Mesupron (upamostat)

Activation of the PLAU-PLAUR pathway is essential for the progression of hypoxia-associated LUAD exhibiting a collagenous phenotype. Blocking the pathway provides a new research perspective for the development of immunotherapy for LUAD.

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.

P2/3, N=61, Terminated, RedHill Biopharma Limited | N=310 --> 61 | Suspended --> Terminated; Part A complete; corporate decision made to cancel Part B.

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.

P2, N=300, Recruiting, Henry M. Jackson Foundation for the Advancement of Military Medicine | Not yet recruiting --> Recruiting

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.