A Biotech Bash - Recs and Wrecks Message Board

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Biotech / Medical : A Biotech Bash - Recs and Wrecks

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To: r. peter Dale who wrote (84)	8/29/1997 7:57:00 PM
From: Miljenko Zuanic	of 171

Peter: What I forgot to mention on last post is that SIB-1058Y and SIB-1765F are actually the some compounds, where 1058y is optical pure enantiomer and 1765f is racemate. Medline abstracts can be extrapolated to 1058Y. My concern is that it appears more potent toward ACh than DA stimulation, with facts that ACh stimulation is prolonged (at least in monkey) which can effects needed terapeutic dose. Sibia does not have (as far as I know) mAChR in development/R&D. Also there is no progress (at least not substantial; Melamine from WL is postsynaptic muscarinic agonist for AD, P III) on mAChR agonist or antagonist. This is advantage for SIBI because they have excellent screening assay for variety NAChR subtype. It is surprise that none big pharma show interested (it does not mean it will not) for this class molecules. SIB-1553 series seams very potent. The question is, again, therapeutic benefit of the elevated ACh in AD. Two approved drugs (Cognex and Aricept) , and three at FDA door (Exelon, Metrifonate and Synapton) are all subtype acetylcholinesterase inhibitors and target is dementia and cognition at AD. By this (big pharma interest) NAChR agonist will not cure AD but will relive symptom. Anyway, story interesting to follow. Combining this with two other programs at SIBI, is problem luck of interest or something else ? mz

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