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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

A Comparison of Physicochemical Property Profiles of Marketed Oral Drugs and Orally Bioavailable Anti-Cancer Protein Kinase Inhibitors in Clinical Development

Author(s): Gill L. Adrian, Verdonk Marcel, Boyle G. Robert and Taylor Richard

Volume 7, Issue 14, 2007

Page: [1408 - 1422] Pages: 15

DOI: 10.2174/156802607781696819

Price: $65


This manuscript describes a comparison of the physicochemical properties of marketed oral drugs with those of 45 structurally confirmed orally bioavailable anti-cancer protein kinase inhibitors currently in different phases of clinical development. It is evident from the data presented that these kinase inhibitors are on average larger (over 110Da), more lipophilic (over 1.5 log units) and more complex (approximately two more rotatable bonds) than those of marketed oral drugs. In contrast, hydrogen bond donor (HBD) and hydrogen bond acceptor (HBA) counts are not significantly different.

Keywords: Protein kinase inhibitor, physicochemical property, marketed oral drug

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