Rmc-4630 (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 2 Clinical Trials
SHP2

Description

RMC-4630 is a SHP2 inhibitor being developed for treatment of KRAS-mutated colorectal cancers and other solid tumors. This compound targets the SHP2 phosphatase, which plays a critical role in oncogenic signaling pathways downstream of mutated KRAS proteins. In colorectal cancer, RMC-4630 is being evaluated in combination with MEK inhibitors like LY3214996 to provide dual pathway blockade in tumors harboring KRAS mutations.

Mechanism of Action

RMC-4630 selectively inhibits SHP2 (Src homology region 2 domain-containing phosphatase-2), an essential mediator of RAS/MAPK signaling. By blocking SHP2 activity, the drug disrupts the transmission of growth signals from mutated KRAS proteins, potentially leading to tumor growth inhibition. The combination approach with MEK inhibitors aims to overcome resistance mechanisms and enhance therapeutic efficacy.

Molecular Targets

Side Effects

Diarrhea Fatigue Nausea Rash Decreased appetite Vomiting Abdominal pain Elevated liver enzymes

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT04916236 Phase 1
Terminated
Combination Therapy of RMC-4630 and LY3214996 in Metastatic KRAS Mutant Cancers
Netherlands
NCT04185883 Phase 1
Active, not recruiting
Sotorasib Activity in Subjects With Advanced Solid Tumors With KRAS p.G12C Mutation (CodeBreak 101)
United States, Australia, Austria, Belgium, Canada, Germany, Italy, Japan, Nethe