RMC-9805
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RMC-9805 is an
investigational drug The United States Food and Drug Administration's Investigational New Drug (IND) program is the means by which a pharmaceutical company obtains permission to start human clinical trials and to ship an experimental drug across state lines (usually ...
that selectively targets the G12D mutation in
KRAS ''KRAS'' ( Kirsten rat sarcoma virus) is a gene that provides instructions for making a protein called K-Ras, a part of the RAS/MAPK pathway. The protein relays signals from outside the cell to the cell's nucleus. These signals instruct the ce ...
dependent cancers. 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. RMC-9805 is currently in a phase 1/1b clinical trial for the treatment of KRAS G12D-mutant solid tumors. 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).


See also

*
ACBI3 ACBI3 is an experimental anticancer drug which is one of the first examples of a proteolysis targeting chimera or PROTAC. It is a bifunctional molecule with two halves joined by a linker; one half binds to a protein found in various forms of can ...
* Adagrasib *
MRTX1133 MRTX1133 is an investigational drug that targets the G12D mutation in KRAS dependent cancers. MRTX1133 was in a phase 1/2 clinical trial for the treatment of solid tumors, however the study was terminated in Q1 2025. MRTX1133 is considered to be ...
*
Olomorasib Olomorasib (LY3537982) is an experimental anticancer drug which acts as an inhibitor of the G12C mutant form of Kirsten rat sarcoma virus (KRAS), an oncogene commonly present in several forms of cancer. It is in early stage clinical trials again ...
*
Sotorasib Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for vario ...


References

Antineoplastic drugs Cyclopropyl compounds Piperazines Pyridines Methoxy compounds Trifluoromethyl compounds Indoles Morpholines Lactones Carboxamides Aziridines Cyclopentyl compounds Pyrazolidines Pyrrolidines {{antineoplastic-drug-stub