Inhibition and induction of CYP enzymes in humans: an update
The cytochrome P450 (CYP) enzyme family is the most important enzyme system catalyzing
the phase 1 metabolism of pharmaceuticals and other xenobiotics such as herbal remedies …
the phase 1 metabolism of pharmaceuticals and other xenobiotics such as herbal remedies …
Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical …
AF Stepan, DP Walker, J Bauman… - Chemical research in …, 2011 - ACS Publications
Because of a preconceived notion that eliminating reactive metabolite (RM) formation with
new drug candidates could mitigate the risk of idiosyncratic drug toxicity, the potential for RM …
new drug candidates could mitigate the risk of idiosyncratic drug toxicity, the potential for RM …
Role of cytochrome P450 2C8 in drug metabolism and interactions
During the last 10-15 years, cytochrome P450 (CYP) 2C8 has emerged as an important drug-
metabolizing enzyme. CYP2C8 is highly expressed in human liver and is known to …
metabolizing enzyme. CYP2C8 is highly expressed in human liver and is known to …
Central role of mitochondria in drug-induced liver injury
D Pessayre, B Fromenty, A Berson… - Drug metabolism …, 2012 - Taylor & Francis
A frequent mechanism for drug-induced liver injury (DILI) is the formation of reactive
metabolites that trigger hepatitis through direct toxicity or immune reactions. Both events …
metabolites that trigger hepatitis through direct toxicity or immune reactions. Both events …
Recent advances in metabolism and toxicity of tyrosine kinase inhibitors
Q Zhao, ZE Wu, B Li, F Li - Pharmacology & Therapeutics, 2022 - Elsevier
Small molecule tyrosine kinase inhibitors (TKIs) are widely used as anticancer drugs
approved by US FDA. However, the toxicities of TKIs to multiple organs have greatly limited …
approved by US FDA. However, the toxicities of TKIs to multiple organs have greatly limited …
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure–activity relationships and discovery strategies to mitigate drug–drug interaction risks
STM Orr, SL Ripp, TE Ballard… - Journal of medicinal …, 2012 - ACS Publications
1. INTRODUCTION Cytochrome P450s (CYPs) constitute a superfamily of hemecontaining
enzymes that catalyze the oxidative metabolism of structurally diverse molecules including …
enzymes that catalyze the oxidative metabolism of structurally diverse molecules including …
Drug discovery for a new generation of covalent drugs
AS Kalgutkar, DK Dalvie - Expert opinion on drug discovery, 2012 - Taylor & Francis
Introduction: The design of target-specific covalent inhibitors is conceptually attractive
because of increased biochemical efficiency through covalency and increased duration of …
because of increased biochemical efficiency through covalency and increased duration of …
Chemicals and drugs forming reactive quinone and quinone imine metabolites
I Klopcic, MS Dolenc - Chemical research in toxicology, 2018 - ACS Publications
Quinones and quinone imines are highly reactive metabolites (RMs) able to induce
dangerous effects in vivo. They are responsible for all kinds of toxicity, for example …
dangerous effects in vivo. They are responsible for all kinds of toxicity, for example …
Activation/inactivation of anticancer drugs by CYP3A4: influencing factors for personalized cancer therapy
F Wang, X Zhang, Y Wang, Y Chen, H Lu… - Drug Metabolism and …, 2023 - ASPET
Cytochrome P450 3A4 (CYP3A4), one of the most important members of the cytochrome
P450 subfamily, is a crucial catalyst in the metabolism of numerous drugs. As it catalyzes …
P450 subfamily, is a crucial catalyst in the metabolism of numerous drugs. As it catalyzes …
A real-world pharmacovigilance study of FDA Adverse Event Reporting System (FAERS) events for osimertinib
Y Yin, Y Shu, J Zhu, F Li, J Li - Scientific reports, 2022 - nature.com
Osimertinib was a third-generation, irreversible epidermal growth factor receptor tyrosine
kinase inhibitor (EGFR-TKI), which approved by the US Food and Drug Administration (FDA) …
kinase inhibitor (EGFR-TKI), which approved by the US Food and Drug Administration (FDA) …