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finasteride

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Description

Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia. [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]

Cross-References

ID SourceID
PubMed CID57363
CHEMBL ID710
CHEBI ID5062
SCHEMBL ID5509
MeSH IDM0027324

Synonyms (162)

Synonym
AB00513901-08
AB00513901-07
BRD-K01095011-001-03-5
(4ar,6as,11ar)-4a,6a-dimethyl-2-oxo-hexadecahydro-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide
4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide(finasteride)
(4ar,6as,7s)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide
4a,6a,9a-trimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid (finasteride)
(r)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide
(4ar,4bs,6as,9as,9bs,11ar)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide
bdbm50334788
(4ar,6as,7s,11ar)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide
(17beta-(n-tert-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one
(4ar,4bs,6as,7s,9as,9bs,11ar)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide
(4ar,6as)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxylic acid tert-butylamide
finasterida
CHEBI:5062 ,
andozac
ym-152
finasteridum
BPBIO1_001027
finasteride, >=98% (hplc), powder
l-652,931
chibro-proscar
propecia
ccris 7438
finasterida [inn-spanish]
brn 4269024
finastid
hsdb 6793
mk-906
n-tert-butyl-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide
finasteridum [inn-latin]
17beta-(n-tert-butylcarbamoyl)-4-aza-5 alpha-androst-1-en-3-one
4-azaandrost-1-ene-17-carboxamide, n-(1,1-dimethylethyl)-3-oxo-, (5alpha,17beta)-
(5alpha,17beta)-(1,1-dimethylethyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide
n-(2-methyl-2-propyl)-3-oxo-4-aza-5-alpha-androst-1-ene-17-beta-carboxamide
(4ar,4bs,6as,7s,9as,9bs,11ar)-n-(1,1-dimethylethyl)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxamide
mk-0906
mk 0906
(4ar,4bs,6as,7s,9as,9bs,11ar)-n-(tert-butyl)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxamide
finpecia
proscar
prostide
NCGC00016965-01
cas-98319-26-7
PRESTWICK3_000717
PRESTWICK2_000717
BSPBIO_000933
MLS001424046
AB00513901
finasteride
smr000466304
MLS000759404
DB01216
cpd000466304
D00321
propecia (tn)
proscar (tn)
98319-26-7
finasteride (jan/usp/inn)
PRESTWICK0_000717
PRESTWICK1_000717
SPBIO_002854
mk 906
propeshia
mk906
MLS001165768
(4ar,4bs,6as,7s,9as,9bs,11ar)-n-tert-butyl-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1h-indeno[5,4-f]quinoline-7-carboxamide
HMS2051F09
HMS2090G22
nsc-759318
CHEMBL710 ,
(1s,3as,3bs,5ar,9ar,9bs,11as)-n-tert-butyl-9a,11a-dimethyl-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide
nsc741485
4-azaandrost-1-ene-17-carboxamide,1-dimethylethyl)-3-oxo-, (5.alpha., 17.beta.)-
finasteride (proscar)
nsc-741485
HMS1570O15
A845840
(1s,3as,3bs,5ar,9ar,9bs,11as)-n-isobutyl-9a,11a-dimethyl-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide;finasteride
HMS2097O15
finasteride [usan:usp:inn:ban]
unii-57gno57u7g
57gno57u7g ,
nsc 759318
nsc 741485
dtxcid50625
dtxsid3020625 ,
NCGC00256334-01
tox21_302744
tox21_201506
NCGC00259057-01
tox21_110717
HMS2235L23
CCG-100937
BCP9000685
BCPP000229
BCP0726000222
finasteride component of entadfi
finasteride [vandf]
finasteride [inn]
finasteride [usp monograph]
finasteride [ep monograph]
finasteride [usan]
finasteride [mart.]
finasteride [who-dd]
finasteride [orange book]
entadfi component finasteride
finasteride [jan]
finasteride [mi]
finasteride [usp impurity]
finasteride [ep impurity]
S1197
AKOS015894916
gtpl6818
HY-13635
CS-1767
(1s,3as,3bs,5ar,9ar,9bs,11as)-n-isobutyl-9a,11a-dimethyl-7-oxo-1,2,3,3a,3b,4,5,5a,6,9b,10,11-dodecahydroindeno[5,4-f]quinoline-1-carboxamide
NC00187
SCHEMBL5509
tox21_110717_1
NCGC00093560-05
KS-1058 ,
DBEPLOCGEIEOCV-WSBQPABSSA-N
(5?,17?)-n-(1,1-dimethylethyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide
finasteride, british pharmacopoeia (bp) reference standard
AB00513901_09
mfcd00869737
(1s,2r,7r,10s,11s,14s,15s)-n-tert-butyl-2,15-dimethyl-5-oxo-6-azatetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-3-ene-14-carboxamide
SR-01000759414-4
sr-01000759414
SR-01000759414-6
finasteride, united states pharmacopeia (usp) reference standard
finasteride, vetranal(tm), analytical standard
finasteride for peak identification, european pharmacopoeia (ep) reference standard
finasteride, european pharmacopoeia (ep) reference standard
HMS3714O15
Q424167
([1-phenyl-meth-(e)-ylidene]-amino)-aceticacidethylester
140375-21-9
BRD-K01095011-001-15-9
EX-A1951
nsc-757443
nsc757443
BF164456
urprosan
finasterida (inn-spanish)
finasteride (usp impurity)
finasteride (ep monograph)
pro-cure
finasteridum (inn-latin)
d11ax10
(5alpha,17beta)-n-(1,1-dimethylethyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide
finasteride (usp monograph)
finasteride (mart.)
g04cb01
finasteride (ep impurity)
(5 alpha, 17 beta)-(1,1-dimethylethyl)-3-oxo-4-azaandrost-1-ene-17-carboxamide
17 beta-(n-tert-butylcarbamoyl)-4-aza-5 alpha-androst-1-en-3-one
finasteride (usan:usp:inn:ban)
1h-indeno[5,4-f]quinoline-7-carboxamide, n-(1,1-dimethylethyl)-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-4a,6a-dimethyl-2-oxo-, (4ar,4bs,6as,7s,9as,9bs,11ar)-
Z1501475008

Research Excerpts

Toxicity

Finasteride has been associated with reversible adverse sexual side effects in multiple randomized, controlled trials for the treatment of male pattern hair loss. Impotence was the most frequent reason for stopping treatment with finasteride.

ExcerptReferenceRelevance
" Finasteride was well tolerated and there was no evidence of increased adverse experiences with increased duration of treatment."( Three-year safety and efficacy data on the use of finasteride in the treatment of benign prostatic hyperplasia.
Stoner, E, 1994
)
0.29
" Impotence was the most frequent reason for stopping treatment with finasteride and was the most commonly reported adverse reaction to the drug."( The safety of finasteride used in benign prostatic hypertrophy: a non-interventional observational cohort study in 14,772 patients.
Edet, E; Freemantle, S; Mann, RD; Pearce, G; Stephens, MD; Wilton, L, 1996
)
0.29
" The results of this study strongly suggest that this drug is acceptably safe when used in accordance with the current prescribing information."( The safety of finasteride used in benign prostatic hypertrophy: a non-interventional observational cohort study in 14,772 patients.
Edet, E; Freemantle, S; Mann, RD; Pearce, G; Stephens, MD; Wilton, L, 1996
)
0.29
"onset, course and resolution of all adverse events during the treatment period."( Efficacy and safety of finasteride therapy for benign prostatic hyperplasia: results of a 2-year randomized controlled trial (the PROSPECT study). PROscar Safety Plus Efficacy Canadian Two year Study.
Afridi, SK; Boake, RC; Elhilali, MM; Fradet, Y; Nickel, JC; Perreault, JP; Pommerville, PJ, 1996
)
0.29
" In the safety analysis, the proportion of patients who experienced any adverse event was similar in the two groups (81."( Efficacy and safety of finasteride therapy for benign prostatic hyperplasia: results of a 2-year randomized controlled trial (the PROSPECT study). PROscar Safety Plus Efficacy Canadian Two year Study.
Afridi, SK; Boake, RC; Elhilali, MM; Fradet, Y; Nickel, JC; Perreault, JP; Pommerville, PJ, 1996
)
0.29
" Within each age cohort, no significant differences were found between the placebo and finasteride-treated patients in the incidence of cardiovascular adverse events."( Comparison of the efficacy and safety of finasteride in older versus younger men with benign prostatic hyperplasia.
Bruskewitz, R; Cook, TJ; Holtgrewe, HL; Kaplan, SA; Lund, RH; Meehan, A; Mobley, D; Narayan, P; Saltzman, B; Waldstreicher, J; Weiner, S; Wells, G, 2001
)
0.31
"To systematically review and evaluate the effectiveness and adverse effects of the alpha-antagonist, terazosin, for treating urinary symptoms associated with benign prostatic obstruction (BPO)."( Terazosin for treating symptomatic benign prostatic obstruction: a systematic review of efficacy and adverse effects.
Howe, W; MacDonald, R; Wilt, TJ, 2002
)
0.31
" Adverse effects were greater than with placebo and included dizziness, asthenia, headache and postural hypotension."( Terazosin for treating symptomatic benign prostatic obstruction: a systematic review of efficacy and adverse effects.
Howe, W; MacDonald, R; Wilt, TJ, 2002
)
0.31
" Adverse effects were generally mild but more frequent than with other alpha-antagonists and associated with a two- to four-fold increase in treatment discontinuation."( Terazosin for treating symptomatic benign prostatic obstruction: a systematic review of efficacy and adverse effects.
Howe, W; MacDonald, R; Wilt, TJ, 2002
)
0.31
" In comparative trials, finasteride demonstrated efficacy similar to that of other antiandrogens, with fewer adverse effects."( Relative safety and efficacy of finasteride for treatment of hirsutism.
Marlowe, KF; Townsend, KA, 2004
)
0.32
" Reported adverse effects have been minimal."( Relative safety and efficacy of finasteride for treatment of hirsutism.
Marlowe, KF; Townsend, KA, 2004
)
0.32
" Five patients in the finasteride and seven in the placebo group reported medication-related adverse events."( A randomized placebo-controlled multicentre study to evaluate the safety and efficacy of finasteride for male chronic pelvic pain syndrome (category IIIA chronic nonbacterial prostatitis).
Downey, J; Nickel, JC; Pontari, MA; Shoskes, DA; Zeitlin, SI, 2004
)
0.32
"To evaluate the efficacy and adverse effects of doxazosin for treating lower urinary tract symptoms (LUTS) compatible with benign prostatic obstruction (BPO)."( Doxazosin for treating lower urinary tract symptoms compatible with benign prostatic obstruction: a systematic review of efficacy and adverse effects.
Howe, RW; MacDonald, R; Wilt, TJ, 2004
)
0.32
" Adverse events reported for combined therapy were similar to those with each monotherapy."( Doxazosin for treating lower urinary tract symptoms compatible with benign prostatic obstruction: a systematic review of efficacy and adverse effects.
Howe, RW; MacDonald, R; Wilt, TJ, 2004
)
0.32
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" 5ARIs were generally well tolerated, with sexual dysfunction the most frequently reported adverse effect, although in only a small proportion of men (1%-8%)."( A review of the clinical efficacy and safety of 5alpha-reductase inhibitors for the enlarged prostate.
Miner, M; Naslund, MJ, 2007
)
0.34
"Sexual adverse experiences such as erectile dysfunction (ED), loss of libido, and ejaculation disorders have been consistent side effects of finasteride in a maximum percentage of 15% after 1 year of therapy."( Finasteride 5 mg and sexual side effects: how many of these are related to a nocebo phenomenon?
Bartoletti, R; Cai, T; Gavazzi, A; Giubilei, G; Gontero, P; Lombardi, G; Mondaini, N, 2007
)
0.34
"The estimation of side effect was conducted at 6 and 12 months using the male sexual function-4 (MSF-4 item) questionnaire and a self-administered questionnaire."( Finasteride 5 mg and sexual side effects: how many of these are related to a nocebo phenomenon?
Bartoletti, R; Cai, T; Gavazzi, A; Giubilei, G; Gontero, P; Lombardi, G; Mondaini, N, 2007
)
0.34
" The burden of this nocebo effect (an adverse side effect that is not a direct result of the specific pharmacological action of the drug) has to be taken into account when managing finasteride sexual side effects."( Finasteride 5 mg and sexual side effects: how many of these are related to a nocebo phenomenon?
Bartoletti, R; Cai, T; Gavazzi, A; Giubilei, G; Gontero, P; Lombardi, G; Mondaini, N, 2007
)
0.34
" Outcome measures included patient self-assessment, hair count, investigator clinical assessment, global photographic assessment, and adverse effects at short term (≤12 months) and long term (≥24 months)."( Efficacy and safety of finasteride therapy for androgenetic alopecia: a systematic review.
Catalano, HN; Guyatt, G; Manzotti, M; Mella, JM; Perret, MC, 2010
)
0.36
" Although the adverse side effects of these agents are thought to be minimal, the magnitude of adverse effects on sexual function, gynecomastia, depression, and quality of life remains ill-defined."( Adverse side effects of 5α-reductase inhibitors therapy: persistent diminished libido and erectile dysfunction and depression in a subset of patients.
Guay, AT; Hansen, ML; Hassani, J; Traish, AM; Zitzmann, M, 2011
)
0.37
"  Prolonged adverse effects on sexual function such as erectile dysfunction and diminished libido are reported by a subset of men, raising the possibility of a causal relationship."( Adverse side effects of 5α-reductase inhibitors therapy: persistent diminished libido and erectile dysfunction and depression in a subset of patients.
Guay, AT; Hansen, ML; Hassani, J; Traish, AM; Zitzmann, M, 2011
)
0.37
"Finasteride has been associated with reversible adverse sexual side effects in multiple randomized, controlled trials for the treatment of male pattern hair loss (MPHL)."( Persistent sexual side effects of finasteride for male pattern hair loss.
Irwig, MS; Kolukula, S, 2011
)
0.37
"Despite their efficacy in the treatment of benign prostatic hyperplasia (BPH) the popularity of inhibitors of 5α-reductase (5ARI) is limited by their association with adverse sexual side effects."( Inhibitors of 5α-reductase-related side effects in patients seeking medical care for sexual dysfunction.
Balercia, G; Corona, G; Forti, G; Maggi, M; Mannucci, E; Maseroli, E; Rastrelli, G; Sforza, A, 2012
)
0.38
" Prescribers of finasteride and men contemplating its use should be made aware of the potential adverse medication effects."( Persistent sexual side effects of finasteride: could they be permanent?
Irwig, MS, 2012
)
0.38
" Safety assessments included International Index of Erectile Function (IIEF) and adverse events."( A 5-year retrospective analysis of 5α-reductase inhibitors in men with benign prostatic hyperplasia: finasteride has comparable urinary symptom efficacy and prostate volume reduction, but less sexual side effects and breast complications than dutasteride.
Chung, DE; Kaplan, SA; Lee, RK; Scofield, S; Te, AE, 2012
)
0.38
" MFX may be a safe and effective treatment option."( Efficacy and safety of 3% minoxidil versus combined 3% minoxidil / 0.1% finasteride in male pattern hair loss: a randomized, double-blind, comparative study.
Tanglertsampan, C, 2012
)
0.38
" Changes in lower urinary tract symptoms secondary to benign prostatic hyperplasia were assessed with the I-PSS, erectile dysfunction improvements were assessed with the IIEF-EF (International Index of Erectile Function-Erectile Function) in sexually active men and safety was assessed by evaluating adverse events."( Efficacy and safety of the coadministration of tadalafil once daily with finasteride for 6 months in men with lower urinary tract symptoms and prostatic enlargement secondary to benign prostatic hyperplasia.
Casabé, A; Da Pozzo, LF; Henderson, RJ; Henneges, C; Roehrborn, CG; Sorsaburu, S; Viktrup, L; Wong, DG; Zepeda, S, 2014
)
0.4
" Tadalafil/finasteride coadministration was well tolerated and most adverse events were mild/moderate."( Efficacy and safety of the coadministration of tadalafil once daily with finasteride for 6 months in men with lower urinary tract symptoms and prostatic enlargement secondary to benign prostatic hyperplasia.
Casabé, A; Da Pozzo, LF; Henderson, RJ; Henneges, C; Roehrborn, CG; Sorsaburu, S; Viktrup, L; Wong, DG; Zepeda, S, 2014
)
0.4
" The number and severity of adverse events were similar among treatment groups."( A randomized, active- and placebo-controlled study of the efficacy and safety of different doses of dutasteride versus placebo and finasteride in the treatment of male subjects with androgenetic alopecia.
Barboza Martínez, J; Barnes, A; Chetty, D; Ferron-Brady, G; Gubelin Harcha, W; Katsuoka, K; Kawashima, M; Tsai, TF; Tsuboi, R, 2014
)
0.4
"Dutasteride can be used to improve urinary symptoms (IPSS and Q max) and reduce TPV but with awareness of its potential adverse events."( Efficacy and safety of dutasteride for the treatment of symptomatic benign prostatic hyperplasia (BPH): a systematic review and meta-analysis.
Choi, JY; Park, T, 2014
)
0.4
" In some patients the treatment is associated with adverse side effects that could become persistent after therapy discontinuation, resulting in the so-called post-finasteride syndrome (PFS)."( A pharmacogenetic survey of androgen receptor (CAG)n and (GGN)n polymorphisms in patients experiencing long term side effects after finasteride discontinuation.
Cauci, S; Cecchin, E; De Mattia, E; Mazzon, G; Toffoli, G; Trombetta, C, 2014
)
0.4
" Molecular events inducing persistent adverse sexual symptoms are unexplored."( Immunohistochemical evaluation of androgen receptor and nerve structure density in human prepuce from patients with persistent sexual side effects after finasteride use for androgenetic alopecia.
Belgrano, E; Cauci, S; Di Loreto, C; La Marra, F; Mazzon, G; Trombetta, C, 2014
)
0.4
"Two meta-analyses conclude that finasteride treatment of androgenic alopecia (AGA) is safe but do not assess quality of safety reporting."( Adverse Event Reporting in Clinical Trials of Finasteride for Androgenic Alopecia: A Meta-analysis.
Aslam, I; Belknap, SM; Brannigan, RE; Cashy, J; Kiguradze, T; Micali, G; Nardone, B; Temps, WH; West, DP; Yarnold, PR, 2015
)
0.42
"For each trial, we assessed quality of adverse event reporting, extracted the number and type of adverse events in treatment and placebo groups, and assessed duration of safety evaluation and adequacy of blinding."( Adverse Event Reporting in Clinical Trials of Finasteride for Androgenic Alopecia: A Meta-analysis.
Aslam, I; Belknap, SM; Brannigan, RE; Cashy, J; Kiguradze, T; Micali, G; Nardone, B; Temps, WH; West, DP; Yarnold, PR, 2015
)
0.42
"Of 34 clinical trials, none had adequate safety reporting, 19 were partially adequate, 12 were inadequate, and 3 reported no adverse events."( Adverse Event Reporting in Clinical Trials of Finasteride for Androgenic Alopecia: A Meta-analysis.
Aslam, I; Belknap, SM; Brannigan, RE; Cashy, J; Kiguradze, T; Micali, G; Nardone, B; Temps, WH; West, DP; Yarnold, PR, 2015
)
0.42
"The aim of the study is to present the effects of BPH pharmacological treatment on the occurrence of sexually adverse effects in men: changes in sexual desire, erectile, ejaculatory and the orgasmic function."( Adverse Effects of Pharmacological Therapy of Benign Prostatic Hyperplasia on Sexual Function in Men.
Bogdanović, D; Djenić, N; Ignjatović, I; Stojanović, N,
)
0.13
" The main adverse effect on sexual function in men is the deterioration in ejaculation or the absence thereof."( Adverse Effects of Pharmacological Therapy of Benign Prostatic Hyperplasia on Sexual Function in Men.
Bogdanović, D; Djenić, N; Ignjatović, I; Stojanović, N,
)
0.13
" Recent preclinical and clinical findings indicate that 5α-R inhibitors evoke not only beneficial, but also adverse effects."( Adverse effects of 5α-reductase inhibitors: What do we know, don't know, and need to know?
Bortolato, M; Garcia-Segura, LM; Melcangi, RC; Traish, AM; Zitzmann, M, 2015
)
0.42
"Concern regarding adverse effects of finasteride is increasing."( An observational retrospective evaluation of 79 young men with long-term adverse effects after use of finasteride against androgenetic alopecia.
Cauci, S; Chiriacò, G; Mazzon, G; Trombetta, C, 2016
)
0.43
"Treatment-induced sexual dysfunctions (SD) are a recurrent and controversial topic in recent literature on the adverse events related to the use of 5-alpha-reductase inhibitors (5ARIs) (1, 2)."( Comments concerning the real risk of sexual adverse events secondary to the use of 5-ARIs.
Pirozzi Farina, F; Pischedda, A, 2016
)
0.43
" Consequently, any possible clinical/paraclinical elements that might predict these adverse effects would be useful in the selection of a therapeutic strategy for male androgenic alopecia."( Are hand preference and sexual orientation possible predicting factors for finasteride adverse effects in male androgenic alopecia?
Baleanu, BC; Georgescu, SR; Motofei, IG; Paunica, S; Rowland, DL; Tampa, M, 2016
)
0.43
" The reported adverse effects are notable in some patients, consisting in signs and symptoms that are encountered both during finasteride administration and after treatment cessation."( Finasteride adverse effects in subjects with androgenic alopecia: A possible therapeutic approach according to the lateralization process of the brain.
Baconi, D; Balalau, C; Baleanu, BC; Constantin, V; Georgescu, SR; Motofei, IG; Paunica, S; Rowland, DL; Stefanescu, E; Tampa, M, 2016
)
0.43
" A review of 20 peer-reviewed articles found that very few side effects, or adverse events, related to sexual function have been reported in studies in which dutasteride or finasteride has been used to treat hair loss in women."( Side Effects Related to 5 α-Reductase Inhibitor Treatment of Hair Loss in Women: A Review.
Eglini, AN; McMichael, AJ; Seale, LR, 2016
)
0.43
" However, little is known about the differences in adverse effects between these two drugs."( Differences in reproductive toxicology between alopecia drugs: an analysis on adverse events among female and male cases.
Li, Q; Wu, M; Yu, Q, 2016
)
0.43
"Finasteride is currently used extensively for male androgenic alopecia and benign prostatic hyperplasia; however, some adverse effects are severe and even persistent after treatment cessation, the so-called 'post-finasteride syndrome'."( Safety Profile of Finasteride: Distribution of Adverse Effects According to Structural and Informational Dichotomies of the Mind/Brain.
Georgescu, SR; Manea, M; Motofei, IG; Păunică, I; Rowland, DL; Sinescu, I, 2017
)
0.46
"Finasteride has proved to be relatively safe and effective in the therapeutic management of male androgenic alopecia."( Post-Finasteride Adverse Effects in Male Androgenic Alopecia: A Case Report of Vitiligo.
Balalau, C; Baleanu, BC; Constantin, VD; Georgescu, SR; Manea, M; Motofei, IG; Paunica, S; Rowland, DL; Sinescu, I; Tampa, M, 2017
)
0.46
" However, they are associated with some transient and even permanent adverse effects."( [Finasteride adverse effects: An update].
Álvarez-Véliz, S; Berroeta-Mauriziano, D; Carrasco-Zuber, JE; Carreño-Orellana, N; Moll-Manzur, C; Porras-Kusmanic, N, 2016
)
0.43
"Treatment of AGA with 5α-reductase inhibitors lead to variable adverse effects and relatively unstable results (therapeutic efficacy ending with treatment cessation), so the choice of optimal therapy is not straightforward."( Androgenetic alopecia; drug safety and therapeutic strategies.
Baconi, DL; Bălălău, C; Constantin, VD; Georgescu, SR; Motofei, IG; Păunică, I; Păunică, S; Rowland, DL; Sârbu, MI; Tampa, M, 2018
)
0.48
" Thus, finasteride preserves important physiological roles of dihydrotestosterone (unrelated to AGA) and, in addition, its adverse effects seem to be (at least in part) predictable."( Androgenetic alopecia; drug safety and therapeutic strategies.
Baconi, DL; Bălălău, C; Constantin, VD; Georgescu, SR; Motofei, IG; Păunică, I; Păunică, S; Rowland, DL; Sârbu, MI; Tampa, M, 2018
)
0.48
" However, the concern regarding adverse effects of finasteride use has been rising."( A randomized, double-blind controlled study of the efficacy and safety of topical solution of 0.25% finasteride admixed with 3% minoxidil vs. 3% minoxidil solution in the treatment of male androgenetic alopecia.
Chalermroj, N; Khunkhet, S; Srisuwanwattana, P; Suchonwanit, P, 2018
)
0.48
" Changes in plasma dihydrotestosterone levels and adverse events were recorded."( A randomized, double-blind controlled study of the efficacy and safety of topical solution of 0.25% finasteride admixed with 3% minoxidil vs. 3% minoxidil solution in the treatment of male androgenetic alopecia.
Chalermroj, N; Khunkhet, S; Srisuwanwattana, P; Suchonwanit, P, 2018
)
0.48
" There were also no systemic adverse events reported by patients in both groups."( A randomized, double-blind controlled study of the efficacy and safety of topical solution of 0.25% finasteride admixed with 3% minoxidil vs. 3% minoxidil solution in the treatment of male androgenetic alopecia.
Chalermroj, N; Khunkhet, S; Srisuwanwattana, P; Suchonwanit, P, 2018
)
0.48
" The two drugs appear to show similar rates of adverse reactions, especially in sexual dysfunction."( The efficacy and safety of dutasteride compared with finasteride in treating men with androgenetic alopecia: a systematic review and meta-analysis.
Cui, Y; Gao, Z; Ma, J; Song, S; Wu, J; Zhou, Z, 2019
)
0.51
" On the other hand, 5-ARI monotherapy and in particular Finasteride alone is currently getting focus of attention especially due to lack of systematic reviews investigating efficacy outcomes and/or adverse events associated."( Efficacy and safety of Finasteride (5 alpha-reductase inhibitor) monotherapy in patients with benign prostatic hyperplasia: A critical review of the literature.
Antonelli, A; Busetto, GM; Celia, A; Chung, BI; Cindolo, L; D'Agostino, D; De Berardinis, E; Del Giudice, F; Kim, JH; Maggi, M; Minervini, A; Porreca, A; Rocco, B; Romagnoli, D; Schiavina, R; Sciarra, A, 2020
)
0.56
"Aim of the present critical review was to analyze current knowledge of clinical efficacy and incidence of adverse events associated with 5-ARI treatment for LUTS/BPH."( Efficacy and safety of Finasteride (5 alpha-reductase inhibitor) monotherapy in patients with benign prostatic hyperplasia: A critical review of the literature.
Antonelli, A; Busetto, GM; Celia, A; Chung, BI; Cindolo, L; D'Agostino, D; De Berardinis, E; Del Giudice, F; Kim, JH; Maggi, M; Minervini, A; Porreca, A; Rocco, B; Romagnoli, D; Schiavina, R; Sciarra, A, 2020
)
0.56
" Parameters of research included prostate specific antigen (PSA), prostate volume (PV), International Prostate Symptom Score (IPPS), postvoid residual urine (PVR), voiding symptoms of IPSS (voiding IPSS), maximum urinary flow rate (Qmax), and adverse events (AEs)."( Efficacy and safety of Finasteride (5 alpha-reductase inhibitor) monotherapy in patients with benign prostatic hyperplasia: A critical review of the literature.
Antonelli, A; Busetto, GM; Celia, A; Chung, BI; Cindolo, L; D'Agostino, D; De Berardinis, E; Del Giudice, F; Kim, JH; Maggi, M; Minervini, A; Porreca, A; Rocco, B; Romagnoli, D; Schiavina, R; Sciarra, A, 2020
)
0.56
" There was no significant difference between the combined group and minoxidil- or finasteride-only groups in the number of patients with moderate and mild improvements, hair density change, or adverse events."( The Efficacy and Safety of Finasteride Combined with Topical Minoxidil for Androgenetic Alopecia: A Systematic Review and Meta-analysis.
Chen, B; Chen, L; Wang, H; Wang, L; Zhang, J, 2020
)
0.56
"To investigate the sexual, physical, and mental adverse effects associated with exposure to 5-alpha reductase inhibitors (5ARIs)."( An evaluation of the federal adverse events reporting system data on adverse effects of 5-alpha reductase inhibitors.
Chughtai, B; Harrell, MB; Ho, K; Kaplan, SA; Te, AE, 2021
)
0.62
" Reports identified one or more adverse effects, along with all concurrent medications."( An evaluation of the federal adverse events reporting system data on adverse effects of 5-alpha reductase inhibitors.
Chughtai, B; Harrell, MB; Ho, K; Kaplan, SA; Te, AE, 2021
)
0.62
"BTA is a safe and effective therapeutic strategy for the treatment of AGA without adverse effects, and BTA combined with FNS exhibited a superior therapeutic effect than BTA alone."( Effectiveness and Safety of Botulinum Toxin Type A in the Treatment of Androgenetic Alopecia.
Feng, X; Yu, S; Zhang, M; Zhao, J; Zhao, Z; Zhou, Y, 2020
)
0.56
"There is ongoing controversy about the adverse events of finasteride, a drug used in the management of alopecia and benign prostatic hyperplasia (BPH)."( Investigation of Suicidality and Psychological Adverse Events in Patients Treated With Finasteride.
Basaria, S; Bhojani, N; Cone, EB; Marchese, M; Nguyen, DD; Paciotti, M; Trinh, QD, 2021
)
0.62
"To investigate the association of suicidality (ideation, attempt, and completed suicide) and psychological adverse events (depression and anxiety) with finasteride use."( Investigation of Suicidality and Psychological Adverse Events in Patients Treated With Finasteride.
Basaria, S; Bhojani, N; Cone, EB; Marchese, M; Nguyen, DD; Paciotti, M; Trinh, QD, 2021
)
0.62
"This pharmacovigilance case-noncase study used disproportionality analysis (case-noncase design) to detect signals of adverse reaction of interest reported with finasteride in VigiBase, the World Health Organization's global database of individual case safety reports."( Investigation of Suicidality and Psychological Adverse Events in Patients Treated With Finasteride.
Basaria, S; Bhojani, N; Cone, EB; Marchese, M; Nguyen, DD; Paciotti, M; Trinh, QD, 2021
)
0.62
"Suicidality and psychological adverse events."( Investigation of Suicidality and Psychological Adverse Events in Patients Treated With Finasteride.
Basaria, S; Bhojani, N; Cone, EB; Marchese, M; Nguyen, DD; Paciotti, M; Trinh, QD, 2021
)
0.62
"VigiBase contained 356 reports of suicidality and 2926 reports of psychological adverse events (total of 3282 adverse events of interest) in finasteride users (3206 male [98."( Investigation of Suicidality and Psychological Adverse Events in Patients Treated With Finasteride.
Basaria, S; Bhojani, N; Cone, EB; Marchese, M; Nguyen, DD; Paciotti, M; Trinh, QD, 2021
)
0.62
"In this pharmacovigilance case-noncase study, significant RORs of suicidality and psychological adverse events were associated with finasteride use in patients younger than 45 years who used finasteride for alopecia."( Investigation of Suicidality and Psychological Adverse Events in Patients Treated With Finasteride.
Basaria, S; Bhojani, N; Cone, EB; Marchese, M; Nguyen, DD; Paciotti, M; Trinh, QD, 2021
)
0.62
" Incidence and type of adverse events, and cause of discontinuation, did not differ meaningfully between topical finasteride and placebo."( Efficacy and safety of topical finasteride spray solution for male androgenetic alopecia: a phase III, randomized, controlled clinical trial.
Blume-Peytavi, U; Falqués, M; Galván, J; Jansat, JM; Massana, E; Otero, R; Piraccini, BM; Scarci, F; Tamarit, ML; Tebbs, V, 2022
)
0.72
" Adverse effects of the drugs were noted."( Efficacy, tolerability, and safety of montelukast versus finasteride for the treatment of moderate acne in women: A prospective, randomized, single-blinded, active-controlled trial.
Goldust, M; Gupta, A; Mohammadnezhad, F; Rokni, GR; Saeedi, M; Sandhu, S; Shadi, S; Sharma, A, 2021
)
0.62
"To highlight treatment options for androgenetic alopecia taking into consideration the efficacy, side effect profiles, practicality of treatment (compliance), and costs to help clinicians offer ethically appropriate treatment regimens to their patients."( Treatment options for androgenetic alopecia: Efficacy, side effects, compliance, financial considerations, and ethics.
Ablon, G; Fischer, DL; Gade, A; Han, H; Nestor, MS, 2021
)
0.62
" Frailty may contribute to both symptom progression and serious adverse events (SAEs), shifting the balance of benefits and harms of drug therapy."( Assessment of Frailty and Association With Progression of Benign Prostatic Hyperplasia Symptoms and Serious Adverse Events Among Men Using Drug Therapy.
Bauer, SR; Covinsky, K; Ensrud, KE; Liu, TT; McVary, KT; Newman, JC; Ricke, WA; Suskind, AM; Walter, LC, 2021
)
0.62
" Topical finasteride, while not FDA-approved, lacks the systemic adverse effects associated with oral finasteride."( Topical finasteride for male and female pattern hair loss: Is it a safe and effective alternative?
Gupta, AK; Talukder, M, 2022
)
0.72
"To review whether topical finasteride is a safe and effective treatment for male and female pattern hair loss."( Topical finasteride for male and female pattern hair loss: Is it a safe and effective alternative?
Gupta, AK; Talukder, M, 2022
)
0.72
" The Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS) database was queried to identify the ten drugs which were associated the most with the adverse drug reactions (ADRs) recorded as "penile curvature" and/or "Peyronie's disease"."( Are finasteride-related penile curvature/Peyronie's disease Adverse Event Reports worthy of further clinical investigation? Disproportionality analysis based on both the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) pharmacovi
Alnajjar, HM; Boeri, L; Cakir, OO; Capogrosso, P; Castiglione, F; Chiappini, S; Deho', F; Fallara, G; Harvey, H; Montorsi, F; Muneer, A; Rewhorn, M; Salonia, A; Schifano, F; Schifano, N, 2023
)
0.91
" The few and widely used monotherapies approved by the US Food and Drug Administration, such as minoxidil or finasteride, are not efficacious in all people and cause adverse events that prevent patient compliance."( Real-World, Open-Label Study of the Efficacy and Safety of a Novel Serum in Androgenetic Alopecia.
Abidi, Z; Arruda, S; Rapaport, J; Sadgrove, NJ; Sadick, N; Swearingen, A, 2023
)
0.91
" esculenta tuber extracts provide potentially safe nutraceutical if applied in the management of benign prostate hyperplasia based on a rat model."( Safety profile of colocasia esculenta tuber extracts in benign prostate hyperplasia.
Agu, PC; Aja, PM; Ajayi, CO; Ifie, JE; Munezero, J; Namale, N; Okoboi, J; Ssedyabane, F; Tusubira, D, 2023
)
0.91

