Potential PAH Treatment Shows Promising Preclinical Results

Potential PAH Treatment Shows Promising Preclinical Results

Reviva Pharmaceuticals recently announced promising preclinical efficacy data for RP5063, a novel dopamine-serotonin modulator for pulmonary arterial hypertension (PAH), at the American Thoracic Society (ATS) 2016 International Conference in California.

RP5063 is a potent inhibitor of serotonin 5-HT receptor, a novel target for the treatment of PAH. The orally active new chemical showed positive efficacy results in the treatment of PAH because it was found to reduce the mean pulmonary arterial pressure, decrease respiratory resistance, and bring blood oxygen levels back to normal.

Studies on RP5063 were conducted in a monocrotaline and a sugen-hypoxia induced PAH rat model – both considered gold standard animal models for evaluating efficacy against PAH. The animals’ histopathology demonstrated that RP5063 succeeded in significantly reducing pulmonary arterial vessels wall thickness and muscular tissue.

Recent research reports that more than 35% of patients with pulmonary hypertension also suffer from mental disorders that include major depressive and panic disorders.

Reviva Pharmaceuticals’ chief medical officer Dr. Marc Cantillon said, in a press release, that a significant number of PAH patients also deal with psychosis and anxiety.

“RP5063’s receptor binding profile has the potential to treat both PAH and any comorbid mental disorders which will make RP5063 especially beneficial in these patient populations,” Cantillon said.

PAH is a progressive, devastating condition characterized by severe constriction of the blood vessels in the lungs which increases blood pressure in pulmonary arteries. There is currently no cure for PAH but approved treatments that include phosphodiesterase-5 (PDE-5) inhibitors or endothelin receptor antagonists, can reduce and delay disease progression.

PAH patients face an estimated 5-year survival rate of 57% from diagnosis, according to data from the Registry to Evaluate Early and Long-term (REVEAL) PAH disease management in patients in the U.S.

Reviva’s founder and chief executive officer, Laxminarayan Bhat said the company would like to pursue an orphan drug designation from the U.S. Food and Drug Administration for RP5063.

“RP5063 novel mechanism of action and demonstrated preclinical proof-of-concept for PAH with functional and structural benefits are very encouraging,” Bhat said.

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