darovasertib

Darovasertib is a first-in-class, orally available small molecule inhibitor of protein kinase C (PKC) with potential antineoplastic and immunosuppressive activities. It selectively inhibits both conventional (α, β) and novel (δ, ϵ, η, θ) PKC isoforms by binding to PKC and blocking its activation. This inhibition disrupts PKC-mediated signaling pathways that are critical for tumor cell proliferation, survival, differentiation, invasion, and metastasis. Darovasertib is being developed primarily for the treatment of uveal melanoma—especially in tumors harboring GNAQ or GNA11 mutations—and has received orphan drug designation from the FDA for this indication. Clinical trials have shown promising activity as monotherapy and in combination with other agents such as binimetinib or crizotinib[1][3][4][5][6][7].

Other names

3-Amino-N-[3-(amino-4-methylpiperdin-1-yl)pyridine-2-yl]-6-[3-(trifluoromethyl)pyridine-2-yl]pyrazine-2-carboxamide