Indiplon
Indiplon (INN na USAN) bụ nonbenzodiazepine, ọgwụ na-eme ka mmadụ kwụsị ịrapara n'ụzọ abụọ - usoro ntọhapụ ozugbo na ihe niile na ndị ọzọ ụra mbụ Nile dị ka maka mmalite ụra, na ntọhapụ gbanwere (nke a na-akpọkwa ntọhapụ a na-achịkwa ma ọ bụ ntọhapụ gbatịrị) maka mmezi ụra.
Ụzọ e si eme ihe
dezieIndiplon na-arụ ọrụ site n'ịkwalite ọrụ nke inhibitory neurotransmitter GABA, dị ka ọtụtụ ihe ndi mádu ziri ihe nọr ka ọzọ na-abụghị benzodiazepine sedatives. Ọ na-ejikọta na α1 subunits nke GABAA receptors na ụbụrụ.[1]
Akụkọ ihe mere eme
dezieA chọpụtara Indiplon na Lederle Laboratories (nke Wyeth mechara nweta) n'afọ ndị 1980 ma kpọọ ya CL 285,489.: 454 Na 1998 Lederle nyere ya ikikere, ya na ndị ọzọ na-achọ ọgwụ, na DOV Pharmaceutical, mmalite nke ndị ọrụ Lederle mbụ guzobere, na Dov nyere ikikere na ọgwụ ahụ nwere ike ịbelata ọnụ nke ndị na ahụ na Neurocrine Biosciences n'otu afọ ahụ.[2][2] N'afọ 2002, Neurocrine sonyeere Pfizer iji mepụta ọgwụ ahụ.[2]
E mere ndokwa maka ntọhapụ Indiplon na 2007, mgbe Sanofi-Aventis' popular hypnotic zolpidem tụfuru ikike ikike ya na United States ma si otú a bụrụ nke dị ọnụ ala. N'afọ 2002, Neurocrine Biosciences abanyela na nkwekọrịta ya na Pfizer iji soro ahịa indiplon na US, na nkwekọ ruru $ 400m.[3] Otú ọ dị, mgbe FDA wepụtara akwụkwọ ozi a na-apụghị ikwenye economy maka usoro ntọhapụ 15 mg gbanwere na akwụkwọ ozi a kwadoro na nkwupụta maka mbipụta 5 mg na 10 mg ozugbo site na FDA na Mee 2006, Pfizer kwụsịrị mmekọrịta ya na Neurocrine.[4][5] Ọnụahịa ngwaahịa Neurocrine dara 60% na akụkọ ahụ.[6]
N'ịgbaso nzaghachi, FDA na Disemba 2007 weere ngwa ọgwụ ọhụrụ nke Neurocrine (NDA) 'kwesịrị ekwesị' na usoro ụlọ Akwụkwọ Anyị mụtara n'aka Onye Okike nke eluigwe 5 na 10 mg, mana rịọrọ ọmụmụ ọhụrụ dị ka ihe dị mkpa maka nkwenye, gụnyere nnwale ahụike na ndị agadi, nyocha nchekwa na-eji mmetụta ọjọọ tụnyere nke ọgwụ ndị a na-ere ahịa, na nyocha tupu ahụike na-enyocha nchekwa indiplon na nke atọ nke ime ime.[7]
N'ịgbaso akwụkwọ ozi FDA nke afọ 2007, Neurocrine kpebiri ịkwụsị mmepe niile nke Indiplon na United States.[7]
Ntụaka
dezie- ↑ (April 2006) "Indiplon is a high-affinity positive allosteric modulator with selectivity for alpha1 subunit-containing GABAA receptors" (PDF). The Journal of Pharmacology and Experimental Therapeutics 317 (1): 369–77. DOI:10.1124/jpet.105.096701. PMID 16399882.
- ↑ 2.0 2.1 2.2 (2010) "Indiplon", GABA and Sleep: Molecular, Functional and Clinical Aspects.. Springer Science & Business Media, 453–464. ISBN 9783034602266.
- ↑ San Diego's Neurocrine Biosciences Scores Second Big Deal in Two Days. The Motley Fool (18 June 2010).
- ↑ Neurocrine's FDA Nightmare. TheStreet.com (16 May 2006).
- ↑ Pfizer Drops Neurocrine Deal. TheStreet.com (22 June 2006).
- ↑ Neurocrine stock price plunges 60 percent:FDA's mixed review of sleeping pill Indiplon could threaten Pfizer-Neurocrine partnership. CNN Money (15 May 2006).
- ↑ 7.0 7.1 Additional Pipeline Projects. Neurocrine (2012-02-16). Archived from the original on 2012-03-27. Retrieved on 2014-06-24.