective ALK inhibitor, alectinib. ALK, HLM, NSCLC
24  2017 Risk Assessment Using Cytochrome P450 Time-Dependent Inhibition Assays at Single Time and Concentration in the Early Stage of Drug Discovery. DDI
25  2017 Time-dependent inhibition of PHD2. 2OG, HIFs, PHDs
26  2016 Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition. CYP3A4, MCH, MCHR1
27  2016 An improved substrate cocktail for assessing direct inhibition and time-dependent inhibition of multiple cytochrome P450s. MRM
28  2016 Application of Static Models to Predict Midazolam Clinical Interactions in the Presence of Single or Multiple Hepatitis C Virus Drugs. ASV, BCV, DCV, DDIs
29  2016 Development and validation of an in vitro, seven-in-one human cytochrome P450 assay for evaluation of both direct and time-dependent inhibition. HLM
30  2016 Inhibition of CYP2B6 by Medicinal Plant Extracts: Implication for Use of Efavirenz and Nevirapine-Based Highly Active Anti-Retroviral Therapy (HAART) in Resource-Limited Settings. EFV, HAART, HDI, NVP
31  2016 Mechanism-Based Inhibition of CYP3A4 by Podophyllotoxin: Aging of an Intermediate Is Important for in Vitro/in Vivo Correlations. ---
32  2016 Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI. LLE, mGluR2, PAMs, PK
33  2016 Single concentration loss of activity assay provides an improved assessment of drug-drug interaction risk compared to IC50-shift. LOA
34  2016 VX-509 (Decernotinib)-Mediated CYP3A Time-Dependent Inhibition: An Aldehyde Oxidase Metabolite as a Perpetrator of Drug-Drug Interactions. DDIs, HLMs
35  2015 Azole antifungal inhibition of buprenorphine, methadone and oxycodone in vitro metabolism. EDDP, HLMs
36  2015 Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility. NAMPT
37  2015 Integration of Physiologically-Based Pharmacokinetic Modeling into Early Clinical Development: An Investigation of the Pharmacokinetic Nonlinearity. FIH, PBPK, PKs
38  2015 Optimization of 2,4-diamino-5-fluoropyrimidine derivatives as protein kinase C theta inhibitors with mitigated time-dependent drug-drug interactions and P-gp liability. P-gp, PKCtheta
39  2015 Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acyl CoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities. CYP3A4
40  2015 P450-Based Drug-Drug Interactions of Amiodarone and its Metabolites: Diversity of Inhibitory Mechanisms. AMIO, DDEA, DDIs, MDEA
41  2015 Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System. ---
42  2015 Time-Dependent Inhibition of hOAT1 and hOAT3 by Anthraquinones. hOAT1, MDCK
43  2014 A numerical method for analysis of in vitro time-dependent inhibition data. Part 1. Theoretical considerations. MM
44  2014 A numerical method for analysis of in vitro time-dependent inhibition data. Part 2. Application to experimental data. ---
45  2014 Cocktail-substrate approach-based high-throughput assay for evaluation of direct and time-dependent inhibition of multiple cytochrome P450 isoforms. DDIs, DI, NCEs
46  2014 Evaluation of drug interaction potential of Labisia pumila (Kacip Fatimah) and its constituents. P-gp, PXR
47  2014 Exploring concepts of in vitro time-dependent CYP inhibition assays. ---
48  2014 Physiologically based pharmacokinetic modeling for assessing the clinical drug-drug interaction of alisporivir. HCV, PBPK
49  2014 Solving time-dependent CYP3A4 inhibition for a series of indole-phenylacetic acid dual antagonists of the PGD(2) receptors CRTH2 and DP. ---
50  2013 Effect of solvents on the time-dependent inhibition of CYP3A4 and the biotransformation of AZD3839 in human liver microsomes and hepatocytes. hHEP, HLM
51  2013 Evaluations of in vitro metabolism, drug-drug interactions mediated by reversible and time-dependent inhibition of CYPs, and plasma protein binding of MMB4 DMS. 4-PA, CYP1A2, DMS, INA, MMB4
52  2013 In vitro inhibition of methadone and oxycodone cytochrome P450-dependent metabolism: reversible inhibition by H2-receptor agonists and proton-pump inhibitors. EDDP, HLM, PPIs
53  2013 Inhibition of CYP2C19 and CYP3A4 by omeprazole metabolites and their contribution to drug-drug interactions. DDI
54  2013 Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism. ID
55  2013 Prediction of crizotinib-midazolam interaction using the Simcyp population-based simulator: comparison of CYP3A time-dependent inhibition between human liver microsomes versus hepatocytes. AUC, HLM, HSP
