Delving into the Latest Updates on BCD-115 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

JSC BIOCAD, JSC-BIOCAD

+ [1]

Target

CDK19 x CDK8

Mechanism

CDK19 inhibitors(Cyclin-dependent kinase 19 inhibitors), CDK8 inhibitors(Cyclin-dependent kinase 8 inhibitors)

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal Diseases

Active Indication

Breast Cancer

Inactive Indication-

Originator Organization

Biocad Medical, Inc.

Active Organization

Biocad Medical, Inc.

Inactive Organization

Biocad CJSC

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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CDK8 and its paralog CDK19 are cyclin-dependent kinases that are core components of the so-called Mediator complex that has essential roles as a positive and negative regulator of gene expression. Several efforts to develop inhibitors have yielded natural and synthetic ATP-competitive compounds including cortistatin A, Sel120, BCD-115, CCT251921 (1), and MSC2530818 (2). Here, we used a hybridization approach starting from CCT251921 and MSC2530818 to derive new inhibitors with the aim of developing highly potent and selective inhibitors of CDK8/19. Initial compounds suffered from rapid aldehyde oxidase-mediated metabolism. This liability was overcome by utilizing a pyrazolopyridine hinge binder with a chlorine at the C-3 position. These efforts resulted in JH-XVI-178 (compound 15), a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.

100 Deals associated with BCD-115

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