Olomorasib
Clinical data
Other namesLY3537982
Identifiers
  • (4M)-2-amino-4-[(4aS)-8-chloro-10-fluoro-12-oxo-3-(prop-2-enoyl)-2,3,4,4a,5,6-hexahydro-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-1-benzothiophene-3-carbonitrile
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC25H19ClF2N4O3S
Molar mass528.96 g·mol−1
3D model (JSmol)
  • C=CC(=O)N1CCN2[C@H](C1)CCOC3=C(C(=C(C=C3C2=O)F)C4=C5C(=C(SC5=C(C=C4)F)N)C#N)Cl
  • InChI=1S/C25H19ClF2N4O3S/c1-2-18(33)31-6-7-32-12(11-31)5-8-35-22-14(25(32)34)9-17(28)20(21(22)26)13-3-4-16(27)23-19(13)15(10-29)24(30)36-23/h2-4,9,12H,1,5-8,11,30H2/t12-/m0/s1
  • Key:OZUPICRWMLEFCS-LBPRGKRZSA-N

Olomorasib (LY3537982) is an experimental anticancer drug which acts as an inhibitor of the G12C mutant form of Kirsten rat sarcoma virus (KRAS), an oncogene commonly present in several forms of cancer. It is in early stage clinical trials against lung and colorectal cancers and advanced solid tumors.[1][2][3][4][5]

See also

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References

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  1. ^ Peng SB, Si C, Zhang Y, Van Horn RD, Lin X, Gong X, et al. (July 2021). "Preclinical characterization of LY3537982, a novel, highly selective and potent KRAS-G12C inhibitor". Cancer Research. 81 (13_Supplement): 1259. doi:10.1158/1538-7445.AM2021-1259.
  2. ^ Miyashita H, Hong DS (2024). "Combining EGFR and KRAS G12C Inhibitors for KRAS G12C Mutated Advanced Colorectal Cancer". Journal of Cancer Immunology. 6 (2): 62–69. doi:10.33696/cancerimmunol.6.086. PMC 11340593. PMID 39175850.
  3. ^ Hollebecque A, Kuboki Y, Murciano-Goroff YR, Yaeger R, Cassier PA, Heist RS, et al. (2024). "Efficacy and safety of LY3537982, a potent and highly selective KRAS G12C inhibitor in KRAS G12C-mutant GI cancers: Results from a phase 1 study". Journal of Clinical Oncology. 42 (3_suppl): 94. doi:10.1200/JCO.2024.42.3_suppl.94.
  4. ^ Burns TF, Dragnev KH, Fujiwara Y, Murciano-Goroff YR, Lee DH, Hollebecque A, et al. (2024). "Efficacy and safety of olomorasib (LY3537982), a second-generation KRAS G12C inhibitor (G12Ci), in combination with pembrolizumab in patients with KRAS G12C-mutant advanced NSCLC". Journal of Clinical Oncology. 42 (16_suppl): 8510. doi:10.1200/JCO.2024.42.16_suppl.8510.
  5. ^ Heist RS, Koyama T, Murciano-Goroff YR, Hollebecque A, Cassier PA, Han J, et al. (2024). "Pan-tumor activity of olomorasib (LY3537982), a second-generation KRAS G12C inhibitor (G12Ci), in patients with KRAS G12C-mutant advanced solid tumors". Journal of Clinical Oncology. 42 (16_suppl): 3007. doi:10.1200/JCO.2024.42.16_suppl.3007.

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