Medicinal chemistry strategies in follow-on drug discovery.
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.
R4CP, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. zhao_hongyu@hotmail.com
Hongyu
H
Zhao
Zongru
Z
Guo
D000818:Animals; D000069059:Atorvastatin; D000069461:Bendamustine Hydrochloride; D001552:Benzazepines / Q000494:pharmacology / Q000627:therapeutic use; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems / Q000379:methods; D055808:Drug Discovery / Q000191:economics / Q000379:methods*; D006538:Heptanoic Acids / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D000077341:Lapatinib; D009588:Nitrogen Mustard Compounds / Q000494:pharmacology / Q000627:therapeutic use; D000069583:Pregabalin; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013449:Sulfonamides; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000096926:Benzenesulfonamides
D000069059:Atorvastatin; D000069461:Bendamustine Hydrochloride; D001552:Benzazepines; D006538:Heptanoic Acids; D000077341:Lapatinib; D009588:Nitrogen Mustard Compounds; D000069583:Pregabalin; D011743:Pyrimidines; D011758:Pyrroles; D011799:Quinazolines; D013449:Sulfonamides; D005680:gamma-Aminobutyric Acid; C506658:lorcaserin; C419664:udenafil; D000096926:Benzenesulfonamides