Chemistry:RMC-9805
From HandWiki
RMC-9805, also known as Zoldonrasib, is an investigational drug that selectively targets the G12D mutation in KRAS dependent cancers.[1][2][3] RMC-9805 functions as molecular glue that forms a non-covalent ligand-mediated protein-protein interaction between cyclophilin A and GTP-bound RAS. Subsequent covalent modification of the mutant Asp12 residue affords selectivity over wild-type RAS.[4][5]
As of 2025, RMC-9805 is in a phase 1/1b clinical trial for the treatment of KRAS G12D-mutant solid tumors.[6] Preliminary data indicated that KRAS G12D–mutant PDAC patients dosed at 1200 mg daily or 600 mg twice daily achieved a 30% objective response rate (n = 12) and 80% disease control rate (n = 32).[7]
See also
References
- ↑ "RMC-9805". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800067273.
- ↑ "KRAS G12D inhibitor RMC-9805". NCI Drug Dictionary. National Cancer Institute. https://www.cancer.gov/publications/dictionaries/cancer-drug/def/kras-g12d-inhibitor-rmc-9805.
- ↑ "Next batter up! Targeting cancers with KRAS-G12D mutations". Trends in Cancer 9 (11): 955–967. November 2023. doi:10.1016/j.trecan.2023.07.010. PMID 37591766.
- ↑ "Targeting KRAS in Pancreatic Ductal Adenocarcinoma: The Long Road to Cure". Cancers 15 (20): 5015. October 2023. doi:10.3390/cancers15205015. PMID 37894382.
- ↑ "KRAS G12D targeted therapies for pancreatic cancer: Has the fortress been conquered?". Frontiers in Oncology 12: 1–9. November 2022. doi:10.3389/fonc.2022.1013902. PMID 36531078.
- ↑ Clinical trial number NCT06040541 for "Study of RMC-9805 in Participants With KRAS G12D-Mutant Solid Tumors" at ClinicalTrials.gov
- ↑ "RMC-9805 Triggers Tumor Regressions in KRAS G12D–Mutant Pancreatic Cancer". 2024-10-28. https://www.onclive.com/view/rmc-9805-triggers-tumor-regressions-in-kras-g12d-mutant-pancreatic-cancer.
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