Page last updated: 2024-12-06

epristeride

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Epristeride is a potent and selective type II 5α-reductase inhibitor. It is a synthetic steroid that blocks the conversion of testosterone to dihydrotestosterone (DHT), a hormone that plays a key role in the development of prostate cancer. Epristeride has shown promise in clinical trials for the treatment of benign prostatic hyperplasia (BPH) and prostate cancer. It is currently being investigated for its potential use in other conditions, such as hair loss and acne. Epristeride is a promising drug candidate for the treatment of a variety of conditions related to androgen metabolism.'

epristeride: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68741
CHEMBL ID290823
CHEMBL ID138225
CHEBI ID31552
SCHEMBL ID61222
MeSH IDM0196485

Synonyms (48)

Synonym
ono 9302
17-beta-n-t-butylcarboxamide-androst-3,5-diene-3-carboxylic acid
(17-beta)-17-(((1,1-dimethylethyl)amino)carbonyl)androsta-3,5-diene-3-carboxylic acid
sk&f 105657
skf 105657
androsta-3,5-diene-3-carboxylic acid, 17-(((1,1-dimethylethyl)amino)carbonyl)-, (17beta)-
17beta-(tert-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
bdbm50031890
(10r,13s,17s)-17-tert-butylcarbamoyl-10,13-dimethyl-2,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthrene-3-carboxylic acid
chembl290823
(10r,13s)-17-tert-butylcarbamoyl-10,13-dimethyl-2,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthrene-3-carboxylic acid
(10r,14s)-17-tert-butylcarbamoyl-10-methyl-13-(s)-methyl-2,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthrene-3-carboxylic acid
17-tert-butylcarbamoyl-10,13-dimethyl-2,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthrene-3-carboxylic acid
bdbm50043604
epristeride
sk&f-105657
ono-9302
D01134
119169-78-7
epristeride (jan/usan/inn)
CHEMBL138225 ,
(8s,9s,10r,13s,14s,17s)-17-(tert-butylcarbamoyl)-10,13-dimethyl-2,7,8,9,11,12,14,15,16,17-decahydro-1h-cyclopenta[a]phenanthrene-3-carboxylic acid
epristeride [usan:inn:ban]
unii-39517a04ps
ccris 8535
39517a04ps ,
dtxcid2028569
dtxsid9048643 ,
cas-119169-78-7
tox21_112993
SCHEMBL61222
epristeride [inn]
epristeride [usan]
epristeride [mi]
androsta-3,5-diene-3-carboxylic acid, 17-(((1,1-dimethylethyl)amino)carbonyl)-, (17.beta.)-
epristeride [who-dd]
epristeride [jan]
17beta-(n-t-butylcarbamoyl)androsta-3,5-diene-3-carboxylic acid
VAPSMQAHNAZRKC-PQWRYPMOSA-N
HY-107385
CS-7978
CHEBI:31552
AKOS030573838
skf105657
Q5383934
MS-26777
androsta-3,5-diene-3-carboxylic acid, 17-[[(1,1-dimethylethyl)amino]carbonyl]-, (17beta)-
Z2037280246

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Epristeride treatment caused significant reduction in ventral prostate weight in a dose-dependent manner."( Effect of epristeride on the expression of IGF-1 and TGF-beta receptors in androgen-induced castrated rat prostate.
Qi, XD; Sun, HZ; Tu, ZH; Wu, SF, 2001
)
1.43

Toxicity

ExcerptReferenceRelevance
" The objective of the current investigation was to research the toxic effects of epristeride and to demonstrate its reversible."( Reversible long-term toxicity of epristeride in beagle dogs.
Feng, J; Qi, XD; Sun, ZY; Tu, ZH; Wu, HY; Zheng, WJ, 1999
)
0.81

