AAN 2025 | First-in-human trial of BHV-2100 for the treatment of pain
Volkan Granit, MD, MSc, Biohaven, New Haven, CT, comments on the development of BHV-2100, a TRPM3 antagonist, as a potential treatment for pain. Dr Granit explains that TRPM3 receptors are involved in pain perception and are expressed in nociceptive neurons. The drug, BHV-2100, targets these receptors and, due to its blood-brain barrier properties, is unlikely to cause addiction or other side effects associated with traditional pain medications. This interview took place at the 77th American Academy of Neurology (AAN) Annual Meeting in San Diego, CA.
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Transcript
BHV2100 is a TRPM3 antagonist. So I guess I get to give a quick background of what TRPs are. TRPs are transient receptor potential channels and basically they are receptors in the sensory neurons that translate environmental stimuli, be it mechanical touch or a chemical or temperature, to electrical stimuli and we appreciate them, understand them as heat or pain. So within those there are specific TRP receptors that are important for pain, especially TRPV1, TRPA1 and a more recently discovered one, TRPM3...
BHV2100 is a TRPM3 antagonist. So I guess I get to give a quick background of what TRPs are. TRPs are transient receptor potential channels and basically they are receptors in the sensory neurons that translate environmental stimuli, be it mechanical touch or a chemical or temperature, to electrical stimuli and we appreciate them, understand them as heat or pain. So within those there are specific TRP receptors that are important for pain, especially TRPV1, TRPA1 and a more recently discovered one, TRPM3. So Biohaven is developing a TRPM3 antagonist which targets pain because, as I said, sensory neurons, the nociceptive neurons, which are pain-sensing neurons, express these receptors. And the theory is that if you block those receptors at the onset, you would block pain where it starts. And importantly, the drug does not cross the blood-brain barrier, meaning it is unlikely to have the problems that traditional chronic pain medications have, being addiction and drowsiness, fatigue, and sleepiness. So the abstract I presented yesterday is an abstract describing the first in human study of BHV 2100. So this is a classic, what they say, SAD, MAD study. That means single ascending dose and multiple ascending dose where we tested BHV2100 first in single doses in healthy volunteers starting with 25 milligrams up to 500 milligrams. Then once we demonstrated that it is safe and well tolerated, we tested it again in volunteers up to 14 days and that went from 25 milligrams daily up to 150 milligrams daily and basically what we observed that the drug was quite well tolerated and safe, there were no serious adverse events, most adverse events were mild, only really one moderate adverse event in the SAD group and one in the MAD group, both of which were completely unrelated to the drug. And importantly, what we have demonstrated that the drug achieves blood levels that are way above EC90. That means effective concentration, 90%. So what we have observed that at least based on what we predict from animal models we’re able to easily achieve levels that are relevant in pain care. We plan to develop this drug for several pain indications including neuropathic pain but also migraine. So that is a brief summary of our study in abstract.
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Disclosures
Employee at Biohaven and Faculty at the University of Miami.
