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CYP Inhibition

Pharmaceutical Services > Drug Development Process > CYP Inhibition

The cytochrome P450s (CYPs) are a superfamily of isoforms, which play an important role in the oxidative metabolism of drugs. Each CYP isoform has a characteristic broad spectrum of catalytic activities of substrates. These are responsible for the large number of drug-drug interactions associated with CYP inhibition. When two or more drugs are administered concurrently, drug-drug interaction becomes a possibility. In vitro systems have been used as screening tools to predict the potential for in vivo drug-drug interaction. Extrapolation of in vitro drug interaction data to in vivo situations requires a good understanding of drug interactions. Ideally, a new drug candidate is not a potent CYP inhibitor or inducer and its metabolism is not readily inhibited by other drugs.

The CYP inhibition assay performed by CANTEST provides:

  • Supersomes and microsomes IC50 and Ki determination
  • Metabolic CYP pathway identification
  • Inhibition mechanism

 

 
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