Drug intelligence / Profile preview

RRx-001 + taxane

Development stage
Unknown
Lead developer
EpicentRx
Modality
Small Molecules
Administration
Intravenous
01

Overview

RRx-001 + taxane refers to the combination therapy of the experimental small molecule RRx-001 (nibrozetone) and a taxane-class chemotherapy agent (such as paclitaxel or nab-paclitaxel). Developed by EpicentRx, RRx-001 is a first-in-class dinitroazetidine derivative that functions as a tumor-activated immunotherapy and chemosensitizer. Its primary mechanisms include the inhibition of the CD47-SIRPα axis and the NLRP3 inflammasome, which leads to the repolarization of tumor-associated macrophages (TAMs) from an immunosuppressive M2 phenotype to an immunostimulatory M1 phenotype. Additionally, RRx-001 acts as a nitric oxide donor under hypoxic conditions and has epigenetic modulating effects. The combination is being evaluated in the Phase 2 QUADRUPLE THREAT trial (NCT02489903) to determine if RRx-001 'priming' can resensitize patients with platinum-resistant small cell lung cancer (SCLC), non-small cell lung cancer (NSCLC), neuroendocrine tumors, and ovarian epithelial cancer to subsequent taxane-based or platinum-based chemotherapy regimens.

Other names
nibrozetone + taxane
02

Targets

CD47 (Cluster of Differentiation 47)KEAP1 (Kelch-like ECH-associated protein 1)Hb (Hemoglobin)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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