Pharmacokinetics

The herbal treatment significantly reduced the peak plasma concentration (C(max), the area under the plasma concentration-time curve (AUC(0-24h) and the elimination half-life (t(1/2) The method was successfully applied to a pharmacokinetic study of finasteride in healthy volunteers following oral administration.

ExcerptReferenceRelevance
" The mean values of the area under the curve (AUC0-24) and Cmax increased linearly in a dose-dependent manner."( Pharmacokinetics and biochemical efficacy after single and multiple oral administration of N-(2-methyl-2-propyl)-3-oxo-4-aza-5 alpha-androst-1-ene-17 beta-carboxamide, a new type of specific competitive inhibitor of testosterone 5 alpha-reductase, in volu
Morikawa, H; Ohtawa, M; Shimazaki, J,
)
0.13
" Multiple-dose coadministration of terazosin and finasteride did not alter the central values of steady-state pharmacokinetic parameters of either drug in a statistically significant manner."( Assessment of the pharmacokinetic-pharmacodynamic interaction between terazosin and finasteride.
Cavanaugh, J; Eason, C; Granneman, GR; Hosmane, B; Locke, C; Samara, EE, 1996
)
0.29
" The aim of this study was to assess the potential pharmacokinetic interaction of doxazosin or terazosin when coadministered with finasteride."( Pharmacokinetic interaction between finasteride and terazosin, but not finasteride and doxazosin.
Chung, M; Hilbert, J; Lawrence, V; Phillips, K; Vashi, V, 1998
)
0.3
" Simulations closely predicted the outcome of the repeat dose study, estimated parameters of the pharmacodynamic modelling were generally close to within 88 to 116% of those from the original model and the individual predictions did not indicate any bias."( Validation of a population pharmacokinetic/pharmacodynamic model for 5 alpha-reductase inhibitors.
Hammarlund-Udenaes, M; Hermann, D; Karlsson, MO; Olsson Gisleskog, P, 1999
)
0.3
" Therefore, we hypothesize that because of its pharmacokinetic parameters and increased potency against r5AR1, GI198745 is more effective than finasteride in preventing the growth of the rat prostate."( 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.
Batchelor, KW; Bramson, HN; Hoffman, CR; Kadwell, SH; Kost, TA; Lee, FW; Overton, LK; Simpson Noel, D; Stuart, JD; Tippin, TK; Yeager, RL, 2001
)
0.31
" Pharmacokinetic studies of VN/85-1 were conducted in male SCID mice."( Potent CYP17 inhibitors: improved syntheses, pharmacokinetics and anti-tumor activity in the LNCaP human prostate cancer model.
Brodie, AM; Handratta, VD; Jelovac, D; Kataria, R; Long, BJ; Njar, VC; Nnane, IP, 2004
)
0.32
" Therefore, we conducted a pharmacokinetic study of oral T in oil, alone or with D or F, in the fasting and fed states in normal men whose endogenous T production was suppressed by the GnRH antagonist acyline."( Oral testosterone in oil: pharmacokinetic effects of 5alpha reduction by finasteride or dutasteride and food intake in men.
Amory, JK; Bremner, WJ; Page, ST,
)
0.13
"We sought to assess the possibility of using pharmacokinetic parameters as a predictor of response to benign prostatic hyperplasia (BPH) pharmacotherapy via a randomized, placebo-controlled, animal preclinical trial using dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI)."( Pharmacokinetic parameters as a potential predictor of response to pharmacotherapy in benign prostatic hyperplasia: a preclinical trial using dynamic contrast-enhanced MRI.
Baudendistel, KT; Henry, H; Heverhagen, JT; Jia, G; Knopp, MV; Levine, AL; Polzer, H; Rosol, TJ; von Tengg-Kobligk, H, 2006
)
0.33
" 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
" The herbal treatment significantly reduced the peak plasma concentration (C(max)), the area under the plasma concentration-time curve (AUC(0-24h)) and the elimination half-life (t(1/2)) of finasteride."( The effect of St. John's wort on the pharmacokinetics, metabolism and biliary excretion of finasteride and its metabolites in healthy men.
Bondesson, U; Hedeland, M; Knutson, L; Lennernäs, H; Lundahl, A, 2009
)
0.35
" The method was successfully applied to a pharmacokinetic study of finasteride in healthy volunteers following oral administration."( Rapid determination of finasteride in human plasma by UPLC-MS/MS and its application to clinical pharmacokinetic study.
Hwang, SK; Kim, EH; Kim, SD; Lee, HW; Lee, M; Lim, MS; Park, J; Phapale, PB; Yoon, YR, 2010
)
0.36
" We developed a pharmacokinetic model incorporating a compartment that represents the binding of finasteride to 5alphaR."( Saturable binding of finasteride to steroid 5alpha-reductase as determinant of nonlinear pharmacokinetics.
Hori, S; Ohtani, H; Satoh, H; Sawada, Y; Suzuki, R, 2010
)
0.36
"Benign prostatic hyperplasia and prostate cancer can be treated with the 5α-reductase inhibitors, finasteride and dutasteride, when pharmacodynamic biomarkers are useful in assessing response."( Simultaneous pharmacokinetic and pharmacodynamic analysis of 5α-reductase inhibitors and androgens by liquid chromatography tandem mass spectrometry.
Andrew, R; Faqehi, AM; Homer, NZ; Hughes, KA; Naredo, G; Stewart, LH; Upreti, R; Walker, BR, 2015
)
0.42
"The primary aim of this study was to evaluate whether there was clinically significant pharmacokinetic (PK) interaction between finasteride and tamsulosin in healthy Chinese male subjects."( Pharmacokinetic interaction of finasteride with tamsulosin hydrochloride: an open-label, randomized, 3-period crossover study in healthy Chinese male volunteers.
Chen, W; Chu, N; Li, X; Wang, G; Wang, J; Xu, H; Yang, M; Yuan, F, 2015
)
0.42
" Pharmacokinetic parameters were estimated via noncompartmental methods."( Pharmacokinetic interaction of finasteride with tamsulosin hydrochloride: an open-label, randomized, 3-period crossover study in healthy Chinese male volunteers.
Chen, W; Chu, N; Li, X; Wang, G; Wang, J; Xu, H; Yang, M; Yuan, F, 2015
)
0.42
" Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior."( Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation.
Ahmed, TA, 2016
)
0.43
" Finally, FSD clinical pharmacokinetic has been investigated on human volunteers."( Development of optimized self-nanoemulsifying lyophilized tablets (SNELTs) to improve finasteride clinical pharmacokinetic behavior.
Ahmed, TA; Aljaeid, BM; El-Say, KM; Hosny, KM, 2018
)
0.48
" An optimized drug micro- and nano-particles were developed, characterized, administered to group of rats, and systemic pharmacokinetic and tissue distribution within target and not-target organs were determined using near-infrared (NIR) spectroscopy technique."( Effect of finasteride particle size reduction on its pharmacokinetic, tissue distribution and cellular permeation.
Ahmed, TA; Al-Abd, AM, 2018
)
0.48

Compound-Compound Interactions

Small increases in serum T were observed with finasteride alone and in combination with MK-386 (approximately 10% and 19% respectively). The bioabsorbable SR-PLLA stent combined withfinasteride therapy provides a promising new alternative in the treatment of acute urinary retention, especially in patien.

ExcerptReferenceRelevance
"5 mg/day, alone or in combination with topical 2% minoxidil, for 20 weeks to determine the effects on scalp hair growth in balding adult male stumptail macaque monkeys."( Hair growth effects of oral administration of finasteride, a steroid 5 alpha-reductase inhibitor, alone and in combination with topical minoxidil in the balding stumptail macaque.
Brunden, MN; Buhl, AE; Diani, AR; Johnson, GA; Kubicek, MF; Mulholland, MJ; Schostarez, HJ; Shull, KL, 1992
)
0.28
" Small increases in serum T were observed with finasteride alone and in combination with MK-386 (approximately 10% and 19%, respectively)."( Effect of MK-386, a novel inhibitor of type 1 5 alpha-reductase, alone and in combination with finasteride, on serum dihydrotestosterone concentrations in men.
Chavez, CM; Constanzer, ML; De Lepeleire, I; De Schepper, PJ; Ebel, DL; Gertz, BJ; Justice, SJ; Lasseter, KC; Schwartz, JI; Shamblen, EC; Van Hecken, A; Wang, DZ; Winchell, GA, 1996
)
0.29
"The bioabsorbable SR-PLLA stent combined with finasteride therapy provides a promising new alternative in the treatment of acute urinary retention, especially in patients unfit for surgical therapy."( A pilot study of a bioabsorbable self-reinforced poly L-lactic acid urethral stent combined with finasteride in the treatment of acute urinary retention from benign prostatic enlargement.
Isotalo, T; Talja, M; Tammela, TL; Törmälä, P; Välimaa, T, 2000
)
0.31
"To evaluate the likelihood of alpha-adrenergic antagonist (alpha-blocker) discontinuation in combination with dutasteride or finasteride among patients aged > or =65 years with enlarged prostate."( Comparative analysis of alpha-blocker utilization in combination with 5-alpha reductase inhibitors for enlarged prostate in a managed care setting among Medicare-aged men.
Davis, EA; Eaddy, MT; Issa, MM; Lin, PJ; Shah, MB, 2008
)
0.35
"To evaluate the clinical effectiveness of transurethral seminal vesiculoscopy (TUSV) combined with finasteride in the treatment of recurrent hemospermia."( [Transurethral seminal vesiculoscopy combined with finasteride for recurrent hematospermia].
Cui, ZQ; Du, J; Gao, EJ; Lu, HK; Wang, YC; Yu, ZY; Zhou, HJ, 2014
)
0.4
"Transurethral seminal vesiculoscopy combined with finasteride is safe and effective for the treatment of recurrent hemospermia."( [Transurethral seminal vesiculoscopy combined with finasteride for recurrent hematospermia].
Cui, ZQ; Du, J; Gao, EJ; Lu, HK; Wang, YC; Yu, ZY; Zhou, HJ, 2014
)
0.4
" However, on the basis of an in vitro-in vivo extrapolation, our data strongly suggested that finasteride is unlikely to cause clinically significant drug-drug interactions mediated via inhibition of the hepatic UGT enzymes involved in drug metabolism in vivo."( In vitro selective inhibition of human UDP-glucuronosyltransferase (UGT) 1A4 by finasteride, and prediction of in vivo drug-drug interactions.
Bae, SH; Bae, SK; Chin, YW; Kim, D; Lee, SJ; Oh, E; Park, JB, 2015
)
0.42
"The on-line preconcentration technique of field-enhanced sample stacking and sweeping (FESS-sweeping) are combined with dispersive liquid-liquid microextraction (DLLME) to monitor the concentrations of finasteride, which is used in the treatment of androgenetic alopecia, and its metabolite, finasteride carboxylic acid (M3), in urine samples."( Determination of finasteride and its metabolite in urine by dispersive liquid-liquid microextraction combined with field-enhanced sample stacking and sweeping.
Chao, YY; Chen, CH; Chen, YL; Lin, YH, 2018
)
0.48
"The goal was to explore the efficacy and side effects of basic fibroblast growth factor (bFGF) combined with minoxidil in the treatment of male patients with early stage of androgenetic alopecia (AGA)."( Clinical observation of basic fibroblast growth factor (bFGF) combined with minoxidil in the treatment of male androgenetic alopecia.
Liu, C; Wu, W; Zhang, Y; Zhao, H, 2022
)
0.72

Bioavailability

Finasteride is well absorbed after oral administration; peak plasma concentration is reached in as little as one hour. Ketoconazole increased the bioavailability of finasteride from 0 to 5 mg.

