Drug intelligence / Profile preview

LDT409

Development stage
Preclinical
Lead developer
University of Toronto
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

LDT409 is a novel small molecule fatty acid mimetic derived from cardanol, a component of cashew nut shell liquid. It acts as a partial pan-PPAR agonist, with potent and balanced affinity for peroxisome proliferator-activated receptor alpha (PPARα) and gamma (PPARγ), and weak activity at PPARδ. Mechanistically, LDT409 functions as a partial agonist at both PPARα and PPARγ, promoting hepatic fatty acid oxidation, reducing hepatic steatosis, decreasing fat accumulation in adipose tissue, increasing lipolysis, inducing browning of white adipose tissue (WAT), upregulating thermogenic genes such as Ucp1, lowering food intake and hyperlipidemia, improving insulin tolerance, increasing energy expenditure and systemic fat utilization. Preclinical studies in mice have shown that LDT409 reverses diet-induced obesity and metabolic dysfunction-associated steatotic liver disease (MASLD), with additional benefits for dyslipidemia and diabetes mellitus. The compound is orally bioavailable with favorable pharmacokinetics supporting chronic dosing regimens[1][2][4][5][6][7][9].

02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)PPARA (Peroxisome proliferator-activated receptor alpha)PPARD (Peroxisome proliferator–activated receptor delta)

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