The DOI matches its Crossref record; 14 of the 14 references it cites were found in a registry or an index.
ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans.
Open accessAbstract
Examination of the structural basis for antiviral activity, oral pharmacokinetics, and hepatic metabolism among a series of symmetry-based inhibitors of the human immunodeficiency virus (HIV) protease led to the discovery of ABT-538, a promising experimental drug for the therapeutic intervention in acquired immunodeficiency syndrome (AIDS). ABT-538 exhibited potent in vitro activity against laboratory and clinical strains of HIV-1 [50% effective concentration (EC50) = 0.022-0.13 microM] and HIV-2 (EC50 = 0.16 microM). Following a single 10-mg/kg oral dose, plasma concentrations in rat, dog, and monkey exceeded the in vitro antiviral EC50 for > 12 h. In human trials, a single 400-mg dose of ABT-538 displayed a prolonged absorption profile and achieved a peak plasma concentration in excess of 5 micrograms/ml. These findings demonstrate that high oral bioavailability can be achieved in humans with peptidomimetic inhibitors of HIV protease.
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Cites
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Self-citationL-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.
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Cited by
Molecular Recognition of Protein−Ligand Complexes: Applications to Drug Design
Babine, R. E., & Bender, S. L. (1997) · Chemical Reviews · doi:10.1021/cr960370z · Cited by 892
Flexner, C. (1998) · New England Journal of Medicine · doi:10.1056/nejm199804303381808 · Cited by 852
INHIBITORS OF HIV-1 PROTEASE: A Major Success of Structure-Assisted Drug Design
Wlodawer, A., & Vondrasek, J. (1998) · Annual Review of Biophysics and Biomolecular Structure · doi:10.1146/annurev.biophys.27.1.249 · Cited by 734
Dealing with the Impact of Ritonavir Polymorphs on the Late Stages of Bulk Drug Process Development
Chemburkar, S. R., Bauer, J., Deming, K., Spiwek, H., Patel, K., Morris, J., Henry, R., Spanton, S., Dziki, W., Porter, W., et al. (2000) · Organic Process Research & Development · doi:10.1021/op000023y · Cited by 687
Danner, S. A., Carr, A., Leonard, J. M., Lehman, L. M., Gudiol, F., Gonzales, J., Raventos, A., Rubio, R., Bouza, E., Pintado, V., et al. (1995) · New England Journal of Medicine · doi:10.1056/nejm199512073332303 · Cited by 567
Metadata
- Authors
- Kempf, D. J., Marsh, K. C., Denissen, J. F., McDonald, E., Vasavanonda, S., Flentge, C. A., Green, B. E., Fino, L., Park, C. H., & Kong, X. P.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1995-03-28
- Volume
- 92
- Issue
- 7
- Pages
- 2484-2488
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2130082288
- Cited by
- 560
- References
- 14
- Type
- conference abstract
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans. https://app.cochat.ai/papers/10.1073/pnas.92.7.2484
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- Kempf, D. J., Marsh, K. C., Denissen, J. F., McDonald, E., Vasavanonda, S., Flentge, C. A., Green, B. E., Fino, L., Park, C. H., & Kong, X. P. (1995). ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.92.7.2484
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