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lapatinib + esomeprazole

Development stage: Unknown
Lead developer: GSK
Modality: Small Molecules
Administration: Oral

Overview

This is not a fixed-dose combination product but represents a drug interaction between lapatinib (an oral tyrosine kinase inhibitor used for HER2-positive breast cancer) and esomeprazole (a proton pump inhibitor). When co-administered, esomeprazole significantly decreases lapatinib bioavailability by approximately 26% (range 6-49%) due to lapatinib's pH-dependent solubility. Lapatinib's aqueous solubility declines significantly at pH >4, which is affected by acid-reducing drugs like esomeprazole.

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)ATP4A (Potassium–transporting ATPase alpha chain 1)EGFR (Epidermal growth factor receptor)

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