Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T27265
|
||||
| Former ID |
TTDS00240
|
||||
| Target Name |
5-alpha reductase
|
||||
| Synonyms |
5 alpha-reductase; Hepatic 5-alpha reductase
|
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| Target Type |
Successful
|
||||
| Disease | Alopecia [ICD9: 704.09; ICD10: L65.9] | ||||
| Acne vulgaris [ICD9: 706.1; ICD10: L70.0] | |||||
| Benign prostatic hyperplasia [ICD9: 600; ICD10: N40] | |||||
| Hirsutism [ICD9: 704.1; ICD10: L68.0] | |||||
| Prostate cancer; Benign prostatic hyperplasia [ICD9: 140-229, 185, 600; ICD10: C61, N40] | |||||
| Prostate cancer [ICD9: 185; ICD10: C61] | |||||
| Prostate disease [ICD10: N42.9] | |||||
| BioChemical Class |
Oxidoreductases acting on CH-CH group of donors
|
||||
| Target Validation |
T27265
|
||||
| EC Number |
EC 1.3.99.5
|
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| Drugs and Mode of Action | |||||
| Drug(s) | Azelaic Acid | Drug Info | Approved | Acne vulgaris | [1], [2], [3] |
| Dutasteride | Drug Info | Approved | Benign prostatic hyperplasia | [4], [5] | |
| Finasteride | Drug Info | Approved | Benign prostatic hyperplasia | [6], [7] | |
| Polyestradiol Phosphate | Drug Info | Approved | Prostate cancer | [3] | |
| Dutasteride | Drug Info | Phase 3 | Prostate cancer | [4], [5] | |
| Dutasteride + tamsulosin | Drug Info | Phase 3 | Prostate cancer; Benign prostatic hyperplasia | [8] | |
| Epristeride | Drug Info | Phase 3 | Hirsutism | [9] | |
| FK-143 | Drug Info | Phase 2 | Prostate disease | [10] | |
| Turosteride | Drug Info | Phase 2 | Prostate disease | [11] | |
| IZONSTERIDE | Drug Info | Phase 1/2 | Hirsutism | [12] | |
| ONO-3805 | Drug Info | Discontinued in Phase 3 | Prostate disease | [13] | |
| CS-891B | Drug Info | Discontinued in Phase 2 | Alopecia | [14] | |
| MK-0963 | Drug Info | Discontinued in Phase 1 | Prostate disease | [15] | |
| MK-434 | Drug Info | Discontinued in Phase 1 | Prostate disease | [16] | |
| GI-197111 | Drug Info | Terminated | Alopecia | [17] | |
| Inhibitor | Azelaic Acid | Drug Info | [18] | ||
| CS-891B | Drug Info | [19] | |||
| Dutasteride | Drug Info | [20] | |||
| Dutasteride + tamsulosin | Drug Info | [21] | |||
| Epristeride | Drug Info | [22] | |||
| Finasteride | Drug Info | [20] | |||
| MK-0963 | Drug Info | [23], [3] | |||
| MK-434 | Drug Info | [24], [3] | |||
| Turosteride | Drug Info | [25] | |||
| Modulator | FK-143 | Drug Info | |||
| GI-197111 | Drug Info | [26] | |||
| IZONSTERIDE | Drug Info | ||||
| ONO-3805 | Drug Info | ||||
| Polyestradiol Phosphate | Drug Info | [27] | |||
| References | |||||
| REF 1 | Azelaic acid. A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentary skin disorders. Drugs. 1991 May;41(5):780-98. | ||||
| REF 2 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7484). | ||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 4 | 5alpha-reductase inhibitors in benign prostatic hyperplasia and prostate cancer risk reduction. Best Pract Res Clin Endocrinol Metab. 2008 Apr;22(2):389-402. | ||||
| REF 5 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7457). | ||||
| REF 6 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
| REF 7 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6818). | ||||
| REF 8 | ClinicalTrials.gov (NCT00090103) Benign Prostatic Hyperplasia Trial With Dutasteride And Tamsulosin Combination Treatment. U.S. National Institutes of Health. | ||||
| REF 9 | Epristeride SmithKline Beecham. IDrugs. 1998 May;1(1):152-7. | ||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003112) | ||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002567) | ||||
| REF 12 | 5alpha-reductase activity in the prostate. Urology. 2001 Dec;58(6 Suppl 1):17-24; discussion 24. | ||||
| REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003081) | ||||
| REF 14 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013642) | ||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003374) | ||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005411) | ||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008867) | ||||
| REF 18 | Inhibition of 5 alpha-reductase activity in human skin by zinc and azelaic acid. Br J Dermatol. 1988 Nov;119(5):627-32. | ||||
| REF 19 | The novel drug CS-891 inhibits 5alpha-reductase activity in freshly isolated dermal papilla of human hair follicles. Eur J Dermatol. 2000 Dec;10(8):593-5. | ||||
| REF 20 | The role of 5-alpha reductase inhibitors in prostate pathophysiology: Is there an additional advantage to inhibition of type 1 isoenzyme? Can Urol Assoc J. 2009 Jun;3(3 Suppl 2):S109-14. | ||||
| REF 21 | Clinical pipeline report, company report or official report of GlaxoSmithKline (2009). | ||||
| REF 22 | Discovery of a novel hybrid from finasteride and epristeride as 5alpha-reductase inhibitor. Bioorg Med Chem Lett. 2011 Jan 1;21(1):475-8. | ||||
| REF 23 | Pharmacodynamics of MK-0963, a new 5 alpha-reductase inhibitor: effects on serum androgen concentrations. Clin Pharmacol Ther. 1994 Jan;55(1):50-4. | ||||
| REF 24 | The effects of progesterone, 4,16-androstadien-3-one and MK-434 on the kinetics of pig testis microsomal testosterone-4-ene-5alpha-reductase activity. J Steroid Biochem Mol Biol. 1997 Mar;60(5-6):353-9. | ||||
| REF 25 | Hormonal effects of turosteride, a 5 alpha-reductase inhibitor, in the rat. J Steroid Biochem Mol Biol. 1993 Nov;46(5):549-55. | ||||
| REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008867) | ||||
| REF 27 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
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