Drug intelligence / Profile preview

lapatinib + pemetrexed

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Lapatinib + pemetrexed is a combination therapy consisting of two small molecule drugs used in oncology. Lapatinib is a dual tyrosine kinase inhibitor that targets the intracellular domains of both epidermal growth factor receptor (EGFR/ERBB1) and human epidermal growth factor receptor 2 (HER2/ERBB2), thereby inhibiting tumor cell proliferation driven by these pathways. Pemetrexed is an antifolate antineoplastic agent that disrupts folate-dependent metabolic processes essential for cell replication by inhibiting multiple enzymes involved in nucleotide synthesis, including thymidylate synthase. This combination has been studied primarily as a second-line treatment for advanced or metastatic non-small-cell lung cancer (NSCLC), with evidence suggesting it is well tolerated and has similar efficacy to pemetrexed monotherapy[1][3][2]. Lapatinib was developed by GlaxoSmithKline, while pemetrexed was developed by Eli Lilly.

Brand names
Tykerb + AlimtaTykerb + Pemfexy
02

Targets

DHFR (Dihydrofolate reductase)EGFR (Epidermal growth factor receptor)GART (GAR transformylase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TS (Thymidylate synthase)

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