2. Academic Validation
  3. Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates

Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates

  • ACS Med Chem Lett. 2018 Jun 28;9(8):838-842. doi: 10.1021/acsmedchemlett.8b00254.
Alexei S Karpov 1,  Tinya Abrams 2,  Suzanna Clark 2,  Ankita Raikar 2,  Joseph A D'Alessio 2,  Michael P Dillon 2,  Thomas G Gesner 2,  Darryl Jones 1,  Marion Lacaud 1,  William Mallet 3,  Piotr Martyniuk 1,  Erik Meredith 2,  Morvarid Mohseni 2,  Cristina M Nieto-Oberhuber 1,  Daniel Palacios 2,  Francesca Perruccio 1,  Grazia Piizzi 1,  Mauro Zurini 1,  Carl Uli Bialucha 2
Affiliations

Affiliations

  • 1 Novartis Institutes for BioMedical Research, CH-4056 Basel, Switzerland.
  • 2 Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.
  • 3 Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.
PMID: 30128077 DOI: 10.1021/acsmedchemlett.8b00254
Abstract

Antibody-drug conjugates (ADCs) are a novel modality that allows targeted delivery of potent therapeutic agents to the desired site. Herein we report our discovery of NAMPT inhibitors as a novel nonantimitotic 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.

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