Guilford (GLFD) - Steadily Rising Message Board

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Biotech / Medical : Guilford (GLFD) - Steadily Rising

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To: SteveG who wrote (73)	8/24/1997 10:14:00 PM
From: Miljenko Zuanic	of 496

Any idea why GLFD tested GPI-1046 at 3 or 10 mg/kg (PNAS: s.c. injection which IMO can give ~50-250 microM plasma conc.) while it is active at picoM (Ki50 ~50pM) in-vitro. This is ~100K to 1M fold increase compared to in-vitro study. At the some time they are telling as that drug has excellent bioaveability (oral) and it pass BBB readily! Did anyone compare two patents (VRTX and GLFD) covering FKBP12 ligands, rotomase enzyme inhibitors? Structures are very similar, some basis unit which are driven from FK 506 structure? Thanks in advance. mz BTW, IMO AMGN will not proceide with GPI-1046 in to PI. They will develop sec.gen. inhibitor.

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