ExcerptReferenceRelevance
" Finasteride is well absorbed after oral administration; peak plasma concentration is reached in as little as one hour."( Finasteride: a 5 alpha-reductase inhibitor.
Steiner, JF, 1993
)
0.29
" It is well absorbed after oral administration, with absolute bioavailability in humans of 63% (range 34-108%)."( Finasteride: the first 5 alpha-reductase inhibitor.
Koronkowski, MJ; Sudduth, SL,
)
0.13
" Finasteride is well absorbed after oral administration and, while the rate of absorption may be slowed postprandially, the presence of food has no effect on the total bioavailability."( Clinical pharmacokinetics and pharmacodynamics of finasteride.
Steiner, JF, 1996
)
0.29
" Dogs showed rapid absorption after oral administration of the low dose, with Cmax reached in the 1-2 hr, bioavailability was estimated to be > 90%."( Disposition and metabolism of finasteride in dogs.
Arison, BH; Carlin, JR; Chiu, SH; Christofalo, P; Ellsworth, RE; Miller, RR; Rosegay, A; VandenHeuvel, WJ, 1997
)
0.3
" Neurosteroid replacement is a potential approach to therapy, but natural neurosteroids have poor bioavailability and may be converted to metabolites with undesired progestational activity."( Enhanced anticonvulsant activity of ganaxolone after neurosteroid withdrawal in a rat model of catamenial epilepsy.
Reddy, DS; Rogawski, MA, 2000
)
0.31
"Two different finasteride (CAS 98319-26-7) tablet formulations were evaluated for their relative bioavailability (Flaxin tablets 5 mg, as the test formulation vs reference formulation, tablets 5 mg) in 23 healthy male volunteers who received a single 5 mg oral dose of each preparation."( Bioequivalence study of finasteride. Determination in human plasma by high-pressure liquid chromatography coupled to tandem mass spectrometry.
de Menezes, FG; de Moraes, ME; de Moraes, MO; De Nucci, G; Ifa, DR; Ribeiro, W, 2001
)
0.31
"As local steroid metabolism controls the bioavailability of active steroidal hormones in the prostate, the aim of this study, was to investigate the effects of absence of 5-alpha reductase (5alpha-r) and aromatase (Aro) enzymes on prostatic cellular and extracellular components after long-term inhibition."( Long-term inhibition of 5-alpha reductase and aromatase changes the cellular and extracellular compartments in gerbil ventral prostate at different postnatal ages.
Campos, SG; Corradi, LS; Góes, RM; Santos, FC; Taboga, SR; Vilamaior, PS, 2009
)
0.35
"The aims of this study were to compare the bioavailability of finasteride ODTs and standard tablets in healthy adult male Han Chinese volunteers and to determine whether any observed differences exceeded Chinese regulatory guidelines for bioequivalence."( Bioequivalence of a single 10-mg dose of finasteride 5-mg oral disintegrating tablets and standard tablets in healthy adult male Han Chinese volunteers: a randomized sequence, open-label, two-way crossover study.
Chen, L; Hu, L; Huang, L; Jiang, X; Lan, K; Li, X; Ren, J; Wang, H; Zou, Q, 2009
)
0.35
"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
" Flavonoids such as silibinin, green tea polyphenols, genistein, curcumin have shown great promise, but avenues to improve their bioavailability are requisite."( Advances in prostate cancer chemoprevention: a translational perspective.
Nambiar, D; Singh, RP, 2013
)
0.39
"35% relative bioavailability compared with a commercial tablet."( Self-microemulsifying systems of Finasteride with enhanced oral bioavailability: multivariate statistical evaluation, characterization, spray-drying and in vivo studies in human volunteers.
ElShafeey, AH; Fagir, W; Hathout, RM; Sammour, OA, 2015
)
0.42
" Pharmacokinetic parameters displayed a higher absorption rate and higher area under the curve of the FIN/DM-β-CyD inclusion complex when compared with the drug alone, which indicates an improvement in the absorption and bioavailability of FIN in the DM-β-CyD inclusion system."( Experimental, molecular docking investigations and bioavailability study on the inclusion complexes of finasteride and cyclodextrins.
Farghaly Aly, U; Mady, FM, 2017
)
0.46
"Enhance FSD bioavailability in male pattern baldness and benign prostatic hyperplasia."( Development of optimized self-nanoemulsifying lyophilized tablets (SNELTs) to improve finasteride clinical pharmacokinetic behavior.
Ahmed, TA; Aljaeid, BM; El-Say, KM; Hosny, KM, 2018
)
0.48
"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

The pharmacology and pharmacokinetics of finasteride are reviewed. Finasteride's clinical efficacy, adverse effects, and dosage in patients with benign prostatic hyperplasia (BPH) are described.

ExcerptRelevanceReference
" Dose-response studies were performed on male rats treated in utero during the period of sexual differentiation with either the potent 5 alpha-reductase inhibitor finasteride or the antiandrogen flutamide."( Comparison of the effects of the 5 alpha-reductase inhibitor finasteride and the antiandrogen flutamide on prostate and genital differentiation: dose-response studies.
Imperato-McGinley, J; Sanchez, RS; Spencer, JR; Vaughan, ED; Yee, B, 1992
)
0.28
"The pharmacology and pharmacokinetics of finasteride are reviewed, and finasteride's clinical efficacy, adverse effects, and dosage in patients with benign prostatic hyperplasia (BPH) are described."( Finasteride: a 5 alpha-reductase inhibitor.
Steiner, JF, 1993
)
0.29
"5-100 mg/day regress prostate enlargement; the recommended dosage is 5 mg once/day."( Finasteride: the first 5 alpha-reductase inhibitor.
Koronkowski, MJ; Sudduth, SL,
)
0.13
" First, while administration of testosterone to eggs incubating at all male-producing and male-biased intermediate temperatures produced females in a dose- and temperature-dependent manner, significant numbers of intersex individuals resulted from high dosage testosterone treatment to eggs incubating at a female-biased intermediate temperature."( Role of reductase and aromatase in sex determination in the red-eared slider (Trachemys scripta), a turtle with temperature-dependent sex determination.
Bergeron, JM; Crews, D, 1994
)
0.29
" Values of t1/2z are higher in elderly men, but no dosage adjustments are necessary."( Clinical pharmacokinetics and pharmacodynamics of finasteride.
Steiner, JF, 1996
)
0.29
" After either dosing route, 45% of the plasma radioactivity (as represented by AUC) was parent drug, 43% was metabolite I, and 1% was metabolite IV."( Disposition and metabolism of finasteride in dogs.
Arison, BH; Carlin, JR; Chiu, SH; Christofalo, P; Ellsworth, RE; Miller, RR; Rosegay, A; VandenHeuvel, WJ, 1997
)
0.3
" Concentrations of DHT and T before and 7 days after treatment did not differ by dosage of finasteride administered."( Effect of finasteride on serum concentrations of dihydrotestosterone and testosterone in three clinically normal sexually intact adult male dogs.
Castner, S; Hardy, SK; Johnston, SD; Kamolpatana, K, 1998
)
0.3
" Thus the model derived from single dose data from healthy volunteers was considered to be valid for the prediction of DHT levels in the patient population after repeated dosing of dutasteride and finasteride."( Validation of a population pharmacokinetic/pharmacodynamic model for 5 alpha-reductase inhibitors.
Hammarlund-Udenaes, M; Hermann, D; Karlsson, MO; Olsson Gisleskog, P, 1999
)
0.3
" In two similar experiments, weanling female rats were dosed for 20 days by gavage with vehicle (0."( Evaluation of the EDSTAC female pubertal assay in CD rats using 17beta-estradiol, steroid biosynthesis inhibitors, and a thyroid inhibitor.
Carney, EW; Crissman, JW; Marty, MS, 1999
)
0.3
" Dosing extended over postnatal days (pnd) 22-35, 36-50, 36-55 and 22-35, with recovery to pnd 55 or 22-55."( The peripubertal male rat assay as an alternative to the Hershberger castrated male rat assay for the detection of anti-androgens, oestrogens and metabolic modulators.
Ashby, J; Lefevre, PA,
)
0.13
" Recently, this assay was evaluated by several laboratories using a variety of dosing schemes."( Evaluation of the male pubertal onset assay to detect testosterone and steroid biosynthesis inhibitors in CD rats.
Carney, EW; Crissman, JW; Marty, MS, 2001
)
0.31
" The recommended dosage is 5 mg a day, however case reports have show effectiveness with lower doses."( The effectiveness of reducing the daily dose of finasteride in men with benign prostatic hyperplasia.
Geller, J; Sullivan, MJ, 2002
)
0.31
" No dosage titration is needed for ER alfuzosin, and its onset of peak action is within days of the start of treatment."( Alfuzosin hydrochloride for the treatment of benign prostatic hyperplasia.
Lee, M, 2003
)
0.32
" Castration of sexually immature Sprague-Dawley rats was performed between post-natal days 42 and 46 whilst dosing of the chemical over 10 days was performed between post-natal days 53 and 67."( Evaluation of the rodent Hershberger assay using three reference endocrine disrupters (androgen and antiandrogens).
Bars, RG; Kennel, PF; Pallen, CT,
)
0.13
" The objective of this study was to identify the optimal dosage of finasteride and to evaluate its efficacy and safety in the treatment of Japanese men with male pattern hair loss."( Finasteride in the treatment of Japanese men with male pattern hair loss.
Harada, S; Hayashi, N; Igarashi, A; Kawashima, M; Kitahara, H; Maeguchi, M; Matsuda, T; Mizuno, A; Murata, Y; Natsumeda, Y; Nogita, T; Takahashi, K; Toda, K; Tsuboi, R; Ueki, R; Yamada, M; Yamazaki, M,
)
0.13
" Although the standard preparation is suitable for once-daily dosing in BPH, it has to be titrated through three steps to its final dose."( After ALLHAT: doxazosin for the treatment of benign prostatic hyperplasia.
Doggrell, SA, 2004
)
0.32
" Higher rates of twice-daily (or 2 units per day) dosing are associated with higher incremental cost-effectiveness ratios."( Cost-effectiveness of tamsulosin, doxazosin, and terazosin in the treatment of benign prostatic hyperplasia.
Chrischilles, EA; Klein, RW; Kreder, KJ; Ohsfeldt, RL,
)
0.13
" However, at their effective dosage regimes, VN/85-1 and VN/87-1 were each as effective as castration and more effective than finasteride or casodex, an anti-androgen used for prostate cancer (PC) therapy."( Potent CYP17 inhibitors: improved syntheses, pharmacokinetics and anti-tumor activity in the LNCaP human prostate cancer model.
Brodie, AM; Handratta, VD; Jelovac, D; Kataria, R; Long, BJ; Njar, VC; Nnane, IP, 2004
)
0.32
" The main reasons of a poor internal validity in 3 studies were the short follow-up, the missing percentage, the absence of a placebo group and a dosage bias."( [Analysis of the scientific evidence of the combination therapy in benign prostatic hyperplasia].
Millán Rodríguez, F, 2005
)
0.33
" It is unclear whether the success was due to a higher dosage of finasteride (2."( Finasteride treatment of female pattern hair loss.
Iorizzo, M; Piraccini, BM; Tosti, A; Vincenzi, C; Voudouris, S, 2006
)
0.33
"05) inhibits growth of LNCaP human prostate cancer xenografts in intact male nude mice, but this inhibition is not as great as that by equimolar oral dosing with dutasteride."( Pharmacologic basis for the enhanced efficacy of dutasteride against prostatic cancers.
Becker, RE; Dalrymple, SL; Denmeade, SR; Isaacs, JT; Xu, Y, 2006
)
0.33
" Thereafter, a dose-response effect of different doses of benzylglucosinolates (0."( Effect of two different extracts of red maca in male rats with testosterone-induced prostatic hyperplasia.
Gasco, M; Gonzales, GF; Maldonado, C; Mormontoy, J; Pajuelo, M; Portella, J; Rodriguez, D; Vasquez, V; Villegas, L, 2007
)
0.34
" There was no suggestion of a dose-response relationship between exposure to 5-alpha reductase inhibitors when the exposure was stratified into tertiles of total exposure (P = ."( Association between 5-alpha reductase inhibition and risk of hip fracture.
Cheetham, TC; Haque, R; Jacobsen, SJ; Loo, RK; Shi, JM, 2008
)
0.35
"Especially in obese men and in those > 70 years old, SHBG dosage is important to calculate FT levels and diagnose hypogonadism."( Laboratory diagnosis of late-onset male hypogonadism andropause.
Buksman, S; Carmo, AM; Clapauch, R; Marinheiro, L; Pessoa, I, 2008
)
0.35
" On the seventh day of each dosing period, serum testosterone, DHT and oestradiol were measured at baseline and 1, 2, 4, 8, 12, 13, 14, 16, 20 and 24 h after the morning dose."( Steady-state pharmacokinetics of oral testosterone undecanoate with concomitant inhibition of 5α-reductase by finasteride.
Amory, JK; Christenson, P; Dudley, RE; Hull, L; Leung, A; Roth, MY; Swerdloff, R; Wang, C, 2011
)
0.37
"Reversed-phase high-performance liquid chromatography (RP-HPLC) and thin-layer chromatography (TLC) methods have been developed and validated for simultaneous estimation of tamsulosin hydrochloride and finasteride in bulk drug and in combined dosage forms."( Validated RP-HPLC and TLC methods for simultaneous estimation of tamsulosin hydrochloride and finasteride in combined dosage forms.
Patel, DB; Patel, NJ, 2010
)
0.36
" In this study, we investigated a dosing time-dependent effect and safety of FIN in rats."( Influence of dosing time on the efficacy and safety of finasteride in rats.
Ando, H; Fujimura, A; Kumazaki, M; Maekawa, T; Motosugi, Y; Takada, M; Tateishi, M; Ushijima, K, 2011
)
0.37
" Dosage analysis showed that lower doses of finasteride were associated with higher overall and prostate cancer risks."( A population-based nested case-control study in taiwan: use of 5α-reductase inhibitors did not decrease prostate cancer risk in patients with benign prostate hyperplasia.
Chang, SN; Kao, CH; Liang, JA; Lin, MC; Muo, CH; Sun, LM; Sung, FC, 2012
)
0.38
" experimental T and DHT levels and prostate size are depicted, demonstrating the model accurately described an approximate 77% decrease in prostate size and nearly complete depletion of prostatic DHT following 21 days of daily finasteride dosing in rats."( A multiscale, mechanism-driven, dynamic model for the effects of 5α-reductase inhibition on prostate maintenance.
Barton, HA; Zager, MG, 2012
)
0.38
" The specified limits for the USP uniformity of dosage units assay (98."( Development and validation of an UPLC method for determination of content uniformity in low-dose solid drugs products using the design space approach.
Fariña, JB; Llabrés, M; Oliva, A, 2013
)
0.39
" For Gleason 2-6 cancers, results were inconsistent across treatment arms with a suggestion of increased risk in the placebo arm only; however, there was no dose-response relationship."( Serum 25-hydroxyvitamin D concentrations and risk of prostate cancer: results from the Prostate Cancer Prevention Trial.
Goodman, PJ; Kristal, AR; Neuhouser, ML; Peters, U; Schenk, JM; Song, X; Tangen, CM; Till, CA; Torkko, KC, 2014
)
0.4
" Furthermore, a dosage analysis showed that higher doses of finasteride were associated with higher osteoporosis diagnosis risk (OR = 1·68; 95% CI, 1·01-2·81), relative to the patients not using 5ARIs."( A population-based nested case-control study: the use of 5-alpha-reductase inhibitors and the increased risk of osteoporosis diagnosis in patients with benign prostate hyperplasia.
Hsieh, YW; Kao, CH; Lin, CL; Lin, WL; Sung, FC; Wu, CH, 2015
)
0.42
" Blood samples were collected up to 48 hours after dosing on study day 1 and up to 24 hours after dosing on study day 9 for determination of plasma concentrations with a validated LC-MS/MS method."( Pharmacokinetic interaction of finasteride with tamsulosin hydrochloride: an open-label, randomized, 3-period crossover study in healthy Chinese male volunteers.
Chen, W; Chu, N; Li, X; Wang, G; Wang, J; Xu, H; Yang, M; Yuan, F, 2015
)
0.42
" Furthermore, the dosage analysis showed that there were no significant associations between ACS risk and uses of a single drug medication regardless the dosages."( 5α-Reductase inhibitors increase acute coronary syndrome risk in patients with benign prostate hyperplasia.
Chou, CH; Kao, CH; Lin, CL; Lin, MC; Sung, FC, 2015
)
0.42
"025); scores were not significantly different between treatments for satisfaction with dosing or side-effects (both P ≥ 0."( Treatment satisfaction and clinically meaningful symptom improvement in men with lower urinary tract symptoms and prostatic enlargement secondary to benign prostatic hyperplasia: Secondary results from a 6-month, randomized, double-blind study comparing f
Casabé, A; Glina, S; Henneges, C; Roehrborn, CG; Sorsaburu, S; Viktrup, L, 2015
)
0.42
"The goal was to develop an optimized transdermal finasteride (FNS) film loaded with drug microplates (MIC), utilizing two-step optimization, to decrease the dosing schedule and inconsistency in gastrointestinal absorption."( Transdermal film-loaded finasteride microplates to enhance drug skin permeation: Two-step optimization study.
Ahmed, TA; El-Say, KM, 2016
)
0.43
"Lyophilized tablets could be considered as a good alternative for conventional solid dosage forms especially when loaded with drug nanosystems."( Development of optimized self-nanoemulsifying lyophilized tablets (SNELTs) to improve finasteride clinical pharmacokinetic behavior.
Ahmed, TA; Aljaeid, BM; El-Say, KM; Hosny, KM, 2018
)
0.48
"FAERS data suggests that finasteride exposure is reported with a diverse collection of symptoms, particularly in younger men on 1 mg dosage compared to older men on 5 mg."( A Review of the FAERS Data on 5-Alpha Reductase Inhibitors: Implications for Postfinasteride Syndrome.
Althof, S; Baas, WR; Butcher, MJ; Clemons, J; Delfino, K; Herberts, M; Holland, B; Kohler, TS; Lwin, A; McVary, KT, 2018
)
0.48
" Murine animal models were divided into 8 groups, Sham rats, BPH rats, BPH rats administered with finasteride (1 mg/kg), BPH rats administered with Pule'an (460 mg/kg), BPH rats administered with low, high dosage of QCJ (860 mg/kg, 2580 mg/kg respectively), BPH rats administered with low, high dosage of Fr."( Chemical profiles of the active fraction from Prinsepia utilis Royle leaves and its anti-benign prostatic hyperplasia evaluation in animal models.
Li, X; Peng, C; Peng, Y; Sun, C; Wu, Y, 2021
)
0.62
"In our previous study, a long-acting injectable (LAI) formulation of finasteride was prepared as a new dosage form of PROPECIA®, and in vivo pharmacokinetics (PKs)-pharmacodynamics (PDs) was evaluated in beagle dogs."( Approaches for estimating the clinical starting dose of new dosage forms: An example of a long-acting injectable formulation of finasteride.
Cho, HY; Hee Kim, J; Wook Kang, D, 2023
)
0.91
" That approach was utilized to estimation of the cited drugs in dosage forms, simultaneously with %recoveries for tadalafil and finasteride of 99."( Synchronous fluorescence as a green and selective method for the simultaneous determination of finasteride and tadalafil in dosage form and spiked human plasma.
Abdelaziz, A; Batekh, AE; Emad, N; Galal, M; Hussien, M; Karem, M; Moukhtar, DA; Salem, H, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
androgen antagonistA compound which inhibits or antagonises the biosynthesis or actions of androgens.
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitorAn EC 1.3.1.* (oxidoreductase acting on CH-CH group of donor, NAD(+) or NADP(+) as acceptor) inhibitor that interferes with the action of of 3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+)), EC 1.3.1.22, the enzyme which converts testosterone (CHEBI:17347) into the more potent androgen 5alpha-dihydrotestosterone.
antihyperplasia drugA drug used for the treatment of hyperplasia (increaced cell production within an organ or tissue).
[role 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]

Drug Classes (3)

