Daraxonrasib (RMC-6236), marketed as Rasonque, was approved by the U.S. Food and Drug Administration (FDA) on August 26, 2026, to treat metastatic pancreatic cancer.

Daraxonrasib is the first broad RAS-targeted medicine and a potent, orally bioavailable, noncovalent RAS(ON) multi-selective tri-complex inhibitor. It directly targets the active, GTP-bound state of RAS by forming a complex with the intracellular chaperone protein cyclophilin A (CypA) and RAS, thereby blocking RAS-effector interactions and inhibiting downstream RAS signaling and tumor cell proliferation.

Daraxonrasib is a bRo5 macrocyclic molecule that occupies a unique composite binding pocket comprising CypA and the SWI/SWII regions of RAS(ON). Its structure-guided optimization enabled broad activity against multiple RAS mutant and wild-type variants.1️⃣

The synthesis of daraxonrasib (RMC-6236) incorporates a cyclopropanecarboxylic acid scaffold2️⃣. Cyclopropanecarboxylic acid derivatives feature a compact, conformationally constrained framework, while the three-membered ring and carboxylic acid group provide versatile handles for structural modification. These characteristics make cyclopropanecarboxylic acid scaffolds useful building blocks for the design and synthesis of bioactive molecules.

📰 References:
1️⃣ https://ir.revmed.com/news-releases/news-release-details/us-fda-approves-revolution-medicines-rasonquetm-daraxonrasib
2️⃣ http://doi.org/10.1021/acs.jmedchem.4c02314

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