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic analysis of the plasma concentration-time data was performed by both non-compartmental and compartmental methods."( Pharmacokinetics and absolute bioavailability of epristeride in healthy male subjects.
Audet, PR; Benincosa, LJ; Jorkasky, DK; Lundberg, D; Zariffa, N, 1996
)
0.55
"kg-1, both the Cmax and AUC increased proportionally with the dosages."( [Pharmacokinetics of epristeride in rats and beagle dogs].
Liu, CX; Wei, GL; Xiao, SH, 2000
)
0.63
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
"The objective of the current investigation was to describe the pharmacokinetics and absolute oral bioavailability of epristeride."( Pharmacokinetics and absolute bioavailability of epristeride in healthy male subjects.
Audet, PR; Benincosa, LJ; Jorkasky, DK; Lundberg, D; Zariffa, N, 1996
)
0.76
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" This long half-life allows for once-daily dosing of epristeride."( Pharmacokinetics and absolute bioavailability of epristeride in healthy male subjects.
Audet, PR; Benincosa, LJ; Jorkasky, DK; Lundberg, D; Zariffa, N, 1996
)
0.8
"09% of the dosage and in feces to 42."( [Pharmacokinetics of epristeride in rats and beagle dogs].
Liu, CX; Wei, GL; Xiao, SH, 2000
)
0.63
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
steroid acidAny steroid substituted by at least one carboxy group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency31.67680.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency23.91450.000221.22318,912.5098AID743036
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency1.50890.000214.376460.0339AID720692
estrogen nuclear receptor alphaHomo sapiens (human)Potency11.33390.000229.305416,493.5996AID743069; AID743075
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)IC50 (µMol)2.44000.00170.48807.5000AID207458; AID207459; AID207460; AID207913; AID215795
3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)Ki3.30000.00500.53031.6000AID207920; AID91251
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.04750.00427.468021.1000AID207591; AID207907
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Rattus norvegicus (Norway rat)Ki0.03000.00500.04010.0882AID207292
3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)IC50 (µMol)0.00530.00010.526710.0000AID205602; AID205603; AID207443; AID207445; AID207446; AID215798; AID91252
3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)Ki0.03000.00060.08690.2300AID207292
3-oxo-5-alpha-steroid 4-dehydrogenase 2Rattus norvegicus (Norway rat)IC50 (µMol)0.05000.00037.329421.1000AID207907
3-oxo-5-alpha-steroid 4-dehydrogenase 2Rattus norvegicus (Norway rat)Ki0.03000.00501.711010.0000AID207292
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
urogenital system development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
liver development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
androgen biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
androgen catabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
sex determination3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
male gonad development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to starvation3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to xenobiotic stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to muscle activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
diterpenoid metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
spinal cord development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
hippocampus development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
thalamus development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
hypothalamus development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
pituitary gland development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cerebral cortex development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cell differentiation3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
male genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
female genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to follicle-stimulating hormone3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to insulin stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
serotonin metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
progesterone metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to estrogen3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
bone development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to growth hormone3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to fungicide3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to cAMP3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to growth factor stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to estradiol stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to testosterone stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to dexamethasone stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to epinephrine stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
steroid biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
androgen biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
steroid catabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
cell-cell signaling3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
androgen metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
male gonad development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to xenobiotic stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
biphenyl metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
dibenzo-p-dioxin metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
phthalate metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
hippocampus development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
hypothalamus development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
cell differentiation3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
male genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
female genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to nutrient levels3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to follicle-stimulating hormone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to testosterone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to peptide hormone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to steroid hormone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
bone development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
testosterone biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
steroid biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
3-oxo-5-alpha-steroid 4-dehydrogenase activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
electron transfer activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
amide binding3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
3-oxo-5alpha-steroid 4-dehydrogenase (NADP+) activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
