Chemistry:Bavisant
Bavisant (INN, USAN; developmental code names BEN-2001 and JNJ-31001074) is a histamine H3 receptor receptor antagonist which was under development for the treatment of narcolepsy and attention deficit hyperactivity disorder (ADHD) but was never marketed.[1][2][3][4] It is taken orally.[1][4]
The drug is potent and highly selective for the histamine H3 receptor (Ki = 5.4 nM).[3][4][5] Bavisant produces wakefulness-promoting effects in animals and humans, but can also cause insomnia.[3][4] Its elimination half-life is 14 to 22 hours while its effective half-life is 13 to 20 hours.[3][5]
Bavisant was under development by BenevolentAI and Johnson & Johnson.[1] It reached phase 2 clinical trials for both narcolepsy and ADHD prior to the discontinuation of its development in 2022.[1] The drug was not effective for the treatment of ADHD in a large clinical trial.[3][4] Besides the preceding indications, it was also studied for the treatment of alcoholism.[3][2] In 2026, bavisant was identified as a potential therapeutic agent for the treatment of multiple sclerosis.[6]
See also
- List of investigational attention deficit hyperactivity disorder drugs
- List of investigational narcolepsy and hypersomnia drugs
- Histamine H3 receptor antagonist
- Wakefulness-promoting agent
References
- ↑ 1.0 1.1 1.2 1.3 "BenevolentAI/Johnson & Johnson". 5 November 2023. https://adisinsight.springer.com/drugs/800031762.
- ↑ 2.0 2.1 "Several down, a few to go: histamine H3 receptor ligands making the final push towards the market?". Expert Opinion on Investigational Drugs 20 (12): 1629–1648. December 2011. doi:10.1517/13543784.2011.625010. PMID 21992603.
- ↑ 3.0 3.1 3.2 3.3 3.4 3.5 "Histamine H3R Antagonists: From Scaffold Hopping to Clinical Candidates". Histamine Receptors. The Receptors. 28. Cham: Springer International Publishing. 2016. pp. 109–155. doi:10.1007/978-3-319-40308-3_5. ISBN 978-3-319-40306-9.
- ↑ 4.0 4.1 4.2 4.3 4.4 "Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder". CNS Drugs 26 (5): 421–434. May 2012. doi:10.2165/11631990-000000000-00000. PMID 22519922.
- ↑ 5.0 5.1 "Pharmacokinetics And Safety Of Bavisant (JNJ-31001074) After Single And Multiple Doses In Healthy Subjects: 1386236". Clinical Pharmacology in Drug Development 1 (4): 199. 2012. https://www.ovid.com/journals/cpdd/abstract/01682548-201210000-00076~pharmacokinetics-and-safety-of-bavisant-jnj-31001074-after.
- ↑ "In silico screening and preclinical validation identify bavisant as a therapeutic candidate for multiple sclerosis". Science Translational Medicine 18 (833). January 2026. doi:10.1126/scitranslmed.ads0633. PMID 41564155.
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