Reactive metabolites: current and emerging risk and hazard assessments

RA Thompson, EM Isin, MO Ogese… - Chemical Research …, 2016 - ACS Publications
Although idiosyncratic adverse drug reactions are rare, they are still a major concern to
patient safety. Reactive metabolites are widely accepted as playing a pivotal role in the …

Metabolic activation and drug‐induced liver injury: in vitro approaches for the safety risk assessment of new drugs

MJ Gómez‐Lechón, L Tolosa… - Journal of Applied …, 2016 - Wiley Online Library
Drug‐induced liver injury (DILI) is a significant leading cause of hepatic dysfunction, drug
failure during clinical trials and post‐market withdrawal of approved drugs. Many cases of …

Modeling reactivity to biological macromolecules with a deep multitask network

TB Hughes, NL Dang, GP Miller… - ACS central …, 2016 - ACS Publications
Most small-molecule drug candidates fail before entering the market, frequently because of
unexpected toxicity. Often, toxicity is detected only late in drug development, because many …

A post‐synthetically modified MOF for selective and sensitive aqueous‐phase detection of highly toxic cyanide ions

A Karmakar, N Kumar, P Samanta… - … A European Journal, 2016 - Wiley Online Library
Selective and sensitive detection of toxic cyanide (CN−) by a post‐synthetically altered metal–
organic framework (MOF) has been achieved. A post‐synthetic modification was employed …

Detection and characterization of ponatinib reactive metabolites by liquid chromatography tandem mass spectrometry and elucidation of bioactivation pathways

AA Kadi, HW Darwish, MW Attwa, SM Amer - RSC advances, 2016 - pubs.rsc.org
Ponatinib (PNT), as a multi-targeted tyrosine kinase inhibitor, is active against T315I and
other BCR-ABL mutants. PNT is registered in the US and EU under the trade name of …

Integrated reactive metabolite strategies

JG Kenna, RA Thompson - Metabolite Safety in Drug …, 2016 - Wiley Online Library
The success of in silico, in vitro, and in vivo methods for DNA‐damaging carcinogens
detection highlights the need to understand the mechanisms by which reactive metabolite …

[图书][B] Identification and mechanistic study of novel drug metabolites by LC-MS

S Martin - 2016 - search.proquest.com
Understanding the metabolic fate of drug candidates in vitro and in vivo is a key component
of drug development. Structural characterisation of drug candidate metabolites is important …