Journal
CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
Volume 100, Issue -, Pages 46-56Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.critrevonc.2016.01.015
Keywords
Nucleoside analog; Lipid conjugate; Drug development; Liposomes
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Funding
- Frances P. Tutwiler Fund
- Doug Coley Foundation for Leukemia Research
- McKay Cancer Research Foundation
- National Institute of Health [NC11K08CA169809-03]
- National Institute of Health (Wake Innovations)
- National Institute of Health (NCI Cancer Center Support Grant (CCSG)) [P30CA012197]
- Wake Innovations
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In the past few decades, nucleoside analog drugs have been used to treat a large variety of cancers. These anti-metabolite drugs mimic nucleosides and interfere with chain lengthening upon incorporation into the DNA or RNA of actively replicating cells. However, efficient delivery of these drugs is limited due to their pharmacokinetic properties, and tumors often develop drug resistance. In addition, nucleoside analogs are generally hydrophilic, resulting in poor bioavailability and impaired blood-brain barrier penetration. Conjugating these drugs to lipids modifies their pharmacokinetic properties and may improve in vivo efficacy. This review will cover recent advances in the field of conjugation of phospholipids to nucleoside analogs. This includes conjugation of myristic acid, 12-thioethyldodecanoic acid, 5-elaidic acid esters, phosphoramidate, and self-emulsifying formulations. Relevant in vitro and in vivo data will be discussed for each drug, as well as any available data from clinical trials. (C) 2016 Elsevier Ireland Ltd. All rights reserved.
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