Daraxonrasib

Daraxonrasib (RMC-6236) is an investigational new drug being evaluated by Revolution Medicines to treat advanced solid tumors with RAS mutations, especially metastatic pancreatic ductal adenocarcinoma (PDAC) containing KRAS G12X mutations.^[1] It has received a breakthrough therapy designation from the U.S. Food and Drug Administration.^[2]

Daraxonrasib

Clinical data
Other names	RMC-6236
Identifiers
IUPAC name trans-(1S,2S)-N-[(7S,13S)-21-ethyl-20-[2-[(1S)-1-methoxyethyl]-5-(4-methylpiperazin-1-yl)-3-pyridinyl]-17,17-dimethyl-8,14-dioxo-15-oxa-4-thia-9,21,27,28-tetrazapentacyclo[17.5.2.12,5.19,13.022,26]octacosa-1(25),2,5(28),19,22(26),23-hexaen-7-yl]-2-methylcyclopropane-1-carboxamide
CAS Number	2765081-21-6
PubChem CID	164726578
IUPHAR/BPS	13368
ChemSpider	115275938
UNII	B6T47Y2UAP
Chemical and physical data
Formula	C44H58N8O5S
Molar mass	811.06 g·mol−1
3D model (JSmol)	Interactive image
SMILES CCN1C2=C3C=C(C=C2)C4=CSC(=N4)C[C@@H](C(=O)N5CCC[C@H](N5)C(=O)OCC(CC3=C1C6=C(N=CC(=C6)N7CCN(CC7)C)[C@H](C)OC)(C)C)NC(=O)[C@H]8C[C@@H]8C
InChI InChI=InChI=1S/C44H58N8O5S/c1-8-51-37-12-11-28-19-31(37)33(40(51)32-20-29(23-45-39(32)27(3)56-7)50-16-14-49(6)15-17-50)22-44(4,5)25-57-43(55)34-10-9-13-52(48-34)42(54)35(21-38-46-36(28)24-58-38)47-41(53)30-18-26(30)2/h11-12,19-20,23-24,26-27,30,34-35,48H,8-10,13-18,21-22,25H2,1-7H3,(H,47,53)/t26-,27-,30-,34-,35-/m0/s1 Key:FVICRBSEYSHKFY-JYQNNKODSA-N

Daraxonrasib is an orally active, multi-selective RAS inhibitor that uses a novel tri-complex mechanism to target the active, GTP-bound form of RAS proteins, including mutant and wild-type types. Unlike conventional RAS inhibitors, it first binds to the chaperone-like protein cyclophilin A to form a complex, which then attaches to active RAS. This interaction blocks downstream effector binding and inhibits oncogenic signaling.^[3]

As of 2025, Daraxonrasib clinical trial is in phase 3 to assess efficacy compared to current standard-of-care chemotherapy.^[4]