Drug intelligence / Profile preview

RRx-001 + cisplatin + carboplatin + etoposide

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

Overview

A combination regimen consisting of **RRx-001**, **cisplatin**, **carboplatin**, and **etoposide** used primarily in the investigational treatment of recurrent or refractory small cell lung cancer (SCLC). **RRx-001** is a novel, "shape-shifting" small molecule developed by EpicentRx that acts as an NLRP3 inflammasome inhibitor, Nrf2 inducer, nitric oxide superagonist, and exerts other mechanisms including inhibition of KEAP1, epigenetic modulation, and tumor microenvironment normalization. RRx-001 is chemically designed to resemble features of antibody-drug conjugates, containing a targeting moiety and a hypoxia-activated payload. Preclinical and clinical studies show RRx-001 can resensitize tumors to platinum drugs and reduce platinum-induced myelotoxicity[1][5]. When given with platinum chemotherapy agents (cisplatin or carboplatin) and etoposide, this regimen leverages the cytotoxic, DNA-damaging activity of cisplatin/carboplatin and etoposide (a topoisomerase II inhibitor) with the immunomodulating, antioxidant, and epigenetically modifying effects of RRx-001 to enhance antitumor activity and potentially mitigate adverse effects[1][5]. This combination is currently under investigation in the phase 3 REPLATINUM trial for SCLC[1][5].

02

Targets

CD47 (Cluster of Differentiation 47)Hb (Hemoglobin)KEAP1 (Kelch-like ECH-associated protein 1)TOP2A (DNA topoisomerase II)DNANLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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