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Drug intelligence / Profile preview
upamostat
- Development stage
- Phase 3
- Lead developer
- RedHill Biopharma
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Upamostat (RHB-107) is an orally bioavailable, first-in-class serine protease inhibitor originally developed by Heidelberg Pharma (formerly WILEX AG) and currently being developed by RedHill Biopharma. It acts as a prodrug of WX-UK1, targeting several human serine proteases including urokinase-type plasminogen activator (uPA), matriptase, and transmembrane protease serine 2 (TMPRSS2). By inhibiting these host-cell proteases, upamostat prevents viral entry (relevant for COVID-19 and potentially Ebola) and interferes with tumor cell invasion and metastasis. It is primarily being evaluated for the early outpatient treatment of COVID-19 in the Phase 2 ACESO PROTECT trial and has historical development in various cancers and inflammatory gastrointestinal diseases.
- Brand names
- Mesupron
- Other names
- upamostat
02
Targets
CTSL (Cathepsin L)TTSP (Type II transmembrane serine protease)PRSS2 (Trypsin-2)PRSS3 (Trypsin-3)PLAU (uPA)ST14 (Matriptase)TMPRSS2 (Transmembrane protease serine 2)
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