Novel, oral therapeutic for migraine well-tolerated in healthy adults
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Key takeaways:
- BHV-2100 was tested in a small cohort of healthy adults aged 18 to 55 years.
- Treatment-emergent adverse events were few and moderate in severity.
SAN DIEGO — A novel, oral therapeutic for treatment of migraine was safe and well-tolerated in single ascending doses in a cohort of healthy adults, according to a speaker at the American Headache Society Annual Scientific Meeting.
“There’s strong mechanistic evidence of the role of triptan-3 in neurogenic inflammation,” Richard Bertz, PhD, senior VP of clinical pharmacology at Biohaven Pharmaceuticals, told attendees. “There’s also an expression profile in the human trigeminal vascular system that indicates a potential functional role in migraine pathophysiology.”
Bertz and colleagues sought to examine safety, tolerability and pharmacokinetics of both single ascending dose (SAD) and multiple ascending dose (MAD) administration of a novel, oral TRPM3 antagonist for migraine, BHV-2100.
Their placebo-controlled phase 1 study included 39 healthy adults aged 18 to 55 years who were randomized 3:1 to receive either a single dose of BHV-2100 (25 mg, 75 mg, 150 mg, 250 mg or 500 mg) or placebo while fasting. The 150 mg dose was administered with a high-fat meal along with famotidine.
A safety review committee analyzed safety, tolerability and pharmacokinetic data after completion of each ascending dose, with samples collected up to 120 hours.
According to results, the novel therapeutic was safe and well-tolerated, with no dose limiting toxicities or serious adverse events recorded; only four moderate treatment-emergent adverse events were logged in the treatment group.
BHV-2100 additionally demonstrated rapid absorption at all doses within 2 to 4 hours, while its pharmacokinetic profile was unaffected by either a high-fat meal or acid-reducing agent.
Researchers additionally noted that data from the MAD are pending, with dosing having been completed.
“We do plan a phase 2 trial to start later this year evaluating three doses, single doses in a proof-of-concept study in doses ranging from 25 to 50 milligrams,” Bertz said.