Dutasteride. Steroid 5α-reductase inhibitor, treatment of BPH

Drugs of the Future

Volumn 24, Issue 3, 1999, Pages 246-253

  Graul, A ^a   Silvestre, J ^a   Castaner J ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

4 [1 (6,6 DIMETHYL 6H DIBENZO[B,D]PYRAN 3 YLMETHYL) 3 INDOLYL]BUTYRIC ACID; 4 [3 [3 [BIS(4 ISOBUTYLPHENYL)METHYLAMINO]BENZOYL] 1H INDOL 1 YL]BUTYRIC ACID; ALFUZOSIN; CS 891; DOXAZOSIN; DOXAZOSIN MESYLATE; DUTASTERIDE; EPRISTERIDE; FINASTERIDE; INDORAMIN; MEPARTRICIN; N [2,2,2 TRIFLUORO 1 PHENYL 1 (TRIFLUOROMETHYL)ETHYL] 3 OXO 4 AZA 5ALPHA ANDROST 1 ENE 17BETA CARBOXAMIDE; PRAZOSIN; SNA 4606 1; STEROID 5ALPHA REDUCTASE INHIBITOR; TAMSULOSIN; TERAZOSIN; UNCLASSIFIED DRUG; Z 350;

CLINICAL TRIAL; DRUG ACTIVITY; DRUG MECHANISM; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; NONHUMAN; PHARMACODYNAMICS; PROSTATE HYPERTROPHY; REVIEW;

EID: 0032905145     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1999.024.03.489139     Document Type: Review

References (31)

