Olomorasib

Last updated
Olomorasib
Olomorasib structure.png
Identifiers
  • 4-[(13aS)-10-chloro-8-fluoro-6-oxo-2-prop-2-enoyl-1,3,4,12,13,13a-hexahydropyrazino[2,1-d][1,5]benzoxazocin-9-yl]-2-amino-7-fluoro-1-benzothiophene-3-carbonitrile
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
Formula C25H19ClF2N4O3S
Molar mass 528.96 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

References

  1. ↑ Peng SB, et al. Abstract 1259: Preclinical characterization of LY3537982, a novel, highly selective and potent KRAS-G12C inhibitor. Cancer Res (2021) 81 (13_Supplement): 1259. doi : 10.1158/1538-7445.AM2021-1259
  2. ↑ Miyashita H, Hong DS. Combining EGFR and KRAS G12C Inhibitors for KRAS G12C Mutated Advanced Colorectal Cancer. J Cancer Immunol (Wilmington). 2024;6(2):62-69. doi : 10.33696/cancerimmunol.6.086 PMID   39175850
  3. ↑ Hollebecque A, et al. 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 2024; 42: Number 3_suppl. doi : 10.1200/JCO.2024.42.3_suppl.94
  4. ↑ Burns TF, et al. 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 2024; 42: Number 16_suppl. doi : 10.1200/JCO.2024.42.16_suppl.8510
  5. ↑ Heist RS, et al. 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 2024; 42: Number 16_suppl. doi : 10.1200/JCO.2024.42.16_suppl.3007
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