Journal
AAPS JOURNAL
Volume 8, Issue 1, Pages E101-E111Publisher
SPRINGER
DOI: 10.1208/aapsj080112
Keywords
cytochrome P450; drug metabolism; toxicity; reactive metabolites
Categories
Funding
- NATIONAL CANCER INSTITUTE [R01CA090426] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF ENVIRONMENTAL HEALTH SCIENCES [P30ES000267, R01ES010546] Funding Source: NIH RePORTER
- NCI NIH HHS [R01 CA90426] Funding Source: Medline
- NIEHS NIH HHS [R01 ES10546, P30 ES00267] Funding Source: Medline
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The cytochrome P450 (P450) enzymes are the major catalysts involved in the metabolism of drugs. Bioavailability and toxicity are 2 of the most common barriers in drug development today, and P450 and the conjugation enzymes can influence these effects. The toxicity of drugs can be considered in 5 contexts: on-target toxicity, hypersensitivity and immunological reactions, off-target pharmacology, bioactivation to reactive intermediates, and idiosyncratic drug reactions. The chemistry of bioactivation is reasonably well understood, but the mechanisms underlying biological responses are not. In the article we consider what fraction of drug toxicity actually involves metabolism, and we examine how species and human interindividual variations affect pharmacokinetics and toxicity.
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