Bavisant

Bavisant
Clinical data
Other namesBEN-2001; BEN2001; JNJ-1074; JNJ1074; JNJ-31001074; JNJ31001074
Routes of
administration
Oral[1]
Drug classHistamine H3 receptor receptor antagonist; Wakefulness-promoting agent
ATC code
  • None
Pharmacokinetic data
Elimination half-life14–22 hours[2][3]
Identifiers
  • (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H27N3O2
Molar mass329.444 g·mol−1
3D model (JSmol)
  • C1CC1N2CCN(CC2)C(=O)C3=CC=C(C=C3)CN4CCOCC4
  • InChI=1S/C19H27N3O2/c23-19(22-9-7-21(8-10-22)18-5-6-18)17-3-1-16(2-4-17)15-20-11-13-24-14-12-20/h1-4,18H,5-15H2
  • Key:BGBVSGSIXIIREO-UHFFFAOYSA-N

Bavisant (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; 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][4][2][5] It is taken orally.[1][5]

The drug is potent and highly selective for the histamine H3 receptor (Ki = 5.4 nM).[2][5][3] Bavisant produces wakefulness-promoting effects in animals and humans, but can also cause insomnia.[2][5] Its elimination half-life is 14 to 22 hours while its effective half-life is 13 to 20 hours.[2][3]

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.[2][5] Besides the preceding indications, it was also studied for the treatment of alcoholism.[2][4] In 2026, bavisant was identified as a potential therapeutic agent for the treatment of multiple sclerosis.[6]

See also

References

  1. ^ a b c d e "BenevolentAI/Johnson & Johnson". AdisInsight. 5 November 2023. Retrieved 21 May 2026.
  2. ^ a b c d e f g Sadek B, Łażewska D, Hagenow S, Kieć-Kononowicz K, Stark H (2016). "Histamine H3R Antagonists: From Scaffold Hopping to Clinical Candidates". Histamine Receptors. The Receptors. Vol. 28. Cham: Springer International Publishing. pp. 109–155. doi:10.1007/978-3-319-40308-3_5. ISBN 978-3-319-40306-9.
  3. ^ a b c Vaidyanathan S, Kramer M, Berwaerts J, Pandina G, Li LY (2012). "Pharmacokinetics And Safety Of Bavisant (JNJ-31001074) After Single And Multiple Doses In Healthy Subjects: 1386236". Clinical Pharmacology in Drug Development. 1 (4): 199.
  4. ^ a b Kuhne S, Wijtmans M, Lim HD, Leurs R, de Esch IJ (December 2011). "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. doi:10.1517/13543784.2011.625010. PMID 21992603.
  5. ^ a b c d e Weisler RH, Pandina GJ, Daly EJ, Cooper K, Gassmann-Mayer C (May 2012). "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. doi:10.2165/11631990-000000000-00000. PMID 22519922.
  6. ^ Gacem N, Bezukladova S, Windener F, Karam T, Ottoboni L, Brambilla E, et al. (January 2026). "In silico screening and preclinical validation identify bavisant as a therapeutic candidate for multiple sclerosis". Science Translational Medicine. 18 (833) eads0633. doi:10.1126/scitranslmed.ads0633. PMID 41564155.