The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
A Comparison of Physiochemical Property Profiles of Development and Marketed Oral Drugs
Abstract
The process of drug discovery applies rigorous selection pressures. Marketed oral drugs will generally possess favorable physiochemical properties with respect to absorption, metabolism, distribution, and clearance. This paper describes a study in which the distributions of physiochemical properties of oral drugs in different phases of clinical development are compared to those already marketed. The aim is to identify the trends in physiochemical properties that favor a drug's successful passage through clinical development and on to the market. Two libraries were created, one of current development oral drugs and one of marketed oral drugs. Statistical analysis of the two showed that the mean molecular weight of orally administered drugs in development decreases on passing through each of the different clinical phases and gradually converges toward the mean molecular weight of marketed oral drugs. It is also clear that the most lipophilic compounds are being discontinued from development.
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Citations
Cites
Molecular properties that influence the oral bioavailability of drug candidates
Veber, D. F., Johnson, S. R., Cheng, H.-Y., Smith, B. R., Ward, K. W., & Kopple, K. D. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm020017n · Cited by 8,420
Pharmaceutical innovation by the seven UK‐owned pharmaceutical companies (1964‐1985).
Prentis, R., Lis, Y., & Walker, Sr. (1988) · British Journal of Clinical Pharmacology · doi:10.1111/j.1365-2125.1988.tb03318.x · Cited by 471
Cited by
The influence of drug-like concepts on decision-making in medicinal chemistry
Leeson, P. D., & Springthorpe, B. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2445 · Cited by 2,403
Self-citationMedicinal chemical properties of successful central nervous system drugs
Pajouhesh, H., & Lenz, G. R. (2005) · NeuroRX · doi:10.1602/neurorx.2.4.541 · Cited by 1,535
The role of ligand efficiency metrics in drug discovery
Hopkins, A. L., Keserü, G. M., Leeson, P. D., Rees, D. C., & Reynolds, C. H. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4163 · Cited by 1,181
Self-citationLipophilicity in drug discovery
Waring, M. J. (2010) · Expert Opinion on Drug Discovery · doi:10.1517/17460441003605098 · Cited by 873
The influence of lipophilicity in drug discovery and design
Arnott, J. A., & Planey, S. L. (2012) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2012.714363 · Cited by 868
Metadata
- Authors
- Wenlock, M. C., Austin, R. P., Barton, P., Davis, A. M., & Leeson, P. D.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2003-03-01
- Volume
- 46
- Issue
- 7
- Pages
- 1250-1256
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2032353075
- Cited by
- 546
- References
- 2
- FWCI
- 26.22
- Type
- journal article
- Language
- en
- Open access
- closed
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