Improving the decision-making process in the structural modification of drug candidates: enhancing metabolic stability.
The activity-exposure-toxicity relationship, which can be described as "the rule of three", presents the single most difficult challenge in the design of drug candidates and their subsequent advancement to the development stage. ADME studies are widely used in drug discovery to optimize the balance of properties necessary to convert lead candidates into drugs that are safe and effective for humans. Metabolite characterization has become one of the key drivers of the drug discovery process, helping to optimize ADME properties and increase the success rate for drugs. Various strategies can influence drug design in the decision-making process in the structural modification of drug candidates to reduce metabolic instability.
Nassar
Alaa-Eldin F
AE
Vion Pharmaceuticals, New Haven, CT, USA. NassarAl@aol.com
Kamel
Amin M
AM
Clarimont
Caroline
C
D000818:Animals; D001702:Biopharmaceutics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003657:Decision Making; D004355:Drug Stability; D006801:Humans; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D010599:Pharmacokinetics; D013329:Structure-Activity Relationship
D004364:Pharmaceutical Preparations