[HTML][HTML] Recent advances in the translation of drug metabolism and pharmacokinetics science for drug discovery and development

Y Lai, X Chu, L Di, W Gao, Y Guo, X Liu, C Lu… - … Pharmaceutica Sinica B, 2022 - Elsevier
Drug metabolism and pharmacokinetics (DMPK) is an important branch of pharmaceutical
sciences. The nature of ADME (absorption, distribution, metabolism, excretion) and PK …

Improving the accuracy of predicted human pharmacokinetics: lessons learned from the AstraZeneca drug pipeline over two decades

M Davies, RDO Jones, K Grime… - Trends in …, 2020 - cell.com
During drug discovery and prior to the first human dose of a novel candidate drug, the
pharmacokinetic (PK) behavior of the drug in humans is predicted from preclinical data. This …

Roles of selected non-P450 human oxidoreductase enzymes in protective and toxic effects of chemicals: review and compilation of reactions

SP Rendić, RD Crouch, FP Guengerich - Archives of Toxicology, 2022 - Springer
This is an overview of the metabolic reactions of drugs, natural products, physiological
compounds, and other (general) chemicals catalyzed by flavin monooxygenase (FMO) …

[HTML][HTML] Towards harmonization of test methods for in vitro hepatic clearance studies

J Louisse, M Alewijn, AACM Peijnenburg… - Toxicology in vitro, 2020 - Elsevier
Non-animal methods for toxicokinetics, such as in vitro hepatic metabolic clearance studies,
play an important role in chemical risk evaluations. To gain regulatory acceptance of such …

[HTML][HTML] Prioritization of mixtures of neurotoxic chemicals for biomonitoring using high-throughput toxicokinetics and mixture toxicity modeling

G Braun, BI Escher - Environment International, 2023 - Elsevier
Modern society continues to pollute the environment with larger quantities of chemicals that
have also become more structurally and functionally diverse. Risk assessment of chemicals …

Utility of chimeric mice with humanized liver for predicting human pharmacokinetics in drug discovery: comparison with in vitro–in vivo extrapolation and allometric …

Y Naritomi, S Sanoh, S Ohta - Biological and Pharmaceutical Bulletin, 2019 - jstage.jst.go.jp
Predicting human pharmacokinetics (PK) such as clearance (CL) and volume of distribution
(Vd) is a critical component of drug discovery. These predictions are mainly performed by in …

Fexinidazole optimization: enhancing anti-leishmanial profile, metabolic stability and hERG safety

AS Surur, CF Chan, FM Bartz, ILK Wong… - RSC Medicinal …, 2024 - pubs.rsc.org
The lack of adequate anti-leishmanial therapies has led to the continued suffering of millions
of people from developing nations. Moreover, optimism for a therapeutic intervention by …

Recent developments in predicting CYP-independent metabolism

NV Dhuria, B Haro, A Kapadia, KA Lobo… - Drug metabolism …, 2021 - Taylor & Francis
As lead optimization efforts have successfully reduced metabolic liabilities due to
cytochrome P450 (CYP)-mediated metabolism, there has been an increase in the frequency …

2, 3, 8-Trisubstituted quinolines with antimalarial activity

PDG Martinez, SH Krake, ML Poggi… - Anais da Academia …, 2018 - SciELO Brasil
Combination therapy drugs are considered a fundamental way to control malaria as it
mimimizes the risk of emergence of resistance to the individual partner drugs. Consequently …

Further considerations towards an effective and efficient oncology drug discovery DMPK strategy

B Williamson, N Colclough, AJ Fretland… - Current Drug …, 2020 - benthamdirect.com
Background: DMPK data and knowledge are critical in maximising the probability of
developing successful drugs via the application of in silico, in vitro and in vivo approaches in …