title: Inherent formulation issues of kinase inhibitors.
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.
authors: Department of Pharmacy and Pharmacology, Netherlands Cancer Institute-Antoni van Leeuwenhoek, Louwesweg 6, 1006 BK Amsterdam, The Netherlands. Electronic address: Maikel.Herbrink@slz.nl.
authors: M
authors: M
authors: Herbrink
authors: Department of Pharmacy and Pharmacology, Netherlands Cancer Institute-Antoni van Leeuwenhoek, Louwesweg 6, 1006 BK Amsterdam, The Netherlands.
authors: J H M
authors: JH
authors: Schellens
authors: Department of Pharmacy and Pharmacology, Netherlands Cancer Institute-Antoni van Leeuwenhoek, Louwesweg 6, 1006 BK Amsterdam, The Netherlands.
authors: J H
authors: JH
authors: Beijnen
authors: Department of Pharmacy and Pharmacology, Netherlands Cancer Institute-Antoni van Leeuwenhoek, Louwesweg 6, 1006 BK Amsterdam, The Netherlands.
authors: B
authors: B
authors: Nuijen
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004339:Drug Compounding / Q000379:methods* / Q000639:trends; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D047428:Protein Kinase Inhibitors
keywords: Bioavailability; Chemotherapy; Formulation; Tyrosine Kinase Inhibitor