Dutasteride: A potent dual inhibitor of 5α-reductase for benign prostatic hyperplasia

Drugs of Today

Volumn 40, Issue 8, 2004, Pages 649-661

  Rabasseda, Xavier ^a  

^a Medical Information Department   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

ANDROSTANOLONE; DUTASTERIDE; FINASTERIDE; PLACEBO; STEROID 5ALPHA REDUCTASE INHIBITOR; TAMOXIFEN; TAMSULOSIN; TERAZOSIN; TESTOSTERONE;

AREA UNDER THE CURVE; ATHEROSCLEROSIS; CLINICAL TRIAL; DIZZINESS; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG STRUCTURE; EJACULATION DISORDER; ENZYME INHIBITION; GYNECOMASTIA; HEADACHE; HUMAN; IMPOTENCE; LIBIDO DISORDER; MALE; META ANALYSIS; MULTIPLE DRUG DOSE; NAUSEA; NONHUMAN; PAIN; PROSTATE HYPERTROPHY; REVIEW; RISK REDUCTION; SIDE EFFECT; TESTOSTERONE BLOOD LEVEL; URINE FLOW RATE; URINE RETENTION; VOMITING;

ADMINISTRATION, ORAL; ANIMALS; AZASTEROIDS; DOUBLE-BLIND METHOD; DRUG ADMINISTRATION SCHEDULE; DRUG EVALUATION, PRECLINICAL; FINASTERIDE; HUMANS; INJECTIONS, INTRAVENOUS; ISOENZYMES; MALE; MIDDLE AGED; PROSTATIC HYPERPLASIA; SPAIN; TESTOSTERONE 5-ALPHA-REDUCTASE;

EID: 4644366496     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2004.40.8.850468     Document Type: Review

References (31)

