Tox on the Web: deadly French drug trial, fatal food, and more!

    Must-read post about the catastrophic phase 1 French drug trial: In a superb must-read post at the Forbes magazine website,  David Kroll discusses what we know about the disastrous drug safety trial in France that left 1 subject dead and 4 others with varying degrees of neurological damage.The drug in question — named BIA 10-2474 — is an inhibitor of the enzyme fatty acid amide hydrolase (FAAH) that was being developed as a new oral analgesic. As Kroll explains: What’s so important about FAAH? Our bodies make several fatty acid amides that include anandamide, a natural stimulator of the cannabinoid receptors upon which chemicals in the marijuana plant act. Anandamide is referred to as an endocannabinoid. The rational is that a drug blocking FAAH will allow naturally-occuring anandamide to accumulate and act on cannabinoid receptors in a manner that won’t produce the psychoactive effects of cannabis. However, since the inhibitory effect of BIA 10-2474 on FAAH is likely irreversible, there are potential problems: . . . any time a small molecule is designed to irreversibly bind to an enzyme, an opportunity arise [sic] for the immune system to recognize it as foreign. In rare cases, the immune system will mount an inflammatory response against it, but also against regions of the normal enzyme surrounding where the drug binds. This response can result in a hypersensitivity or autoimmune reaction in a subset of individuals whereby the immune system a...
Source: The Poison Review - Category: Toxicology Authors: Tags: Medical bia 10-2474 fatty acid amide hydrolase inhibitor litvenenko polonium-210 putin tox on the web Source Type: news