Drug intelligence / Profile preview

4-MUST

Development stage
Phase 3
Lead developer
Valenta Pharm
Modality
Small Molecules
Administration
Oral
01

Overview

4-MUST is a pharmaceutical drug developed by Valenta Pharm JSC. It is a 128 mg tablet formulation containing trimebutine 4-methylumbelliferyl sulfate. Trimebutine is a multimodal small molecule drug primarily used for functional gastrointestinal disorders. Its mechanism of action involves acting as an agonist on peripheral mu, kappa, and delta opioid receptors, modulating the release of gastrointestinal peptides such as motilin, vasoactive intestinal peptide, gastrin, and glucagon. Additionally, it inhibits voltage-gated L-type calcium channels, inward rectifier potassium channels, and calcium-dependent potassium channels, and exhibits antagonistic effects on muscarinic acetylcholine receptors. These actions collectively regulate gastrointestinal motility, accelerating gastric emptying, inducing premature phase III of the migrating motor complex, and modulating colonic contractile activity, while also helping to relieve abdominal pain and modulate visceral sensitivity. 4-MUST is currently being investigated for the treatment of chronic cholecystitis and biliary dyskinesia.

Brand names
4-MUST
Other names
4-Methylumbelliferyl Trimebutine Sulfate
02

Targets

KCNN1 (Small conductance calcium-activated potassium channel protein 1)DOR (Opioid Receptor Delta 1)GCG (Glucagon)Kir (Inward-rectifier potassium channels)KOR (Kappa opioid receptor)MLNR (Human motilin receptor)MOR (Mu opioid receptor)mAChR (Muscarinic acetylcholine receptors)LTCC (Voltage-gated calcium channel (L-type))

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