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Anticancer drug, cyclophosphamide, is metabolised in the body by glutathionation reaction. What is the type of this reaction ?

  • A.Reduction
  • B.Glucuronidation
  • C.Conjugation
  • D.Oxidation

Answer: C

Glutathionation is a conjugation reaction.

Drug metabolism runs in two phases. Phase I reactions (oxidation, reduction, hydrolysis) add or expose a functional group; cyclophosphamide is itself activated this way by liver cytochrome P450 enzymes. Phase II reactions conjugate the drug or its metabolite with an endogenous molecule to make it more water-soluble for excretion. Attaching glutathione, catalysed by glutathione S-transferases, is one of these, and it detoxifies reactive metabolites such as acrolein and phosphoramide mustard.

Reduction and oxidation are phase I reactions. Glucuronidation is also a conjugation, but with glucuronic acid, not glutathione, so it is not the name of this reaction.

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