KPT-9274 + niacin

KPT-9274 + niacin is a combination therapy composed of **KPT-9274**, an orally bioavailable, first-in-class dual inhibitor of **p21-activated kinase 4 (PAK4)** and **nicotinamide phosphoribosyltransferase (NAMPT)**, and **niacin** (extended-release form), a form of vitamin B3. KPT-9274 exerts anti-tumor activity by blocking growth and survival signaling via PAK4 inhibition and suppressing cellular metabolism through NAMPT inhibition, leading to reduced **NAD^+** levels, cell cycle arrest, apoptosis, and impaired DNA repair. Niacin supplementation is co-administered to mitigate dose-limiting toxicities of KPT-9274—most notably kidney injury and EPO deficiency—without compromising anti-tumor efficacy. This combination is under clinical evaluation in cancers including advanced solid malignancies and non-Hodgkin’s lymphoma[1][3][5][6].

Other names

niacin ERvitamin B3 extended releasenicotinic acid extended release