Drug intelligence / Profile preview

ASP3082 + cisplatin + pemetrexed + pembrolizumab

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

This is a **combination regimen** consisting of *ASP3082*, *cisplatin*, *pemetrexed*, and *pembrolizumab* for the treatment of advanced solid tumors with KRAS G12D mutations. - **ASP3082** is an investigational, orally available small-molecule proteolysis-targeting chimera (PROTAC) that selectively degrades the KRAS G12D-mutated protein by recruiting E3 ubiquitin ligase, leading to targeted degradation of the oncoprotein in tumors. - **Cisplatin** is a platinum-based chemotherapy agent that forms DNA crosslinks inhibiting DNA synthesis and function. - **Pemetrexed** is an antifolate cytotoxic chemotherapy agent inhibiting multiple folate-dependent enzymes involved in nucleotide synthesis. - **Pembrolizumab** is a humanized monoclonal antibody targeting PD-1, acting as an immune checkpoint inhibitor to enhance antitumor immunity. This combination is being studied in Phase 1 clinical trials for adult patients with locally advanced or metastatic solid tumors harboring *KRAS G12D* mutations, including pancreatic, colorectal, and non-small cell lung cancers[1][4][7][9].

Other names
pembrolizumabcisplatinpemetrexed
02

Targets

DNATS (Thymidylate synthase)DHFR (Dihydrofolate reductase)PDCD1 (Programmed cell death protein 1 receptor)KRASG12D (Kirsten rat sarcoma viral oncogene homolog (KRAS) G12D mutant)

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