Drug intelligence / Profile preview

ML00253764

Development stage
Preclinical
Lead developer
Millennium Pharmaceuticals
Modality
Small Molecules
Administration
Subcutaneous
01

Overview

ML00253764 is a brain-penetrant, nonpeptidic small molecule antagonist of the melanocortin 4 receptor (MC4R). Originally developed by Millennium Pharmaceuticals, it was identified for its potential to prevent tumor-induced weight loss (cachexia) and regulate energy homeostasis. More recently, ML00253764 has been investigated for its direct anticancer properties, demonstrating antiproliferative and proapoptotic activities in glioblastoma and breast cancer cell lines, particularly when combined with metronomic chemotherapy such as temozolomide.

Other names
2-[2-[2-(5-bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole2-[2-[2-(5-bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole hydrochlorideML 00253764ML00253764ML-00253764
02

Targets

MC3R (Melanocortin Receptor Type 3)MC4R (Melanocortin 4 receptor)MC5R (Melanocortin 5 Receptor)

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