High-Throughput Screening — Brains Versus Brawn
Several authors have highlighted an apparent decline in the productivity of the pharmaceutical industry as measured by new drug introductions. Horrobin (2000) has stated that total worldwide new chemical entities (NCE) launched every year have fallen from 80–100 per year in the 1960s to 50–60 per year in the 1980s to 30–40 per year in the late 1990s. From this analysis is missing the link between NCE production and successful marketed drugs. Only the top 160 drugs make enough revenue to repay the cost of development. Against this background, the industry is optimistic that technology will transform the downturn in productivity and move to its highest level of innovation as it exploits the fruits of mapping the human genome. Within this new paradigm, drug metabolism departments are reshaping. Screening is now a common term within industrial departments and used with full understanding in terms of the commitment to producing data on many compounds within a rapid timescale. However, in the race to adapt, meet customer needs and be ahead of the pack, has the science moved too fast and lost its traditional roots?
KeywordsPermeability Phenyl Angiotensin Histamine Adrenaline
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- Collins JL, Blanchard SG, Boswell GE, Charifson PF, Cobb JE, Henke BR, Hull-Ryde EA, Kazmierski WM, Kale DH, Leesnitzer LM, Lehmann J, Lenhard JM, Orband-Miller L, Gray-Nunez Y, Parks DJ, Plunkett KD, Tong W-Q (1998) N-(2-benzoylphenyl)-1-tyrosine PPARy agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety. J Med Chem 41: 5037–5054Google Scholar
- Hipskind PA, Lobb KL, Nixon JA, Britton TC, Bruns RF, Catlow J, DieckmanMcGinty DK, Gackenheimer SL, Giter BD, Iyengar S, Schober, DA, Simmons RMA, Swanson S, Zarrinmayeh H, Zimmerman, DM, Gehlet DR (1997) Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists. J Med Chem 40: 3712–3714PubMedCrossRefGoogle Scholar
- Horrobin DF (2000) Innovation in the pharmaceutical industry. J Royal Soc Med 93: 341–345Google Scholar
- Huhn B, McCarthy PA, Gibbs EM (1996) The glitazone family of antidiabetic agents. Curr Pharm Des 2: 85–102Google Scholar
- Siegl PKS (1993) Discovery of losartan, the first specific non-peptide angiotensin II receptor antagonist. J Hypertens 11: 519 - S22Google Scholar
- Weinstock J, Keenan RM, Samanen J, Hempel J, Finkelstein JA., Franz RG, Gaitanopoulos DE, Girard GR, Gleason JG, Hill DT, Morgan TM, Peishoff CE, Aiyar N, Brooks DP, Frederickson TA, Ohlstein EH, Ruffolol RR, Stack, EF, Sulpizio AC, Weidley EF, Edwards RNI (1991) 1-(Carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists. J Med Chem 34: 1514–1517Google Scholar