Chemistry:Lanepitant
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| Other names | LY303870; N-[(R)-2-Indol-3-yl-1-[[N-(o-methoxybenzyl)acetamido]methyl]ethyl][1,4'-bipiperidine]-1'-acetamide |
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| Formula | C33H45N5O3 |
| Molar mass | 559.755 g·mol−1 |
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Lanepitant (INN,[1]:48 code name LY303870), developed by Eli Lilly, is a drug which acts as a selective antagonist of the NK1 receptor, and was one of the first compounds developed that act at this target.[2] It was under development as a potential analgesic drug, but despite promising results in initial animal studies, human clinical trials against migraine, arthritis and diabetic neuropathy all failed to show sufficient efficacy to support further development, with the drug being only marginally more effective than placebo and inferior to older comparison drugs such as naproxen.[3][4][5] Failure of analgesic action was thought to be due to poor penetration of the blood–brain barrier in humans, but research has continued into potential applications in the treatment of other disorders with a peripheral site of action, such as corneal neovascularization.[6]
References
- ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 39". World Health Organization. 1998. https://www.who.int/medicines/publications/druginformation/innlists/RL39.pdf. Retrieved 17 November 2016.
- ↑ "Pharmacological characterization of LY303870: a novel, potent and selective nonpeptide substance P (neurokinin-1) receptor antagonist". The Journal of Pharmacology and Experimental Therapeutics 275 (2): 737–44. November 1995. PMID 7473161.
- ↑ "Lanepitant, an NK-1 antagonist, in migraine prevention". Cephalalgia 21 (2): 102–6. March 2001. doi:10.1046/j.1468-2982.2001.00161.x. PMID 11422091.
- ↑ "Study of the analgesic effect of lanepitant in patients with osteoarthritis pain". Clinical Pharmacology and Therapeutics 67 (4): 419–26. April 2000. doi:10.1067/mcp.2000.105243. PMID 10801252.
- ↑ "Dose-response study of the analgesic effect of lanepitant in patients with painful diabetic neuropathy". Clinical Neuropharmacology 24 (1): 16–22. 2001. doi:10.1097/00002826-200101000-00004. PMID 11290877.
- ↑ "NK1 receptor antagonists as a new treatment for corneal neovascularization". Investigative Ophthalmology & Visual Science 55 (10): 6783–94. September 2014. doi:10.1167/iovs.14-14553. PMID 25228541.
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