Drug intelligence / Profile preview

RRD-251

Development stage
Preclinical
Lead developer
H. Lee Moffitt Cancer Center & Research Institute
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

RRD-251 is a small molecule inhibitor that selectively disrupts the protein-protein interaction between the retinoblastoma tumor suppressor protein (Rb) and the Raf-1 kinase. Developed by researchers at the H. Lee Moffitt Cancer Center, RRD-251 targets a non-canonical signaling pathway where Raf-1 binds and phosphorylates Rb early in the cell cycle, facilitating E2F release and S-phase entry independently of the Mek/MAPK pathway. Preclinical studies in pancreatic adenocarcinoma models have shown that RRD-251 significantly reduces tumor cell proliferation, migration, and invasion while inducing apoptosis. It has also demonstrated synergistic effects when combined with gemcitabine and has shown efficacy in reducing primary tumor growth and liver metastasis in vivo.

02

Targets

RAF1 (c-Raf-1 (Y340D/Y341D))Retinoblastoma protein–Raf-1 proto-oncogene serine/threonine-protein kinase interfaceRB1 (Retinoblastoma-associated Protein)

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