56  2012 Assessment of the time-dependent inhibition (TDI) potential of test compounds with human liver microsomes by IC50 shift method using a nondilution approach. DDIs
57  2012 Discovery of novel PI3-kinase delta specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition. ---
58  2012 Drug-drug interaction potential of marketed oncology drugs: in vitro assessment of time-dependent cytochrome P450 inhibition, reactive metabolite formation and drug-drug interaction prediction. DDI
59  2012 Evaluation of time-dependent cytochrome p450 inhibition in a high-throughput, automated assay: introducing a novel area under the curve shift approach. ---
60  2012 Predicting drug interaction potential with a physiologically based pharmacokinetic model: a case study of telithromycin, a time-dependent CYP3A inhibitor. AUC, CYP3A4, i.v, PBPK, PK
61  2012 Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. ---
62  2012 Statistical methods for analysis of time-dependent inhibition of cytochrome p450 enzymes. ---
63  2012 The current status of time dependent CYP inhibition assay and in silico drug-drug interaction predictions. DDI
64  2012 Use of a multistaged time-dependent inhibition assay to assess the impact of intestinal metabolism on drug-drug interaction potential. AUC
65  2011 Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. CB, RMs
66  2011 CYP3A time-dependent inhibition risk assessment validated with 400 reference drugs. ---
67  2011 Determination of time-dependent inactivation of CYP3A4 in cryopreserved human hepatocytes and assessment of human drug-drug interactions. HLM
68  2011 Evaluation of different approaches to identifying a higher throughput assay for time-dependent inhibition (TDI). pHLM
69  2011 Identification of cytochrome P450 (CYP) isoforms involved in the metabolism of corynoline, and assessment of its herb-drug interactions. HLMs
70  2011 Reversible time-dependent inhibition of cytochrome P450 enzymes by duloxetine and inertness of its thiophene ring towards bioactivation. SNRI
71  2010 Integrated in silico-in vitro strategy for addressing cytochrome P450 3A4 time-dependent inhibition. DDIs, NCEs
72  2010 Time-dependent inhibition (TDI) of CYP3A4 and CYP2C9 by noscapine potentially explains clinical noscapine-warfarin interaction. ---
73  2010 Use of stable isotope labeled probes to facilitate liquid chromatography/mass spectrometry based high-throughput screening of time-dependent CYP inhibitors. HLM
74  2009 In vitro and in silico identification and characterization of thiabendazole as a mechanism-based inhibitor of CYP1A2 and simulation of possible pharmacokinetic drug-drug interactions. DDI, MBI, TBZ
75  2009 Mechanism-based inhibition of cytochrome P450 enzymes: an evaluation of early decision making in vitro approaches and drug-drug interaction prediction methods. DDI, PBPK
76  2009 Prediction of human drug-drug interactions from time-dependent inactivation of CYP3A4 in primary hepatocytes using a population-based simulator. CYP3A4, DDIs, HLM
77  2009 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. DDI, MBI, NMEs
78  2008 An examination of IC50 and IC50-shift experiments in assessing time-dependent inhibition of CYP3A4, CYP2D6 and CYP2C9 in human liver microsomes. ---
79  2008 The use of hepatocytes in evaluating time-dependent inactivation of P450 in vivo. ---
80  2008 Time-dependent inhibition of human drug metabolizing cytochromes P450 by tricyclic antidepressants. HLM, MBI, MIC, TCAs
81  2007 Differential time-dependent inactivation of P450 3A4 and P450 3A5 by raloxifene: a key role for C239 in quenching reactive intermediates. ---
82  2007 Kinetics of the time-dependent inactivation of CYP2D6 in cryopreserved human hepatocytes by methylenedioxymethamphetamine (MDMA). DEX, DF, MDMA
83  2007 Time-dependent CYP inhibition. MBI
84  2006 Pharmacokinetic consequences of time-dependent inhibition using the isolated perfused rat liver model. AUC
85  2002 Modeling phasic insulin release: immediate and time-dependent effects of glucose. TDP
86  1992 Responsiveness and memory of the pancreatic B-cells to the insulin secretagogues D-glucose and L-arginine in prediabetic and diabetic rabbits. TDP
87  1989 Beta-cell memory to insulin secretagogues: characterization of the time-dependent inhibitory control system in the isolated rat pancreas. TDP
88  1987 Biphasic insulin release as the expression of combined inhibitory and potentiating effects of glucose. TDP