Drug intelligence / Profile preview

D3S-001 + carboplatin + pemetrexed

Development stage
Unknown
Lead developer
D3 Bio
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

D3S-001 + carboplatin + pemetrexed is a combination therapy being investigated for the treatment of advanced solid tumors harboring the KRAS G12C mutation, including non-small cell lung cancer (NSCLC), colorectal cancer, pancreatic cancer, and other solid tumors. The combination consists of: - D3S-001, an orally administered, next-generation KRAS G12C inhibitor developed in China, designed to covalently and selectively inhibit KRAS G12C-mutant proteins in cancer cells, thereby blocking a key oncogenic driver pathway and halting tumor cell proliferation and survival. - Carboplatin, a platinum-based chemotherapeutic agent that causes DNA crosslinking and damage, leading to apoptosis in rapidly dividing cells. - Pemetrexed, a folate antimetabolite chemotherapy that inhibits multiple enzymes involved in purine and pyrimidine synthesis, disrupting DNA and RNA synthesis in tumor cells. This combination regimen is currently under evaluation in Phase 1 and Phase 2 clinical studies for patients with advanced solid tumors harboring the KRAS G12C mutation. Trials are assessing its safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary antitumor efficacy, particularly in patients resistant to other KRAS G12C inhibitors. D3S-001 has shown promising anti-tumor activity, high KRAS G12C target engagement, and manageable side effects. The combination arm with carboplatin and pemetrexed aims to enhance response rates by using both targeted and cytotoxic mechanisms[1][3][5].

02

Targets

GART (GAR transformylase)DHFR (Dihydrofolate reductase)DNAKRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)TS (Thymidylate synthase)

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