Delving into the Latest Updates on ABT-046 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

DGAT1

Mechanism

DGAT1 inhibitors(Diacylglycerol O-acyltransferase 1 inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Hyperlipidemias

Originator Organization

Abbott Laboratories

Active Organization-

Inactive Organization

Abbott Laboratories

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC20H22N4O2

InChIKeyBWUXSHHOKODNAK-HDJSIYSDSA-N

CAS Registry1031336-60-3

Author: Rozema, Michael J. ; Beno, David W. A. ; Dayton, Brian D. ; Falls, Hugh D. ; Gao, Ju ; Klix, Russel C. ; Cullen, Steven C. ; Xin, Xili ; Plata, Dan ; Larson, Kelly J. ; Wang, Xiaojun ; Judd, Andrew S. ; Hansen, T. Matthew ; King, Andrew J. ; Dhaon, Madhup K. ; Voorbach, Martin J. ; Yeh, Vince S. C. ; Reilly, Regina M. ; Lau, Yau Y. ; Marsh, Kennan C. ; Segreti, Jason A. ; Kym, Philip R. ; Zhao, Gang ; Brodjian, Sevan ; Brune, Michael E. ; Souers, Andrew J. ; Stoner, Eric J. ; Collins, Christine A. ; Cox, Bryan F. ; Grihalde, Nelson ; Mittelstadt, Scott W. ; Hajduk, Philip

A high-throughput screen against human DGAT-1 led to the identification of a core structure that was subsequently optimized to afford the potent, selective, and orally bioavailable compound 14. Oral administration at doses ≥0.03 mg/kg significantly reduced postprandial triglycerides in mice following an oral lipid challenge. Further assessment in both acute and chronic safety pharmacology and toxicology studies demonstrated a clean profile up to high plasma levels, thus culminating in the nomination of 14 as clinical candidate ABT-046.

100 Deals associated with ABT-046

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