Bisphosphonate prodrugs.
Bisphosphonates (BP) are pyrophosphate analogs having a P-C-P backbone. The oral bioavailability of BPs is ca. 1%, due to high ionisation at physiological pH. Using the prodrug approach, oral absorption can be increased by masking one or more ionizable groups (clodronate, etidronate), or using a targeting carrier system (alendronate, pamitronate).
Vepsäläinen
Jouko J
JJ
Department of Chemistry, University of Kuopio, Finland. vepsalai@messi.uku.fi
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D004002:Clodronic Acid / Q000031:analogs & derivatives; D004164:Diphosphonates / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics*; D016503:Drug Delivery Systems; D012968:Etidronic Acid / Q000031:analogs & derivatives; D006801:Humans; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D007408:Intestinal Absorption; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
D004164:Diphosphonates; D011355:Prodrugs; D004002:Clodronic Acid; D012968:Etidronic Acid