Drug intelligence / Profile preview

Apatinib + pemetrexed

Development stage
Phase 4
Lead developer
Hengrui Therapeutics
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Apatinib + pemetrexed is a combination therapy used primarily in the treatment of advanced non-small cell lung cancer (NSCLC), especially after failure of prior lines of chemotherapy. Apatinib is an orally bioavailable small molecule tyrosine kinase inhibitor that selectively targets vascular endothelial growth factor receptor 2 (VEGFR2), thereby inhibiting tumor angiogenesis[3][5]. Pemetrexed is a folate analog antimetabolite that disrupts folate-dependent metabolic processes essential for cell replication and is approved for use in NSCLC and malignant pleural mesothelioma[7]. The combination has shown synergistic antitumor effects by enhancing antiangiogenic activity and delaying resistance to antiangiogenic therapy[2][5]. Clinical studies have demonstrated promising efficacy and manageable safety profiles for this regimen in heavily pretreated NSCLC patients[1][5].

Other names
apatinib mesylate
02

Targets

DHFR (Dihydrofolate reductase)GART (GAR transformylase)TS (Thymidylate synthase)VEGFR2 (Vascular endothelial growth factor receptor 2)

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