Bisphosphonate prodrugs

Curr Med Chem. 2002 Jun;9(12):1201-8. doi: 10.2174/0929867023369998.

Abstract

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).

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Clodronic Acid / analogs & derivatives
  • Diphosphonates / chemical synthesis
  • Diphosphonates / chemistry*
  • Diphosphonates / pharmacokinetics*
  • Drug Delivery Systems
  • Etidronic Acid / analogs & derivatives
  • Humans
  • Hydrogen-Ion Concentration
  • Hydrolysis
  • Intestinal Absorption
  • Prodrugs / chemical synthesis
  • Prodrugs / chemistry*
  • Prodrugs / pharmacokinetics*
  • Structure-Activity Relationship
  • Tissue Distribution

Substances

  • Diphosphonates
  • Prodrugs
  • Clodronic Acid
  • Etidronic Acid