The DOI matches its Crossref record.
Cyclosporine metabolism in human liver: Identification of a cytochrome P-450III gene family as the major cyclosporine-metabolizing enzyme explains interactions of cyclosporine with other drugs
Abstract
The rate of formation of the three initial metabolites of cyclosporine metabolism has been determined in liver microsomes of 15 kidney transplant donors. Interindividual variation in metabolite formation was considerable but all three metabolites varied in parallel. An antiserum raised against a steroid-inducible rat cytochrome P-450 (P-450 PCN) strongly inhibited the formation of these metabolites. Immunoquantitation of the protein recognized by a monoclonal antibody reacting with human cytochromes P-450 of the P-450III gene family, homologues of rat P-450 PCN and rabbit P-4503C, revealed a high degree of correlation with microsomal cyclosporine metabolism. The data suggest that this cytochrome P-450 is the major cyclosporine-metabolizing enzyme in human liver. The substrate specificity and the known inducers and inhibitors of this cytochrome P-450 explain several clinically observed drug interactions with cyclosporine.
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Cited by
Effects of the Antifungal Agents on Oxidative Drug Metabolism: Clinical Relevance
Venkatakrishnan, K., von Moltke, L. L., & Greenblatt, D. J. (2000) · Clinical Pharmacokinetics · doi:10.2165/00003088-200038020-00002 · Cited by 508
Christopher Gorski, J., Hall, S. D., Jones, D. R., & VandenBranden, M. (1994) · Biochemical Pharmacology · doi:10.1016/0006-2952(94)90543-6 · Cited by 395
Pharmacokinetic drug interactions with oral contraceptives
Back, D. J., & Orme, M. L. (1990) · Clinical Pharmacokinetics · doi:10.2165/00003088-199018060-00004 · Cited by 209
Cyclosporin A disposition following acute traumatic brain injury
Empey, P. E., McNamara, P. J., Young, B., Rosbolt, M. B., & Hatton, J. (2006) · Journal of Neurotrauma · doi:10.1089/neu.2006.23.109 · Cited by 58
Metadata
- Authors
- Kronbach, T., Fischer, V., & Meyer, U. A.
- Venue
- Clinical Pharmacology and Therapeutics
- Publisher
- Wiley
- Published
- 1988-06
- Volume
- 43
- Issue
- 6
- Pages
- 630-635
- ISSN
- 0009-9236 (ISSN-L)
- 1532-6535
- OpenAlex
- W2091509247
- Cited by
- 533
- References
- 0
- FWCI
- 23.00
- Type
- journal article
- Language
- en
- Open access
- closed
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