CYP2B6 - CYP2B6 Ligands

CYP2B6 Ligands

Following is a table of selected substrates, inducers and inhibitors of CYP2B6.

Inhibitors of CYP2B6 can be classified by their potency, such as:

  • Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance.
  • Moderate inhibitor being one that causes at least a 2-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 2-fold increase in the plasma AUC values, or 20-50% decrease in clearance.
Substrates Inhibitors Inducers
  • Alfentanil (opioid analgesic)
  • Bupropion (antidepressant)
  • Cyclophosphamide (Alkylating antineoplastic agent)
  • Efavirenz (NNRTI)
  • Ifosfamide (Alkylating antineoplastic agent)
  • methadone (opiate replacement therapy)
  • Nevirapine (NNRTI)
  • Propofol (anesthetic)
  • Sertraline
  • sorafenib (protein kinase inhibitor)
  • tamoxifen (SERM)
  • Valproic acid (anticonvulsant)
Strong:
Orphenadrine (analgesic)

Unspecified potency

  • ticlopidine (antiplatelet)
  • ThioTEPA (anticancer)
  • Curcumin (constituent of turmeric)
  • rifampicin (bactericidal)
  • carbamazepine (anticonvulsant, mood stabilizer)
  • phenobarbital (anticonvulsant )
  • phenytoin (antiepileptic)

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