Cluster headache is a specific disorder of extremely painful debilitating headaches that occur in cycles usually lasting 4 to 8 weeks followed by a pain-free remission period that can also be continuous. In its chronic form, cluster headache sufferers are pain-free for less than 1 month in a year. Like migraine, cluster headache is classified as either a vascular headache or trigeminal autonomic cephalgia. The intense pain is caused by blood vessel dilation which creates pressure on the trigeminal nerve. While this process is the immediate cause of the pain, the underlying cause or causes are not yet fully understood.

Conventional treatments for cluster headache and migraine are based on the administration of a vasoconstrictor to act against dilation of blood vessels (considered the cardinal mechanism of pain production). However, the efficacy of drug treatments that have no direct effects on blood vessels has cast doubt on the vasoconstrictor hypothesis. It appears more likely that these drugs are successful because they stabilize serotonergic neurotransmission. The hypothalamus has also been implicated as a possible cause of cluster headache since headache attacks frequently strike around the same time each day and during a particular season (one of the main functions of the hypothalamus is the regulation of the biological clock).

Cluster headache patients discovered on their own that use of either LSD or psilocybin, both Schedule I controlled substances, can bring partial or complete relief from cluster attacks. Eventually presented to Dr. Halpern and colleagues, the next step of evaluation led to his group publishing a case series on 53 cluster headache patients who used one or both of these drugs to treat their condition. The descriptions of treatment efficacy in this publication suggest LSD and psilocybin are better at aborting acute attacks than either oxygen or triptans and that LSD and psilocybin are better at both inducing and extending remission than standard drugs. Free from LSD-like intoxication, BOL-148 may be especially therapeutic at a dose level not possible with LSD. Powerful positive treatment results on attack abortion, cycle interruption, and extension of remission have been captured and no currently approved medications offer such comprehensive symptom relief.

Our studies also indicate BOL-148 is non-toxic. Results show that ingesting three pills of BOL-148 (avg. 3 mg. per pill) across 10 days either breaks a cluster headache cycle or considerably improves the frequency and intensity of attacks, even resulting in a change from chronic to episodic form, with remission extending for many months or longer. Except for very mild alterations of subjective state for about 2-hours and no sympathetic reactions, no other side effects have been observed. Unlike pure LSD, BOL-148 is not a Schedule I substance. It was originally used as an LSD placebo in the 1950s and has legally been given in basic research to over 300 human subjects, including in the United States.