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Darovasertib

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Chemical compound

Pharmaceutical compound
Darovasertib
Clinical data
Other namesIDE196, LXS196
Identifiers
IUPAC name
  • 3-amino-N--6-pyrazine-2-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC22H23F3N8O
Molar mass472.476 g·mol
3D model (JSmol)
SMILES
  • CC1(CCN(CC1)C2=C(N=CC=C2)NC(=O)C3=NC(=CN=C3N)C4=C(C=CC=N4)C(F)(F)F)N
InChI
  • InChI=InChI=1S/C22H23F3N8O/c1-21(27)6-10-33(11-7-21)15-5-3-9-29-19(15)32-20(34)17-18(26)30-12-14(31-17)16-13(22(23,24)25)4-2-8-28-16/h2-5,8-9,12H,6-7,10-11,27H2,1H3,(H2,26,30)(H,29,32,34)
  • Key:XXJXHXJWQSCNPX-UHFFFAOYSA-N

Darovasertib is an investigational new drug that is being evaluated for the treatment of metastatic uveal melanoma and other cancers. It is a first-in-class oral, small molecule inhibitor of protein kinase C (PKC).

It selectively targets mutant forms of PKC found in tumors with GNAQ or GNA11 mutations, which are present in approximately 90% of uveal melanoma cases. The U.S. Food and Drug Administration (FDA) granted orphan drug designation to darovasertib for the treatment of uveal melanoma on May 2, 2022, highlighting its potential to address an unmet medical need in this rare and aggressive form of eye cancer. As of 2024, darovasertib is in clinical development, with ongoing phase 1/2 trials evaluating its efficacy both as a monotherapy and in combination with other agents, such as binimetinib and crizotinib.

References

  1. ^ Cao L, Chen S, Sun R, Ashby CR, Wei L, Huang Z, et al. (2023). "Darovasertib, a novel treatment for metastatic uveal melanoma". Frontiers in Pharmacology. 14: 1232787. doi:10.3389/fphar.2023.1232787. PMC 10419210. PMID 37576814.
  2. Rodrigues A, Cosman R, Joshua AM (May 2023). "LXS196 for Metastatic Uveal Melanoma - finally some progress". British Journal of Cancer. 128 (10): 1791–1793. doi:10.1038/s41416-023-02199-w. PMC 10147608. PMID 36859685.
  3. "Darovasertib - IDEAYA Biosciences". AdisInsight. Springer Nature Switzerland AG.


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