Chemistry:NBI-75043
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.[1][2][3][4] It is taken orally.[1][5] The drug has been found to enhance both slow wave sleep and REM sleep in rodents.[4] Its elimination half-life was found to be 6.7 hours orally and 9.1 hours by intravenous injection in a clinical study.[5] For comparison, diphenhydramine had a half-life of 12 hours and 9.3 hours by these respective routes in the same study.[5] The chemical synthesis of NBI-75043 has been described.[4] NBI-75043 was under development by Neurocrine Biosciences.[1] It entered phase 1 clinical trials for insomnia in 2006 and completed a phase 1 trial the same year.[1][2] No further development was reported after that and its development was eventually discontinued.[1][2] Studies of NBI-75043 were published in 2009.[4][5]
See also
References
- ↑ 1.0 1.1 1.2 1.3 1.4 "NBI 75043". 28 February 2011. https://adisinsight.springer.com/drugs/800024034.
- ↑ 2.0 2.1 2.2 "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. September 2010. 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.".
- ↑ "Impact of preformulation on drug development". Expert Opinion on Drug Delivery 10 (9): 1239–1257. September 2013. 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.".
- ↑ 4.0 4.1 4.2 4.3 "Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia". Journal of Medicinal Chemistry 52 (17): 5307–5310. September 2009. doi:10.1021/jm900933k. PMID 19663387.
- ↑ 5.0 5.1 5.2 5.3 Cite error: Invalid
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