Synthesis and evaluation of 3'-[F]fluorothymidine-5'-squaryl as a bioisostere of 3'-[F]fluorothymidine-5'-monophosphate.

The squaryl moiety has emerged as an important phosphate bioisostere with reportedly greater cell permeability. It has been used in the synthesis of several therapeutic drug molecules including nucleoside and nucleotide analogues but is yet to be evaluated in the context of positron emission tomography (PET) imaging. We have designed, synthesised and evaluated 3'-[F]fluorothymidine-5'-squaryl ([F]SqFLT) as a bioisostere to 3'-[F]fluorothymidine-5'-monophosphate ([F]FLTMP) for imaging thymidylate kinase (TMPK) activity.

Analysis and results of the recombinant factor VIIa extended-use registry.

This paper describes the analysis of recombinant factor VIIa (rFVIIa; NovoSeven; Novo Nordisk, Bagsvaerd, Denmark) use in 40 patients with intractable bleeding in the UK. All cases were reported on the 'rFVIIa extended use database' (Traumanet) between its launch in February 1999 and 12 March 2002. Twenty-one other cases reporting rFVIIa use in different circumstances were excluded from the analysis.