Drug intelligence / Profile preview

atorvastatin + erlotinib

Development stage
Preclinical
Lead developer
Roche
Modality
Small Molecules
Administration
Oral
01

Overview

Atorvastatin + erlotinib is a combination of two small molecule drugs, each with distinct mechanisms of action. Atorvastatin is an HMG-CoA reductase inhibitor (statin) used primarily to lower cholesterol and reduce cardiovascular risk by inhibiting the endogenous production of cholesterol in the liver. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used mainly in the treatment of certain cancers, such as non-small cell lung cancer and pancreatic cancer. Both drugs are metabolized by CYP3A4 and transported by OATP2B1, ABCB1, and ABCG2 transporters. Preclinical studies indicate that co-administration can result in pharmacokinetic interactions; specifically, atorvastatin may inhibit CYP3A-mediated metabolism of erlotinib, reducing its clearance, while erlotinib may lower systemic exposure to atorvastatin[3]. The combination has been explored for potential synergistic effects on tumor growth arrest but is not an approved or established fixed-dose pharmaceutical product[9][3].

02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)SLCO2B1 (Organic anion transporting polypeptide 2B1)SLCO1B3 (Organic anion transporting polypeptide 1B3)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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