University of Missouri

Yasser Nashed

Ashim K Mitra

Soumyajit Majumdar

Ritesh Jain

A method of treating a patient for a condition wherein the bioactive agent of choice is DRUG, wherein DRUG is a substrate that is effluxed by the P-gp transporter, is provided, the method comprising administering to the patient an effective amount of a compound of formula (I):DRUG-X&#x2014;Y&#x2014;Z&#x2014;Z'&#x2014;R&#x2003;&#x2003;(I)wherein each X, Y, Z, and Z&#x2032; is independently Met, Val, Thr, Tyr, Trp, Ser, Ala, or Gly; R is H or an amino-protecting group; n is 1, and each n&#x2032;, or n&#x2033; is independently 0 or 1; or a pharmaceutically acceptable salt thereof, with the proviso that DRUG is not acyclovir or ganciclovir and that DRUG is non-peptidyl.

Peptidyl prodrugs that resist P-glycoprotein mediated drug efflux

Dipeptide, and tripeptide and tetrapeptide ester derivatives of bioactive agents are provided wherein the parent agents are substrates effluxed by the P-gp transporter. The derivatives are useful in treating the same condition as the bioactive agent. Also disclosed is a method for preparing a bioactive agent for targeted delivery by nutrient or peptide transporters comprising linking the agent to one or more groups of the formula &#x2014;X&#x2014;Y-Z-Z'-R; wherein each X, Y, Z, and Z&#x2032; is independently Met, Val, Thr, Tyr, Trp, Ser, Ala or Gly; R is independently H or an amino-protecting group; n=1, and each, n&#x2032;, or n&#x2033; is independently 0 or 1.

Growing community of inventors

Thousand Oaks, CA, United States of America

Yasser Nashed