NBI-75043

Last updated

NBI-75043
NBI-75043.svg
Clinical data
Other namesNBI75043; NBI-1; "Compound 2a" [1]
Routes of
administration 		Oral [2] [3]
Drug class H1 receptor antagonist; Antihistamine; Sedative; Hypnotic
ATC code
  • None
Pharmacokinetic data
Elimination half-life Oral: 6.7 hours [3]
IV Tooltip Intravenous injection: 9.1 hours [3]
Identifiers
  • N,N-dimethyl-2-[3-[(1R)-1-pyridin-2-ylethyl]-1-benzothiophen-2-yl]ethanamine
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C19H22N2S
Molar mass 310.46 g·mol−1
3D model (JSmol)
  • C[C@@H](C1=CC=CC=N1)C2=C(SC3=CC=CC=C32)CCN(C)C
  • InChI=1S/C19H22N2S/c1-14(16-9-6-7-12-20-16)19-15-8-4-5-10-17(15)22-18(19)11-13-21(2)3/h4-10,12,14H,11,13H2,1-3H3/t14-/m0/s1
  • Key:NANQRVOKMXDMNL-AWEZNQCLSA-N

NBI-75043 is a potent and highly selective histamine H1 receptor antagonist or antihistamine which was under development for the treatment of insomnia but was never marketed. [2] [4] [5] [1] It is taken orally. [2] [3] The drug has been found to enhance both slow wave sleep and REM sleep in rodents. [1] Its elimination half-life was found to be 6.7 hours orally and 9.1 hours by intravenous injection in a clinical study. [3] For comparison, diphenhydramine had a half-life of 12 hours and 9.3 hours by these respective routes in the same study. [3] The chemical synthesis of NBI-75043 has been described. [1] NBI-75043 was under development by Neurocrine Biosciences. [2] It entered phase 1 clinical trials for insomnia in 2006 and completed a phase 1 trial the same year. [2] [4] No further development was reported after that and its development was eventually discontinued. [2] [4] Studies of NBI-75043 were published in 2009. [1] [3]

See also

References

  1. 1 2 3 4 5 Moree WJ, Li BF, Jovic F, Coon T, Yu J, Gross RS, et al. (September 2009). "Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia". Journal of Medicinal Chemistry. 52 (17): 5307–5310. doi:10.1021/jm900933k. PMID   19663387.
  2. 1 2 3 4 5 6 "NBI 75043". AdisInsight. 28 February 2011. Retrieved 15 January 2026.
  3. 1 2 3 4 5 6 7 Madan A, O'Brien Z, Wen J, O'Brien C, Farber RH, Beaton G, et al. (March 2009). "A pharmacokinetic evaluation of five H(1) antagonists after an oral and intravenous microdose to human subjects". British Journal of Clinical Pharmacology. 67 (3): 288–298. doi:10.1111/j.1365-2125.2008.03351.x. PMC   2675039 . PMID   19523012.
  4. 1 2 3 Beaton G, Moree WJ (September 2010). "The expanding role of H1 antihistamines: a patent survey of selective and dual activity compounds 2005-2010". Expert Opinion on Therapeutic Patents. 20 (9): 1197–1218. doi:10.1517/13543776.2010.510516. PMID   20716024. This compound appears to be NBI-75043, which was reported to have entered Phase I trials in 2006 [128]. No further development activity has been disclosed.
  5. ↑ Bharate SS, Vishwakarma RA (September 2013). "Impact of preformulation on drug development". Expert Opinion on Drug Delivery. 10 (9): 1239–1257. doi:10.1517/17425247.2013.783563. PMID   23534681. NBI-75043 (22) is a highly selective and potent H1 receptor antagonist that was under evaluation for safety and efficacy in the treatment of insomnia.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.