RRx-001, a downregulator of the CD47- SIRPα checkpoint pathway, does not cause anemia or thrombocytopenia. (3rd April 2021)

• Record Type: Journal Article
• Authors: Oronsky, Bryan; Cabrales, Pedro; Caroen, Scott; Guo, Xiaoning; Scribner, Curtis; Oronsky, Arnold; Reid, Tony R.
• Is Part Of: Expert opinion on drug metabolism and toxicology. Volume 17:Number 4(2021)
• Page Start: 355
• Page End: 357
• Publication Date: 2021-04-03
• Subjects: Oncology -- immunotherapy -- checkpoint inhibitor -- CD47 -- SIRPα -- PPAR-γ -- antibody -- small molecule; Drugs -- Toxicology -- Periodicals; Drugs -- Metabolism -- Periodicals; 615.7
• DOI: 10.1080/17425255.2021.1876025
• Languages: English
• ISSNs: 1742-5255

Abstract

ABSTRACT: Introduction : The CD47 and SIRPα checkpoint pathway has garnered much interest within the anti-cancer research community, with multiple experimental checkpoint inhibitors targeting CD47 and SIRPα in development. The use of such checkpoint inhibitors may however be limited by hematologic toxicity. Areas covered : We report on RRx-001, the first known small molecule downregulator of CD47 and SIRPα, which has shown a lack of hematologic toxicity in clinical trials. Expert opinion : RRx-001 is the first reported small molecule downregulator of CD47 and SIRPα and lacks any notable hematologic or systemic toxicity as demonstrated in clinical trials to date. Small molecule RRx-001 could be used in combination with or in place of CD47 targeting antibodies for anti-cancer treatment.