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Issue 2, 2016
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Discovery of AZD8165 – a clinical candidate from a novel series of neutral thrombin inhibitors

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Abstract

A novel series of neutral thrombin inhibitors has been developed using a selection process based on docking experiments and property calculations and predictions. This work resulted in the identification of the highly potent thrombin inhibitor compound 85 (Ki = 300 pM) and the corresponding propionate prodrug 5 (AZD8165) as a candidate for clinical evaluation in the treatment of thrombosis and related diseases. AZD8165 was found to be safe and well tolerated and delivered the expected pharmacological response in a phase I trial in healthy male volunteers.

Graphical abstract: Discovery of AZD8165 – a clinical candidate from a novel series of neutral thrombin inhibitors

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Supplementary files

Article information


Submitted
15 Oct 2015
Accepted
19 Nov 2015
First published
27 Nov 2015

Med. Chem. Commun., 2016,7, 272-281
Article type
Research Article
Author version available

Discovery of AZD8165 – a clinical candidate from a novel series of neutral thrombin inhibitors

K. Abrahamsson, P. Andersson, J. Bergman, U. Bredberg, J. Brånalt, A.-C. Egnell, U. Eriksson, D. Gustafsson, K.-J. Hoffman, S. Nielsen, I. Nilsson, S. Pehrsson, M. O. Polla, T. Skjaeret, M. Strimfors, C. Wern, M. Ölwegård-Halvarsson and Y. Örtengren, Med. Chem. Commun., 2016, 7, 272
DOI: 10.1039/C5MD00479A

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