SAN DIEGO—Neurana Pharmaceuticals, Inc., a biotechnology pharmaceutical company focused on the treatment of neuromuscular conditions, has announced the publication of a driving study which demonstrates the tolerability and safety of tolperisone in the Journal of Clinical Pharmacy and Therapeutics.
The article, entitled “An assessment of the centrally acting muscle relaxant tolperisone on driving ability and cognitive effects compared to placebo and cyclobenzaprine,” reports results from the Phase 1, three-way, randomized, blinded, three-period crossover study. As the article notes, the study “was designed to test the non‐inferiority of tolperisone relative to placebo, with a cyclobenzaprine test versus placebo to confirm the sensitivity of the driving simulator to detect treatment effects.”
Study participants who received tolperisone experienced no impact on driving performance compared to placebo; in contrast, participants who received cyclobenzaprine showed significant impairment compared to placebo (P < .01). Self-reported sleepiness, motivation and driving performance showed no significant effects for tolperisone compared to placebo. The study also notes that tolperisone only has a half‐life of 2‐3 hours, while cyclobenzaprine has a long half‐life of over 18 hours — so cyclobenzaprine accumulated in the system over the 3 dosing days.
The study used three criteria to demonstrate that tolperisone did not impair driving performance: “(1) driving performance (SDLP, a validated driving performance measure) was not statistically different from placebo following dosing on day 1, the morning following the first day of dosing (day 2) or on day 3 at steady state; (2) under all 3 tolperisone dosing conditions, SDLP did not exceed the upper limit of the 95% confidence interval for the effect of alcohol at 0.05% BAC; and (3) symmetry analysis showed that the distribution of the paired differences between placebo and tolperisone was not asymmetrical around zero (for all 3 tolperisone dosing conditions).”
“Given the effects of SMRs [skeletal muscle relaxants] on driving ability and their widespread use (in particularly cyclobenzaprine) in the treatment of LBP [lower back pain], the healthcare community has prioritized the need to develop an effective therapeutic option that is not associated with sleepiness, somnolence and driving impairment,” says the article.
The study participants who received active control cyclobenzaprine reported increased sleepiness (day 1), decreased motivation (days 1 and 2) and worse driving performance (days 1 and 2). Incidence of adverse events was similar for tolperisone and placebo, but was greater for cyclobenzaprine.
“The results from the study provide evidence that tolperisone does not impact driving ability nor cognitive function,” said Randall Kaye, M.D., chief medical officer of Neurana Pharmaceuticals. “Once efficacy is established, tolperisone may be able to treat patients without the common drowsiness and impact on cognitive functioning associated with other known skeletal muscle relaxants, potentially representing an important alternative for the treatment of acute muscle spasms.”