RPT1G

RPT1G is a first-in-class, small molecule hyperbolic inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), developed for oncology and other indications. Unlike previous NAMPT inhibitors that completely block enzyme activity and cause significant toxicity, RPT1G partially inhibits and stabilizes NAMPT in a catalytically active state, reducing but never fully eliminating its function. This unique mechanism allows selective targeting of cancer cells with high metabolic demand while preserving essential NAD+ biosynthesis in healthy cells, resulting in improved safety and efficacy profiles. Preclinical studies show robust single-agent activity against hematologic malignancies such as acute myeloid leukemia (AML) and B-cell acute lymphoblastic leukemia (B-ALL), as well as strong synergy with BCL-2 inhibitors like venetoclax and PARP inhibitors like olaparib—especially in resistant disease models. Remedy Plan Therapeutics is the developer, currently advancing RPT1G through Phase 1 clinical trials in healthy volunteers to support future oncology trials[1][3][4][5].