Prodrug strategies in drug design

  • 12/28/16 3:30 PM

Instructor: Dr Saghi Sepehri, PhD of Medicinal Chemistry

Date: Wednesday, December 28, 2016

Start Time: 12:00

Venue: Meeting Room

* For faculties

Presentation language: English

Abstract

Prodrugs are bioreversible derivatives of pharmacologically active agents that must undergo an enzymatic and/or chemical transformation in vivo to release the active parent drug. The basic aim of prodrug design is to mask undesirable drug properties, such as low solubility in water or lipid membranes, low target selectivity, chemical instability, undesirable taste, irritation or pain after local administration, presystemic metabolism and toxicity. In general, the rationale behind the use of prodrugs is to optimize the absorption, distribution, metabolism, excretion, and unwanted toxicity (socalled ADMET properties) of the parent drugs. A prodrug should increase the bioavailability and therapeutic effectiveness of a parent drug.