Drug intelligence / Profile preview

tislelizumab + pemetrexed + cisplatin

Development stage
Unknown
Lead developer
BeiGene
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
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Overview

Tislelizumab + pemetrexed + cisplatin is a combination regimen for the treatment of advanced nonsquamous non–small cell lung cancer (NSCLC). **Tislelizumab** is a humanized IgG4 anti–PD-1 monoclonal antibody engineered to minimize Fcγ receptor binding to macrophages, thus reducing antibody-dependent phagocytosis of T cells. It blocks the interaction of PD-1 with its ligands (PD-L1 and PD-L2), enhancing T-cell–mediated antitumor responses. **Pemetrexed** is a folate antimetabolite that inhibits several enzymes involved in purine and pyrimidine synthesis, impeding DNA and RNA synthesis in cancer cells. **Cisplatin** is a platinum-based chemotherapeutic that causes DNA cross-linking and apoptosis. The combination, as tested in the RATIONALE 304/BGB-A317-304 phase III trial, prolongs progression-free survival and improves objective response rates compared to chemotherapy alone in first-line treatment of advanced or metastatic nonsquamous NSCLC[1][2][5].

02

Targets

GART (GAR transformylase)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)DNA

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