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. 2021 Apr;17(4):355-357.
doi: 10.1080/17425255.2021.1876025. Epub 2021 Jan 22.

RRx-001, a downregulator of the CD47- SIRPα checkpoint pathway, does not cause anemia or thrombocytopenia

Bryan Oronsky  1 , Pedro Cabrales  2 , Scott Caroen  1 , Xiaoning Guo  3 , Curtis Scribner  1 , Arnold Oronsky  4 , Tony R Reid  1
Affiliations

RRx-001, a downregulator of the CD47- SIRPα checkpoint pathway, does not cause anemia or thrombocytopenia

Bryan Oronsky et al. Expert Opin Drug Metab Toxicol. 2021 Apr.

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.

Keywords: CD47; Oncology; PPAR-γ; SIRPα; antibody; checkpoint inhibitor; immunotherapy; small molecule.

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