Drug intelligence / Profile preview

ORG 43553

Development stage
Preclinical
Lead developer
Icahn School of Medicine
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

Org 43553 is a synthetic, low-molecular-weight, orally active allosteric agonist of the luteinizing hormone/choriogonadotropin receptor (LHCGR). Originally developed by Organon (later acquired by Schering-Plough and Merck & Co.) for the treatment of female infertility (ovulation induction), Org 43553 has been evaluated in Phase I clinical trials. More recently, researchers at the Icahn School of Medicine at Mount Sinai have investigated Org 43553 for the treatment of obesity, demonstrating that it acts directly on LHCGR in adipocytes to increase energy expenditure, reduce visceral fat accumulation, and promote a healthier body fat distribution without altering serum testosterone levels.

Other names
5-amino-2-methylsulfanyl-4-[3-(2-morpholin-4-yl-acetylamino)-phenyl]-thieno[2,3-d]pyrimidine-6-carboxylic acid tert-butylamidetert-butyl 5-amino-2-methylthio-4-(3-(2-(morpholin-4-yl)-acetamido)-phenyl)-thieno[2,3-d]pyrimidine-6-carboxamide
02

Targets

LHCGR (Luteinizing hormone/choriogonadotropin receptor)

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