Medicinal chemistry strategies in follow-on drug discovery

Drug Discov Today. 2009 May;14(9-10):516-22. doi: 10.1016/j.drudis.2009.02.008. Epub 2009 Mar 5.

Abstract

Drug discovery targeting novel mechanisms has become extremely expensive and risky. The annual first-in-class drug approvals have not been satisfactory in the past decade (two to six per year) despite an increased R&D budget. Follow-on programs targeting proven mechanisms are less risky and costly but can produce drugs with meaningful differentiations and thus can play an important supporting role. This article will discuss the medicinal chemistry strategies that have been utilized by the pharmaceutical industry to exploit validated therapeutic targets.

Publication types

  • Review

MeSH terms

  • Animals
  • Atorvastatin
  • Bendamustine Hydrochloride
  • Benzazepines / pharmacology
  • Benzazepines / therapeutic use
  • Chemistry, Pharmaceutical / methods*
  • Clinical Trials as Topic
  • Drug Delivery Systems / methods
  • Drug Discovery / economics
  • Drug Discovery / methods*
  • Heptanoic Acids / chemical synthesis*
  • Heptanoic Acids / pharmacology
  • Heptanoic Acids / therapeutic use
  • Humans
  • Lapatinib
  • Nitrogen Mustard Compounds / pharmacology
  • Nitrogen Mustard Compounds / therapeutic use
  • Pregabalin
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology
  • Pyrroles / therapeutic use
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology
  • Quinazolines / therapeutic use
  • Sulfonamides
  • gamma-Aminobutyric Acid / analogs & derivatives
  • gamma-Aminobutyric Acid / chemistry
  • gamma-Aminobutyric Acid / pharmacology
  • gamma-Aminobutyric Acid / therapeutic use

Substances

  • Benzazepines
  • Heptanoic Acids
  • Nitrogen Mustard Compounds
  • Pyrimidines
  • Pyrroles
  • Quinazolines
  • Sulfonamides
  • Lapatinib
  • Pregabalin
  • gamma-Aminobutyric Acid
  • lorcaserin
  • Bendamustine Hydrochloride
  • Atorvastatin
  • udenafil