New European patent covers Reviva’s brilaroxazine in PH

Therapy improved lung function, reduced inflammation in PAH, IPF models

Patricia Inácio, PhD avatar

by Patricia Inácio, PhD |

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Reviva Pharmaceuticals has been granted a patent in Europe that covers using brilaroxazine, formerly RP5063, for pulmonary hypertension (PH).

The patent covers patients with pulmonary arterial hypertension (PAH) and those who develop PH associated with chronic obstructive pulmonary disease (COPD), an inflammatory lung disorder, or sickle cell disease.

“Building on […] promising clinical data, potent anti-inflammatory and antifibrotic [anti-scarring] activities and significant reduction in pulmonary arterial pressure has been shown in translational animal models for PAH following brilaroxazine treatment,” Laxminarayan Bhat, PhD, founder, president, and CEO of Reviva, said in a company press release. “We look forward to further evaluating brilaroxazine’s unique multimodal mechanism of action with clinical development expansion opportunities in PH and PAH.”

Brilaroxazine has also been granted patent protection in the U.S., China, and Japan.

“This latest patent further secures the broad therapeutic potential of brilaroxazine for inflammatory conditions driven by underlying disruption in serotonin signaling like pulmonary hypertension,” Bhat said.

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Studies back brilaroxazine’s effectiveness

Serotonin and dopamine are molecules best known as chemical messengers in the brain. Serotonin regulates mood, sleep, digestion, wound healing, and sexual desire, among other functions, whereas dopamine’s roles include tuning movement, memory, motivation, and mood. Both act by binding to protein receptors on the surface of cells.

Brilaroxazine has shown affinity and selectivity for serotonin and dopamine receptors. Research has revealed the role of both serotonin and dopamine receptors in blood vessels of the lung and therefore in developing PH. Modulating the activity of these receptors could help treat the disease.

In studies with animal models of PAH and idiopathic pulmonary fibrosis (IPF), meaning of an unknown cause, brilaroxazine improved lung function and reduced inflammation.

Based on this preclinical evidence, the U.S. Food and Drug Administration (FDA) granted orphan drug status to brilaroxazine for PAH and IPF. An orphan drug designation is designed to encourage therapies for rare and serious diseases through benefits such as exemption from FDA fees and seven years of market exclusivity, if approved.

Recent topline data from the Phase 3 RECOVER-1 clinical trial (NCT05184335) in people with schizophrenia showed brilaroxazine safely reduced key proinflammatory signaling molecules over a placebo.

“Brilaroxazine has demonstrated a favorable clinical safety and tolerability profile in over 800 subjects to date from multiple clinical trials,” Bhat said. “A significant reduction in key proinflammatory biomarkers following brilaroxazine treatment was recently shown in a large, global, pivotal Phase 3 study in patients with schizophrenia.”

A Conversation With Rare Disease Advocates