Drug intelligence / Profile preview

rh-endostatin + carboplatin + pemetrexed + pd-1 antibody

Development stage
Preclinical
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Recombinant Proteins and Enzymes, Small Molecules
Administration
Intravenous
01

Overview

This combination therapy integrates four distinct components with complementary mechanisms of action for treating advanced non-small cell lung cancer (NSCLC): 1. **rh-Endostatin (Endostar)**: A recombinant human endostatin that inhibits angiogenesis by blocking neovascularization and affecting multiple pathways including VEGF expression. It organizes neovascularization, facilitates chemotherapy drug entry into tumor cells, induces apoptosis of endothelial cells, and inhibits tumor growth and micrometastases[1][3]. 2. **Carboplatin**: A platinum-based chemotherapy agent that damages DNA in cancer cells, preventing replication. 3. **Pemetrexed**: An antifolate chemotherapy drug that inhibits multiple enzymes involved in folate metabolism and DNA synthesis. 4. **PD-1 antibody**: An immune checkpoint inhibitor that blocks the interaction between PD-1 on T cells and PD-L1 on tumor cells, enhancing T cell responses and mediating antitumor activity[6][8]. The combination aims to simultaneously target tumor vasculature, directly kill cancer cells, and activate the immune system against the tumor.

02

Targets

VEGFR2 (Vascular endothelial growth factor receptor 2)GART (GAR transformylase)PDCD1 (Programmed cell death protein 1 receptor)DHFR (Dihydrofolate reductase)DNAVEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)TS (Thymidylate synthase)

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