Drug intelligence / Profile preview

HM01

Development stage
Preclinical
Lead developer
Helsinn
Modality
Small Molecules
Administration
Oral
01

Overview

HM01 is a potent, centrally penetrant small molecule agonist of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a). It has high oral bioavailability and robust blood-brain barrier penetration, with demonstrated efficacy in animal models for alleviating constipation and delayed gastric emptying, and potential activity for treating neurodegenerative disease-related gastrointestinal dysfunction. HM01 exhibits strong binding affinity to human GHS-R1a (Ki ~1.4 nM) and efficiently activates receptor-mediated intracellular calcium signaling (EC50 ~1.25 nM). Its development is largely as a research tool and preclinical candidate for gastrointestinal motility disorders and potentially as a neuroprotectant.

Other names
ghrelin agonist HM013((1R)-1-(2,3-dichloro-4-methoxyphenyl)ethyl)-1-methyl-1-((4S)-1,3,3-trimethylpiperidin-4-yl)urea
02

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