Darovasertib

Darovasertib
Clinical data
Other names	IDE196, LXS196
Identifiers
	IUPAC name 3-amino-N-[3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl]-6-[3-(trifluoromethyl)pyridin-2-yl]pyrazine-2-carboxamide;
CAS Number	1874276-76-2;
PubChem CID	118873253;
IUPHAR/BPS	11186;
DrugBank	DB16059;
ChemSpider	57617794;
UNII	E0YF0M8O09;
KEGG	D12139;
ChEMBL	ChEMBL3982723;
Chemical and physical data
Formula	C22H23F3N8O
Molar mass	472.476 g·mol−1
3D model (JSmol)	Interactive image;
	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).^[1]

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.^[1] 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.^[1] 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.^[2]

References

^ ^a ^b ^c Cao L, Chen S, Sun R, Ashby CR, Wei L, Huang Z, Chen ZS (2023). "Darovasertib, a novel treatment for metastatic uveal melanoma". Frontiers in Pharmacology. 14: 1232787. doi:10.3389/fphar.2023.1232787. PMC 10419210. PMID 37576814.
^ "Darovasertib - IDEAYA Biosciences". AdisInsight. Springer Nature Switzerland AG.

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[Cao_2023-1] Cao L, Chen S, Sun R, Ashby CR, Wei L, Huang Z, Chen ZS (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] "Darovasertib - IDEAYA Biosciences". AdisInsight. Springer Nature Switzerland AG.

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