Drug intelligence / Profile preview

MDL 101146

Development stage
Preclinical
Modality
Peptides, Small Molecules
Administration
Oral
01

Overview

**MDL 101146** is a synthetic small molecule belonging to the class of dipeptides. It acts as an orally active and potent inhibitor of human neutrophil elastase (HNE), a serine proteinase implicated in the degradation of connective tissue macromolecules and associated with chronic inflammatory diseases. In preclinical models such as collagen-induced arthritis in rats and hamsters it has demonstrated efficacy by reducing joint swelling and clinical scores. The compound is notable for its metabolic stability compared to related analogs[1][3][5][7]. Its primary mechanism involves direct inhibition of HNE activity.

Other names
N-(4-(4-Morpholinylcarbonyl)benzoyl)valyl-N-(3,3,4,4,4-pentafluoro-1-(1-methylethyl)-2-oxobutyl)prolinamideL-Prolinamide, N-(4-(4-morpholinylcarbonyl)benzoyl)-L-valyl-N-(3,3,4,4,4-pentafluoro-1-(1-methylethyl)-2-oxobutyl)-(2S)-1-[(2S)-3-methyl-2-[[4-(morpholine-4-carbonyl)benzoyl]amino]butanoyl]-N-(5,5,6,6,6-pentafluoro-2-methyl–4–oxohexan–3–yl)pyrrolidine–2-carboxamideCHEMBL76746CHEMBL-76746CHEMBL 76746UNII:749Y52DBP2
02

Targets

ELANE (Human Neutrophil Elastase)

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