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CRPC - Possible repurposing of the drug Riociguat used for the management of chronic thromboembolic pulmonary hypertension

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Riociguat is a stimulator of soluble guanylate cyclase indicated for the management of persistent or recurrent chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension. This is in-vitro study shows the drug may be useful for CRPC.

“Riociguat decreased castration-resistant tumor growth and increased apoptotic markers, with elevated cGMP levels correlating significantly with lower tumor burden. Riociguat treatment reorganized the tumor vasculature and eliminated hypoxic tumor niches, decreasing CD44+ tumor progenitor cells and increasing the radiosensitivity of castration-resistant tumors. Thus, this study showed that enhancing sGC activity can inhibit CRPC emergence and progression through tumor cell–intrinsic and extrinsic effects. Riociguat can be repurposed to overcome CRPC, with noninvasive monitoring of cGMP levels as a marker for on-target efficacy.”

Stimulating Soluble Guanylyl Cyclase with the Clinical Agonist Riociguat Restrains the Development and Progression of Castration-Resistant Prostate Cancer

Cancer Res (2025) 85 (1): 134–153.

doi.org/10.1158/0008-5472.C...

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