Delving into the Latest Updates on Monzosertib with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CDC7

Mechanism

CDC7 inhibitors(Cell division cycle 7-related protein kinase inhibitors)

Therapeutic Areas

Neoplasms

Active Indication

Solid tumor

Inactive Indication-

Originator Organization

Carna Biosciences, Inc.

Active Organization

Carna Biosciences, Inc.

Inactive Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

Login to view timeline

Structure

Molecular FormulaC21H22F3N5O4

InChIKeyDNTVXDZWVOVLOD-UHFFFAOYSA-N

CAS Registry1402057-88-8

CDC7, a serine-threonine kinase, plays conserved and important roles in regulation of DNA replication and has been recognized as a potential anticancer target. We report here the optimization of a series of furanone analogues starting from compound 1 with a focus on ADME properties suitable for clinical development. By replacing the 2-chlorobenzene moiety in 1 with various aliphatic groups, we identified compound 24 as a potent CDC7 inhibitor with excellent kinase selectivity and favorable oral bioavailability in multiple species. Oral administration of 24 demonstrated robust in vivo antitumor efficacy in a colorectal cancer xenograft model. Compound 24 (AS-0141) is currently in phase I clinical trials for the treatment of solid cancers.

100 Deals associated with Monzosertib

Login to view more data