Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates
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 |
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Date Deposited: | 28 Jul 2018 00:45 |
Last Modified: | 28 Jul 2018 00:45 |
URI: | https://oak.novartis.com/id/eprint/36030 |