Drug intelligence / Profile preview

RNK05047

Development stage
Phase 2
Lead developer
Ranok Therapeutics
Modality
Small Molecules
Administration
Intravenous (iv)
01

Overview

RNK05047 is a first-in-class, small-molecule, tumor-selective protein degrader that targets bromodomain-containing protein 4 (BRD4), a key epigenetic regulator of oncogenes such as MYC and BCL2 involved in diverse cancer types. Developed using Ranok Therapeutics' proprietary CHAMP (Chaperone-mediated Protein Degradation) technology, it works by binding both BRD4 and members of the heat-shock protein 90KD (HSP90) chaperone family. This chemically induced proximity leads to selective degradation of BRD4 via the ubiquitin-proteasome system in tumor cells, downregulating BRD4-regulated gene expression while sparing related BET proteins like BRD2 and BRD3. The approach aims to improve safety and efficacy compared to non-selective BET inhibitors by preferentially degrading BRD4 in tumors. Clinical trials are ongoing for advanced solid tumors and diffuse large B-cell lymphoma[1][3][5][7][9].

Other names
BRD4 protein degrader RNK05047BRD-4 protein degrader RNK05047BRD 4 protein degrader RNK05047
02

Targets

BRD4 (Bromodomain-containing protein 4)HSP90 (Heat shock protein 90 chaperone complex)

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