Delving into the Latest Updates on CHDI-390576 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

HDACs

Action

inhibitors

Mechanism

HDAC inhibitors(Histone deacetylase inhibitors)

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

CHDI Foundation, Inc.

Active Organization-

Inactive Organization

Biofocus, Inc.

CHDI Foundation, Inc.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC19H13F4N3O2

InChIKeyLMGDHGQJJLEAPQ-UHFFFAOYSA-N

CAS Registry1629729-98-1

Author: Dominguez, Celia ; Matthews, Kim L ; Breccia, Perla ; Maillard, Michel C ; Aziz, Omar ; Luckhurst, Christopher A ; Haughan, Alan F ; Yates, Dawn ; Stott, Andrew J ; Bürli, Roland W ; Beaumont, Vahri ; Raphy, Gilles ; Wishart, Grant ; Thomas, Beth ; Munoz-Sanjuan, Ignacio ; Lamers, Marieke ; Wall, Michael ; Leonard, Phil

We have identified a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor 22, with >500-fold selectivity over class I HDACs (1,2,3) and ∼150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform. Dose escalation pharmacokinetic analysis demonstrated that upon oral administration, compound 22 can reach exposure levels in mouse plasma, muscle and brain in excess of cellular class IIa HDAC IC₅₀ levels for ∼8 h. Given the interest in aberrant class IIa HDAC function for a number of neurodegenerative, neuromuscular, cardiac and oncology indications, compound 22 (also known as CHDI-390576) provides a selective and potent compound to query the role of class IIa HDAC biology, and the impact of class IIa catalytic site occupancy in vitro and in vivo.

100 Deals associated with CHDI-390576

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