Delving into the Latest Updates on DA-302168S with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

GLP-1R

Action

agonists

Mechanism

GLP-1R agonists(Glucagon-like peptide 1 receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

ObesityDiabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Chengdu Di'ao Pharmaceutical Group Co. Ltd.

Active Organization

Chengdu Di'ao Pharmaceutical Group Co. Ltd.

Inactive Organization-

License Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC33H24ClF2N3O5

InChIKeyZWQNIWWZDWNMQA-QFIPXVFZSA-N

CAS Registry2969158-02-7

Glucagon-like peptide-1 receptor (GLP-1R) holds pivotal importance as a therapeutic target for type 2 diabetes (T2D) and obesity. Several oral small-molecule agonists targeting GLP-1R have been developed to date. Nevertheless, these agonists suffer from several limitations, including low potency, poor pharmacokinetics, and unfavorable safety profiles. Here, we report the discovery of compound 29 (DA-302168S), which exhibits higher potency both in vitro/in vivo while mitigating the risk of drug-drug interaction compared to other reported candidate compounds. Preclinical studies show full efficacy in cAMP activation, glucose reduction, and appetite suppression. Safety assessments reveal minimal risks with hERG IC₅₀ > 30 μM and no significant off-target toxicity. Its favorable pharmacokinetics support once-daily oral dosing, improving patient compliance. These findings suggest that compound 29 offers a promising therapeutic option for the management of T2D and obesity. Notably, it has successfully completed phase I clinical trials and is currently undergoing phase II clinical trials.

100 Deals associated with DA-302168S

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Obesity	Phase 2	China	Chengdu Di'ao Pharmaceutical Group Co. Ltd.	26 Mar 2025
Diabetes Mellitus, Type 2	Phase 1	China	Chengdu Di'ao Pharmaceutical Group Co. Ltd.	18 Apr 2024