Drug intelligence / Profile preview

RWJ-56423

Development stage
Preclinical
Lead developer
Johnson Services
Modality
Small Molecules
01

Overview

RWJ-56423 is an experimental small molecule inhibitor of human mast cell tryptase, a serine protease released during mast cell degranulation. It is a synthetic organic compound with the molecular formula C20H26N6O4S and has demonstrated potent and selective inhibition of tryptase in preclinical studies (Ki = 10 nM), with some activity against trypsin but selectivity over other serine proteases such as kallikrein, plasmin, and thrombin. The drug was developed by Johnson & Johnson for potential use in allergic or inflammatory disorders such as asthma. Although it showed promise in preclinical models for antagonizing antigen-induced asthmatic responses, it has not advanced beyond preclinical development[1][3][5][9][10].

Other names
(2S,4R)-1-acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-hydroxypyrrolidine-2-carboxamidebenzothiazole ketone (2S)-6
02

Targets

TPSB2 (Mast Cell Tryptase)PRSS1 (Trypsin family)

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