ClassDescription
aza-steroidAn aza-steroid is a steroid where in the carbon skeleton a carbon atom is replaced by nitrogen.
3-oxo steroidAny oxo steroid where an oxo substituent is located at position 3.
delta-lactamA lactam in which the amide bond is contained within a six-membered ring, which includes the amide nitrogen and the carbonyl carbon.
[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 (41)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency51.42960.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency45.27160.173734.304761.8120AID1346859; AID1346924
SMAD family member 3Homo sapiens (human)Potency45.27160.173734.304761.8120AID1346859; AID1346924
TDP1 proteinHomo sapiens (human)Potency8.92150.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency4.50030.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency24.11330.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743063
progesterone receptorHomo sapiens (human)Potency51.96200.000417.946075.1148AID1346795
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency44.43110.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency21.72840.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency42.24160.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency30.33960.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency58.19040.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency48.19480.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743075; AID743078; AID743079; AID743080
GVesicular stomatitis virusPotency0.87090.01238.964839.8107AID1645842
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency8.61710.001024.504861.6448AID743212
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency6.84480.023723.228263.5986AID743222
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency51.702619.739145.978464.9432AID1159509
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency45.55910.000323.4451159.6830AID743065; AID743066; AID743067
mitogen-activated protein kinase 1Homo sapiens (human)Potency6.30960.039816.784239.8107AID1454
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency48.01930.000627.21521,122.0200AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency3.98110.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency14.18370.004611.374133.4983AID624296; AID624297
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency60.44740.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency0.87090.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency0.87090.01238.964839.8107AID1645842
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency60.44740.001551.739315,848.9004AID1259244
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency0.87090.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency0.87090.01238.964839.8107AID1645842
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)51.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)28.20000.11007.190310.0000AID1443980; AID1443989; AID1473738
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)2.00000.00002.800510.0000AID625248
Androgen receptorRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00101.979414.1600AID39178
3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)IC50 (µMol)2.49100.00170.48807.5000AID1272918; AID1573001; AID1573006; AID1573008; AID1803328; AID207453; AID207454; AID207456; AID207459; AID207596; AID207758; AID207759; AID207760; AID207765; AID207913; AID207914; AID207916; AID215796; AID242533; AID299269; AID703695; AID91250
3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)Ki0.25800.00500.53031.6000AID207887; AID207919
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Rattus norvegicus (Norway rat)IC50 (µMol)180.00780.00427.468021.1000AID1166503; AID1263196; AID1573010; AID207301; AID207604
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Rattus norvegicus (Norway rat)Ki0.05950.00500.04010.0882AID207426; AID207427; AID207595
3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)IC50 (µMol)24.24340.00010.526710.0000AID1166503; AID1272903; AID1573000; AID1573007; AID1573009; AID1803329; AID205601; AID205602; AID205603; AID207440; AID207441; AID207443; AID207446; AID207613; AID207734; AID207735; AID207924; AID215799; AID227856; AID242430; AID299270; AID703552; AID91252
3-oxo-5-alpha-steroid 4-dehydrogenase 2Rattus norvegicus (Norway rat)IC50 (µMol)0.32860.00037.329421.1000AID1573011; AID207301; AID207451; AID207902; AID597647
3-oxo-5-alpha-steroid 4-dehydrogenase 2Rattus norvegicus (Norway rat)Ki0.07700.00501.711010.0000AID207426; AID207427
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)1.00000.00002.398310.0000AID625247
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (147)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
steroid biosynthetic process3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
androgen biosynthetic process3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
estrogen biosynthetic process3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
hippocampus development3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
C21-steroid hormone metabolic process3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
response to corticosterone3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
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)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (68)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
3-keto sterol reductase activity3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
3-beta-hydroxy-delta5-steroid dehydrogenase activity3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
steroid delta-isomerase activity3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
protein binding3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
5alpha-androstane-3beta,17beta-diol dehydrogenase activity3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
oxidoreductase activity, acting on the CH-OH group of donors, NAD or NADP as acceptor3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
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)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (41)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
nucleolus3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
mitochondrial inner membrane3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
mitochondrial intermembrane space3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
endoplasmic reticulum3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
endoplasmic reticulum membrane3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
smooth endoplasmic reticulum membrane3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
intercellular bridge3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
intracellular membrane-bounded organelle3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
cytoplasm3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 1Homo sapiens (human)
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)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
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)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (424)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID550804Inhibition of human prostate 5alpha-reductase type 2 assessed as formation dihydrotestosterone from [4-14C] testosterone2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Discovery of a novel hybrid from finasteride and epristeride as 5α-reductase inhibitor.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID774937Inhibition of testosterone propionate-induced prostate hyperplasia in Wistar rat assessed as ratio of prostate weight to body weight at 5 mg/kg, ip co-administered with testosterone propionate for 14 days (Rvb = 3.1634 +/- 0.1264 no unit)2013European journal of medicinal chemistry, Nov, Volume: 69Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID703549Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of body weight gain at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1217653Renal clearance in castrated pig at 0.8 mg/kg, administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
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.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID207916Inhibitory activity against 5-alpha-reductase type 1 in cell culture system using LNCaP cells (androgen-sensitive human prostatic cancer cell line)2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
A novel class of inhibitors for steroid 5alpha-reductase: synthesis and evaluation of umbelliferone derivatives.
AID207887Inhibitory activity against recombinant Steroid 5-alpha-reductase type I expressed in CHO cells2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID20789Bioavailability in dog (male Beagle) i.v. administration1994Journal 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.
AID486431Antiproliferative activity against human DU145 cells assessed as growth inhibition at 2 ug/mL after 48 hrs by MTT assay relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID174355Percent conversion of testosterone to dihydrotestosterone in prostate of rats at 10 mg/kg of compound given perorally1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
AID1573010Inhibition of type 1 5alpha reductase in rat prostate2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1272914Decrease in ventral prostate organ weight in male wistar rat at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1225523Reduction in proliferating cell nuclear antigen expression in prostate tissue in BPH-induced Sprague-Dawley rat model at 5 mg/kg, po daily for 4 weeks by Western blot analysis2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Effects of resveratrol on benign prostatic hyperplasia by the regulation of inflammatory and apoptotic proteins.
AID242448Displacement of [3H]R-1881 from Androgen receptor of PC3-AR cells; - = not determined2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
AID1263206Increase of diameter of pigmented spot of flank organs in gonadectomized golden hamster at 1 mg/kg, sc qd for 6 days co-administered with 1 mg/kg of testosterone (Rvb = 2.03 +/- 0.63 millimeter)2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID207919Binding affinity for human 5 alpha reductase 1 isozyme1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID299270Inhibition of steroid 5-alpha reductase type 2 expressed in HEK 293 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Evaluation of 4'-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5alpha-reductase.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1217615Cmax in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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.
AID1489058Elimination half-life in Sprague-Dawley rat at 0.2 mg/kg, po by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1263193Cytotoxicity against human PC3 cells assessed as growth inhibition at 50 uM2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID1489054Cytotoxicity against human PC3 cells after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473832Ratio of drug concentration at steady state in human in alopecia patient at 1 mg, po QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID597653Inhibition of testosterone propionate-induced castrated Wistar rat benign prostatic hyperplasia model assessed as prostate gland arrangement order at 10 mg/kg, iv by histochemistry2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1217614Cmax in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217687Apparent biliary clearance in castrated pig at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID486433Antiproliferative activity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID1487741Decrease in progesterone level in human MCF7 cells at 1 to 10 uM after 24 hrs by ELISA2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Targeting progesterone metabolism in breast cancer with l-proline derived new 14-azasteroids.
AID1217583Terminal half life in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1515146Antagonist activity at alpha1 androgen receptor (unknown origin) assessed as reduction in R1881-induced response at 10 uM by dual-luciferase reporter gene assay relative to control2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID1217680Liver extraction ratio in castrated pig at 0.2 mg/kg, iv measured based on clearance by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272905Increase in body weight gain in male wistar rat at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=9.412+/-1.632g%)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID17979Bioavailability in dog (Beagle) at t1/2 (dose 5 mg/kg i.v.)1995Journal 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.
AID207596Compound was evaluated for the inhibition of human Steroid 5-alpha-reductase type 1 from recombinant CHO cells1998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis of benzo[c]quinolizin-3-ones: selective non-steroidal inhibitors of steroid 5 alpha-reductase 1.
AID1217558Biliary excretion in castrated pig assessed as unchanged drug level at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1601345Antagonist activity at androgen receptor (unknown origin) assessed as inhibition of R1881-induced receptor transactivation at 10 uM by dual-luciferase reporter gene assay relative to control2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety.
AID774928Inhibition of testosterone propionate-induced prostate hyperplasia in Wistar rat assessed as retention of normal cell morphology at 5 mg/kg, ip co-administered with testosterone propionate for 14 days by hematoxylin/eosin staining method2013European journal of medicinal chemistry, Nov, Volume: 69Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition.
AID23617Plasma half life in beagles after iv administration of 5 mg/kg. 1995Journal 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.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1515144Antiproliferative activity against human LNCAP cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID39178In vitro antagonist activity against rat prostatic androgen receptor (AR)1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding.
AID468985Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 3 uM after 7 hrs2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone.
AID1217650Drug excretion in castrated pig urine assessed as fraction of the dose excreted at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217661AUC (0 to 6 hrs) in castrated pig plasma withdrawn from portal vein at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217587Absorption rate constant in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217559Biliary excretion in castrated pig assessed as unchanged drug level at 0.2 mg/kg, iv measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217611AUC (0 to 6 hrs) in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1217565Drug metabolism in castrated pig plasma withdrawn from portal vein assessed as omega-hydroxy finasteride metabolite formation by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272906Effect on organ weight in male wistar rat assessed as liver tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=2.994+/- 0.254 g/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID774935Inhibition of testosterone propionate-induced prostate hyperplasia in Wistar rat at 5 mg/kg, ip co-administered with testosterone propionate for 14 days2013European journal of medicinal chemistry, Nov, Volume: 69Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition.
AID486428Antiproliferative activity against human DU145 cells assessed as growth inhibition at 0.01 ug/mL after 48 hrs by MTT assay relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID597648Toxicity in testosterone propionate-induced castrated Wistar rat benign prostatic hyperplasia model assessed as body weight at 2 to 50 mg/kg, iv for 14 days2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
AID748445Half life in human liver microsomes at 1 uM in presence of NADPH2013ACS medicinal chemistry letters, Jun-13, Volume: 4, Issue:6
Metabolically Stable tert-Butyl Replacement.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1272903Inhibition of human 5alpha-2 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione incubated for 30 mins by radioactivity-based HPLC analysis2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID597655Inhibition of testosterone propionate-induced castrated Wistar rat benign prostatic hyperplasia model assessed as decrease in epithelial protrusions at 10 mg/kg, iv by histochemistry2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
AID1713216Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line.
AID1263200Increase of prostate weight in gonadectomized golden hamster at 1 mg/kg, sc qd for 6 days co-administered with 1 mg/kg of testosterone (Rvb = 50.4 +/- 9.9 mg)2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID703547Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of dorsal prostate weight gain at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID207456In vitro inhibition of human steroid 5-alpha-reductase type I in Du-145 cells1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Synthesis and in vitro activity of 17 beta-(N-alkyl/arylformamido)- and 17 beta-[(N-alkyl/aryl)alkyl/arylamido]-4-methyl-4-aza-3-oxo-5 alpha-androstan-3-ones as inhibitors of human 5 alpha-reductases and antagonists of the androgen receptor.
AID1489056Growth inhibition of human PC3 cells at 80 uM after 48 hrs by MTT assay relative to control2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID1217567Drug metabolism in castrated pig plasma withdrawn from hepatic vein assessed as omega-hydroxy finasteride metabolite formation by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272908Effect on organ weight in male wistar rat assessed as dorsal prostate tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=50.325+/-7.519 mg/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID703548Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of ventral prostate weight gain at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
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.
AID1601347Antiproliferative activity against AR-rich human LNCaP-hr cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety.
AID1166505Displacement of [3H]MIB from rat prostate cytosol androgen receptor at 1x10'-10 to 1x10'-7 M relative to control2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3.
AID215796Compound was tested for inhibition of Type I 5-alpha-reductase in Human genital skin (Hs68) foreskin fibroblast cells.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
AID703545Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of testis weight gain per 100 gram of body weight at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1263207Increase of seminal vesicles weight in gonadectomized golden hamster at 1 mg/kg, sc qd for 6 days co-administered with 1 mg/kg of testosterone (Rvb = 96.11 +/- 12.5 mg)2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID1217679Hepatic clearance in castrated pig at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1272915Decrease in dorsal prostate organ weight in male wistar rat at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1806971In vivo inhibition of PNMT in Sprague-Dawley rat assessed as decrease in epinephrine level in adrenal gland at 1 mg, sc once daily treated for 20 days and measured after 24 hrs post last dose by liquid chromatography tandem mass spectrometry analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Three-Dimensional Proteome-Wide Scale Screening for the 5-Alpha Reductase Inhibitor Finasteride: Identification of a Novel Off-Target.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1651800Suppression of serum DHT level in Sprague-Dawley rat model of testosterone propionate-induced benign prostatic hyperplasia at 10 mg/kg, po by ELISA2020Journal of natural products, 04-24, Volume: 83, Issue:4
Oleanolic Acid Ameliorates Benign Prostatic Hyperplasia by Regulating PCNA-Dependent Cell Cycle Progression
AID1217646Drug excretion in castrated pig urine assessed as unchanged drug level at 0.8 mg/kg administered as intrajejunal dose measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217685Biliary excretion in castrated pig assessed as fraction of the dose excreted at 0.2 mg/kg, iv measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1489059Tmax in Sprague-Dawley rat at 0.2 mg/kg, po by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID1573007Inhibition of human type 2 5alpha reductase2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1217688Apparent biliary clearance in castrated pig at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1869222Suppression of testosterone propionate induced 5AR2 expression in human LNCaP cells pretreated with TP for 1 hr followed by compound addition at 10 uM by Western blotting analysis2022Journal of natural products, 06-24, Volume: 85, Issue:6
Voratins A-C: Pyridinium Alkaloids from the Marine Dinoflagellate
AID1217622Tmax in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID703552Inhibition of human type-2 5-alpha reductase expressed in HEK293 cells using [3H]-androstenedione as substrate after 30 mins by HPLC analysis2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1217557Biliary excretion in castrated pig assessed as unchanged drug level at 0.8 mg/kg administered as intrajejunal dose measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
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.
AID207604Compound was tested for the inhibitory activity against Steroid 5-alpha-reductase type 1 in rat1998Bioorganic & medicinal chemistry letters, Mar-03, Volume: 8, Issue:5
Structure activity relationship study of known inhibitors of the enzyme 5 alpha-reductase (5AR).
AID207608Compound was evaluated for the inhibition of human Steroid 5-alpha-reductase type 2 receptor from human prostate homogenates1998Bioorganic & medicinal chemistry letters, Oct-20, Volume: 8, Issue:20
Synthesis of benzo[c]quinolizin-3-ones: selective non-steroidal inhibitors of steroid 5 alpha-reductase 1.
AID1217693Cmax in castrated pig bile at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID207595Inhibition of recombinant Steroid 5-alpha-reductase type I was evaluated as binding affinity (in vitro)1995Journal 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.
AID1217579Terminal half life in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217585Absorption rate constant in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID207285Ratio of IC50 to that of 10x compound against Steroid 5-alpha-reductase1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding.
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.
AID1651810Induction of PARP1 cleavage in prostate tissue of Sprague-Dawley rat model of testosterone propionate-induced benign prostatic hyperplasia at 10 mg/kg, po by Western blot analysis2020Journal of natural products, 04-24, Volume: 83, Issue:4
Oleanolic Acid Ameliorates Benign Prostatic Hyperplasia by Regulating PCNA-Dependent Cell Cycle Progression
AID1489049Inhibition of rat liver 5alpha-reductase using testosterone as substrate incubated for 30 mins measured for 10 mins by fluorescence assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID207427Ability to inhibit Steroid 5-alpha-reductase in rat using Isotope method [3H]T to [3H]-DHT]1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
A practical synthesis of 3-substituted delta 3,5(6)-steroids as new potential 5 alpha-reductase inhibitor.
AID242430Inhibition of [1-beta-2beta-3H]- -testosterone binding to human steroid 5-alpha-reductase type 2 of BPH tissue at 10 uM2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID1397332Inhibition of testosterone-induced flank organ enlargement in golden hamster assessed as reduction in diameter of pigmented spot at 1 mg/kg, sc administered daily for 6 days measured post last dose by calliper method2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Activity of steroid 4 and derivatives 4a-4f as inhibitors of the enzyme 5α-reductase 1.
AID207735Inhibition of Steroid 5-alpha-reductase type 2 from human benign prostatic hyperplasia (BPH) tissue2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.
AID207440In vitro inhibition of human steroid 5-alpha-reductase type 2 in SW-13-transfected cells1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Synthesis and in vitro activity of 17 beta-(N-alkyl/arylformamido)- and 17 beta-[(N-alkyl/aryl)alkyl/arylamido]-4-methyl-4-aza-3-oxo-5 alpha-androstan-3-ones as inhibitors of human 5 alpha-reductases and antagonists of the androgen receptor.
AID1217616Cmax in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID207441In vitro inhibition of human Steroid 5-alpha-reductase type 2 in transfected SW-13 cells using [3H]- delta4-Androstenedione as substrate1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and in vitro evaluation of 4-substituted N-(1,1-dimethylethyl)-3-oxo-4-androstene-17 beta-carboxamides as 5 alpha-reductase inhibitors and antiandrogens.
AID1217676Liver extraction ratio in castrated pig at 0.8 mg/kg, administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1397340Inhibition of testosterone-induced increase in seminal vesicle weight in golden hamster at 1 mg/kg, sc administered daily for 6 days measured post last dose2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Activity of steroid 4 and derivatives 4a-4f as inhibitors of the enzyme 5α-reductase 1.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1217677Hepatic clearance in castrated pig at 0.8 mg/kg, administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1806970In vivo inhibition of PNMT in Sprague-Dawley rat assessed as increase in norepinephrine level in adrenal gland at 1 mg, sc administered once daily for 20 days and measured after 24 hrs post last dose by liquid chromatography tandem mass spectrometry analy2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Three-Dimensional Proteome-Wide Scale Screening for the 5-Alpha Reductase Inhibitor Finasteride: Identification of a Novel Off-Target.
AID1651802Suppression of 5-alpha reductase2 mRNA expression in Sprague-Dawley rat model of testosterone propionate-induced benign prostatic hyperplasia at 10 mg/kg, po by qRT-PCR method2020Journal of natural products, 04-24, Volume: 83, Issue:4
Oleanolic Acid Ameliorates Benign Prostatic Hyperplasia by Regulating PCNA-Dependent Cell Cycle Progression
AID207453Binding affinity to recombinant human Steroid 5-alpha-reductase type I was evaluated1995Journal 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.
AID1601346Antiproliferative activity against AR-deficient human PC3 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 10-15, Volume: 27, Issue:20
Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety.
AID1217654Renal clearance in castrated pig at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID703550Toxicity in Wistar rat assessed as mortality at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1443989Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles preincubated for 10 mins followed by ATP addition measured after 10 to 2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1217695Ratio of AUC in bile to plasma withdrawn from portal vein in castrated pig at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID353555Inhibition of 5-alpha-reductase in rat liver microsome assessed as conversion of [14C] testosterone to [14C] dihydrotestosterone2009Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8
Ganoderic acid DM: anti-androgenic osteoclastogenesis inhibitor.
AID1217560Fraction unbound in pig plasma2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID207898Compound was tested in vitro for inhibitory activity against 5-alpha reductase isozyme homogenated from transfected Namalwa1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID207893Inhibition of Steroid 5-alpha-reductase type I from rat ventral prostate (RVP)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.
AID1217663AUC (0 to 6 hrs) in castrated pig plasma withdrawn from femoral vein at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217609AUC (0 to 6 hrs) in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217561Volume of distribution at steady state in human2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217651Drug excretion in castrated pig urine assessed as fraction of the dose excreted at 0.2 mg/kg, iv measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID591082Inhibition of Mycobacterium tuberculosis 3 beta hydroxysteriod dehydrogenase2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Inhibition of the M. tuberculosis 3β-hydroxysteroid dehydrogenase by azasteroids.
AID1217678Liver extraction ratio in castrated pig at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1166507Cytotoxicity against Swiss mouse primary peritoneal macrophages assessed as growth inhibition at 50 uM after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3.
AID1263194Cytotoxicity against human MCF7 cells as growth inhibition at 50 uM2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID1473826AUC in alopecia patient at 1 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1217613AUC (0 to 6 hrs) in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1489061AUC (0 to t) in Sprague-Dawley rat at 0.2 mg/kg, po by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID1272911Effect on organ weight in male wistar rat assessed as adrenal tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=14.762 +/-0.600 mg/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID242533Inhibition of [1-beta-3H]-androstenedione binding to human steroid 5-alpha-reductase type I expressed in DU-145 cells at 10 uM2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
AID1651795Suppression of prostate tissue weight in Sprague-Dawley rat model of testosterone propionate-induced benign prostatic hyperplasia at 10 mg/kg, po relative to control2020Journal of natural products, 04-24, Volume: 83, Issue:4
Oleanolic Acid Ameliorates Benign Prostatic Hyperplasia by Regulating PCNA-Dependent Cell Cycle Progression
AID1217686Apparent biliary clearance in castrated pig at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID597646Inhibition of testosterone propionate-induced castrated Wistar rat benign prostatic hyperplasia model assessed as decrease in seminal vesicles weight at 10 mg/kg, iv for 14 days2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
AID1487743Decrease in 5alpha-DHP level in human MCF7 cells at 1 to 10 uM after 24 hrs by ELISA2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Targeting progesterone metabolism in breast cancer with l-proline derived new 14-azasteroids.
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.
AID1473827AUC in benign prostate hyperplasia patient at 5 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1217610AUC (0 to 6 hrs) in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID597654Inhibition of testosterone propionate-induced castrated Wistar rat benign prostatic hyperplasia model assessed as decrease in pseudostratified epithelia at 10 mg/kg, iv by histochemistry2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
AID207740Inhibitory activity against steroid 5-alpha-reductase type 2 in human prostate homogenates2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1515143Antiproliferative activity against human DU145 cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
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.
AID207765Inhibitory concentration against human recombinant steroid 5-alpha-reductase type I in stably transfected chinese hamster ovary (CHO) 1827 cells using [3H]testosterone.2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Synthesis, biological activity, and three-dimensional quantitative structure-activity relationship model for a series of benzo[c]quinolizin-3-ones, nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
AID1217683Biliary excretion in castrated pig assessed as fraction of the dose excreted at 0.8 mg/kg administered as intrajejunal dose measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1651808Downregulation of prostate Bcl-xL expression in Sprague-Dawley rat model of testosterone propionate-induced benign prostatic hyperplasia at 10 mg/kg, po by Western blot analysis2020Journal of natural products, 04-24, Volume: 83, Issue:4
Oleanolic Acid Ameliorates Benign Prostatic Hyperplasia by Regulating PCNA-Dependent Cell Cycle Progression
AID1217582Terminal half life in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1263197Inhibition of human prostate type 2 5alpha-reductase assessed as transformation of testosterone to dihydrotestosterone2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID207613Evaluated for the inhibitory activity against human steroid 5-alpha-reductase type 2 from human BPH tissue at 210 nM of testosterone2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2.
AID442239Inhibition of human 5 alpha reductase assessed as -log of ratio of IC50 of drug to the IC50 of reference compound2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
3D-QSAR studies on unsaturated 4-azasteroids as human 5alpha-reductase inhibitors: a self organizing molecular field analysis approach.
AID1713217Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of testosterone-induced cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line.
AID1713218Antiproliferative activity against androgen-sensitive human LNCAP cells assessed as inhibition of DHT-induced cell growth at 50 uM incubated for 48 hrs by sulforhodamine B assay relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line.
AID486432Antiproliferative activity against human DU145 cells assessed as growth inhibition at 5 ug/mL after 48 hrs by MTT assay relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID91250Inhibition 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.
AID1217697Ratio of AUC in bile to plasma withdrawn from portal vein in castrated pig at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217664Apparent half-life of the terminal disposition phase in castrated pig plasma withdrawn from portal vein at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217689AUC (0 to 6 hrs) in castrated pig bile at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID3436Inhibition of recombinant rat 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.
AID1573011Inhibition of type 2 5alpha reductase in rat prostate2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID1473831Ratio of drug concentration at steady state in human in benign prostate hyperplasia patient at 5 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1487740Decrease in SRD5A1 level in human MCF7 cells at 1 to 10 uM after 24 hrs by ELISA2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Targeting progesterone metabolism in breast cancer with l-proline derived new 14-azasteroids.
AID174356Percent conversion of testosterone to dihydrotestosterone in prostate of rats at 1 mg/kg of compound given perorally1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
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.
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.
AID1225517Reduction in prostate weight in BPH-induced Sprague-Dawley rat model at 5 mg/kg, po daily for 4 weeks in presence testosterone propionate of 10 mg/kg, intramuscular injection for 4 weeks2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Effects of resveratrol on benign prostatic hyperplasia by the regulation of inflammatory and apoptotic proteins.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1377312Inhibition of Francisella tularensis FabI enoyl reductase assessed as dissociation half life preincubated for 5 hrs in presence of NADH followed by crotonyl-CoA substrate addition by spectrophotometric method2017European journal of medicinal chemistry, Sep-29, Volume: 138Covalent inhibitors design and discovery.
AID1217580Terminal half life in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217620Tmax in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID207914In 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.
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.
AID703542Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of epididymis weight gain at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1573006Inhibition of human type 1 5alpha reductase2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID1217691AUC (0 to 6 hrs) in castrated pig bile at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272910Effect on organ weight in male wistar rat assessed testis tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=1054.099+/- 55.648 mg/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1217627Ratio of drug level in blood to plasma in human measured after 30 to 300 mins by HPLC-UV analysis2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID189540% reduction in prostate weight when compared with T-treated controls was measured in castrated rat at 10 mg/kg/day po administration1995Journal 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.
AID1217647Drug excretion in castrated pig urine assessed as unchanged drug level at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217681Liver extraction ratio in castrated pig at 0.2 mg/kg, iv measured based on AUC by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217568Drug excretion in castrated pig bile assessed as omega-hydroxy finasteride metabolite formation by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1489050Inhibition of rat liver 5alpha-reductase at 50 uM using testosterone as substrate incubated for 30 mins measured for 10 mins by fluorescence assay relative to control2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID1217584Terminal half life in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID205608Inhibitory activity against 5-alpha Reductase-2 on human prostate homogenates from surgically derived benign hyperplastic tissue1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
19-nor-10-azasteroids: a novel class of inhibitors for human steroid 5alpha-reductases 1 and 2.
AID1443991Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1217566Drug metabolism in castrated pig plasma withdrawn from femoral vein assessed as omega-hydroxy finasteride metabolite formation by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID188534In vivo evaluation in chronic castrated rat to inhibit T-stimulated prostate growth expressed as percentage reduction1993Journal of medicinal chemistry, Dec-24, Volume: 36, Issue:26
6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5 alpha-reductase.
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.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1217698Ratio of AUC in bile to plasma withdrawn from hepatic vein in castrated pig at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID3228Binding affinity for 3-beta-hydroxysteroid dehydrogenase1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID1573000Inhibition of human type 2 5alpha reductase expressed in HEK293 cells2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID174357Percent conversion of testosterone to dihydrotestosterone in prostate of rats at 30 mg/kg of compound given perorally1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
AID1217696Ratio of AUC in bile to plasma withdrawn from portal vein in castrated pig at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID703541Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of liver weight gain per 100 gram of body weight at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1217586Absorption rate constant in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID307900Inhibition of steroid 5-alpha-reductase activity in Sprague-Dawley rat liver microsomes after 10 mins2007Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14
The anti-androgen effect of ganoderol B isolated from the fruiting body of Ganoderma lucidum.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1272909Effect on organ weight in male wistar rat assessed as seminal vesicles tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=175.439+/-12.833 mg/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1263196Inhibition of rat liver type 1 5alpha-reductase assessed as transformation of testosterone to dihydrotestosterone2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID26442Half-life after intravenous administration of 10 mg/kg/day dose in male beagles1994Journal 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.
AID1573009Inhibition of type 2 5alpha reductase in human prostate2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID1166506Cytotoxicity against human PC3 cells assessed as growth inhibition at 50 uM after 48 hrs by SRB assay2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3.
AID1217694Cmax in castrated pig bile at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
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.
AID1473830Ratio of drug concentration at steady state in human in alopecia patient at 1 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1217608AUC (0 to 6 hrs) in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1473829Drug concentration at steady state in benign prostate hyperplasia patient at 5 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID188535In vivo inhibition of T stimulated prostate growth in rats was reported after oral administration at a dose 10 mg/kg/day1994Journal 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.
AID1391633Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by CCK8 assay
AID1217569Drug excretion in castrated pig urine assessed as omega-hydroxy finasteride metabolite formation by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
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.
AID207900Inhibitory activity of compound towards 5-alpha reductase from rat at 100 nM concentration1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1473828Drug concentration at steady state in alopecia patient at 1 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1651807Downregulation of prostate Bcl2 expression in Sprague-Dawley rat model of testosterone propionate-induced benign prostatic hyperplasia at 10 mg/kg, po by Western blot analysis2020Journal of natural products, 04-24, Volume: 83, Issue:4
Oleanolic Acid Ameliorates Benign Prostatic Hyperplasia by Regulating PCNA-Dependent Cell Cycle Progression
AID1806972Effect on PNMT protein expression level in Sprague-Dawley rat at 1 mg, sc once daily treated for 20 days and measured after 24 hrs post last dose by western blot analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Three-Dimensional Proteome-Wide Scale Screening for the 5-Alpha Reductase Inhibitor Finasteride: Identification of a Novel Off-Target.
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.
AID174354Percent conversion of testosterone to dihydrotestosterone in prostate of rats at 0 mg/kg of compound given perorally1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
AID1713219Cytotoxicity against Wistar rat PBMC assessed as inhibition of cell growth at 50 uM incubated for 24 hrs by sulforhodamine B assay relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis of 17β-N-arylcarbamoylandrost-4-en-3-one derivatives and their anti-proliferative effect on human androgen-sensitive LNCaP cell line.
AID1869223Suppression of testosterone propionate induced AR expression in human LNCaP cells pretreated with TP for 1 hr followed by compound addition at 10 uM by Western blotting analysis2022Journal of natural products, 06-24, Volume: 85, Issue:6
Voratins A-C: Pyridinium Alkaloids from the Marine Dinoflagellate
AID1217618Cmax in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1217578Tmax in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID242071In vitro inhibitory concentration against Cytochrome P450 17 expressed in E. coli; - = not determined2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
AID1217665Apparent half-life of the terminal disposition phase in castrated pig plasma withdrawn from hepatic vein at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1166504Inhibition of human prostate 5alpha-reductase type 2 assessed as conversion of [3H]testosterone to dihydrotestosterone2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3.
AID1473833Ratio of drug concentration at steady state in human in benign prostate hyperplasia patient at 5 mg, po QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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.
AID1489060Cmax in Sprague-Dawley rat at 0.2 mg/kg, po by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID207759Inhibition of Human steroid 5-alpha-reductase type I expressed in HEK293 cells2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2.
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.
AID774936Inhibition of testosterone propionate-induced prostate hyperplasia in Wistar rat assessed as seminal vesicle weight at 5 mg/kg, ip co-administered with testosterone propionate for 14 days (Rvb = 1.6071 +/- 0.0821 g)2013European journal of medicinal chemistry, Nov, Volume: 69Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition.
AID227856Inhibitory concentration against human recombinant steroid 5-alpha-reductase type 2 in stably transfected chinese hamster ovary 1827 cells using [3H]testosterone2004Journal of medicinal chemistry, Jul-01, Volume: 47, Issue:14
Synthesis, biological activity, and three-dimensional quantitative structure-activity relationship model for a series of benzo[c]quinolizin-3-ones, nonsteroidal inhibitors of human steroid 5alpha-reductase 1.
AID1272916Decrease in vas deferens organ weight in male wistar rat at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID174358Percent conversion of testosterone to dihydrotestosterone in prostate of rats at 3 mg/kg of compound given perorally1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1272917Decrease in epididymis organ weight in male wistar rat at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1166503Inhibition of rat liver 5alpha-reductase type 1 assessed as conversion of [3H]testosterone to dihydrotestosterone2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Effect of dehydroepiandrosterone derivatives on the activity of 5α-reductase isoenzymes and on cancer cell line PC-3.
AID1217617Cmax in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272904Cytotoxicity against human DU145 cells by rapid colorimetric assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1397339Inhibition of testosterone-induced increase in prostate weight in golden hamster at 1 mg/kg, sc administered daily for 6 days measured post last dose2018Bioorganic & medicinal chemistry, 08-07, Volume: 26, Issue:14
Activity of steroid 4 and derivatives 4a-4f as inhibitors of the enzyme 5α-reductase 1.
AID215799Compound 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.
AID1272912Effect on organ weight in male wistar rat assessed as vas deferens tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=67.613+/-3.248 mg/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
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.
AID1217699Ratio of AUC in bile to plasma withdrawn from hepatic vein in castrated pig at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272918Inhibition of human 5alpha-1 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione incubated for 30 mins by radioactivity-based HPLC analysis2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID1515145Antiproliferative activity against human RWPE1 cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID207734Inhibition of Human steroid 5-alpha-reductase type II expressed in HEK293 cells2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2.
