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Inherent formulation issues of kinase inhibitors.

M Herbrink ,
J H M Schellens ,
J H Beijnen ,
B Nuijen

Abstract

The small molecular Kinase Inhibitor (smKI) drug class is very promising and rapidly expanding. All of these drugs are administered orally. The clear relationship between structure and function has led to drugs with a general low intrinsic solubility. The majority of the commercial pharmaceutical formulations of the smKIs are physical mixtures that are limited by the low drug solubility of a salt form. This class of drugs is therefore characterized by an impaired and variable bioavailability rendering them costly and their therapies suboptimal. New formulations are sparingly being reported in literature and patents. The presented data suggests that continued research into formulation design can help to develop more efficient and cost-effective smKI formulation. Moreover, it may also be of help in the future design of the formulations of new smKIs.

More about this publication

Journal of controlled release : official journal of the Controlled Release Society

Volume 239
Pages 118-27
Publication date 10-10-2016

Full text links

Publisher website (DOI) 10.1016/j.jconrel.2016.08.036
Europe PubMed Central 27578098
Pubmed 27578098

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