Get Pharmacokinetics: Regulatory - Industrial - Academic PDF

By Welling P.G.

Providing a distinct, multidisciplinary procedure, this cutting-edge moment version information the speedily altering function that scientific and non-clinical pharmacokinetics and drug metabolism play within the discovery and improvement of drug therapies-emphasizing usually neglected regulatory, medical, and monetary concerns.

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Receptor scintigraphy with a radioiodinated somatostatin analogue: Radiolabelling, purification, biologic activity, and in vivo application in animals, J. Nucl. Med. 31 (1990) 1501–1509. , High affinity binding sites for a somatostatin-28 analog in rat brain, Life Sci. 28 (1981) 2191–2198. , Analogs of somatostatin selectively label distinct subtypes of somatostatin receptors in rat brain, J. Pharmacol. Exp. Ther. 252 (1989) 510–517. , DOTA-Lanreotide: A novel somatostatin analog for tumour diagnosis and therapy, Endocrinology 140 (1999) 5136–5148.

These problems can be overcome using somatostatin analogues labelled with metallic radionuclides, such as 111In, 90Y, 64 Cu, 67/68Ga and the radiolanthanides. 7]. The most common strategy involves covalent coupling of DOTA derivatives to the N-terminal (D)Phe residue of [Tyr3]-octreotide or [Tyr3]-octreotate, yielding peptide–chelator conjugates that are able to effectively complex with a host of useful therapeutic radionuclides. Lutetium-177 is increasingly being viewed as a potential radionuclide for use in in vivo therapy because of its favourable decay characteristics.

In the light of the relatively rapid clearance of the radiopharmaceutical, an incubation time of 1 h was chosen, as only 9% of the injected activity remained in the blood after that period of time. 7 μg/mL) and subjected to MN analysis. The ethics committee of IPEN-CNEN, São Paulo, approved this study, and all donors gave their consent for the use of their blood cells for the study. After incubation, samples were washed three times with RPMI 1640 medium and then subjected to cytokinesis blocked MN assay.

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