Concept of pharmacologic target‐mediated drug disposition in large‐molecule and small‐molecule compounds
G An - The Journal of Clinical Pharmacology, 2020 - Wiley Online Library
Target‐mediated drug disposition (TMDD) is a term to describe a nonlinear pharmacokinetic
(PK) phenomenon that is caused by high‐affinity binding of a compound to its …
(PK) phenomenon that is caused by high‐affinity binding of a compound to its …
Importance of Target‐Mediated Drug Disposition (TMDD) of Small‐Molecule Compounds and Its Impact on Drug Development—Example of the Class Effect of HSD‐1 …
With more potent drug candidates being developed, the incidence of target‐mediated drug
disposition (TMDD) in small‐molecule compounds has significantly increased in the past …
disposition (TMDD) in small‐molecule compounds has significantly increased in the past …
Covalent immune proximity-induction strategy using SuFEx-engineered bifunctional viral peptides
HM McCann, BPM Lake, KS Hoffman… - ACS Chemical …, 2022 - ACS Publications
Covalent antibody recruiting molecules (cARMs) constitute a proximity-inducing chemical
strategy to modulate the recognition and elimination of cancer cells by the immune system …
strategy to modulate the recognition and elimination of cancer cells by the immune system …
Pharmacokinetic modeling of warfarin І–model-based analysis of warfarin enantiomers with a target mediated drug disposition model reveals CYP2C9 genotype …
The objective of this study is to characterize the impact of the CYP2C9 genotype on warfarin
drug-drug interactions when warfarin is taken together with fluconazole, a cytochrome P450 …
drug-drug interactions when warfarin is taken together with fluconazole, a cytochrome P450 …
A physiological-based pharmacokinetic model embedded with a target-mediated drug disposition mechanism can characterize single-dose warfarin pharmacokinetic …
Warfarin, a commonly prescribed oral anticoagulant medication, is highly effective in treating
deep vein thrombosis and pulmonary embolism. However, the clinical dosing of warfarin is …
deep vein thrombosis and pulmonary embolism. However, the clinical dosing of warfarin is …
[HTML][HTML] Population Target-Mediated Pharmacokinetic/Pharmacodynamic Modeling to Evaluate SPI-62 Exposure and Hepatic 11β-Hydroxysteroid Dehydrogenase …
N Wu, DA Katz, G An - Clinical pharmacokinetics, 2023 - Springer
Introduction SPI-62 is a small-molecule 11β-hydroxysteroid dehydrogenase type 1 (HSD-1)
inhibitor exhibiting complicated nonlinear pharmacokinetics (PK) in human. Previously, we …
inhibitor exhibiting complicated nonlinear pharmacokinetics (PK) in human. Previously, we …
A Target‐Mediated Drug Disposition Model to Explain Nonlinear Pharmacokinetics of the 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor SPI‐62 in Healthy …
SPI‐62 is a selective and potent small‐molecule inhibitor of 11β‐hydroxysteroid
dehydrogenase type 1 (HSD‐1). SPI‐62 has demonstrated substantial and complex …
dehydrogenase type 1 (HSD‐1). SPI‐62 has demonstrated substantial and complex …
[HTML][HTML] Rapid screening and in vivo target occupancy quantitative evaluation of xanthine oxidase inhibitors based on drug-target binding kinetics research strategy: A …
X Li, W Yang, H Chen, F Pan, W Liu, D Qi, S Yu… - Biomedicine & …, 2023 - Elsevier
Chrysanthemum morifolium Ramat. is a kind of food and drug dual-use traditional Chinese
medicine possessing multiple pharmacological and biochemical benefits. In our study, a …
medicine possessing multiple pharmacological and biochemical benefits. In our study, a …
A Pharmacometrics Model to Characterize a New Type of Target-Mediated Drug Disposition (TMDD)–Nonlinear Pharmacokinetics of Small-Molecule PF-07059013 …
In general, small-molecule target-mediated drug disposition (TMDD) is caused by the
interaction of a drug with its high-affinity, low-capacity pharmacological target. In the current …
interaction of a drug with its high-affinity, low-capacity pharmacological target. In the current …
Characterizing the Nonlinear Pharmacokinetics and Pharmacodynamics of BI 187004, an 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibitor, in Humans by a …
X Yuan, G An - The Journal of Clinical Pharmacology, 2024 - Wiley Online Library
BI 187004, a selective small‐molecule inhibitor of 11β‐hydroxysteroid dehydrogenase‐1
(11β‐HSD1), displayed complex nonlinear pharmacokinetics (PK) in humans. Following …
(11β‐HSD1), displayed complex nonlinear pharmacokinetics (PK) in humans. Following …