Drug intelligence / Profile preview

lapatinib + topotecan

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

Overview

A combination therapy consisting of lapatinib, a dual tyrosine kinase inhibitor targeting EGFR and HER2, and topotecan, a topoisomerase I inhibitor. Lapatinib also inhibits breast cancer resistance protein (BCRP) and P-glycoprotein (Pgp), which are transporters involved in topotecan resistance. The combination was developed to potentially overcome resistance to topotecan through lapatinib's inhibition of these drug efflux transporters.

Other names: lapatinib + topotecan

Targets

ABCG2 (Breast cancer resistance protein)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)ABCB1 (P-glycoprotein)TOP1 (DNA Topoisomerase I)

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