Prodrug strategies to improve the oral absorption of peptide mimetics

Ronald T. Borchardt, Gian Camenisch, Erin Hugger, Wei Wang, David C. Sane, Guy L. Wheeler, Che Ping Cheng, Binghe Wang

Research output: Contribution to journalConference articlepeer-review

Abstract

Coumarine acid linker was used to prepare cyclic prodrugs of the RGD peptide mimetic MK-383 and several of its analogs. The corresponding cyclic prodrugs were designed to be sensitive to esterases and underwent bioconversion. These cyclic prodrugs have physicochemical properties that enhanced the cell membrane permeation and underwent bioconversion in blood and tissues to the RGD peptide mimetics. The cyclic coumarinic acid-bases prodrug of the RGD peptide mimetic MK-383 exhibited potent antithrombotic activity when orally administered to dogs.

Original languageEnglish (US)
Pages (from-to)257-258
Number of pages2
JournalAmerican Chemical Society, Polymer Preprints, Division of Polymer Chemistry
Volume40
Issue number1
StatePublished - Mar 1999
Externally publishedYes
EventProceedings of the 1999 ACS Anaheim Meeting - Anaheim, CA, USA
Duration: Mar 21 1999Mar 25 1999

ASJC Scopus subject areas

  • Polymers and Plastics

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