Current prodrug design for drug discovery.
Prodrugs are inactive compounds which are metabolized either chemically or enzymatically in a controlled or predictable manner to the parent active drug inside the body. Prodrugs can enhance the therapeutic efficacy and/or reduce adverse effects via different mechanisms, including increased solubility, improved permeability and bioavailability, prolonged half-life, and tissue-targeted delivery. Besides the prodrug itself, optimization of vehicles and other enhancement techniques is important as well. Strategies to improve the oral bioavailability and achieve tumor-specific targeting have been the most important developments in prodrug design during the last 5 years. This review describes recent developments in orally administered and tumor-targeted prodrugs. Pharmacokinetic and pharmacodynamic evaluations of these prodrugs are systematically introduced in this review.
Hsieh
Pei-Wen
PW
Pharmaceutics Laboratory, Graduate Institute of Natural Products, Chang Gung University, Kweishan, Taoyuan, Taiwan.
Hung
Chi-Feng
CF
Fang
Jia-You
JY
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D010539:Permeability; D011355:Prodrugs / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D012995:Solubility
D000970:Antineoplastic Agents; D011355:Prodrugs