Drug intelligence / Profile preview

SBI-797812

Development stage
Preclinical
Lead developer
Sanford Burnham Prebys Medical Discovery Institute
Modality
Small Molecules
Administration
Oral, Intraperitoneal
01

Overview

SBI-797812 is a small molecule that acts as an **activator of nicotinamide phosphoribosyltransferase (NAMPT)**, a pivotal enzyme in the biosynthesis of NAD^+^. SBI-797812 binds to the NAMPT active site and shifts the enzyme’s equilibrium toward production of nicotinamide mononucleotide (NMN), the main NAD^+^ precursor in mammalian cells[1][3][5][6][8]. It increases NAMPT’s affinity for ATP, stabilizes its phosphorylated form, promotes pyrophosphate by-product consumption, and suppresses feedback inhibition of NAMPT by NAD^+^[1][2][3][8]. These actions boost NMN and NAD^+^ levels in cultured cells and elevate hepatic NAD^+^ in mice, making NAMPT a “super catalyst” for NAD^+^ biosynthesis[1][2][7]. SBI-797812 was developed from a high-throughput screen for NAMPT activators and is structurally similar to active-site NAMPT inhibitors[1]. Primary indication: research and potential therapy for conditions where NAD^+^ elevation may be beneficial, including metabolic and age-related disorders[1][2][3][8]. Current status: preclinical development[3].

02

Targets

NAMPT

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