Drug intelligence / Profile preview

gemcitabine + rigosertib

Development stage
Unknown
Lead developer
Onconova Therapeutics
Modality
Small Molecules
Administration
Intravenous
01

Overview

This combination drug consists of **gemcitabine**, a nucleoside antimetabolite that inhibits DNA synthesis, and **rigosertib** (ON 01910.Na), a first-in-class, small-molecule Ras mimetic that inhibits multiple signaling pathways including polo-like kinase 1 (PLK1) and phosphoinositide 3-kinase (PI3K). Developed as an antineoplastic regimen for metastatic pancreatic adenocarcinoma, the combination was studied in a phase II/III randomized controlled trial but failed to demonstrate improved survival or response compared to gemcitabine alone. Rigosertib acts as a non-ATP-competitive inhibitor of RAS signaling, PLK1, and PI3K pathways, potentially interfering with cell cycle progression and oncogenic signaling[1][3][5][7].

Brand names
Estybon
Other names
rigosertib + gemcitabine
02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)RBD (SARS-CoV-2 spike receptor-binding domain)DNAPLK1 (Polo like kinase 1)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)

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