1. Batchelor, K.W., Frye, S.V. (Glaxo Wellcome plc). Androstenones. EP 719277, EP 719278, JP 97502729, JP 97502731, US 5565467, WO 9507926, WO 9507927.
2. Rasmusson, G.H., Reynolds, G.F., Steinberg, N.G., Walton, E., Patel, G.F., Liang, T., Cascieri, M.A., Cheung, A.H., Brooks, J.R., Berman, C. Azasteroids: Structure-activity relationships for inhibition of 5α-reductase and of androgen receptor binding. J Med Chem 1986, 29: 2298-315.
3. Bakshi, R.K., Rasmusson, G.H., Patel, G.F., Mosley, R.T., Chang, B., Ellsworth, K., Harris, G.S., Tolman, R.L. 4-Aza-3-oxo-5α-androst-1-ene-17β-N-aryl carboxamides as dual inhibitors of human type 1 and type 2 steroid 5α-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5α-reductase inhibitory potency. J Med Chem 1995, 38: 3189-92. (Erratum J Med Chem 1996, 39: 1192.).
4. Berry, S.J., Coffey, D.S., Walsh, P.C., Ewing, L.L. The development of human benign prostatic hyperplasia with age. J Urol 1984, 132: 474-9.
5. Di Silverio, F., Flammia, G.P., Sciarra, A., Caponera, M., Mauro, M., Buscarini, M., Tavani, M., D'Eramo, G. Plant extracts in benign prostatic hyperplasia. Minerva Urol Nefrol 1993, 45: 143-9.
6. Lowe, F.C., Ku, J.C. Phytotherapy in treatment of benign prostatic hyperplasia: A critical review. Urology 1996, 48: 12-20.
7. Wilt, T.J., Ishani, A., Stark, G., MacDonald, R., Lau, J., Mulrow, C. Saw palmetto extracts for treatment of benign prostatic hyperplasia: A systematic review. JAMA - J Am Med Assoc 1998, 280: 1604-9.
8. Frye, S.V. Discovery and development of GG745, a potent inhibitor of both isozymes of 5alpha-reductase. 216th ACS Natl Meet (Aug 23-27, Boston) 1998, Abst MEDI 178.
9. Tian, G., Mook, R.A. Jr., Moss, M.L, Frye, S.V. Mechanism of time-dependent inhibition of 5α-reductases by Δ1-4-azasteroids: Toward perfection of rates of time-dependent inhibition by using ligand-binding energies. Biochemistry 1995, 34: 13453-9.
10. Bramson, H.N., Hermann, D., Batchelor, K.W., Lee, F.W., James, M.K., Frye, S.V. Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR. J Pharmacol Exp Ther 1997, 282: 1496-502.
11. Frye, S.V., Bramson, H.N., Hermann, D.J., Lee, F.W., Sinhababu, A.K., Tian, G. Discovery and development of GG745, a potent inhibitor of both isozymes of 5α-reductase. In: Integration of Pharmaceutical Discovery and Development: Case Studies, R. Borchardt, R.M. Freidinger, T.K. Sawyer, PL. Smith (Eds.), 1998, Plenum Press, New York, 1998, 393-422.
12. Nystrom, D.D., Yeager, R.L., Halm, K.A., Chism, J., Moss, M.L. Pharmacokinetics of GG745 in rats following single or multiple oral dosing. 4th Int ISSX Meet (Aug 27-31, Seattle) 1995, Abst 296.
13. Hermann, D.J., Davis, I.M., Wilson, T.H. Effects of GI198745 (GG745), a novel 5α-reductase (5AR) inhibitor, on dihydrotestostemne (DHT). Clin Pharmacol Ther 1996, 59(2): Abst PIII-18.
14. Gisleskog, P.O., Hermann, D., Hammarlund-Udenaes, M., Karlsson, M.O. A model for the turnover of dihydrotestosterone in the presence of the irreversible 5alpha-reductase inhibitors GI198745 and finasteride. Clin Pharmacol Ther 1998, 64: 636-47.
15. Gisleskog, P.O., Hermann, D., Hammarlund-Udenaes, M., Karlsson, M.O. The pharmacokinetic modelling of GI198745 (dutasteride), a compound with parallel linear and nonlinear elimination. Br J Clin Pharmacol 1999, 47: 53-8.
16. Hermann, D.J., Wilson, T.H., Morrill, B.B. A 28-day evaluation of GI198745 (GG745), a potent dual 5α-reductase (5AR) inhibitor, in BPH patients. J Urol 1997, 157(4, Suppl.): Abst 1227.
17. Hobbs, S., Hermann, D.J., Gabriel, H., Wilson, T., Morrill, B., Clark, R.V. Marked suppression of dihydrotestosterone in men by a novel 5α-reductase inhibitor, GI198745. Fertil Steril 1998, 70(3, Suppl. 1): Abst P-1063.
18. Glaxo Wellcome issues new R&D pipeline. Prous Science Daily Essentials Feb 22, 1999.
19. Sawaya, M.E. Novel agents for the treatment of alopecia. Semim Cutan Med Surg 1998, 17: 276-83.
20. Levy, M.A., Brandt, M., Heys, J.R., Holt, D.A., Metcalf, B.W. Inhibition of rat liver steroid 5α-reductase by 3-androstene-3-carboxylic acids: Mechanism of enzyme-inhibitor interaction. Biochemistry 1990, 29: 2815-24.
21. Levy, M.A., Brandt, M., Holt, D.A., Metcalf, B.W. Interaction between rat prostatic steroid 5α-reductase and 3-carboxy-17β-substituted steroids: Novel mechanism of enzyme inhibition. J Steroid Biochem 1989, 34: 571-5.
22. Yasuda, N., Fujino, K., Shiraji, T., Nambu, F., Kondo, K. Effects of steroid 5α-reductase inhibitor ONO-9302 and antiandrogen allylestrenol on the prostatic growth, and plasma and prostatic hormone levels in rats. Jpn J Pharmacol 1997, 74: 243-52.
23. Levy, M.A., Brandt, M., Sheedy, K.M., Dinh, J.T., Holt, D.A., Garrison, L.M., Bergsma, D.J., Metcalf, B.W. Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5α-reductase isoform 2. J Steroid Biochem Mol Biol 1994, 48: 197-206.
24. Sudduth, S.L., Koronkowski, M.J., Sharifi, R. et al. Finasteride: The first 5α-reductase inhibitor. Pharmacotherapy 1993, 13: 309-29.
25. Sawada, K., Hirai, H., Golden, P., Okada, S., Sawada, Y, Hashimoto, M., Tanaka, H. (1-Benzylindole-3-yl)alkanoic acids: Novel nonsteroidal inhibitors of steroid 5α-reductase (I). Chem Pharm Bull 1998, 46: 1683-7.
26. Di Salle, E., Giudici, D., Radice, A., Zaccheo, T., Ornati, G., Nesi, M., Panzeri, A., Delos, S., Martin, P.M. PNU 157706, a novel dual type I and II 5α-reductase inhibitor. J Steroid Biochem Mol Biol 1998, 64: 179-86.
27. Hirosumi, J., Nakayama, O., Fagan, T., Sawada, K., Chida, N., Inami, M., Takahashi, S., Kojo, H., Notsu, Y., Okuhara, M. FK143, a novel nonsteroidal inhibitor of steroid 5α-reductase: (1). In vitro effects on human and animal prostatic enzymes. J Steroid Biochem Mol Biol 1995, 52: 357-63.
28. Hirosumi, J., Nakayama, O., Fagan, T., Takahashi, S., Kojo, H., Notsu, Y., Okuhara, M. FK143, a novel nonsteroidal testosterone 5α-reductase inhibitor: Its effects on human and animal prostates. Can J Physiol Pharmacol 1994, 72(Suppl. 1): Abst P5.1.10.
29. Nakakoshi, M., Kimura, K.-I., Nakajima, N., Yoshihama, M. SNA-4606-1, a new member of elaiophylins with enzyme inhibition activity against testosterone 5α-reductase. J Antibiot 1999 52: 175-7.
30. Fukuda, Y. et al. Pharmacological properties of Z-350, which possesses α1-adrenoceptor antagonistic and steroid 5α-reductase inhibitory actions: (1). In vitro studies. Jpn J Pharmacol 1998, 76(Suppl. 1): Abst P-439.
31. Burback, B., Jersey, J.A., Allen, M., Newton, D. Development, validation and application of an assay to measure GI198745X collected on glass fiber disks. Pharm Res 1996, 13(9, Suppl.): Abst APQ 1183.