Target Information

Target General Infomation
Target ID
T27265
Former ID
TTDS00240
Target Name
5-alpha reductase
Synonyms
5 alpha-reductase; Hepatic 5-alpha reductase
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 [ICD9: 185; ICD10: C61]
Prostate disease [ICD10: N42.9]
Prostate cancer; Benign prostatic hyperplasia [ICD9: 140-229, 185, 600; ICD10: C61, N40]
BioChemical Class
Oxidoreductases acting on CH-CH group of donors
Target Validation
T27265
EC Number
EC 1.3.99.5
Drugs and Mode of Action
Drug(s) Azelaic Acid Drug Info Approved Acne vulgaris [528549], [542507], [551871]
Dutasteride Drug Info Approved Benign prostatic hyperplasia [536709], [542481]
Finasteride Drug Info Approved Benign prostatic hyperplasia [536361], [541900]
Polyestradiol Phosphate Drug Info Approved Prostate cancer [551871]
Dutasteride Drug Info Phase 3 Prostate cancer [536709], [542481]
Dutasteride + tamsulosin Drug Info Phase 3 Prostate cancer; Benign prostatic hyperplasia [521609]
Epristeride Drug Info Phase 3 Hirsutism [529459]
FK-143 Drug Info Phase 2 Prostate disease [545399]
Turosteride Drug Info Phase 2 Prostate disease [545243]
IZONSTERIDE Drug Info Phase 1/2 Hirsutism [526225]
ONO-3805 Drug Info Discontinued in Phase 3 Prostate disease [545383]
CS-891B Drug Info Discontinued in Phase 2 Alopecia [547178]
MK-0963 Drug Info Discontinued in Phase 1 Prostate disease [545468]
MK-434 Drug Info Discontinued in Phase 1 Prostate disease [545935]
GI-197111 Drug Info Terminated Alopecia [546539]
Inhibitor Azelaic Acid Drug Info [537740]
CS-891B Drug Info [525936]
Dutasteride Drug Info [537501]
Dutasteride + tamsulosin Drug Info [550963]
Epristeride Drug Info [531271]
Finasteride Drug Info [537501]
MK-0963 Drug Info [533979], [551871]
MK-434 Drug Info [534422], [551871]
Turosteride Drug Info [533947]
Modulator FK-143 Drug Info
GI-197111 Drug Info [546540]
IZONSTERIDE Drug Info
ONO-3805 Drug Info
Polyestradiol Phosphate Drug Info [556264]
References
Ref 521609ClinicalTrials.gov (NCT00090103) Benign Prostatic Hyperplasia Trial With Dutasteride And Tamsulosin Combination Treatment. U.S. National Institutes of Health.
Ref 5262255alpha-reductase activity in the prostate. Urology. 2001 Dec;58(6 Suppl 1):17-24; discussion 24.
Ref 528549Azelaic acid. A review of its pharmacological properties and therapeutic efficacy in acne and hyperpigmentary skin disorders. Drugs. 1991 May;41(5):780-98.
Ref 529459Epristeride SmithKline Beecham. IDrugs. 1998 May;1(1):152-7.
Ref 536361Natural 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 5367095alpha-reductase inhibitors in benign prostatic hyperplasia and prostate cancer risk reduction. Best Pract Res Clin Endocrinol Metab. 2008 Apr;22(2):389-402.
Ref 541900(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 542481(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 542507(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 545243Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002567)
Ref 545383Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003081)
Ref 545399Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003112)
Ref 545468Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003374)
Ref 545935Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005411)
Ref 546539Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008867)
Ref 547178Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013642)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525936The 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 531271Discovery of a novel hybrid from finasteride and epristeride as 5alpha-reductase inhibitor. Bioorg Med Chem Lett. 2011 Jan 1;21(1):475-8.
Ref 533947Hormonal effects of turosteride, a 5 alpha-reductase inhibitor, in the rat. J Steroid Biochem Mol Biol. 1993 Nov;46(5):549-55.
Ref 533979Pharmacodynamics of MK-0963, a new 5 alpha-reductase inhibitor: effects on serum androgen concentrations. Clin Pharmacol Ther. 1994 Jan;55(1):50-4.
Ref 534422The 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 537501The 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 537740Inhibition of 5 alpha-reductase activity in human skin by zinc and azelaic acid. Br J Dermatol. 1988 Nov;119(5):627-32.
Ref 546540Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008867)
Ref 550963Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

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