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Calderasib

Calderasib
Clinical data
Other namesMK-1084
Identifiers
  • (5P,17aM)-20-chloro-2-[(2S,5R)-2,5-dimethyl-4-(prop-2-enoyl)piperazin-1-yl]-14,17-difluoro-6-(propan-2-yl)-11,12-dihydro-4H-1,18-ethenopyrido[4,3-e]pyrimido[1,6-g][1,4,7,9]benzodioxadiazacyclododecin-4-one
PubChem CID
UNII
ChEMBL
Chemical and physical data
FormulaC32H31ClF2N6O4
Molar mass637.08 g·mol−1
3D model (JSmol)
  • C[C@@H]1CN([C@H](CN1C(=O)C=C)C)C2=NC(=O)N3C4=C(C=CN=C4C(C)C)OCCOC5=C(C=CC(=C5C6=C(C=C2C3=N6)Cl)F)F
  • InChI=InChI=1S/C32H31ClF2N6O4/c1-6-24(42)39-14-18(5)40(15-17(39)4)30-19-13-20(33)27-25-21(34)7-8-22(35)29(25)45-12-11-44-23-9-10-36-26(16(2)3)28(23)41(31(19)37-27)32(43)38-30/h6-10,13,16-18H,1,11-12,14-15H2,2-5H3/t17-,18+/m1/s1
  • Key:BBIVCWWQPMOKAC-MSOLQXFVSA-N

Calderasib is an investigational new drug that is being developed by Merck Sharp & Dohme for the treatment of solid tumors. It targets tumors that express G12C mutated KRAS protein.[1][2][3]

It has been awarded a breakthrough therapy designation by the U.S. Food and Drug Administration.[4]

References

  1. ^ "Calderasib". AdisInsight. Springer Nature Switzerland AG. Retrieved 3 July 2026.
  2. ^ Ma X, Sloman DL, Duggal R, Anderson KD, Ballard JE, Bharathan I, et al. (July 2024). "Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor". Journal of Medicinal Chemistry. 67 (13): 11024–11052. doi:10.1021/acs.jmedchem.4c00572. PMID 38924388.
  3. ^ Remon J, La-Cava G, Borgeaud M, Saw SP, Hendriks LE, Ricciuti B (June 2026). "KRAS G12C-mutant non-small cell lung cancer: A practical guide for clinicians". Cancer Treatment Reviews. 147 103144. doi:10.1016/j.ctrv.2026.103144. PMID 42114275.
  4. ^ "FDA Grants Breakthrough Therapy Designation for Calderasib (MK-1084), an Investigational KRAS G12C Inhibitor, for Certain Patients with Newly Diagnosed Metastatic KRAS G12C-Mutant Non-Small Cell Lung Cancer (NSCLC)". Merck.com. Merck & Co., Inc. 2026-05-29.
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