AID242435Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells; - = not determined2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Novel C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens: synthesis, in vitro biological activity, pharmacokinetics, and antitumor activity in the LAPC4 human prostate cancer xenograft model.
AID299269Inhibition of steroid 5-alpha reductase type 1 expressed in HEK 293 cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Evaluation of 4'-substituted bicyclic pyridones as non-steroidal inhibitors of steroid 5alpha-reductase.
AID207301In vitro inhibitory activity against rat prostatic steroid 5-alpha-reductase1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding.
AID597645Inhibition of testosterone propionate-induced castrated Wistar rat benign prostatic hyperplasia model assessed as decrease in prostate weight at 10 mg/kg, iv for 14 days2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
AID1217619Cmax in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
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.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1391635Cytotoxicity against human DU145 cells assessed as growth inhibition after 24 hrs by CCK8 assay
AID1573008Inhibition of type 1 5alpha reductase in human prostate2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
AID703543Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of vas deferens weight gain at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1217563Oral absorption in human2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1647965Inhibition of steroid 5-alpha-reductase in human LNCAP cells assessed as reduction in 5- dihydrotestosterone formation incubated for 60 mins by LC-MS analysis2020Journal of natural products, 02-28, Volume: 83, Issue:2
Quintaquinone, a Merosesquiterpene from the Yellow Sponge
AID207760In vitro inhibitory activity against Steroid 5-alpha-reductase type I of human DU 145 prostatic tumor cell line2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.
AID354805Inhibition of 5alpha reductase from human prostatic hyperplasia1996Journal of natural products, May, Volume: 59, Issue:5
Determination of oenothein B as the active 5-alpha-reductase-inhibiting principle of the folk medicine Epilobium parviflorum.
AID1217621Tmax in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1217612AUC (0 to 6 hrs) in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID203349In vitro inhibition of 5-alpha-dihydrotestosterone stimulated shionogi cell proliferation; NA is not active1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and in vitro evaluation of 4-substituted N-(1,1-dimethylethyl)-3-oxo-4-androstene-17 beta-carboxamides as 5 alpha-reductase inhibitors and antiandrogens.
AID1217649Drug excretion in castrated pig urine assessed as fraction of the dose excreted at 0.8 mg/kg administered as intrajejunal dose measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID703695Inhibition of human type-1 5-alpha reductase expressed in HEK293 cells using [3H]-androstenedione as substrate after 30 mins by HPLC analysis2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1443992Total Cmax in human administered as single dose2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
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.
AID1515142Antiproliferative activity against human PC3 cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1391634Cytotoxicity against human LNCAP cells assessed as growth inhibition after 24 hrs by CCK8 assay
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1263195Cytotoxicity against human SKLU1 cells as growth inhibition at 50 uM2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID486429Antiproliferative activity against human DU145 cells assessed as growth inhibition at 0.5 ug/mL after 48 hrs by MTT assay relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID1217581Terminal half life in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID273114Ventral prostate involution in CD1 mouse at 30 mg/kg, po after 7 days2006Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
Benzopyrans are selective estrogen receptor beta agonists with novel activity in models of benign prostatic hyperplasia.
AID1217577Tmax in castrated pig plasma withdrawn from hepatic vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217684Biliary excretion in castrated pig assessed as fraction of the dose excreted at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1489062AUC (0 to infinity) in Sprague-Dawley rat at 0.2 mg/kg, po by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID1225519Reduction in serum dihydrotestosterone in BPH-induced Sprague-Dawley rat model at 5 mg/kg, po daily for 4 weeks by ELISA2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Effects of resveratrol on benign prostatic hyperplasia by the regulation of inflammatory and apoptotic proteins.
AID1487718Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Targeting progesterone metabolism in breast cancer with l-proline derived new 14-azasteroids.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1217692Cmax in castrated pig bile at 0.8 mg/kg administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272913Effect on organ weight in male wistar rat assessed as epididymis tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=187.356+/- 5.961 mg/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID207758Evaluated for the inhibitory activity against human steroid 5-alpha-reductase type I in human DU-145 cell assay at 5 nM of androstenedione2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2.
AID486438Antiandrogenic activity in ip dosed Sprague-Dawley rat assessed as increase of serum testosterone level after 6 hrs by ELISA (Rvb = 0.742 +/- 0.07 ng/ml)2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID207454In vitro inhibition of human Steroid 5-alpha-reductase type I in transfected 293 cells using [3H]- delta4-Androstenedione as substrate1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Synthesis and in vitro evaluation of 4-substituted N-(1,1-dimethylethyl)-3-oxo-4-androstene-17 beta-carboxamides as 5 alpha-reductase inhibitors and antiandrogens.
AID1217652Renal clearance in castrated pig at 0.8 mg/kg, administered as intrajejunal dose by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217588Absorption rate constant in castrated pig plasma withdrawn from femoral vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID468984Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 0.3 uM after 7 hrs2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Potent and selective steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 7, an enzyme that catalyzes the reduction of the key hormones estrone and dihydrotestosterone.
AID486430Antiproliferative activity against human DU145 cells assessed as growth inhibition at 1 ug/mL after 48 hrs by MTT assay relative to control2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID1217690AUC (0 to 6 hrs) in castrated pig bile at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID597647Inhibition of rat 5-alpha-reductase type 2 by Lineweaver-Burk plot2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
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.
AID1217666Apparent half-life of the terminal disposition phase in castrated pig plasma withdrawn from femoral vein at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1487719Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Targeting progesterone metabolism in breast cancer with l-proline derived new 14-azasteroids.
AID1217623Tmax in castrated pig plasma withdrawn from portal vein at 0.8 mg/kg administered as intrajejunal dose 20 mins after ketoconazole administration by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID207278Inhibition of human steroid 5-alpha-reductase1998Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
Novel 17-azolyl steroids, potent inhibitors of human cytochrome 17 alpha-hydroxylase-C17,20-lyase (P450(17) alpha): potential agents for the treatment of prostate cancer.
AID774938Inhibition of testosterone propionate-induced prostate hyperplasia in Wistar rat assessed as prostate weight at 5 mg/kg, ip co-administered with testosterone propionate for 14 days (Rvb = 0.838 +/- 0.0293 g)2013European journal of medicinal chemistry, Nov, Volume: 69Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition.
AID1217682Total plasma clearance in castrated pig at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217662AUC (0 to 6 hrs) in castrated pig plasma withdrawn from hepatic vein at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1272907Effect on organ weight in male wistar rat assessed as ventral prostate tissue weight per 100g at 5ml/kg, po qd measured on 15th day after 24 hrs of last dose (Rvb=59.494+/- 4.733 mg/100g)2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5α-reductase inhibitors.
AID207924Inhibitory activity against human 5-alpha Reductase-1 expressed in DU-145 cells1997Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
19-nor-10-azasteroids: a novel class of inhibitors for human steroid 5alpha-reductases 1 and 2.
AID207902Compound was tested in vitro for inhibitory activity against type 2 5-alpha reductase Isozyme homogenated from rat epididymis1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Indole derivatives as a new class of steroid 5 alpha-reductase inhibitors.
AID1869226Suppression of testosterone propionate induced PSA expression in human LNCaP cells pretreated with TP for 1 hr followed by compound addition at 10 uM by Western blotting analysis2022Journal of natural products, 06-24, Volume: 85, Issue:6
Voratins A-C: Pyridinium Alkaloids from the Marine Dinoflagellate
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID207754Inhibition of Steroid 5-alpha-reductase type 2 of rat ventral prostate (RVP)2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Synthesis and evaluation of 2'-substituted 4-(4'-carboxy- or 4'-carboxymethylbenzylidene)-N-acylpiperidines: highly potent and in vivo active steroid 5alpha-reductase type 2 inhibitors.
AID774930Inhibition of testosterone propionate-induced prostate hyperplasia in Wistar rat assessed as reduction in histoarchitecture disruption at 5 mg/kg, ip co-administered with testosterone propionate for 14 days by hematoxylin/eosin staining method2013European journal of medicinal chemistry, Nov, Volume: 69Identification and characterization of novel indole based small molecules as anticancer agents through SIRT1 inhibition.
AID703546Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of seminal vesicle weight gain per 100 gram of body weight at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID1263198Displacement of [3H}-MIB from rat prostate cytosol androgen receptor assessed as relative binding affinity2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5α-reductase and on cancer cell line SK-LU-1.
AID1806969Inhibition of human recombinant PNMT using AdoMet and DL-norepinephrine hydrocloride as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence based analysis relative to control2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Three-Dimensional Proteome-Wide Scale Screening for the 5-Alpha Reductase Inhibitor Finasteride: Identification of a Novel Off-Target.
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.
AID207426Ability to inhibit Steroid 5-alpha-reductase in rat using Enzyme kinetics method.1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
A practical synthesis of 3-substituted delta 3,5(6)-steroids as new potential 5 alpha-reductase inhibitor.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID486434Cytotoxicity against Balb/C mouse macrophages assessed as cell viability after 24 hrs by MTT assay2010European journal of medicinal chemistry, Jun, Volume: 45, Issue:6
Synthesis, antiproliferative, acute toxicity and assessment of antiandrogenic activities of some newly synthesized steroidal lactams.
AID1217562Total plasma clearance in human2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217564Volume of distribution at steady state in castrated pig at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID703544Anti-benign prostatic hyperplasia activity in Wistar rat assessed as reduction of adrenal weight gain per 100 gram of body weight at 1 mg/kg, po qd for 14 days measured on day 152012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of novel unsaturated carboxysteroids as human 5α-reductase inhibitors: a legitimate approach.
AID207451Inhibitory activity was measured on rat 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.
AID1743297Inhibition of 5-alpha reductase in rat liver microsomes assessed as inhibition of DHT formation using testosterone as substrate incubated for 10 mins by NADPH assay2020European journal of medicinal chemistry, Nov-01, Volume: 205The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.
AID1217700Ratio of AUC in bile to plasma withdrawn from hepatic vein in castrated pig at 0.2 mg/kg, iv by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID1217648Drug excretion in castrated pig urine assessed as unchanged drug level at 0.2 mg/kg, iv measured during 6 hrs sampling by UPLC-tandem mass spectrometry2011Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 39, Issue:5
In vivo investigation in pigs of intestinal absorption, hepatobiliary disposition, and metabolism of the 5α-reductase inhibitor finasteride and the effects of coadministered ketoconazole.
AID205601Binding affinity for human 5-alpha reductase 2 isozyme1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1573001Inhibition of human type 1 5alpha reductase expressed in HEK293 cells2018Journal of medicinal chemistry, 07-26, Volume: 61, Issue:14
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
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.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID597656Inhibition of testosterone propionate-induced castrated Wistar rat benign prostatic hyperplasia model assessed as decrease in hyperplasia of interstitial tissues at 10 mg/kg, iv by histochemistry2011Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
Synthesis and bioactivity of new Finasteride conjugate.
AID1489063Retention time in Sprague-Dawley rat plasma at 0.2 mg/kg, po measured after 24 hrs by total ion chromatographic method2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5α-androst-17β-amide derivatives as dual 5α-reductase inhibitors and androgen receptor antagonists.
AID1487720Cytotoxicity against HEK293 cells after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
Targeting progesterone metabolism in breast cancer with l-proline derived new 14-azasteroids.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID18033285α-R1 Activity Assay from Article 10.3109/14756366.2012.729827: \\In vivo and in vitro effect of androstene derivatives as 5a-reductase type 1 enzyme inhibitors.\\2013Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 28, Issue:6
In vivo and in vitro effect of androstene derivatives as 5α-reductase type 1 enzyme inhibitors.
AID18033295α-R2 Activity Assay from Article 10.3109/14756366.2012.729827: \\In vivo and in vitro effect of androstene derivatives as 5a-reductase type 1 enzyme inhibitors.\\2013Journal of enzyme inhibition and medicinal chemistry, Dec, Volume: 28, Issue:6
In vivo and in vitro effect of androstene derivatives as 5α-reductase type 1 enzyme inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1346052Human steroid 5 alpha-reductase 2 (1.-.-.- Oxidoreductases)1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,341)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (0.17)18.7374
1990's566 (24.18)18.2507
2000's818 (34.94)29.6817
2010's745 (31.82)24.3611
2020's208 (8.89)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials405 (16.11%)5.53%
Reviews455 (18.10%)6.00%
Case Studies99 (3.94%)4.05%
Observational5 (0.20%)0.25%
Other1,550 (61.65%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (67)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Comparative,Randomized,Single-dose,2-way Crossover Bioavailability Study of Dr.Reddy's Laboratories Limited Finasteride Tablets 1 mg and Merck & Co., Propecia Under Fasting Condition. [NCT01133444]Phase 124 participants (Actual)Interventional2002-04-30Completed
A Randomized, Single-dose, Two-treatment, Two-way, Crossover Bioequivalence Study of Finasteride 5 mg Tablets (Dr. Reddy's Laboratories Limited) With the Reference Formulation PROSCAR® 5 mg Tablet (Merck & Co., Inc.) Under Fed Conditions in Healthy Adult [NCT01264302]Phase 126 participants (Actual)Interventional2006-11-30Completed
Establishing the Benefits of Adherence to Enlarged Prostate Treatment: A Validation Study Linking Adherence to Outcomes Using the Market Scan Database [NCT01381510]54,459 participants (Actual)Observational2010-06-30Completed
Comparative,Randomized,Single-dose,2-way Crossover Bioavailability Study of Dr.Reddy's Laboratories Limited Finasteride Tablets 1 mg and Merck & Co., Propecia in Healthy Adult Males Under Fed Condition. [NCT01133457]Phase 124 participants (Actual)Interventional2002-04-30Completed
High Risk Prostate Cancer Prevention Study [NCT01174953]18 participants (Actual)Interventional2010-07-31Completed
Neoadjuvant Finasteride for Patients With Non-small Cell Lung Cancer [NCT02055170]Phase 24 participants (Actual)Interventional2014-06-30Terminated(stopped due to Unable to improve on poor accrual to study.)
A Double-Blind, Randomized, Placebo-Controlled Dose-Ranging Study Evaluating the Efficacy and Safety of Once Weekly High Dose Oral Finasteride in the Treatment of Severe Nodulocystic Acne [NCT02502669]Phase 2106 participants (Actual)Interventional2015-07-31Completed
Phase 2 Multicenter Randomized Two Dose Level and Non-Inferiority Clinical Evaluation of Transrectal Administration of NX-1207 for the Treatment of BPH [NCT00759135]Phase 285 participants (Actual)Interventional2007-05-31Completed
A Multicentre, Randomized, Double-blind, Parallel-group, Controlled Study, to Assess the Efficacy and Safety of P-3074 Cutaneous Spray, Solution, in the Treatment of Male Pattern Baldness [NCT03004469]Phase 3458 participants (Actual)Interventional2016-08-02Completed
A Relative Bioavailability Study of Finasteride 5 mg Tablets Under Non-Fasting Conditions [NCT00835796]Phase 120 participants (Actual)Interventional2002-06-30Completed
A Relative Bioavailability Study of Finasteride 5 mg Tablets Under Fasting Conditions [NCT00835666]Phase 132 participants (Actual)Interventional2002-06-30Completed
Single-Dose Fasting In Vivo Bioequivalence Study of Finasteride Tablets (5 mg; Mylan) and Proscar Tablets (5 mg; Merck) in Healthy Male Volunteers [NCT00648791]Phase 129 participants (Actual)Interventional2004-09-30Completed
Benefits of Adherence to 5-alpha Reductase Inhibitor Treatment in Men With Enlarged Prostate: An Assessment of Medicare and Medicaid Patients Using the MarketScan Database [NCT01376258]28,903 participants (Actual)Observational2010-10-31Completed
A Randomized, Single-dose, Two-treatment, Two-way, Crossover Bioequivalence Study of Finasteride 5 mg Tablets (Dr. Reddy's Laboratories Limited) With the Reference Formulation PROSCAR® 5 mg Tablet (Merck & Co., Inc.) Under Fasting Conditions in Healthy Ad [NCT01264289]Phase 126 participants (Actual)Interventional2006-11-30Completed
Improving Prostate Biopsy Efficiency: The Finasteride Challenge Test [NCT01296672]Phase 4383 participants (Actual)Interventional2011-02-28Completed
H-36371: Finasteride as a Method of Managing Testosterone-Induced Erythrocytosis [NCT02548117]Phase 30 participants (Actual)Interventional2016-02-29Withdrawn(stopped due to Funding was not available.)
Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase 2A Study of Setipiprant Tablets in Androgenetic Alopecia in Males [NCT02781311]Phase 2169 participants (Actual)Interventional2016-07-14Completed
A Phase 2 Study of Bicalutamide Plus Finasteride in Men With MRI Detectable Prostate Nodules Undergoing Active Surveillance [NCT02146937]Phase 20 participants (Actual)Interventional2014-03-31Withdrawn(stopped due to Due to lack of accrual for this study. PI decided to close the study.)
A Randomized, Open-Label, Exploratory, Pharmacokinetic, Sequential Single Ascending Dose Study of IVL3001 Versus Propecia (Finasteride) Tablets in Healthy Adult Participants [NCT04945226]Phase 1/Phase 240 participants (Actual)Interventional2021-09-21Completed
Imperial Prostate 4: Comparative Health Research Outcomes of NOvel Surgery in Prostate Cancer [NCT04049747]2,450 participants (Anticipated)Interventional2019-12-11Recruiting
Randomized, 2-Way Crossover Bioequivalence Study Finasteride 5 mg Tablet and Proscar Administrated as 1 x 5 mg Tablet in Healthy Subjects Under Fed Conditions [NCT00871247]Phase 126 participants (Actual)Interventional2004-11-30Completed
Effectiveness and Safety of Topical Finasteride and Minoxidil Combination Compared to Topical Minoxidil for The Treatment of Male Androgenetic Alopecia [NCT05990400]Phase 2/Phase 340 participants (Anticipated)Interventional2023-05-01Recruiting
The Efficacy of Topical Finasteride in the Treatment of Idiopathic Hirsutism [NCT00564252]56 participants (Actual)Interventional2006-02-28Completed
5-Alpha Reductase 2 as a Marker of Resistance to 5ARI Therapy [NCT04288427]120 participants (Anticipated)Interventional2020-09-25Recruiting
Efficacy of 3% Minoxidil Versus Combined 3% Minoxidil and 0.1% Finasteride for Male Pattern Hair Loss: a Randomized, Double-blinded, Comparative Study [NCT01391156]Phase 340 participants (Actual)Interventional2011-03-31Completed
MK0906 Phase III Double-Blind Comparative Study - Benign Prostate Hyperplasia [NCT00127179]Phase 3600 participants (Actual)Interventional2004-01-01Completed
A Randomized, Double Blind, Placebo Controlled Clinical Trial of L-SeMet Supplementation and Finasteride Treatment of Patients With Prostate Cancer Prior to Robotic Prostatectomy/Brachytherapy [NCT00736645]Phase 255 participants (Actual)Interventional2008-08-31Completed
A Feasibility Study of Oral Hormonal Therapy and Radiation for Non-metastatic, Intermediate or High Risk Prostate Cancer in Men 70 and Older or With Medical Comorbidities [NCT01342367]74 participants (Actual)Interventional2010-12-17Active, not recruiting
A Randomized Controlled Trial Evaluating the Tissue Effects of Preoperative Finasteride Versus Placebo for Patients With Clinically Organ-Confined Prostate Cancer [NCT00438464]Phase 2204 participants (Actual)Interventional2007-02-28Completed
Study Evaluating the Association of CAG Repeat Polymorphisms and Finasteride Response in Women With Androgenetic Alopecia [NCT01052870]Phase 112 participants (Actual)Interventional2008-12-31Completed
On Label, Randomized, Double-Blind, Placebo-Controlled Trial of Preoperative Finasteride in Patients Undergoing Transurethral Resection of the Prostate (TURP) [NCT00564460]Phase 30 participants (Actual)Interventional2008-02-29Withdrawn(stopped due to Change of practice pattern. Green light laser)
Randomized, 2-Way Crossover Bioequivalence Study Finasteride 5 mg Tablet and Proscar Administrated as 1 x 5 mg Tablet in Healthy Subjects Under Fasting Conditions. [NCT00870480]Phase 126 participants (Actual)Interventional2004-11-30Completed
Single-Dose Food In Vivo Bioequivalence Study of Finasteride Tablets (5 mg; Mylan) to Proscar® Tablets (5 mg; Merck) in Healthy Male Volunteers [NCT00650377]Phase 130 participants (Actual)Interventional2004-10-31Completed
A Study of the Efficacy and Safety of Multiple Doses of Dutasteride Versus Placebo and Finasteride in the Treatment of Male Subjects With Androgenetic Alopecia [NCT01231607]Phase 3917 participants (Actual)Interventional2010-10-28Completed
A Phase 3b, Randomized, Double-blind, Placebo-controlled Parallel-design Study to Evaluate the Efficacy and Safety of Tadalafil Co-administered With Finasteride for 6 Months in Men With Lower Urinary Tract Symptoms and Prostatic Enlargement Secondary to B [NCT01139762]Phase 3696 participants (Actual)Interventional2010-09-30Completed
A Within-subject, Randomized, Evaluator-blinded, Vehicle-controlled Study to Assess the Photosensitization Potential of Finasteride Cutaneous Solution(P-3074) in Human Subjects [NCT02791243]Phase 158 participants (Actual)Interventional2016-05-09Completed
A Phase III, Randomized, Double-Blind, Placebo Controlled Trial of PROSCAR in Men With Initial Negative Prostate Biopsies [NCT00542243]Phase 319 participants (Actual)Interventional2008-02-29Completed
Pharmacokinetics of a Novel Oral Testosterone Undecanoate Formulation With Concomitant Inhibition of 5alpha-Reductase by Finasteride [NCT00842751]Phase 211 participants (Actual)Interventional2009-07-31Completed
Minimally Invasive Surgical Therapy Consortium for Benign Prostatic Hyperplasia [NCT00064649]Phase 349 participants (Actual)Interventional2004-04-30Terminated(stopped due to Inability to recruit required sample size.)
Prostate Medication, Metabolism and Gut Microbiota [NCT06001619]Phase 4100 participants (Anticipated)Interventional2022-12-01Recruiting
Pathophysiology-Guided Therapy for Sleep Apnea in the Elderly [NCT02703220]Phase 4100 participants (Anticipated)Interventional2015-07-03Recruiting
Kinetics of the Finasteride Prostate Induced Apoptosis [NCT00130767]Phase 490 participants Interventional2004-12-31Active, not recruiting
Pilot Study for the Evaluation of Finasteride in the Treatment of Chronic Central Serous Chorioretinopathy [NCT00837252]Phase 1/Phase 25 participants (Actual)Interventional2009-02-28Completed
The Use of Finasteride to Reduce Hematuria and Hematospermia Following TRUS Prostate Biopsy [NCT00600691]Phase 229 participants (Actual)Interventional2008-03-31Terminated(stopped due to Did not achieve enrollment goal and decided to terminate early)
Medical Therapy of Prostatic Symptoms [NCT00021814]Phase 33,407 participants (Actual)Interventional1995-12-31Completed
5-Alpha Reductase and Anabolic Effects of Testosterone [NCT00475501]Phase 260 participants (Actual)Interventional2007-01-31Completed
Oral Androgens in Man-6: Pharmacokinetics of Slow and Fast Release, External Matrix Oral Testosterone Formulations in Normal Men With Experimental Hypogonadism [NCT00663793]Phase 116 participants (Actual)Interventional2008-10-31Completed
A Prospective Multicentric Open Label Randomized Bio-Interventional Phase I/II Pilot Study To Evaluate The Safety And Efficacy Of Autologous Human Platelet Lysate (HPL) For Treatment Of Androgenetic Alopecia (AGA) [NCT01643629]Phase 1/Phase 220 participants (Anticipated)Interventional2012-01-31Active, not recruiting
Demonstrating the Clinical and Economic Benefit of 5 Alpha Reductase Inhibitor Adherence in Benign Prostatic Hyperplasia [NCT01334723]35,032 participants (Actual)Observational2010-04-30Completed
A Multicenter, Randomized, Double-blind, Clinical Study to Investigate the Efficacy and Safety of Treatment With Tamsulosin 0.2mg Mono and Tamsulosin 0.2mg, Finasteride 5mg Combination Therapy in Patients With LUTS/BPH [NCT01736033]Phase 4545 participants (Actual)Interventional2012-02-29Active, not recruiting
Open Label, Randomized Comparative Study to Evaluate the Pharmacokinetic Characteristics Between Coadministered Finasteride Tablet and Tamsulosin HCl Tablet and GL2701 Capsule, in Healthy Subjects [NCT01829893]Phase 126 participants (Actual)Interventional2012-01-31Completed
Clinical Progression and Costs in Benign Prostatic Hyperplasia Patients Treated With Early Versus Delayed Combination Therapy [NCT01435954]13,551 participants (Actual)Observational2010-08-31Completed
Extension Study for the Evaluation of Finasteride in the Treatment of Chronic Central Serous Chorioretinopathy [NCT01227993]Phase 1/Phase 23 participants (Actual)Interventional2010-10-31Completed
The Effect of Short Term Use of Finasteride Versus Cyproterone Acetate on Perioperative Blood Loss With Mono Polar Transurethral Resection of Prostate [NCT04848181]Early Phase 160 participants (Actual)Interventional2019-07-01Completed
A Phase II Study of Enzalutamide Plus Dutasteride/Finasteride as First Line Treatment for Vulnerable Patients ≥ 65 Years With Systemic Prostate Cancer [NCT02213107]Phase 240 participants (Anticipated)Interventional2014-09-30Active, not recruiting
MICTUS (Multicentre Investigation to Characterise the Effect of Tamsulosin on Urinary Symptoms): A Multicentre, Double-blind, Randomised, Parallel Group Study, Aimed at Characterising the Effect of Tamsulosin, an Uroselective α1- Receptor Blocking Agent, [NCT02244229]Phase 4403 participants (Actual)Interventional1998-04-30Completed
An Open Label Study of 5α-reductase Inhibition on the Regulation of Insulin Action and Metabolic Phenotype in Healthy Volunteers. [NCT01923090]Phase 212 participants (Anticipated)Interventional2012-08-31Recruiting
A Phase III, Randomized Clinical Trial to Study the Safety and Efficacy of MK-906 (Finasteride) and Tamsulosin Administered Either Alone or Concomitantly in Patients With Benign Prostatic Hyperplasia (BPH) [NCT01534351]Phase 31 participants (Actual)Interventional2013-08-01Terminated(stopped due to Business Reasons)
The Use of 5mg Finasteride Versus 200mg Spironolactone and Topical 5% Minoxidil in Treating Postmenopausal Female Androgenetic Alopecia [NCT02483195]Phase 40 participants (Actual)Interventional2016-08-31Withdrawn(stopped due to PI indicating she was withdrawing her study submission due to lack of funding as of 6/20/2016)
A Phase-I, Open Label, Multi-Centre Clinical Study to Assess the Safety, Tolerability and Usability of FOL100 Lotion in Comparison to Oral Finasteride, for the Treatment of Androgenetic Alopecia [NCT05611593]Phase 166 participants (Anticipated)Interventional2022-10-20Recruiting
A Randomized, Active-Controlled, Double-Blind, Parallel Design, Multi-Center, Phase III Clinical Trial to Evaluate the Efficacy and Safety of GV1001 in Patients With Benign Prostatic Hyperplasia (BPH) [NCT04032067]Phase 3423 participants (Actual)Interventional2019-10-30Completed
National, Multicentre, Randomized, Double-blind, Double-dummy Phase III Clinical Trial to Evaluate the Efficacy and Safety of Finlândia Hair Lotion Association in the Treatment of Androgenetic Alopecia. [NCT04594018]Phase 3190 participants (Anticipated)Interventional2023-10-31Not yet recruiting
Higher-Than-Replacement Testosterone Plus Finasteride Treatment After SCI [NCT02248701]Phase 233 participants (Actual)Interventional2017-04-27Terminated(stopped due to Enrollment difficulties)
A Double-Blind, Placebo-Controlled, Multicenter Study To Examine the Effects of Finasteride 1 MG on Serum Prostate-Specific Antigen in Men With Androgenetic Alopecia [NCT00396175]Phase 3355 participants Interventional1998-03-31Completed
A Phase II Trial of Potency-Sparing Hormonal Therapy in Patients With Elevated Serum PSA After Radiation Therapy or Radical Prostatectomy for Prostate Cancer [NCT00003323]Phase 2101 participants (Actual)Interventional1998-05-31Completed
Phase II, Randomized, Placebo-Controlled Study for the Evaluation of Finasteride in the Treatment of Chronic Central Serous Chorioretinopathy [NCT01585441]Phase 26 participants (Actual)Interventional2012-04-30Terminated(stopped due to This study was terminated early due to lack of enrollment.)
Clinical and Economic Outcomes of Patients Utilizing Combination Therapy for Enlarged Prostates: A Henry Ford Database Assessment [NCT01386983]332 participants (Actual)Observational2009-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Grade -- Specimen (Primary)
NCT00438464 (24) [back to overview]Characteristics of Blood Biomarkers: Dihydrotestosterone (ng/dL) Percentage Change
NCT00438464 (24) [back to overview]Characteristics of Blood Biomarkers: Estradiol (ng/dL) Percentage Change
NCT00438464 (24) [back to overview]Characteristics of Blood Biomarkers: Estrone (ng/dL) Percentage Change
NCT00438464 (24) [back to overview]Characteristics of Blood Biomarkers: Prostate-specific Antigen (ng/mL) Percentage Change (%)
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Zonal Origin of Tumor Foci Per Radical Prostatectomy Specimen (RPS)
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Exhibiting Detectable Staining Within Finasteride Treatment Arm for Biomarker Subgroups
NCT00438464 (24) [back to overview]Characteristics of Blood Biomarkers: Testosterone (ng/dL) Percentage Change
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Cancer Foci
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Exhibiting Detectable Staining Within Placebo Treatment Arm for Biomarker Subgroups (Mean)
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Within Placebo Treatment Arm for Biomarker Subgroups
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 3 (GG3) Biomarker Subgroups at Prostatectomy
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 3 (GG3) Biomarker Subgroups at Prostatectomy
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 4 (GG4) Biomarker Subgroup at Prostatectomy
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 4 (GG4) Biomarker Subgroup at Prostatectomy
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Grade -- Specimen (Secondary)
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Score
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Upgrade Between Biopsy and Prostatectomy
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Lymph Node Status
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Margin of Resection (MOR)
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Tumor Volume (Cubic Centimeter)
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Tumor, Node, Metastasis (TNM) Stage
NCT00438464 (24) [back to overview]Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Zonal Origin -- Dominant Tumor Focus
NCT00438464 (24) [back to overview]Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Exhibiting Detectable Staining Within Finasteride Treatment Arm for Biomarker Subgroups (Mean)
NCT00475501 (11) [back to overview]Dietary Protein Intake
NCT00475501 (11) [back to overview]Life Satisfaction
NCT00475501 (11) [back to overview]Hematocrit
NCT00475501 (11) [back to overview]Grip Strength kg
NCT00475501 (11) [back to overview]Geriatric Depression Scale
NCT00475501 (11) [back to overview]Benton Judgment of Line Orientation Test
NCT00475501 (11) [back to overview]30 Minute Recall Portion of Rey Osterrieth Complex Figure (ROCF) Test
NCT00475501 (11) [back to overview]1 Repetition Maximum (1-RM) Strength Testing
NCT00475501 (11) [back to overview]Lumbar Spine L2-L4 Bone Mineral Density
NCT00475501 (11) [back to overview]Trail-Making Test, Part A
NCT00475501 (11) [back to overview]Transrectal Ultrasound Sizing of Prostate
NCT00663793 (3) [back to overview]Area Under the Curve-Serum T
NCT00663793 (3) [back to overview]Area Under the Curve-E2
NCT00663793 (3) [back to overview]Area Under the Curve-serum DHT
NCT00736645 (2) [back to overview]Effects of Selenium and Finasteride and Their Combination on Apoptosis Induction
NCT00736645 (2) [back to overview]Effects of Selenium and Finasteride and Their Combination on PSA Level
NCT00835666 (3) [back to overview]AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)
NCT00835666 (3) [back to overview]AUCinf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)
NCT00835666 (3) [back to overview]Cmax - Maximum Observed Concentration
NCT00835796 (3) [back to overview]AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)
NCT00835796 (3) [back to overview]AUCinf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)
NCT00835796 (3) [back to overview]Cmax - Maximum Observed Concentration
NCT00837252 (12) [back to overview]Change in Serum Dihydrotestosterone (DHT) Concentration at Month 3 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Visual Acuity at Month 6 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Visual Acuity at Month 3 Compared to Baseline.
NCT00837252 (12) [back to overview]Change in Urinary Cortisol Level at Month 6 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Center-Subfield Macular Thickness at Month 6 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Subretinal Fluid Volume at Month 6 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Center-Subfield Macular Thickness at Month 3 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Subretinal Fluid Volume at Month 3 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Serum Testosterone Level at Month 6 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Serum Testosterone Level at Month 3 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Serum Dihydrotestosterone (DHT) Concentration at Month 6 Compared to Baseline
NCT00837252 (12) [back to overview]Change in Urinary Cortisol Level at Month 3 Compared to Baseline
NCT00842751 (3) [back to overview]Maximum Testosterone Concentration
NCT00842751 (3) [back to overview]Serum Estradiol Concentration
NCT00842751 (3) [back to overview]Serum Dihydrotestosterone Concentration
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Intercourse Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Overall Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Sexual Desire Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) Question 3 and 4 Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Prostate Symptom Score (IPSS) Quality of Life Index From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in International Prostate Symptom Score (IPSS) Subscores Index From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in Total International Prostate Symptom Score (IPSS) From Baseline to 4 and 26 Weeks
NCT01139762 (14) [back to overview]Clinician Global Impression of Improvement (CGI-I) at 26 Weeks
NCT01139762 (14) [back to overview]Patient Global Impression of Improvement (PGI-I) at 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Orgasmic Function Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01139762 (14) [back to overview]Change in Post Void Residual (PVR) Volume From Baseline to 26 Weeks
NCT01139762 (14) [back to overview]Change in Total International Prostate Symptom Score (IPSS) From Baseline to 12 Weeks
NCT01139762 (14) [back to overview]Treatment Satisfaction Scale - Benign Prostatic Hyperplasia (TSS-BPH) at 26 Weeks
NCT01139762 (14) [back to overview]Change in International Index of Erectile Function (IIEF) - Erectile Function Domain Scores From Baseline to 4, 12, and 26 Weeks
NCT01227993 (7) [back to overview]Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at One Year Compared to Baseline
NCT01227993 (7) [back to overview]Change in Serum Testosterone Levels at Two Years Compared to Baseline
NCT01227993 (7) [back to overview]Change in Best-corrected Visual Acuity (BCVA) in the Fellow Eye at Two Years Compared to Baseline
NCT01227993 (7) [back to overview]Change in Best-corrected Visual Acuity (BCVA) in the Fellow Eye at One Year Compared to Baseline
NCT01227993 (7) [back to overview]Change in 24-hour Urine Cortisol Levels at Two Years Compared to Baseline
NCT01227993 (7) [back to overview]Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at Two Years Compared to Baseline
NCT01227993 (7) [back to overview]Change in Serum DHT Levels at Two Years Compared to Baseline
NCT01231607 (17) [back to overview]Global Assessment of Improvement From Baseline to Week 24 Assessed for Vertex and Frontal Views Separately
NCT01231607 (17) [back to overview]Change From Baseline in Investigator Photographic Assessment Questionnaire (IPAQ) Scores Assessed at Week 24 for Vertex and Frontal Views Separately
NCT01231607 (17) [back to overview]Change From Baseline in Investigator Photographic Assessment Questionnaire (IPAQ) Scores Assessed at Week 12 for Vertex and Frontal Views Separately
NCT01231607 (17) [back to overview]Change From Baseline in Hair Growth Index (HGI) Scores at Weeks 12 and 24
NCT01231607 (17) [back to overview]Change From Baseline in Target Area Hair Count Within a 2.54 cm (1 Inch) Diameter Circle at the Vertex at Week 12 as Assessed by MT
NCT01231607 (17) [back to overview]Change From Baseline in Target Area Hair Count Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex, as Assessed by MT at Week 12
NCT01231607 (17) [back to overview]Change From Baseline in Target Area Hair Count Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex at Week 24, as Assessed by MT
NCT01231607 (17) [back to overview]Change From Baseline (BL) in Target Area Hair Count (HC) Within a 2.54 Centimeter (cm) (1 Inch) Diameter Circle at the Vertex at Week 24, as Assessed by Macrophotographic Technique (MT)
NCT01231607 (17) [back to overview]Change From Baseline in Total Hair Growth Satisfaction Scale (HGSS) Scores at Weeks 12 and 24
NCT01231607 (17) [back to overview]Number of Participants With the Indicated Change From Baseline (BL) in the Stage (S) of Androgenic Alopecia (AGA) According to the Norwood-Hamilton Scale at Week 12 (W12)
NCT01231607 (17) [back to overview]Change From Baseline in Target Area Hair Width Within a 2.54 cm (1 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT
NCT01231607 (17) [back to overview]Number of Participants With the Indicated Change From Baseline (BL) in the Stage (S) of Androgenic Alopecia (AGA) According to the Norwood-Hamilton Scale at Week 24
NCT01231607 (17) [back to overview]Serum Concentration of Dutasteride at Week 12, Week 24, and Follow-up (Week 26)
NCT01231607 (17) [back to overview]Serum Dihydrotestosterone (DHT) at Week 12, Week 24, and Follow-up (Week 26)
NCT01231607 (17) [back to overview]Change From Baseline in Terminal Hair Count (THC) Within a 2.54 cm (1 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT
NCT01231607 (17) [back to overview]Change From Baseline in Terminal Hair Count Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT
NCT01231607 (17) [back to overview]Change From Baseline in Target Area Hair Width Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT
NCT01296672 (3) [back to overview]Pre/Post Ratio PSA Area Under the Curve (AUC)
NCT01296672 (3) [back to overview]T2:ERG ( A Gene on Chromosome 21q22.2 That Encodes an Androgen-regulated Transmembrane Serine Protease Ratio to Estrogen Related Gene) Score AUC
NCT01296672 (3) [back to overview]PCA3 (Prostate Cancer Antigen 3)Score AUC
NCT01334723 (8) [back to overview]Mean BPH-Related Costs for Participants With an MPR >=70% Versus <70%
NCT01334723 (8) [back to overview]Mean BPH-Related Costs for Participants With an MPR >=75% Versus <75%
NCT01334723 (8) [back to overview]Mean BPH-Related Costs for Participants With an MPR >=80% Versus <80%
NCT01334723 (8) [back to overview]Number of Participants With Risk of Acute Urinary Retention and Surgery Based on an MPR Threshold of 70%
NCT01334723 (8) [back to overview]Number of Participants With Risk of Acute Urinary Retention and Surgery Based on an MPR Threshold of 75%
NCT01334723 (8) [back to overview]Number of Participants With Risk of Acute Urinary Retention and Surgery Based on an MPR Threshold of 80%
NCT01334723 (8) [back to overview]Mean Length of 5-ARI Therapy
NCT01334723 (8) [back to overview]BPH-Related Costs for Every 30 Days of 5-ARI Therapy
NCT01342367 (2) [back to overview]Percentage of Participants Free From Biochemical Failure
NCT01342367 (2) [back to overview]Quality of Life Was Measured by the Expanded Prostate Cancer Index Composite (EPIC) Hormonal Health-related Quality of Life Questionnaire
NCT01386983 (2) [back to overview]Number of Participants With Clinical Progression
NCT01386983 (2) [back to overview]Dollar Amount of Enlarged Prostate (EP)-Related Medical Costs Incurred Per Month
NCT01534351 (2) [back to overview]Number of Participants Who Experienced an Adverse Event
NCT01534351 (2) [back to overview]Number of Participants Who Discontinued Treatment Due to an Adverse Event
NCT01585441 (23) [back to overview]Changes in Mean Macular Sensitivity in the Study Eye at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Changes in Mean Macular Sensitivity in the Study Eye at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants Presenting No Change in Autofluorescence Patterns at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants Presenting No Change in Autofluorescence Patterns at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Changes in Best-corrected Visual Acuity (BCVA) in the Study Eye at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants Presenting No Change in Fluid Leakage at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants Presenting No Change in Fluid Leakage at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants Presenting No Change in Size of Existing Plaque(s) on Indocyanine Green (ICG) Angiography at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants Presenting No Change in Size of Existing Plaque(s) on Indocyanine Green (ICG) Angiography at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants Who Withdrew From the Study
NCT01585441 (23) [back to overview]Percent Change in Subretinal Fluid Volume in the Study Eye at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Proportion of Participants With a Reduction in Subretinal Fluid Volume ≥ 50% at 3 Months Compared to Baseline
NCT01585441 (23) [back to overview]Proportion of Participants With an Improvement in Best-corrected Visual Acuity (BCVA) ≥ 15 Letters at 3 Months Compared to Baseline.
NCT01585441 (23) [back to overview]Change in Serum Testosterone Concentration at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Change in Serum Testosterone Concentration at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Change in Central Retinal Thickness in the Study Eye at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Change in Central Retinal Thickness in the Study Eye at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Change in Serum Dihydrotestosterone (DHT) Concentration at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Change in Serum Dihydrotestosterone (DHT) Concentration at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Number of Participants With Adverse Reactions Related to the Investigational Product
NCT01585441 (23) [back to overview]Change in Urinary Levels of Cortisol at Month 3 Compared to Baseline
NCT01585441 (23) [back to overview]Change in Urinary Levels of Cortisol at the Safety Visit Compared to Baseline
NCT01585441 (23) [back to overview]Changes in Best-corrected Visual Acuity (BCVA) in the Study Eye at Month 3 Compared to Baseline
NCT02248701 (6) [back to overview]Absolute Change in Walking Speed
NCT02248701 (6) [back to overview]Percent Change in Hip Bone Mineral Density
NCT02248701 (6) [back to overview]Percent Change in Neuromuscular Function
NCT02248701 (6) [back to overview]Percent Change in Total Body Fat
NCT02248701 (6) [back to overview]Percent Change in Visceral Fat
NCT02248701 (6) [back to overview]Percent Changes in Muscle Cross-Sectional Area
NCT02781311 (2) [back to overview]Change From Baseline in Target Area Hair Count (TAHC) at Week 24
NCT02781311 (2) [back to overview]Subject Self-Assessment (SSA) Score in Hair Growth at Week 24
NCT03004469 (9) [back to overview]Adjusted Mean Change From Baseline in Target Area Hair Width (TAHW) in the Vertex at Weeks 12 and 24
NCT03004469 (9) [back to overview]Adjusted Mean Change From Baseline in Participants Hair Growth/Loss at Weeks 12 and 24, Assessed for the Vertex by Blind Assessor
NCT03004469 (9) [back to overview]Adjusted Mean Change From Baseline in Participants Hair Growth/Loss Assessed for the Vertex by Investigator at Weeks 12 and 24
NCT03004469 (9) [back to overview]Adjusted Mean Change From Baseline in Hair Growth Assessed by Target Area Hair Count (TAHC) in the Vertex at Week 24
NCT03004469 (9) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious TEAEs
NCT03004469 (9) [back to overview]Local Tolerability as Assessed by Incidence Rate of Skin Irritation Event Via Severity Score for Skin Irritation Scale
NCT03004469 (9) [back to overview]Adjusted Mean Change From Baseline in Hair Growth Assessed by TAHC in the Vertex at Week 12
NCT03004469 (9) [back to overview]Adjusted Mean International Index of Erectile Function (IIEF-2) Scores at Weeks 4, 8, 12 and 24
NCT03004469 (9) [back to overview]Adjusted Mean Overall Male Hair Growth Questionnaire (MHGQ) Score as Assessed by the Participant at Weeks 12 and 24

Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Grade -- Specimen (Primary)

Frequency of Grade 3 and Grade 4 tumors in two treatment groups: Participants consist of men with adenocarcinoma of the prostate, clinical stage T1c or T2, with a Gleason score of 6 or 7 and a PSA level < 10 ng/mL, who are scheduled to undergo prostatectomy. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
Grade 3Grade 4
Arm I (Finasteride)6523
Arm II (Placebo)7518

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Characteristics of Blood Biomarkers: Dihydrotestosterone (ng/dL) Percentage Change

Characteristics of blood biomarkers using pretreatment and posttreatment values. Dihydrotestosterone (DHT) blood test measures serum concentrations of dihydrotestosterone and is closely related to those of testosterone. (NCT00438464)
Timeframe: Baseline biopsy to prostatectomy following maximum 6 week treatment period

Interventionpercentage of change (Median)
Arm I (Finasteride)-64.8
Arm II (Placebo)-3.6

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Characteristics of Blood Biomarkers: Estradiol (ng/dL) Percentage Change

Characteristics of blood biomarkers using pretreatment and posttreatment values. Blood test used to measure Estradiol. (NCT00438464)
Timeframe: Baseline biopsy to prostatectomy following maximum 6 week treatment period

Interventionpercentage of change (Median)
Arm I (Finasteride)7.2
Arm II (Placebo)0

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Characteristics of Blood Biomarkers: Estrone (ng/dL) Percentage Change

Characteristics of blood biomarkers using pretreatment and posttreatment values. Blood test used to measure Estrone (E1), one of the three estrogens, which also includes estriol and estradiol. (NCT00438464)
Timeframe: Baseline biopsy to prostatectomy following maximum 6 week treatment period

Interventionpercentage of change (Median)
Arm I (Finasteride)-8.9
Arm II (Placebo)0

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Characteristics of Blood Biomarkers: Prostate-specific Antigen (ng/mL) Percentage Change (%)

Characteristics of blood biomarkers using pretreatment and posttreatment values. Prostate-specific antigen (PSA) blood test measuring protein produced by prostate cells. (NCT00438464)
Timeframe: Baseline biopsy to prostatectomy following maximum 6 week treatment period

Interventionpercentage of change (Median)
Arm I (Finasteride)-39.4
Arm II (Placebo)-4.6

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Zonal Origin of Tumor Foci Per Radical Prostatectomy Specimen (RPS)

Tumor distribution within zones of the prostate using radical prostatectomy specimen (RPS) where number of foci categorized by zone defined as: PZ, peripheral zone; TZ, transition zone; CZ, central zone. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
PZPZ + TZPZ + TZ + CZPZ + CZTZ
Arm I (Finasteride)3549203
Arm II (Placebo)3850213

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Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Exhibiting Detectable Staining Within Finasteride Treatment Arm for Biomarker Subgroups

Molecular marker expression compared between tumor foci, characteristics of blood biomarkers using pretreatment and posttreatment values. VEGF denotes vascular epithelial growth factor, ERβ estrogen receptor beta, AR androgen receptor, SRD5A2, 3-oxo-5α-steroid 4-dehydrogenase 2, UBE2C, ubiquitin-conjugating enzyme E2C. P values are based on non-parametric Wilcoxon rank-sum test. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period

,
InterventionPercentage of tumor cell involvement (Median)
VEGF (N=37,48)ERβ (N=35,48)AR (N=35,48)Ki-67 (N=37,48)SRD5A2 (N=45,38)UBE2C (N=34,46)Caspase (N=38,47)
Within GG3, Finasteride Arm8015.075.21.11000.40.2
Within GG4, Finasteride Arm858.063.71.3950.30.06

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Characteristics of Blood Biomarkers: Testosterone (ng/dL) Percentage Change

Characteristics of blood biomarkers using pretreatment and posttreatment values. Blood tests used for measuring the amount of testosterone in the blood. (NCT00438464)
Timeframe: Baseline biopsy to prostatectomy following maximum 6 week treatment period

Interventionpercentage of change (Median)
Arm I (Finasteride)13
Arm II (Placebo)-4.6

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Cancer Foci

Diagnosis of a small focus of prostatic adenocarcinoma on a prostate needle biopsy from pathologist's identification of an architecturally abnormal focus of epithelial structures at rather low magnification. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
1 Focus2 Foci3 Foci4 Foci>/= 5 Foci
Arm I (Finasteride)1518281315
Arm II (Placebo)1120282015

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Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Exhibiting Detectable Staining Within Placebo Treatment Arm for Biomarker Subgroups (Mean)

Molecular marker expression compared between tumor foci, characteristics of blood biomarkers using pretreatment and posttreatment values. VEGF denotes vascular epithelial growth factor, ERβ estrogen receptor beta, AR androgen receptor, SRD5A2, 3-oxo-5α-steroid 4-dehydrogenase 2, UBE2C, ubiquitin-conjugating enzyme E2C. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period.