1. Stuart, J.D., Lee, F.W., Simpson, N.D. et al. Pharmacokinetic parameters and mechanisms of inhibition of rat type 1 and 2 steroid 5alpha-reductases: Determinants for different in vivo activities of GI198745 and finasteride in the rat. Biochem Pharmacol 2001, 62: 933-42.
2. Bramson, H.N., Hermann, D., Batchelor, K.W. et al. Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR. J Pharmacol Exp Ther 1997, 282: 1496-502.
3. Frye, S.V., Bramson, H.N., Hermann, D.J. et al. Discovery and development of GG745, a potent inhibitor of both isozymes of 5 alpha-reductase. Pharm Biotechnol 1998, 11: 393-422.
4. 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.
5. Munster, U., Hammer, S., Blume-Peytavi, U., Schafer-Korting, M. Testosterone metabolism in human skin cells in vitro and its interaction with estradiol and dutasteride. Skin Pharmacol Appl Skin Physiol 2003, 16: 356-66.
6. 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.
7. Clark, R.V., Haberer, L.J., Horton, J.R., Foster, C.D. No evidence of drug interactions between GI 198745, a novel dual 5 alpha reductase inhibitor, and alpha 1 adrenergic antagonists. J Urol 2000, 163 (4, Suppl.): Abst. 975.
8. Hermann, D.J., Davis, I.M., Wilson, T.H. Effects of GI198745 (GG745), a novel 5alpha-reductase (5AR) inhibitor, on dihydrotestosterone (DHT). Clin Pharmacol Ther 1996, Abst. PIII-18.
9. Roehrborn, C.G., Andriole, G., Boyle, P., Hoefner, K. Effect of the dual Salpha-reductase inhibitor dutasteride on endocrine parameters and prostate volume. Eur Urol Suppl 2002, 1: Abst. 417.
10. Clark, R.V., Hermann, D.J., Gabriel, H. et al. Effective suppression of dihydrotestosterone (DHT) by GI198745, a novel, dual 5alpha-reductase inhibitor. 94th Annu Meet Am Urol Assoc (May 1-6, Dallas) 1999, Abst. 1037.
11. Andriole, G., Roehrborn, C.G., Boyle, P. Effect of the dual 5alpha-reductase inhibitor, dutasteride, on serum total PSA, free PSA and the ratio F/T PSA. J Urol 2002, 167 (4, Suppl.): Abst. 844.
12. Roehrborn, C.G., Boyle, P., Gabriel, H. et al. Relationship between serum PSA and total prostate and transition zone volume in men with clinical BPH. 94th Annu Meet Am Urol Assoc (May 1-6, Dallas) 1999, Abst. 1405.
13. Roehrborn, C.G., Boyle, P., Nickel, J.C., Hoefner, K., Andriole, G. Efficacy and safety of a dual inhibitor of 5alpha-reductase types 1 and 2 (dutasteride) in men with benign prostatic hyperplasia. Urology 2002, 60: 434-41.
14. O'Leary, M.P., Roehrborn, C., Andriole, G. et al. Improvements in benign prostatic hyperplasia-specific quality of life with dutasteride, the novel dual 5alpha-reductase inhibitor. BJU Int 2003, 92: 262-6.
15. Roehrborn, C.G., Ramsdell, J., Siami, P., Wachs, B.H., Rosenblatt, S. Prostate volume at baseline predicts the margin of therapeutic response with the 5alpha-reductase inhibitor, dutasteride. J Urol 2002, 167 (4, Suppl.): Abst. 1483.
16. Roehrborn, C.G., Andriole, G., Nickel, C., Boyle, P., Hoefner, K. Long-term effect of dutasteride on symptoms, BPH-specific health status and urinary flow rate. BJU Int 2002, 90 (Suppl. 2): Abst. P-1.2.19.
17. Boyle, P., Roehrborn, C.G., Andriole, G., Nickel, C., Hoefner, K. The impact of the dual 5alpha-reductase inhibitor dutasteride on outcomes of benign prostatic hyperplasia (BPH). BJU Int 2002, 90 (Suppl. 2): Abst. P-1.2.16.
18. Boyle, P., Andriole, G., Nickel, C., Roehrborn, C.G. Effect of the dual 5alpha-reductase inhibitor dutasteride on total and transitional zone prostate volume. BJU Int 2002, 90 (Suppl. 2): Abst. P-1.2.05.
19. Boyle, P., Roehrborn, C.G., Andriole, G., Nickel, C., Hoefner, K. The impact of dutasteride, a novel 5alpha-reductase inhibitor, on the hallmarks of BPH. Progression and outcomes. Eur Urol Suppl 2002, 190 (1): Abst. 418.
20. Barkin, J., Guimaraes, M., Do Castelo, V. et al. Dutasteride provides sustained symptom relief following short term combination treatment with tamsulosin. J Urol 2002, 167 (4, Suppl.): Abst. 1481.
21. Barkin, J., Guimaraes, M., Jacobi, G. et al. The 5alpha-reductase inhibitor (5ARI) dutasteride provides sustained symptom relief following short-term combination treatment. BJU Int 2002, 90 (Suppl. 2): Abst. P-1.2.09.
22. Barkin, J., Guimaraes, M., Jacobi, G. et al. Alpha-blocker therapy can be withdrawn in the majority of men following initial combination therapy with the dual 5alpha-reductase inhibitor dutasteride. Eur Urol 2003, 44: 461-6.
23. Hermann, D.J., Wilson, T.H., Morrill, B.B. A 28-day evaluation of GI198745 /GG745), a potent dual 5alpha-reductase (R) inhibitor, in BPH patients. J Urol 1997, 157 (4, Suppl.): Abst. 1227.
24. Hobbs, S., Hermann, D.J., Gabriel, H. et al. Marked suppression of dihydrotestosterone in men by a novel 5alpha-reductase inhibitor, GI198745. Fertil Steril 1998, 70 (3, Suppl. 1): Abst. P-1063.
25. Roehrborn, C.G., Andriole, G., Nickel, C. et al. Effect of dutasteride, a novel dual 5alpha-reductase inhibitor, on BPH related signs and symptoms. J Urol 2002, 167 (4, Suppl.): Abst. 1043.
26. Roehrborn, C.G., Andriole, G., Nickel, C., Boyle, P. Effect of the dual 5alpha-reductase inhibitor dutasteride on endocrine parameters. J Urol 2002, a67 (4, Suppl.): Abst. 1049.
27. Clark, R.V. Hormonal effects of GI 198745, a novel 5 alpha reductase inhibitor. 81st Annu Meet Endocr Soc (Jun 12-15, San Diego) 1999, Abst. P3-380.
28. Clark, R., Huffman, C., Haberer, L. et al. Marked suppression of dihydrotestosterone (DHT) by dutasteride has no adverse effect on spermatogenesis in healthy men. BJU Int 2002, 90 (Suppl. 2): Abst. P-1.2.10.
29. Clark, R., Haberer, L., Huffman, C. Marked suppression of dihydrotestosterone by GI198745 a novel 5alpha-reductase inhibitor, does not affect lipoprotein levels in men. 83rd Annu Meet Endocr Soc (Jun 20-23, Denver) 2001, Abst. P2-486.
30. Clark, R.V., Huffman, C., Haberer, L.J. et al. Marked suppression of dihydrotestosterone (DHT) by dutasteride has no adverse effect on spermatogenesis in healthy men. 84th Annu Meet Endocr Soc (Jun 19-22, San Francisco) 2002, Abst. P2-673.
31. Andriole, G.L., Kirby, R. Safety and tolerability of the dual 5alpha-reductase inhibitor dutasteride in the treatment of benign prostatic hyperplasia. Eur Urol 2003, 44: 82-8.