BIA 10-2474
| File:BIA 10-2474.svg | |
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| Formula | C17H21N5O2 |
| Molar mass | 327.388 g·mol−1 |
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BIA 10-2474 is an experimental FAAH enzyme inhibitor[1] tested by the Portuguese pharmaceutical company Bial. The drug, tested for pain relief,[2][3] interacts with the human endocannabinoid system.[4][5]
The chemical structure of BIA 10-2474 is likely[original research?] disclosed in the US Patent application US2015/0174103,[6] which is a selection invention from the family of compounds claimed in WO 2010/074588. This is most likely[original research?] PubChem CID 72734378.[7]
FAAH degrades neurotransmitters like anandamide,[8] which can affect eating and sleep patterns, and pain relief.[9][10] FAAH inhibitors have been proposed for a range of nervous-system disorders including anxiety, alcoholism and pain. Bial holds several patents on FAAH enzyme inhibitors.[11][10] The experimental drug is marked as intended for "Neurological and Psychiatric Pathologies"[12] on Bial's website.
Animal testing of the drug was carried out on chimpanzees in July 2015. On 9 July 2015,[13] Biotrial, a contract research organization, began testing the drug in a human phase one clinical trial. In the city of Rennes, 90 volunteers, all men aged 28 to 49, had volunteered to be dosed with the drug.[14] A new phase of the experiment evaluating multiple doses started on 7 January 2016, with six volunteers receiving multiple doses. The first man who received multiple doses was hospitalized at the Rennes University Hospital on 10 Jan, with the others then progressively being hospitalized. Biotrial stopped the experiment on 11 Jan. The first patient to be hospitalized was left brain dead.[15] However, Merck (MK-4409) [16] [17] and Pfizer (PF-04457845) have previously taken FAAH inhibitors into the clinic without experiencing such adverse events.
See also
- TGN1412, a drug trialed in 2006 in London, which also resulted in injuries
References
- ^ Reuters Editorial (15 January 2016). "BRIEF-Bial says firmly committed to ensure wellbeing of test participants". Reuters.
{{cite web}}:|author=has generic name (help) - ^ "BIA 10-2474".
- ^ "BIA 102474".
- ^ Angeline Benoit,Makiko Kitamura (15 January 2016). "France Ties Brain-Dead Person to Tests of Bial-Portela Drug". Bloomberg.com.
- ^ "France/Monde - Essai thérapeutique : 90 personnes ont pris la molécule".
- ^ "UREA COMPOUNDS AND THEIR USE AS ENZYME INHIBITORS" (PDF).
- ^ Pubchem. "SCHEMBL15559209".
- ^ Debora Mackenzie. "Six in hospital after French pain relief drug trial goes wrong". New Scientist.
- ^ "The Discovery and Development of Inhibitors of Fatty Acid Amide Hydrolase (FAAH)". PubMed Central (PMC).
- ^ a b Google
Patentscope
WO application 2015016729, Laszlo Erno Kiss, DE NORONHA Rita GUSMÃO, DA COSTA PEREIRA Carla Patrícia ROSA, Rui PINTO, "Urea compounds and their use as faah enzyme inhibitors", published Feb 5, 2015, assigned to BIAL - ^ "Patent WO2015016729A1 - Urea compounds and their use as faah enzyme inhibitors".
- ^ "Pipeline".
- ^ http://www.bioworld.com/content/six-hospitalized-bial-clinical-trial-france-0
- ^ Matthias Blamont (15 January 2016). "French drug trial disaster leaves one brain dead, five injured". Reuters.
- ^ "France clinical trial: 90 given drug, one man brain-dead". BBC News.
- ^ Chobanian; et al. (10 April 2014). "Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain". ACS Med. Chem. Lett.
{{cite web}}: Explicit use of et al. in:|author=(help) - ^ Merck (15 October 2009). "Merck Pipeline, Oct 2009" (PDF). Merck.
External links
- Bial pipleline
- Urea compounds and their use as faah enzyme inhibitors - Patent
- [1] - Selection patent