Drug intelligence / Profile preview

mesupron + gemcitabine

Development stage
Unknown
Lead developer
Heidelberg Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Mesupron + gemcitabine is a combination therapy studied primarily in locally advanced or metastatic pancreatic cancer. **Mesupron** (also known as upamostat, WX-671, or LH011) is an orally available serine protease inhibitor prodrug that targets the human urokinase plasminogen activator (uPA) system, impacting extracellular matrix degradation and tumor metastasis. After administration, mesupron is converted to the active metabolite WX-UK1, a selective inhibitor of uPA and certain other serine proteases, leading to antineoplastic and antimetastatic effects. **Gemcitabine** is a nucleoside analog and antimetabolite cytotoxic drug that inhibits DNA synthesis in proliferating cells. The combination is under investigation to improve survival and response rates compared to gemcitabine monotherapy in pancreatic cancer[1][2][4].

Other names
WX-671 + gemcitabineupamostat + gemcitabineLH011 + gemcitabine
02

Targets

PLAU (uPA)DNA

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