CYP2C8 - CYP2C8 Ligands

CYP2C8 Ligands

Following is a table of selected substrates, inducers and inhibitors of 2C8.

Inhibitors of CYP2C8 can be classified by their potency, such as:

  • Strong inhibitor being one that causes at least a five-fold increase in the plasma AUC values, or more than 80% decrease in clearance.
  • Moderate inhibitor being one that causes at least a two-fold increase in the plasma AUC values, or 50-80% decrease in clearance.
  • Weak inhibitor being one that causes at least a 1.25-fold but less than two-fold increase in the plasma AUC values, or 20-50% decrease in clearance.
Selected inducers, inhibitors and substrates of CYP2C8
Substrates Inhibitors Inducers
  • amodiaquine (antimalarial, anti-inflammatory)
  • cerivastatin (statin)
  • paclitaxel (chemotherapeutic)
  • repaglinide (antidiabetic)
  • torasemide (loop diuretic)
  • sorafenib (tyrosine kinase inhibitor)
  • rosiglitazone (antidiabetic) - converted to active metabolites

Strong:

  • gemfibrozil (hypolipidemic)

Moderate

  • trimethoprim (antibiotic)

Unspecified potency

  • thiazolidinediones (antidiabetic)
  • montelukast (leukotriene receptor antagonist)
  • quercetin (antiinflammatory)
  • rifampicin (antibiotic)

Where classes of agents are listed, there may be exceptions within the class.

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