Darovasertib

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][2]

Other namesIDE196, LXS196

CAS Number

• 1874276-76-2

PubChem CID

• 118873253

IUPHAR/BPS

• 11186

Quick facts Clinical data, Other names ...

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

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It selectively targets PKC activation by constitutively active mutant forms GNAQ or GNA11, 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.^[3]