Delving into the Latest Updates on PF-06649298 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

NaCT

Mechanism

NaCT inhibitors(solute carrier family 13 member 5 inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Hyperlipidemias

Inactive Indication-

Originator Organization

China Pharmaceutical University

Active Organization

China Pharmaceutical University

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC16H22O5

InChIKeyQNFWRHKLBLSSPB-MRXNPFEDSA-N

CAS Registry1854061-16-7

In the face of escalating metabolic disease prevalence, largely driven by modern lifestyle factors, this study addresses the critical need for novel therapeutic approaches. We have identified the sodium-coupled citrate transporter (NaCT or SLC13A5) as a target for intervention. Utilizing rational drug design, we developed a new class of SLC13A5 inhibitors, anchored by the hydroxysuccinic acid scaffold, refining the structure of PF-06649298. Among these, LBA-3 emerged as a standout compound, exhibiting remarkable potency with an IC₅₀ value of 67 nM, significantly improving upon PF-06649298. In vitro assays demonstrated LBA-3's efficacy in reducing triglyceride levels in OPA-induced HepG2 cells. Moreover, LBA-3 displayed superior pharmacokinetic properties and effectively lowered triglyceride and total cholesterol levels in diverse mouse models (PCN-stimulated and starvation-induced), without detectable toxicity. These findings not only spotlight LBA-3 as a promising candidate for hyperlipidemia treatment but also exemplify the potential of targeted molecular design in advancing metabolic disorder therapeutics.

100 Deals associated with PF-06649298

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