Woolsey gets 3 US patents covering ROCK inhibitor Bravyl
2 formulations aimed at patients with swallowing difficulties
Woolsey Pharmaceuticals has received three new U.S. patents covering innovations related to Bravyl (oral fasudil), its investigational amyotrophic lateral sclerosis (ALS) medication.
The patents cover the use of oral fasudil to slow the progression of sporadic ALS, as well as solid and liquid formulations of fasudil for people with swallowing difficulties (dysphagia).
The new formulations are designed to be easier to swallow while retaining the efficacy and stability of the active ingredients. The drug’s developer, Woolsey Pharmaceuticals, said it will create a dysphagia-friendly formulation of Bravyl, to be called Bravyl-DF.
“These robust and strategically vital patents are part of 36 patent families we have filed for fasudil, a number of which have already issued,” Sven Jacobson, Woolsey’s CEO, said in a company press release. “These newest patents serve to reaffirm our unwavering commitment to driving innovation in ALS treatment.”
People with ALS often have elevated levels of the Rho kinase (ROCK). The enzyme has many important roles, but it also counteracts nerve cell regeneration and growth and promotes inflammation and cell death. ROCK inhibitors have emerged as a promising therapeutic strategy to reduce nerve cell death in ALS and other neurodegenerative conditions. Bravyl is designed to treat sporadic ALS by targeting that protein.
ROCK inhibitor approved in Japan
Fasudil is approved in Japan for certain types of stroke. Studies in ALS animal models have shown that it can promote nerve cell regeneration and ease inflammation, leading to better motor function and prolonged survival.
Bravyl’s safety and efficacy are being tested in an open-label Phase 2a trial, REAL (NTC05218668), which is expected to enroll about 40 people with sporadic ALS at sites in the U.S. and Australia.
The trial is being conducted in two parts. First, 31 participants received a 180 mg daily dose of Bravyl for six months. Results showed that levels of neurofilament light chain (NfL), a biomarker of nerve cell damage that normally increases over time in ALS patients, decreased significantly, by 15.5%.
Compared with an external group of matched patients from an ALS study database, REAL participants also experienced a significantly slower decline in lung function and muscle strength — by 42% and 50%, respectively — and tended to have slower deterioration in the ability to perform everyday activities, as measured with the  ALS Functional Rating Scale-Revised (ALSFRS-R).
The treatment was generally well tolerated.
The second part of REAL is now testing a higher dose of 300 mg per day in about 15 more patients to help determine the optimal dose for a future Phase 2b trial. In both parts of the trial, patients had the option to continue receiving Bravyl for an additional 2.5 years.
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