Drug intelligence / Profile preview

9-ING-41 + irinotecan

Development stage
Phase 2
Lead developer
Actuate Therapeutics
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

**9-ING-41 + irinotecan** is an investigational combination therapy consisting of 9-ING-41, a first-in-class, intravenously administered, maleimide-based small molecule potent and selective inhibitor of **Glycogen Synthase Kinase-3 beta (GSK-3β)**, together with **irinotecan**, a topoisomerase I inhibitor used in cancer chemotherapy. 9-ING-41 acts by downregulating the NF-κB pathway and reducing the expression of NF-κB target genes, leading to suppressed tumor growth, induction of apoptosis, and overcoming chemotherapy resistance[1][3][5][7]. The combination is being studied in phase 1/2 clinical trials for advanced refractory malignancies, including pediatric cancers and pancreatic cancer, with the goal of enhancing the antitumor efficacy of standard cytotoxic chemotherapy such as irinotecan by sensitizing tumors to DNA-damaging agents[7].

02

Targets

TOP1 (DNA Topoisomerase I)GSK3 (Glycogen synthase kinase 3 beta)NF-κB

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