Karpov, Alexei and Abrams, Tinya and Clark, Suzy and Raikar, Ankita and D'Alessio, Tony and Gesner, Tom and Jones, Darryl and Lacaud-Baumlin, Marion and Martyniuk, Piotr and Meredith, Erik and Mohseni, Mori and Nieto-Oberhuber, Cristina and Palacios, Daniel and Perruccio, Francesca and Zurini, Mauro and Bialucha, Carl (2018) Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates. ACS Medicinal Chemistry Letters. ISSN 19485875

Abstract

Antibody-Drug Conjugates (ADCs) are a novel modality which allows targeted delivery of potent therapeutic agents to the desired site. Herein we report our discovery of NAMPT inhibitors as a novel non-antimitotic payload for ADCs. The resulting anti-c-Kit conjugates (ADC-3 and ADC-4) demonstrated in vivo efficacy in the c-Kit positive gastrointestinal stromal tumor GIST-T1 xenograft model in a target-dependent manner.

Item Type:	Article
Date Deposited:	28 Jul 2018 00:45
Last Modified:	28 Jul 2018 00:45
URI:	https://oak.novartis.com/id/eprint/36030