Lenabasum Explained

Lenabasum (also known as ajulemic acid, 1',1'-dimethylheptyl-delta-8-tetrahydrocannabinol-11-oic acid, DMH-D8-THC-11-OIC, AB-III-56, HU-239, IP-751, CPL 7075, CT-3, JBT-101, Anabasum, and Resunab) is a synthetic cannabinoid that shows anti-fibrotic and anti-inflammatory effects in pre-clinical studies without causing a subjective "high".[1] Although its design was inspired by a metabolite of delta-9-THC known as delta-9-THC-11-oic acid, lenabasum is an analog of the delta-8-THC metabolite delta-8-THC-11-oic acid.[2] [3] It is being developed for the treatment of inflammatory and fibrotic conditions such as systemic sclerosis, dermatomyositis and cystic fibrosis.[4] It does not share the anti-emetic effects of some other cannabinoids, but may be useful for treating chronic inflammatory conditions where inflammation fails to resolve.[5] Side effects include dry mouth, tiredness, and dizziness. The mechanism of action is through activation of the CB2 receptor leading to production of specialized proresolving eicosanoids such as lipoxin A4 and prostaglandin J2. Studies in animals at doses up to 40 mg/kg show minimal psychoactivity of lenabasum, compared to that produced by tetrahydrocannabinol.[6] Lenabasum is being developed by Corbus Pharmaceuticals (formerly JB Therapeutics) for the treatment of orphan chronic life-threatening inflammatory diseases.[7] Development since been discontinued.[8]

Notes and References

  1. Burstein SH, Karst M, Schneider U, Zurier RB . Ajulemic acid: A novel cannabinoid produces analgesia without a "high" . Life Sciences . 75 . 12 . 1513–1522 . August 2004 . 15240185 . 10.1016/j.lfs.2004.04.010 .
  2. Vann RE, Cook CD, Martin BR, Wiley JL . Cannabimimetic properties of ajulemic acid . The Journal of Pharmacology and Experimental Therapeutics . 320 . 2 . 678–686 . February 2007 . 17105826 . 10.1124/jpet.106.111625 . 15593252 .
  3. Motwani MP, Bennett F, Norris PC, Maini AA, George MJ, Newson J, Henderson A, Hobbs AJ, Tepper M, White B, Serhan CN, MacAllister R, Gilroy DW . 6 . Potent Anti-Inflammatory and Pro-Resolving Effects of Anabasum in a Human Model of Self-Resolving Acute Inflammation . Clinical Pharmacology and Therapeutics . 104 . 4 . 675–686 . October 2018 . 29238967 . 6175297 . 10.1002/cpt.980 .
  4. Mitchell VA, Aslan S, Safaei R, Vaughan CW . Effect of the cannabinoid ajulemic acid on rat models of neuropathic and inflammatory pain . Neuroscience Letters . 382 . 3 . 231–235 . July 2005 . 15925096 . 10.1016/j.neulet.2005.03.019 . 582590 .
  5. Burstein S . Ajulemic acid (IP-751): synthesis, proof of principle, toxicity studies, and clinical trials . The AAPS Journal . 7 . 1 . E143–E148 . June 2005 . 16146336 . 2751505 . 10.1208/aapsj070115 .
  6. Vann RE, Cook CD, Martin BR, Wiley JL . Cannabimimetic properties of ajulemic acid . The Journal of Pharmacology and Experimental Therapeutics . 320 . 2 . 678–686 . February 2007 . 17105826 . 2633725 . 10.1124/jpet.106.111625 .
  7. Web site: Companies To Watch: Corbus Pharmaceuticals. www.lifescienceleader.com. 2019-05-20.
  8. Web site: Lenabasum . AdisInsight .

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