Delving into the Latest Updates on ACH-000143 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

MTNR1A x MTNR1B

Action

agonists

Mechanism

MTNR1A agonists(Melatonin receptor 1A agonists), MTNR1B agonists(Melatonin receptor 1B agonists)

Therapeutic Areas

Digestive System Disorders

Active Indication

Metabolic dysfunction-associated steatotic liver disease

Inactive Indication-

Originator Organization

Aché Laboratórios Farmacêuticos SA

Active Organization

Aché Laboratórios Farmacêuticos SA

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

The modulation of melatonin signaling in peripheral tissues holds promise for treating metabolic diseases like obesity, diabetes, and nonalcoholic steatohepatitis. Here, several benzimidazole derivatives have been identified as novel agonists of the melatonin receptors MT1 and MT2. The lead compounds 10b, 15a, and 19a demonstrated subnanomolar potency at MT1/MT2 receptors, high oral bioavailability in rodents, peripherally preferred exposure, and excellent selectivity in a broad panel of targets. Two-month oral administration of 10b in high-fat diet rats led to a reduction in body weight gain similar to dapagliflozin with superior results on hepatic steatosis and triglyceride levels. An early toxicological assessment indicated that 10b (also codified as ACH-000143) was devoid of hERG binding, genotoxicity, and behavioral alterations at doses up to 100 mg/kg p.o., supporting further investigation of this compound as a drug candidate.

100 Deals associated with ACH-000143

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