Pathway Erlotinib Pathway, Pharmacokinetics

Model human liver cell showing genes involved in the transportation and metabolism of Erlotinib.
Erlotinib Pathway, Pharmacokinetics
erlotinib erlotinib abcb1 abcg2 cyp1a2 cyp3a5 cyp2c8 ugt1a1 cyp1a1 cyp3a4 egfr pathway
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Erlotinib is a synthetic anilinoquinazoline compound that selectively binds to the ATP-binding site of the epidermal growth factor receptor (EGFR)-TK, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain (PMID: 14676101; PMID: 15217965). Erlotinib also inhibits ATP-binding cassette transporter-mediated drug efflux, which in turn strongly increases the intracellular concentrations of co-administrated drug molecules that are transporter substrates. Erlotinib is given orally to adults with advanced stages of certain carcinomas, with diarrhea and rash as known adverse reactions.

After oral administration, erlotinib is widely distributed throughout the body. Erlotinib is metabolized in the liver by cytochrome P450s, primarily by CYP3A4 and CYP1A1, but CYP3A5 also plays a minor role in erlotinib metabolism. In addition to its role as an ABC transporter inhibitor, erlotinib has also been implicated as an inhibitor of CYP2C8 and UGT1A1 activity. Therefore, erlotinib may inhibit the metabolism of co-administered drugs that are substrates of CYP2C8 and UGT1A1.

Authors: Tina Hernandez-Boussard, David Flockhart, Xing Jian Lou.
M. Whirl-Carrillo, E.M. McDonagh, J. M. Hebert, L. Gong, K. Sangkuhl, C.F. Thorn, R.B. Altman and T.E. Klein. "Pharmacogenomics Knowledge for Personalized Medicine" Clinical Pharmacology & Therapeutics (2012) 92(4): 414-417. Full text
Therapeutic Categories:
  • Anticancer agents

Entities in the Pathway

Genes (9)

Drugs/Drug Classes (1)

Relationships in the Pathway

Arrow FromArrow ToControllersPMID
CYP2C8 CYP2C8 erlotinib
EGFR EGFR erlotinib
erlotinib OSI 420 CYP1A1, CYP1A2, CYP3A4, CYP3A5 11432895, 16166415, 16381666, 16490804, 16890575, 17575239, 19733976
UGT1A1 UGT1A1 erlotinib 19850672, 20580994
erlotinib erlotinib ABCB1, ABCG2 15155841, 15492275, 16651435, 17312388

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