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DRUG:

WX-UK1

i
Other names: WX-UK1, WX UK1
Associations
Trials
Company:
Heidelberg Pharma, RedHill
Drug class:
Serine protease inhibitor, uPAR inhibitor
Associations
Trials
11ms
Phase I Trial of Upamostat Combined With Gemcitabine in Locally Unresectable or Metastatic Pancreatic Cancer: Safety and Preliminary Efficacy Assessment. (PubMed, Cancer Med)
Combining LH011 at doses ranging from 100 to 600 mg with gemcitabine every 21 days demonstrated manageable safety and tolerability. However, tumor response did not significantly differ among the dose groups, suggesting the need for further investigation.
P1 data • Journal
|
CA 19-9 (Cancer antigen 19-9)
|
gemcitabine • Mesupron (upamostat) • WX-UK1
over1year
Combined Antitumor Effect of the Serine Protease Urokinase Inhibitor Upamostat and the Sphingosine Kinase 2 Inhibitor Opaganib on Cholangiocarcinoma Patient-Derived Xenografts. (PubMed, Cancers (Basel))
Mouse weights and PAX165 tumor volumes were measured. Tumor volumes in the upamostat, opaganib, and upamostat plus opaganib groups were significantly decreased compared to the control group.
Journal
|
PRSS3 (Serine Protease 3) • PRSS1 (Serine Protease 1) • SPHK1 (Sphingosine Kinase 1)
|
Mesupron (upamostat) • WX-UK1 • Yeliva (opaganib)
3years
MECHANISTIC EFFECTS OF UPAMOSTAT AND OPAGANIB IN CHOLANGIOCARCINOMA CELL LINES (AASLD 2022)
Upamostat and its active metabolite WX-UK1 have been shown to inhibit serine proteases. Upamostat and opaganib in combination have significant inhibitory effects on both CCA cell migration and viability in vitro which may prevent tumor progression. Both drugs have an established clinical safety profile and may be effective in targeted treatment of CCA patients.
Preclinical
|
HER-2 (Human epidermal growth factor receptor 2)
|
Mesupron (upamostat) • WX-UK1 • Yeliva (opaganib)