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Elironrasib

Elironrasib
Clinical data
Other namesRMC-6291
Identifiers
  • 1-[4-(dimethylamino)-4-methylpent-2-ynoyl]-N-[(2S)-1-[[(6S,8S,14S)-22-ethyl-21-[2-[(1S)-1-methoxyethyl]-3-pyridinyl]-18,18-dimethyl-9,15-dioxo-5,16-dioxa-2,10,22,28-tetrazapentacyclo[18.5.2.12,6.110,14.023,27]nonacosa-1(26),20,23(27),24-tetraen-8-yl]amino]-3-methyl-1-oxobutan-2-yl]-4-fluoro-N-methylpiperidine-4-carboxamide
CAS Number
PubChem CID
UNII
ChEMBL
Chemical and physical data
FormulaC55H78FN9O8
Molar mass1012.282 g·mol−1
3D model (JSmol)
  • CCN1C2=C3C=C(C=C2)N4CCO[C@H](C4)C[C@@H](C(=O)N5CCC[C@H](N5)C(=O)OCC(CC3=C1C6=C(N=CC=C6)[C@H](C)OC)(C)C)NC(=O)[C@H](C(C)C)N(C)C(=O)C7(CCN(CC7)C(=O)C#CC(C)(C)N(C)C)F
  • InChI=InChI=1S/C55H78FN9O8/c1-13-64-44-19-18-37-30-40(44)41(48(64)39-16-14-24-57-46(39)36(4)71-12)32-53(5,6)34-73-51(69)42-17-15-25-65(59-42)50(68)43(31-38-33-63(37)28-29-72-38)58-49(67)47(35(2)3)61(11)52(70)55(56)22-26-62(27-23-55)45(66)20-21-54(7,8)60(9)10/h14,16,18-19,24,30,35-36,38,42-43,47,59H,13,15,17,22-23,25-29,31-34H2,1-12H3,(H,58,67)/t36-,38-,42-,43-,47-/m0/s1
  • Key:HJNFYLSFWYRSHS-CMZSUCOPSA-N

Elironrasib is an investigational new drug that is being developed by REVOLUTION Medicines for the treatment of solid tumors. It is a RAS(ON) G12C-Selective KRAS inhibitor.[1][2][3][4][5]

References

  1. ^ "Elironrasib - REVOLUTION Medicines". AdisInsight. Springer Nature Switzerland AG.
  2. ^ Wei X, Blaj C, Ali Al-Radhawi M, Lai LP, Maldonato BJ, Yang YC, et al. (June 2026). "Abrogation of Oncogenic RAS Signaling by a RAS(ON) Inhibitor Doublet Primes Immune-Refractory KRASG12C-Mutant NSCLC for Immune Checkpoint Blockade". Cancer Discovery. 16 (6): 1152–1175. doi:10.1158/2159-8290.CD-25-1616. PMC 13223541. PMID 41670434.
  3. ^ Solanki HS, Shah H, Imbody D, Desai B, Kato R, Miroshnychenko D, et al. (January 2026). "RAS-GTP Inhibition Overcomes Acquired Resistance to KRASG12C Inhibitors Mediated by Oncogenic and Wild-Type RAS Activation in Non-Small Cell Lung Cancer". Cancer Research. 86 (2): 467–484. doi:10.1158/0008-5472.CAN-25-0600. PMC 12962340. PMID 41165456.
  4. ^ ""The RAS Dam Has Broken"". Cancer Discovery. 16 (1): OF1. January 2026. doi:10.1158/2159-8290.CD-NW2025-0108. PMID 41405236.
  5. ^ Cregg J, Pota K, Tomlinson AC, Yano J, Marquez A, Liu Y, et al. (March 2025). "Discovery of Elironrasib (RMC-6291), a Potent and Orally Bioavailable, RAS(ON) G12C-Selective, Covalent Tricomplex Inhibitor for the Treatment of Patients with RAS G12C-Addicted Cancers". Journal of Medicinal Chemistry. 68 (6): 6041–6063. doi:10.1021/acs.jmedchem.4c02313. PMID 39993169.
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