NADPH binding3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
3-oxo-5-alpha-steroid 4-dehydrogenase activity3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
protein binding3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
testosterone dehydrogenase [NAD(P)] activity3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
amide binding3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
3-oxo-5alpha-steroid 4-dehydrogenase (NADP+) activity3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membrane3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
neuronal cell body3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
perinuclear region of cytoplasm3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cell body fiber3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
endoplasmic reticulum membrane3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
neuronal cell body3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
cell body fiber3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID207446Inhibitory activity measured on human steroid 5-alpha-reductase type 21995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent.
AID1698010Hepatic clearance in human administered through iv dosing
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1698004Fraction unbound in cynomolgus monkey plasma
AID207460Inhibitory concentration against human Steroid 5-alpha-reductase type I in DU 145 cell culture using 3H androstenedione 5 nM as substrate1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
N-substituted 4-(5-indolyl)benzoic acids. Synthesis and evaluation of steroid 5alpha-reductase type I and II inhibitory activity.
AID1698001Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID1698009Hepatic clearance in cynomolgus monkey at < 1 mg/kg, iv administered as cassette dosing
AID1698006Ratio of drug level in cynomolgus monkey blood to plasma administered through iv dosing by LC-MS/MS analysis
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID207920In vitro inhibitory activity against human type 1 5-alpha reductase1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
6-Azasteroids: structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID207458Inhibition of recombinant Steroid 5-alpha-reductase type I was evaluated as binding affinity of the compound1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent.
AID91252Inhibition of recombinant human 5-alpha reductase-2 at a concentration of 5 microL after pre-incubation for 10 minutes1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5 alpha-reductase.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID215795In vitro inhibition of DHT production in Hs 68 (human genital fibroblast) cells.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
AID215798Compound was tested for inhibition of Type II 5-alpha-reductase in Human Prostate Homogenates (HPH)1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
AID1698011Fraction unbound in human plasma
AID1698002Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis
AID3435Inhibition of recombinant human adrenal 3-beta-hydroxy-delta-5-steroid dehydrogenase1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent.
AID1698007Ratio of drug level in human blood to plasma administered through iv dosing by LC-MS/MS analysis
AID207913Inhibition of type 1 steroid-5-alpha-reductase1994Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23
4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase.
AID437555Inhibition of human steroid 5 alpha-reductase2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Self organizing molecular field analysis on a series of human 5alpha-reductase inhibitors: unsaturated 3-carboxysteroid.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID91251Inhibition of recombinant human 5-alpha reductase-1 at a concentration of 5 microL after pre-incubation for 10 minutes1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5 alpha-reductase.
AID207292In vitro inhibitory activity against Steroid 5-alpha-reductase was determined in human prostatic tissue expressed as apparent inhibition constant; Range is 30-361990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Inhibition of steroid 5 alpha-reductase by unsaturated 3-carboxysteroids.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID207591Inhibitory activity against rat Steroid 5-alpha-reductase type I using 18213 3H testosterone 210 nM as substrate1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
N-substituted 4-(5-indolyl)benzoic acids. Synthesis and evaluation of steroid 5alpha-reductase type I and II inhibitory activity.
AID207443Inhibition of recombinant human Steroid 5-alpha-reductase type 21995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID207432In vitro inhibitory activity against Steroid 5-alpha-reductase was determined in rat ventral prostates expressed as apparent inhibition constant; Range is 20-301990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Inhibition of steroid 5 alpha-reductase by unsaturated 3-carboxysteroids.
AID3434In vitro inhibitory activity against human adrenal 3-beta hydroxy-delta 5-teroid isomerase1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
6-Azasteroids: structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase.
AID1697999Dissociation constant, acidic pKa of compound measured up to 18 mins by capillary electrophoresis
AID207459Inhibition of recombinant human Steroid 5-alpha-reductase type I1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency.
AID205603In vitro inhibitory activity against human type 2 5-alpha reductase1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
6-Azasteroids: structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID207904Inhibitory concentration on human 5-alpha reductase isozyme1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID207445Inhibitory activity against human Steroid 5-alpha-reductase type 2 using 18213 3H testosterone 210 nM as substrate1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
N-substituted 4-(5-indolyl)benzoic acids. Synthesis and evaluation of steroid 5alpha-reductase type I and II inhibitory activity.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1698000Apparent permeability in dog MDCKII-LE cells at pH 7.4
AID205602Inhibition of type 2 steroid-5-alpha-reductase1994Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23
4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase.
AID207907Inhibition of rat 5-alpha reductase isozyme.1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (45)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's24 (53.33)18.2507
2000's14 (31.11)29.6817
2010's4 (8.89)24.3611
2020's3 (6.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.61 (24.57)
Research Supply Index3.95 (2.92)
Research Growth Index4.21 (4.65)
Search Engine Demand Index36.71 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (8.51%)5.53%
Reviews1 (2.13%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other42 (89.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]