Drug intelligence / Profile preview

RMC-6236 + 5-fluorouracil

Development stage
Unknown
Lead developer
REVOLUTION Medicines
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

**RMC-6236 + 5-fluorouracil** is an investigational combination therapy for solid tumors, specifically targeting cancers driven by KRAS mutations, such as colorectal and pancreatic cancers. RMC-6236 is an oral, non-covalent, multi-selective inhibitor of the active, GTP-bound state of both mutant and wild-type RAS isoforms, inhibiting RAS-GTP signaling and thereby blocking pathways critical to tumor cell growth and survival. 5-fluorouracil (5-FU) is an antimetabolite chemotherapeutic that inhibits thymidylate synthase and disrupts both DNA and RNA synthesis, leading to impaired cell division and apoptosis in rapidly dividing tumor cells. The combination is being evaluated in phase I/II clinical trials to determine safety and efficacy for advanced gastrointestinal cancers, reflecting an approach to block the oncogenic RAS pathway while impairing nucleic acid synthesis for synergistic antitumor activity[1][2][7][10].

Other names
Daraxonrasib + 5-fluorouracil
02

Targets

HRAS (H-Ras protein)TS (Thymidylate synthase)RNAP (Bacterial dna-dependent RNA polymerase)PPIA (Peptidyl-prolyl cis-trans isomerase A)

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