,
InterventionPercentage of tumor cell involvement (Mean)
VEGF (N=55,61)ERβ (N=55,62)AR (N=54,62)Ki-67 (N=54,62)SRD5A2 (N=47,69)UBE2C (N=55,62)Caspase (N=55,61)
GG3, Within Placebo Arm63.714.872.41.564.70.50.2
GG4, Within Placebo Arm59.716.768.61.764.90.50.06

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Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Within Placebo Treatment Arm for Biomarker Subgroups

Molecular marker expression compared between tumor foci, characteristics of blood biomarkers using pretreatment and posttreatment values. VEGF denotes vascular epithelial growth factor, ERβ estrogen receptor beta, AR androgen receptor, SRD5A2, 3-oxo-5α-steroid 4-dehydrogenase 2, UBE2C, ubiquitin-conjugating enzyme E2C. P values are based on non-parametric Wilcoxon rank-sum test. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period.

,
InterventionPercentage of tumor cell involvement (Median)
VEGF (N=55,61)ERβ (N=55,62)AR (N=54,62)Ki-67 (N=54,62)SRD5A2 (N=47,69)UBE2C (N=55,62)Caspase (N=55,61)
Within GG3, Placebo Arm906.678.31.3900.30.08
Within GG4, Placebo Arm709.575.91.4900.30.04

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Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 3 (GG3) Biomarker Subgroups at Prostatectomy

Molecular marker expression based on tissue microarray (TMA) derived from dominant tumor focus. Staining microarrays for high-throughput assessment of candidate gene expression and data modeling constructed with a tissue microarray apparatus and 0.6-mm biopsy cores, representative of tumor grades and scores (Gleason Grades 3 (GG3) and Gleason Grade 4 (GG4)). The percentage of tumor cells exhibiting detectable staining, scored as 0 to 10 where higher score designates more involvement, as applicable for: vascular epithelial growth factor (VEFG), estrogen receptor beta (ERβ), androgen receptor (AR), 3-oxo-5α-steroid 4-dehydrogenase 2 (SRD5A2), ubiquitin-conjugating enzyme E2C (UBE2C), and Cleaved Caspase 3 (Caspase). P values are based on non-parametric Wilcoxon rank-sum test. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period

,
InterventionPercentage tumor cell involvement (Median)
VEGF (N=37,55)ERβ (N=35, 55)AR (N=35, 54)Ki-67 (N=37,54)SRD5A2 (N=45,47)UBE2C (N=34,55)Caspase (N=38,55)
Finasteride Arm Within GG38015.075.21.11000.40.2
Placebo Arm Within GG3906.678.31.3900.30.08

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Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 3 (GG3) Biomarker Subgroups at Prostatectomy

Molecular marker expression compared between tumor foci using Biomarkers pretreatment and posttreatment values. Staining microarrays for high-throughput assessment of candidate gene expression and data modeling constructed with a tissue microarray apparatus and 0.6-mm biopsy cores, representative of tumor grades and scores (Gleason Grades 3 (GG3) and Gleason Grade 4 (GG4)). The percentage of tumor cells exhibiting detectable staining, scored as 0 to 10 where higher score designates more involvement, as applicable for: VEGF denotes vascular epithelial growth factor, ERβ estrogen receptor beta, AR androgen receptor, SRD5A2, 3-oxo-5α-steroid 4-dehydrogenase 2, UBE2C, ubiquitin-conjugating enzyme E2C. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period.

,
InterventionPercentage of tumor cell involvement (Mean)
VEGF (N=37,55)ERβ (N=35, 55)AR (N=35, 54)Ki-67 (N=37,54)SRD5A2 (N=45,47)UBE2C (N=34,55)Caspase (N=38,55)
Finasteride Arm Within GG363.918.169.81.672.90.50.4
Placebo Arm Within GG363.714.872.41.564.70.50.2

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Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 4 (GG4) Biomarker Subgroup at Prostatectomy

Biomarkers using pretreatment and posttreatment values. Staining microarrays for high-throughput assessment of candidate gene expression and data modeling constructed with a tissue microarray apparatus and 0.6-mm biopsy cores, representative of tumor grades and scores (Gleason Grades 3 (GG3) and Gleason Grade 4 (GG4)). The percentage of tumor cells exhibiting detectable staining, scored as 0 to 10 where higher score designates more involvement, as applicable for: VEGF denotes vascular epithelial growth factor, ERβ estrogen receptor beta, AR androgen receptor, SRD5A2, 3-oxo-5α-steroid 4-dehydrogenase 2, UBE2C, ubiquitin-conjugating enzyme E2C. P values are based on non-parametric Wilcoxon rank-sum test. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period

,
InterventionPercentage of tumor cell involvement (Median)
VEGF (N=48,61)ERβ (N=48,62)AR (N=48,62)Ki-67 (N=48,62)SRD5A2 (N=38,69)UBE2C (N=46,62)Caspase (N=47,61)
Finasteride Arm Within GG4858.063.711.3950.30.06
Placebo Arm Within GG4709.575.91.4900.30.04

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Comparison of Biomarkers Between Treatment Arms: Percentage Change of Tumor Cells Exhibiting Detectable Staining Within Gleason Grade 4 (GG4) Biomarker Subgroup at Prostatectomy

Molecular marker expression compared between tumor foci using biomarkers pretreatment and posttreatment values. Staining microarrays for high-throughput assessment of candidate gene expression and data modeling constructed with a tissue microarray apparatus and 0.6-mm biopsy cores, representative of tumor grades and scores (Gleason Grades 3 (GG3) and Gleason Grade 4 (GG4)). The percentage of tumor cells exhibiting detectable staining, scored as 0 to 10 where higher score designates more involvement, as applicable for: VEGF denotes vascular epithelial growth factor, ERβ estrogen receptor beta, AR androgen receptor, SRD5A2, 3-oxo-5α-steroid 4-dehydrogenase 2, UBE2C, ubiquitin-conjugating enzyme E2C. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period.

,
InterventionPercentage of tumor cell involvement (Mean)
VEGF (N=48,61)ERβ (N=48,62)AR (N=48,62)Ki-67 (N=48,62)SRD5A2 (N=38,69)UBE2C (N=46,62)Caspase (N=47,61)
Finasteride Arm Within GG463.615.064.31.871.80.50.1
Placebo Arm Within GG459.816.768.61.764.90.50.06

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Grade -- Specimen (Secondary)

Frequency of Grade 3, Grade 4 and Grade 5 tumors in two treatment groups: Participants will consist of men with adenocarcinoma of the prostate, clinical stage T1c or T2, with a Gleason score of 6 or 7 and a PSA level < 10 ng/mL, who are scheduled to undergo prostatectomy. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
Grade 3Grade 4Grade 5
Arm I (Finasteride)31534
Arm II (Placebo)24645

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Score

Frequency of Grade 3 and Grade 4 tumors in two treatment groups: Participants consist of men with adenocarcinoma of prostate, clinical stage T1c or T2, with Gleason score of 6 or 7 and PSA level < 10 ng/mL, who are scheduled to undergo prostatectomy. 2005 International Society of Urological Pathologists recommendations for Gleason scoring (GS) used to grade tumors based upon its microscopic appearance: a primary grade is assigned to most common tumor pattern, and a second grade to next most common tumor pattern. Gleason score (GS) is sum of the two Gleason grades, based on scale of 2-10 with lowest numbers indicating slow-growing tumor unlikely to spread and highest numbers indicating an aggressive tumor. Gleason grade = 1-5; Gleason score = 2-10; 5 and 10 indicate worst prognosis. American Joint Committee on Cancer (AJCC) staging describes extent of disease progression utilizing TNM scoring system: Tumor size, Lymph Nodes affected, Metastases. Higher stage cancers are more advanced. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
Gleason Score 6Gleason Score 7Gleason Score 8Gleason Score 9
Arm I (Finasteride)127123
Arm II (Placebo)107814

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Gleason Upgrade Between Biopsy and Prostatectomy

Change in Gleason Score from biopsy to prostatectomy where an upgrade refers to a higher Gleason Score signifying worsening of tumor. Gleason scoring (GS) to based on microscopic appearance using 2005 International Society of Urological Pathologists recommendation. (NCT00438464)
Timeframe: Baseline biopsy to prostatectomy following maximum 6 week treatment period

,
Interventionparticipants (Number)
NoYes
Arm I (Finasteride)6326
Arm II (Placebo)7024

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Lymph Node Status

Status of cancer spread to lymph nodes; PN0 Cancer that has not spread to the lymph nodes. Cancer that has not spread to the lymph nodes. The N category describes whether the cancer has spread into nearby lymph nodes. NX means the nearby lymph nodes cannot be evaluated. N0 means nearby lymph nodes do not contain cancer. Numbers after the N (such as N1, N2, and N3) describe the size, location, and/or the number of nearby lymph nodes affected by cancer. The higher the N number, the greater the cancer spread to nearby lymph nodes. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
PN0PN1pNX
Arm I (Finasteride)46241
Arm II (Placebo)43249

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Margin of Resection (MOR)

Edge or border of tissue removed in cancer surgery. The margin is described as negative or clean when the pathologist finds no cancer cells at the edge of the tissue, suggesting that all of the cancer has been removed. The margin is described as positive or involved when the pathologist finds cancer cells at the edge of the tissue, suggesting that all of the cancer has not been removed. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
PositiveNegativeEquivocal
Arm I (Finasteride)17675
Arm II (Placebo)16762

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Tumor Volume (Cubic Centimeter)

Characteristics of tumor considering total zone cancer volume, and cancer volume using zonal foci categorized as: PZ, peripheral zone; TZ, transition zone; CZ, central zone. (NCT00438464)
Timeframe: Baseline biopsy to prostatectomy following maximum 6 week treatment period

,
Interventioncubic centimeter (Median)
TotalPZ Cancer focus/fociTZ cancer focus/foci
Arm I (Finasteride)1.00.60.0
Arm II (Placebo)0.80.50.0

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Tumor, Node, Metastasis (TNM) Stage

American Joint Committee on Cancer (AJCC) system 6th edition (2002) describing amount and spread of cancer body, using TNM. T describes the size of the tumor and any spread of cancer into nearby tissue; N describes spread of cancer to nearby lymph nodes; and M describes metastasis (spread of cancer to other parts of the body). Numbers after the T (such as T1, T2, T3, and T4) describe tumor size and/or amount of spread into nearby structures. The higher the T number, the larger the tumor and/or the more it has grown into nearby tissues where T3a reflects tumor has spread through the capsule on one or both sides; and T3b reflects tumor has invaded one or both seminal vesicles. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
pT2pT3apT3b
Arm I (Finasteride)73115
Arm II (Placebo)74155

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Pathologic Characteristics of Radical Prostatectomy Specimens After Treatment: Zonal Origin -- Dominant Tumor Focus

Dominant tumor focus, distribution within zones of the prostate using radical prostatectomy specimen (RPS) where number of foci categorized by zone defined as: PZ, peripheral zone; TZ, transition zone; CZ, central zone. Dominant tumor focus is the largest, index lesion, single high risk focus of the prostate cancer. (NCT00438464)
Timeframe: Assessment following maximum 6 week treatment period and prostatectomy

,
Interventionparticipants (Number)
PZTZ
Arm I (Finasteride)6722
Arm II (Placebo)7321

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Comparison of Biomarkers Between Gleason Grades GG3 & GG4: Percentage of Tumor Cells Exhibiting Detectable Staining Within Finasteride Treatment Arm for Biomarker Subgroups (Mean)

Molecular marker expression compared between tumor foci, characteristics of blood biomarkers using pretreatment and posttreatment values. VEGF denotes vascular epithelial growth factor, ERβ estrogen receptor beta, AR androgen receptor, SRD5A2, 3-oxo-5α-steroid 4-dehydrogenase 2, UBE2C, ubiquitin-conjugating enzyme E2C. (NCT00438464)
Timeframe: At prostatectomy following maximum 6 week treatment period

,
InterventionPercentage of tumor cell involvement (Mean)
VEGF (N=37,48)ERβ (N=35,48)AR (N=35,48)Ki-67 (N=37,48)SRD5A2 (N=45,38)UBE2C (N=34,46)Caspase (N=38,47)
GG3, Within Finasteride Arm63.918.169.81.672.90.50.4
GG4, Within Finasteride Arm63.715.064.31.871.80.50.1

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Dietary Protein Intake

"Dietary protein intake will be assessed using a 3-day food log and subjects will be counseled to increase protein intake if needed using the guide Healthy Ways to Eat More Protein." (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventiongm/body weight (kg) (Mean)
protein intake baselineprotein intake 3 monthsprotein intake 6 monthsprotein intake 9 monthsprotein intake 12 months n = 1,1,2,5
Arm 10.970.870.741.151.18
Arm 21.060.941.271.200.74
Arm 30.991.491.051.261.39
Arm 41.001.120.930.821.05

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Life Satisfaction

Life Satisfaction: is a written test of psychological well-being that will be performed at baseline, after 3, 6, 9 and 12 months of treatment. This is a 20-point scale, with a possible range of scores from 0 to 20. A higher score represents greater life satisfaction. (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventionpoints (Mean)
Life Satisfaction A baselineLife Satisfaction A 3 monthsLife Satisfaction A 6 monthsLife Satisfaction A 9 monthsLife Satisfaction A 12 months
Arm 113.8312.6713.7014.7515.17
Arm 212.0812.1114.4413.4412.5
Arm 311.3512.2711.2011.5712.17
Arm 412.6914.1313.5413.1713.83

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Hematocrit

Hematocrit was assessed as a part of routine blood analysis at the indicated time points. (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Intervention% volume (Mean)
hematocrit baseline %change hematocrit 3 months %change hematocrit 6 months %change hematocrit 9 months %change hematocrit 12 months %
Arm 142.63.64.0444.0715.22
Arm 241.20.6110.5570.63-1.175
Arm 342.04.5934.3313.384.173
Arm 440.3-0.060.514-0.155-0.192

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Grip Strength kg

Grip strength in the dominant arm will be measured by using a dynamometer. Testing will be performed at baseline, after 3, 6, 9 and 12 months of treatment. (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventionkg (Mean)
grip strength baseline kgchange grip strength 3 month kgchange grip strength 6 month kgchange grip strength 9 month kgchange grip strength 12 month kg
Testosterone Finasteride18.20.4851.001.3311.174
Testosterone Vehicle17.01.662.021.5581.909
Vehicle Finasteride16.9-0.0450.8121.251.477
Vehicle Placebo17.4720.212-0.0350.1520.72

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Geriatric Depression Scale

"Geriatric Depression Scale (GDS): This 15-item, yes/no questionnaire will be administered at baseline, after 3, 6, 9 and 12 months of treatment.~The minimum score is 0 = no depressive symptoms The maximum score is 15 = a very high level of depressive symptoms" (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventionunits on a scale (Mean)
depression baselinedepression 3 monthsdepression 6 monthsdepression 9 monthsdepression 12 months
Testosterone Finasteride4.933.235.03.693.73
Testosterone Vehicle2.381.801.50.883.33
Vehicle Finasteride3.082.902.221.892.88
Vehicle Placebo2.131.671.622.921.83

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Benton Judgment of Line Orientation Test

"Benton Judgment of Line Orientation Test is a standardized test with 30 items that is specific for visual spatial cognition. Tests will be administered at baseline, after 3, 6, 9 and 12 months of treatment.~The minimum score is 0, indicating low visual spatial cognition. The maximum score is 30, indicating high visual spatial cognition" (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventionunits on a scale (Mean)
Benton baselineBenton 3 monthsBenton 6 monthsBenton 9 monthsBenton 12 months
Arm 124.5425.0025.9025.3825.67
Arm 224.3925.4025.1123.8925.5
Arm 325.8825.0726.025.7926.17
Arm 424.6925.6725.0824.9224.08

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30 Minute Recall Portion of Rey Osterrieth Complex Figure (ROCF) Test

"Rey Osterrieth Complex Figure (ROCF) test is a widely used standardized neuropsychological test for assessing visuospatial constructional functions, visuographic memory, and some aspects of planning.~The drawing is scored by a blinded neuropsychologist on a scale of 0 to 30 with 30 representing a perfect drawing." (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventionunits on a scale (Mean)
Rey baselineRey 3 monthRey 6 monthRey 9 monthRey 12 month
Arm 112.4216.6815.7615.2516.86
Arm 213.5412.8516.1715.1715
Arm 312.8216.2717.3818.0819.27
Arm 412.812.51415.5516.45

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1 Repetition Maximum (1-RM) Strength Testing

1-RM strength testing for 5 exercises will be performed using dynamic resistance exercise machines. Testing will be performed before treatment (baseline), at 3, 6, 9 and 12 months after treatment. (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventionkg (Mean)
leg press baseline Kgleg press 3-months change kgleg press 6-months change kgleg press 9-months change kgleg press 12-months change kg
Arm 1129.19.19210.22714.41614.773
Arm 2109.4-1.34-1.136-5.550
Arm 3137.29.67913.77810.4912.5
Arm 4118.8-2.442.7272.021.515

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Lumbar Spine L2-L4 Bone Mineral Density

Dual x-ray absorptiometry (DXA): We will assess bone mineral density (BMD) and body composition using a fan-bean densitometer (Lunar Prodigy, General Electric Medical Systems). (NCT00475501)
Timeframe: baseline, 12 months

,,,
Interventiongm/cc (Mean)
L2-L4 spine BMD baseline gm/ccchange L2-L4 spine BMD 12 month gm/cc
Arm 11.030.049
Arm 21.020.002
Arm 30.990.053
Arm 41.07-0.020

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Trail-Making Test, Part A

Trail-Making Test, Part A: is a standardized test of cognitive function which specifically assesses working memory, visual processing, visual spatial skills, selective and divided attention, and psychomotor coordination. the test is scored as seconds required to successful completion of the task with a lower score representing better performance. The mean score on test is 30.75 second with a standard deviation of 16.27. (NCT00475501)
Timeframe: baseline, 3 months, 6 months, 9 months, 12 months

,,,
Interventionsec (Mean)
Trails A baselineTrails A 3 monthsTrails A 6 monthsTrails A 9 monthsTrails A 12 months
Arm 137.5938.532.931.029.17
Arm 246.4242.139.038.5640.0
Arm 336.6533.5331.229.0732.5
Arm 444.044.3336.9243.1743.75

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Transrectal Ultrasound Sizing of Prostate

Transrectal ultrasound sizing of prostate will be performed using the B&K Diagnostic System 3535, with 7 mega hertz transrectal probe at baseline and after 6 and 12 months of treatment. (NCT00475501)
Timeframe: baseline, 6 month, 12 months

,,,
Interventioncc (Mean)
postate volume baseline ccchange prostate volume 6 months ccchange prostate volume 12 months cc
Arm 126.47.62611.42
Arm 229.7-1.984-4.93
Arm 337.1-3.927-1.72
Arm 436.9-1.474-2.891

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Area Under the Curve-Serum T

(NCT00663793)
Timeframe: 14 days

,
Interventionnmol*h/L (Mean)
external matrix 'immediate' releaseexternal matrix 'fast' releaseexternal matrix 'slow' release
Testosterone Only143144162
Testosterone Plus Finasteride198384237

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Area Under the Curve-E2

(NCT00663793)
Timeframe: 14 Days

,
Interventionnmol*h/L (Mean)
external matrix 'immediate' releaseexternal matrix 'fast' releaseexternal matrix 'slow' release
Testosterone Only181219611944
Testosterone Plus Finasteride224120023129

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Area Under the Curve-serum DHT

(NCT00663793)
Timeframe: 14-days

,
Interventionnmol*h/L (Mean)
external matrix 'immediate' releaseexternal matrix 'fast' releaseexternal matrix 'slow' release
Testosterone Only364239
Testosterone Plus Finasteride232626

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Effects of Selenium and Finasteride and Their Combination on Apoptosis Induction

Compare cleaved caspase 3 values with Finasteride Placebo + Selenium Placebo group (Arm C). The Wilcoxon Rank Sum Test was used to test the difference of cleaved caspase 3 values of Arm A, Arm B, Arm D with Arm C. (NCT00736645)
Timeframe: 1 year

Interventionpercentage of apoptotic cells (Median)
Arm A: Finasteride + Selenium Placebo0.1
Arm B: Finasteride + Selenium0
Arm C: Finasteride Placebo + Selenium Placebo0
Arm D: Finasteride Placebo + Selenium0

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Effects of Selenium and Finasteride and Their Combination on PSA Level

Compare PSA levels with Finasteride Placebo + Selenium Placebo group (Arm C). The Wilcoxon Rank Sum Test was used to test the difference of PSA levels of Arm A, Arm B, Arm D with Arm C. (NCT00736645)
Timeframe: 1 year

Interventionng/mL (Median)
Arm A: Finasteride + Selenium Placebo1.9
Arm B: Finasteride + Selenium1.9
Arm C: Finasteride Placebo + Selenium Placebo2.0
Arm D: Finasteride Placebo + Selenium2.1

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AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)

Bioequivalence based on AUC0-t (NCT00835666)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Finasteride247.327
Proscar®250.822

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AUCinf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)

Bioequivalence based on AUCinf (NCT00835666)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Finasteride252.848
Proscar®256.783

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Cmax - Maximum Observed Concentration

Bioequivalence based on Cmax (NCT00835666)
Timeframe: Blood samples collected over 36 hour period

Interventionng/mL (Mean)
Finasteride35.550
Proscar®35.393

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AUC0-t - Area Under the Concentration-time Curve From Time Zero to Time of Last Non-zero Concentration (Per Participant)

Bioequivalence based on AUC0-t (NCT00835796)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Finasteride266.412
Proscar®271.183

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AUCinf - Area Under the Concentration-time Curve From Time Zero to Infinity (Extrapolated)

Bioequivalence based on AUCinf (NCT00835796)
Timeframe: Blood samples collected over 36 hour period

Interventionng*h/mL (Mean)
Finasteride274.802
Proscar®280.371

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Cmax - Maximum Observed Concentration

Bioequivalence based on Cmax (NCT00835796)
Timeframe: Blood samples collected over 36 hour period

Interventionng/mL (Mean)
Finasteride33.037
Proscar®32.242

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Change in Serum Dihydrotestosterone (DHT) Concentration at Month 3 Compared to Baseline

The concentration of dihydrotestosterone (DHT) in blood serum was assessed from each participant at baseline and at Month 3. The mean change from baseline to Month 3 is reported here in picograms of DHT per milliliter of serum. (NCT00837252)
Timeframe: 3 Months

Interventionpg/mL (Mean)
Finasteride-246

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Change in Visual Acuity at Month 6 Compared to Baseline

Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. This acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters the Snellen measurement is 20/20. (NCT00837252)
Timeframe: 6 months

InterventionETDRS letters (Mean)
Finasteride-3

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Change in Visual Acuity at Month 3 Compared to Baseline.

Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. This acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters the Snellen measurement is 20/20. (NCT00837252)
Timeframe: 3 months

InterventionETDRS letters (Mean)
Finasteride0

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Change in Urinary Cortisol Level at Month 6 Compared to Baseline

The amount of cortisol found in urine was assessed from each participant at baseline and at Month 6. The mean change from baseline to Month 6 is reported here in micrograms. (NCT00837252)
Timeframe: 6 Months

Interventionµg (Mean)
Finasteride-2

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Change in Center-Subfield Macular Thickness at Month 6 Compared to Baseline

Central-subfield macular thickness was assessed by spectral-domain optical coherence tomography (Cirrus HD-OCT; Carl Zeiss Meditec, Dublin, CA), a non-invasive imaging technique that uses long-wavelength light to capture micrometer-resolution cross-sectional images from biological tissue. (NCT00837252)
Timeframe: 6 months

Interventionµm (Mean)
Finasteride-69

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Change in Subretinal Fluid Volume at Month 6 Compared to Baseline

"Subretinal fluid volume was calculated after manually outlining the inner and outer borders of the subretinal fluid packet in the optical coherence tomography (OCT) images using the Edit Segmentation function of the Cirrus HD-OCT software. In cases where a pigment epithelial detachment was present, the volume of the pigment epithelial detachment was included in the calculation of subretinal fluid volume." (NCT00837252)
Timeframe: 6 Months

InterventionµL (Mean)
Finasteride-0.53

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Change in Center-Subfield Macular Thickness at Month 3 Compared to Baseline

Central-subfield macular thickness was assessed by spectral-domain optical coherence tomography (Cirrus HD-OCT; Carl Zeiss Meditec, Dublin, CA), a non-invasive imaging technique that uses long-wavelength light to capture micrometer-resolution cross-sectional images from biological tissue. (NCT00837252)
Timeframe: 3 months

Interventionµm (Mean)
Finasteride-86

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Change in Subretinal Fluid Volume at Month 3 Compared to Baseline

"Subretinal fluid volume was calculated after manually outlining the inner and outer borders of the subretinal fluid packet in the optical coherence tomography (OCT) images using the Edit Segmentation function of the Cirrus HD-OCT software. In cases where a pigment epithelial detachment was present, the volume of the pigment epithelial detachment was included in the calculation of subretinal fluid volume." (NCT00837252)
Timeframe: 3 Months

InterventionµL (Mean)
Finasteride-0.58

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Change in Serum Testosterone Level at Month 6 Compared to Baseline

The concentration of testosterone in blood serum was assessed from each participant at baseline and at Month 6. The mean change from baseline to Month 6 is reported here in nanograms of testosterone per decaliter of serum. (NCT00837252)
Timeframe: 6 Months

Interventionng/dL (Mean)
Finasteride-0.4

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Change in Serum Testosterone Level at Month 3 Compared to Baseline

The concentration of testosterone in blood serum was assessed from each participant at baseline and at Month 3. The mean change from baseline to Month 3 is reported here in nanograms of testosterone per decaliter of serum. (NCT00837252)
Timeframe: 3 Months

Interventionng/dL (Mean)
Finasteride0.38

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Change in Serum Dihydrotestosterone (DHT) Concentration at Month 6 Compared to Baseline

The concentration of dihydrotestosterone (DHT) in blood serum was assessed from each participant at baseline and at Month 6. The mean change from baseline to Month 6 is reported here in picograms of DHT per milliliter of serum. (NCT00837252)
Timeframe: 6 Months

Interventionpg/mL (Mean)
Finasteride-296

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Change in Urinary Cortisol Level at Month 3 Compared to Baseline

The amount of cortisol found in urine was assessed from each participant at baseline and at Month 3. The mean change from baseline to Month 3 is reported here in micrograms. (NCT00837252)
Timeframe: 3 Months

Interventionµg (Mean)
Finasteride3

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Maximum Testosterone Concentration

Area under the curve of serum testosterone Pharmacokinetic measures time-weighted mean concentration calculated as area under the concentration curve (AUC) divided by time from initiation of dosing for the morning dose and corrected for differences in baseline hormone concentration. (NCT00842751)
Timeframe: 0,1,2,4,8,and 12-hour post dose

Interventionng*hr/dL (Geometric Mean)
Acyline +Testosterone Undecanoate + Placebo471
Acyline +Testosterone Undecanoate + 0.5mg Finasteride444
Acyline +Testosterone Undecanoate + 1mg Finasteride543

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Serum Estradiol Concentration

Area under the curve of serum estradiol (NCT00842751)
Timeframe: 0,1,2,4,8,and 12-hour post dose

Interventionng*hr/dL (Geometric Mean)
Acyline +Testosterone Undecanoate + Placebo7.9
Acyline + Testosterone Undecanoate + 0.5mg Finasteride6.5
Acyline +Testosterone Undecanoate + 1mg Finasteride7.2

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Serum Dihydrotestosterone Concentration

Area under the curve of serum dihydrotestosterone (NCT00842751)
Timeframe: 0,1,2,4,8,and 12-hour post dose

Interventionng*hr/dL (Geometric Mean)
Acyline +Testosterone Undecanoate + Placebo154
Acyline + Testosterone Undecanoate + 0.5mg Finasteride118
Acyline + Testosterone Undecanoate + 1mg Finasteride125

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Change in International Index of Erectile Function (IIEF) - Intercourse Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks

Self-reported intercourse satisfaction over the past 4 weeks. IIEF-intercourse satisfaction is the sum of Questions 6, 7 and 8 of the IIEF. Scores range from 0 (low/no satisfaction) to 5 (high satisfaction) for each question, with the total possible score for the 3 questions of 0 to 15. Higher total scores indicate higher satisfaction. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.460.08-0.26
Tadalafil1.361.681.72

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Change in International Index of Erectile Function (IIEF) - Overall Satisfaction Domain Scores From Baseline to 4, 12, and 26 Weeks

Self-reported overall satisfaction over the past 4 weeks. IIEF-Overall Satisfaction is the sum of Questions 13 and 14 of IIEF questionnaire. Scores range from 1 (low/no satisfaction) to 5 (high satisfaction) for each question, with the total possible score for the 2 questions ranging from 2 to 10. Higher total scores indicate higher satisfaction. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.100.310.40
Tadalafil0.911.381.61

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Change in International Index of Erectile Function (IIEF) - Sexual Desire Domain Scores From Baseline to 4, 12, and 26 Weeks

Sexual desire domain scores is the sum of Questions 11 and 12 from the IIEF questionnaire. Scores range from 1 (low/no desire) to 5 (high desire) for each question, with the total possible score for the 2 questions ranging from 2 to 10. Higher total scores indicate higher desire. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.47-0.23-0.05
Tadalafil0.460.560.71

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Change in International Index of Erectile Function (IIEF) Question 3 and 4 Scores From Baseline to 4, 12, and 26 Weeks

IIEF Question 3 asks how often a participant was able to penetrate his partner over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). IIEF Question 4 asks whether/how often a participant was able to maintain an erection after penetration over the past 4 weeks. Scores range from 0 (did not attempt intercourse) to 5 (almost always or always). Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
Question 3 - 4 weeksQuestion 3 - 12 weeksQuestion 3 - 26 weeksQuestion 4 - 4 weeksQuestion 4 - 12 weeksQuestion 4 - 26 weeks
Placebo-0.320.04-0.07-0.210.130.06
Tadalafil0.420.720.680.490.740.68

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Change in International Prostate Symptom Score (IPSS) Quality of Life Index From Baseline to 4, 12, and 26 Weeks

"IPSS Quality of Life Index assesses participant response to the following question: If you were to spend the rest of your life with your urinary condition just the way it is now, how would you feel about that? Response options are Delighted (0); Pleased (1); Mostly satisfied (2); Mixed-about equally satisfied and dissatisfied (3); Mostly dissatisfied (4); Unhappy (5); Terrible (6), with a total range of 0-6. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction." (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.32-0.76-0.92
Tadalafil-0.63-0.95-1.10

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Change in International Prostate Symptom Score (IPSS) Subscores Index From Baseline to 4, 12, and 26 Weeks

IPSS storage (irritative) subscore is the sum of Questions 2, 4 and 7 of the 7-component IPSS questionnaire. Scores range from 0 (no irritative symptoms) to 5 (frequent irritative symptoms), with total subscore of the 3 questions for irritative subscore range from 0 to 15. IPSS voiding (obstructive) subscore is the sum of Questions 1, 3, 5 and 6 of the IPSS questionnaire. Scores range from 0 (no obstructive symptoms) to 5 (frequent obstructive symptoms), with total subscore of the 4 questions of the obstructive score range from 0 to 20. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
IPSS storage (irritative) subscore - 4 weeksIPSS storage (irritative) subscore - 12 weeksIPSS storage (irritative) subscore - 26 weeksIPSS voiding (obstructive) subscore - 4 weeksIPSS voiding (obstructive) subscore - 12 weeksIPSS voiding (obstructive) subscore - 26 weeks
Placebo-0.76-1.34-1.66-1.47-2.37-2.77
Tadalafil-1.27-1.74-2.00-2.65-3.41-3.50

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Change in Total International Prostate Symptom Score (IPSS) From Baseline to 4 and 26 Weeks

The International Prostate Symptom Score (IPSS) is a rating scale for severity of lower urinary tract symptoms (LUTS). The IPSS has a 7-component questionnaire. Each question is scored on a scale from 0 (none/no symptoms) to 5 (frequent symptoms), for a total score range of 0 to 35. Higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks26 weeks
Placebo-2.29-4.47
Tadalafil-3.95-5.51

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Clinician Global Impression of Improvement (CGI-I) at 26 Weeks

Clinician Global Impression of Improvement (CGI-I) measures clinician's perception of participant improvement at the time of assessment compared with the start of treatment. Number of participants is reported by the categorized score ranging from 1 (very much better) to 7 (very much worse). (NCT01139762)
Timeframe: 26 weeks

,
Interventionparticipants (Number)
1 = Very much improved2 = Much improved3 = Minimally improved4 = No change5 = Minimally worse6 = Much worse7 = Very much worse
Placebo2297106481061
Tadalafil231299847550

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Patient Global Impression of Improvement (PGI-I) at 26 Weeks

Patient Global Impression of Improvement (PGI-I) measures the participant's perception of improvement at the time of assessment compared with the start of treatment. Number of participants is reported by the categorized score ranging from 1 (very much better) to 7 (very much worse). (NCT01139762)
Timeframe: 26 weeks

,
Interventionparticipants (Number)
1 = Very much better2 = Much better3 = Little better4 = No change5 = A little worse6 = Much worse7 = Very much worse
Placebo298211252571
Tadalafil21124102491021

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Change in International Index of Erectile Function (IIEF) - Orgasmic Function Domain Scores From Baseline to 4, 12, and 26 Weeks

Orgasmic Function domain scores is the sum of Questions 9 and 10 from the IIEF questionnaire. Scores range from 0 (low/no orgasm) to 5 (high orgasm) for each question, with the total possible score for the 2 questions ranging from 0 to 10. Higher total scores indicate higher orgasm. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-0.630.18-0.18
Tadalafil0.901.080.89

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Change in Post Void Residual (PVR) Volume From Baseline to 26 Weeks

Postvoid Residual Volume (PVR) is determined using a portable, calibrated ultrasound device. It consists of the average of a minimum of 3 scans where the residual bladder volume was calculated by averaging the most accurate of the 3 imaging attempts. (NCT01139762)
Timeframe: Baseline, 26 weeks

Interventionmilliliters (mL) (Mean)
Tadalafil-24.8
Placebo-23.1

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Change in Total International Prostate Symptom Score (IPSS) From Baseline to 12 Weeks

The International Prostate Symptom Score (IPSS) is a rating scale for severity of lower urinary tract symptoms (LUTS). The IPSS has a 7-component questionnaire. Each question is scored on a scale from 0 (none/no symptoms) to 5 (frequent symptoms), for a total score range of 0 to 35. Higher numerical scores from the IPSS questionnaire represent greater severity of symptoms. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline total IPSS, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 12 weeks

Interventionunits on a scale (Least Squares Mean)
Tadalafil-5.18
Placebo-3.76

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Treatment Satisfaction Scale - Benign Prostatic Hyperplasia (TSS-BPH) at 26 Weeks

The TSS-BPH was a validated participant-rated instrument that measured participant satisfaction with treatment based on a 13-item questionnaire. It consists of 10 items on a Likert-like scale with scores ranging from 1 (higher satisfaction) to 5 (lower satisfaction), 1 item with score ranging from 0 (higher satisfaction) to 5 (lower satisfaction), and 2 yes/no questions. The mean score for each participant ranges from 0.9 (higher satisfaction) to 5.0 (lower satisfaction). Data presented are the average of mean scores for each treatment group. (NCT01139762)
Timeframe: 26 weeks

Interventionunits on a scale (Mean)
Tadalafil2.0
Placebo2.1

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Change in International Index of Erectile Function (IIEF) - Erectile Function Domain Scores From Baseline to 4, 12, and 26 Weeks

Self-reported erectile function over the past 4 weeks. IIEF- EF is the sum of Questions 1-5 and 15 of the IIEF. Questions 1-5 are scored 0 (low/no erectile function) to 5 (high erectile function) and Question 15 is scored 1 (very low confidence) to 5 (very high confidence), for a total score ranging from 1 to 30. Higher scores represent better erectile function. Least Squares (LS) Mean values were obtained from a mixed model repeated measures (MMRM) analysis. Model includes treatment, region, visit, baseline IIEF, and visit-by-treatment interaction. (NCT01139762)
Timeframe: Baseline, 4 weeks, 12 weeks, 26 weeks

,
Interventionunits on a scale (Least Squares Mean)
4 weeks12 weeks26 weeks
Placebo-1.140.63-0.02
Tadalafil3.714.714.71

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Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at One Year Compared to Baseline

Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. Acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters, the equivalent Snellen measurement is 20/20. (NCT01227993)
Timeframe: Baseline and 1 year

InterventionETDRS letters (Mean)
Finasteride0

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Change in Serum Testosterone Levels at Two Years Compared to Baseline

The concentration of testosterone in blood serum was assessed from each participant at baseline and at two years. The mean change from baseline to two years is reported here in nanograms of testosterone per decaliter of serum. (NCT01227993)
Timeframe: Baseline and 2 years

Interventionng/dL (Mean)
Finasteride-28.67

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Change in Best-corrected Visual Acuity (BCVA) in the Fellow Eye at Two Years Compared to Baseline

Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. Acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters, the equivalent Snellen measurement is 20/20. (NCT01227993)
Timeframe: Baseline and 2 years

InterventionETDRS letters (Mean)
Finasteride-1.00

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Change in Best-corrected Visual Acuity (BCVA) in the Fellow Eye at One Year Compared to Baseline

Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. Acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters, the equivalent Snellen measurement is 20/20. (NCT01227993)
Timeframe: Baseline and 1 year

InterventionETDRS letters (Mean)
Finasteride0.33

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Change in 24-hour Urine Cortisol Levels at Two Years Compared to Baseline

The amount of cortisol found in urine was assessed from each participant at baseline and at two years. The mean change from baseline to two years is reported here in micrograms. (NCT01227993)
Timeframe: Baseline and 2 years

Interventionµg (Mean)
Finasteride2.75

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Change in Best-corrected Visual Acuity (BCVA) in the Study Eye at Two Years Compared to Baseline

Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. Acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters, the equivalent Snellen measurement is 20/20. (NCT01227993)
Timeframe: Baseline and 2 years

InterventionETDRS letters (Mean)
Finasteride0

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Change in Serum DHT Levels at Two Years Compared to Baseline

The concentration of dihydrotestosterone (DHT) in blood serum was assessed from each participant at baseline and at two years. The mean change from baseline to two years is reported here in picograms of DHT per milliliter of serum. (NCT01227993)
Timeframe: Baseline and 2 years

Interventionpg/mL (Mean)
Finasteride10.67

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Global Assessment of Improvement From Baseline to Week 24 Assessed for Vertex and Frontal Views Separately

A central panel of 3 dermatologists independently assessed change in hair growth from Baseline to Week 24 using a 7-point scale: greatly decreased (-3), moderately decreased (-2), slightly decreased (-1), no change (0), slightly increased (1), moderately increased (2), and greatly increased (3). The median score, across the 3 panel members, is summarized. This assessment was performed by comparing the global photographs obtained at Baseline with those subsequently obtained at Week 24. This assessment was made separately based on the global photography of the vertex and frontal views. (NCT01231607)
Timeframe: Baseline and Week 24

,,,,
Interventionscores on a scale (Least Squares Mean)
Vertex view, n=172, 174, 176, 167, 164Frontal/Superior view, n=171, 174, 176, 167, 165
Dutasteride 0.02 mg-0.09-0.10
Dutasteride 0.1 mg0.420.36
Dutasteride 0.5 mg0.630.58
Finasteride 1 mg0.490.34
Placebo-0.15-0.14

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Change From Baseline in Investigator Photographic Assessment Questionnaire (IPAQ) Scores Assessed at Week 24 for Vertex and Frontal Views Separately

The IPAQ was completed by the Investigator or designee by comparing the global photographs obtained at Baseline with those obtained at Week 12. This assessment was made separately based on the global photography of the vertex and frontal views. The change from Baseline in hair growth was assessed using the following 7-point scale: -3 = greatly decreased, -2 = moderately decreased, -1 = slightly decreased, 0 = no change, +1 = slightly increased, +2 = moderately increased, +3 = greatly increased. (NCT01231607)
Timeframe: Baseline and Week 24

,,,,
Interventionscores on a scale (Least Squares Mean)
Vertex viewFrontal view
Dutasteride 0.02 mg0.370.28
Dutasteride 0.1 mg1.030.78
Dutasteride 0.5 mg1.301.11
Finasteride 1 mg1.070.88
Placebo0.360.30

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Change From Baseline in Investigator Photographic Assessment Questionnaire (IPAQ) Scores Assessed at Week 12 for Vertex and Frontal Views Separately

The IPAQ was completed by the Investigator or designee by comparing the global photographs obtained at Baseline with those obtained at Week 12. This assessment was made separately based on the global photography of the vertex and frontal views. The change from Baseline in hair growth was assessed using the following 7-point scale: -3 = greatly decreased, -2 = moderately decreased, -1 = slightly decreased, 0 = no change, +1 = slightly increased, +2 = moderately increased, +3 = greatly increased. (NCT01231607)
Timeframe: Baseline and Week 12

,,,,
Interventionscores on a scale (Least Squares Mean)
Vertex viewFrontal view
Dutasteride 0.02 mg0.350.33
Dutasteride 0.1 mg0.620.54
Dutasteride 0.5 mg0.780.55
Finasteride 1 mg0.700.55
Placebo0.480.30

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Change From Baseline in Hair Growth Index (HGI) Scores at Weeks 12 and 24

"Participant-perceived change in HG was assessed by 3 questions (each scored on a 7-point scale) on a health outcome questionnaire: Since the start of treatment, when I look at my thinning area, I can see..., Since the start of treatment, my hair now covers…, and Since the start of treatment, the appearance (thickness/quality/amount) of the thinning area on my head is… -3, Much less; -2, Moderately less; -1, Slightly less; 0, The same amount; 1, Slightly more; 2, Moderately more; 3, Much more scalp. The scores for the 3 questions were summed to obtain the HGI total score (-9 to 9)." (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24

,,,,
Interventionscores on a scale (Least Squares Mean)
Week 12, n=171, 171, 172, 166, 160Week 24, n=172, 174, 177, 167, 165
Dutasteride 0.02 mg0.91.1
Dutasteride 0.1 mg1.72.8
Dutasteride 0.5 mg2.03.2
Finasteride 1 mg1.72.5
Placebo1.21.1

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Change From Baseline in Target Area Hair Count Within a 2.54 cm (1 Inch) Diameter Circle at the Vertex at Week 12 as Assessed by MT

The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 12 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 12

InterventionHair count (Least Squares Mean)
Placebo-4.0
Dutasteride 0.02 mg22.9
Dutasteride 0.1 mg59.6
Dutasteride 0.5 mg82.3
Finasteride 1 mg50.9

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Change From Baseline in Target Area Hair Count Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex, as Assessed by MT at Week 12

The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 12 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 12

InterventionHair count (Least Squares Mean)
Placebo-0.4
Dutasteride 0.02 mg5.1
Dutasteride 0.1 mg12.8
Dutasteride 0.5 mg17.1
Finasteride 1 mg10.8

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Change From Baseline in Target Area Hair Count Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex at Week 24, as Assessed by MT

The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 24 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 24

InterventionHair count (Least Squares Mean)
Placebo-0.3
Dutasteride 0.02 mg4.2
Dutasteride 0.1 mg12.4
Dutasteride 0.5 mg18.1
Finasteride 1 mg12.1

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Change From Baseline (BL) in Target Area Hair Count (HC) Within a 2.54 Centimeter (cm) (1 Inch) Diameter Circle at the Vertex at Week 24, as Assessed by Macrophotographic Technique (MT)

The primary target area HC was based on the nonvellus hair (>=30 micrometers [μm] in width; thick and noticeable hair) count within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 24 value minus the BL value. (NCT01231607)
Timeframe: Baseline and Week 24

InterventionHair count (Least Squares Mean)
Placebo-4.9
Dutasteride 0.02 mg17.1
Dutasteride 0.1 mg63.0
Dutasteride 0.5 mg89.6
Finasteride 1 mg56.5

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Change From Baseline in Total Hair Growth Satisfaction Scale (HGSS) Scores at Weeks 12 and 24

Participant satisfaction with hair appearance/growth was assessed by 5 questions (each scored on a 7-point scale: How satisfied do you feel about: [1] The overall appearance of your hair; [2] The appearance of the thinning area[s] [TAs] on your head; [3] The amount of scalp that can be seen in the TAs; [4] The amount of hair in the TAs; [5] The growth of hair in the TAs): -3, Very dissatisfied (DS); -2, DS; -1, Somewhat DS; 0, Neutral (neither satisfied nor DS); 1, Somewhat satisfied (SA); 2, SA; 3, Very SA. The scores for the 5 questions were summed to obtain the HGSS total score (-15 to 15). (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24

,,,,
Interventionscores on a scale (Least Squares Mean)
Week 12, n=171, 174, 173, 170, 160Week 24, n=172, 176, 177, 170, 165
Dutasteride 0.02 mg7.98.3
Dutasteride 0.1 mg9.811.5
Dutasteride 0.5 mg8.412.5
Finasteride 1 mg8.510.8
Placebo8.59.3

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Number of Participants With the Indicated Change From Baseline (BL) in the Stage (S) of Androgenic Alopecia (AGA) According to the Norwood-Hamilton Scale at Week 12 (W12)

"The investigator/designee assessed the stage (Stage I to Stage VII) of AGA (i.e., male pattern baldness [MPB]) by utilizing the Norwood-Hamilton scale, used to measure the progression of MPB. Stage VII indicates worse balding than stage I. Assessment was made by direct visual examination (aided by pictures) of the participant at Baseline and Week 12 (W12). v, vertex; most of the hair loss (commonly seen with advancing age) is on the vertex. a, type a variant; major features are (1) the entire anterior hairline border recedes in unison; (2) there is no simultaneous balding of the vertex." (NCT01231607)
Timeframe: Baseline and Week 12

,,,,
Interventionparticipants (Number)
BL S IIIv to W12 S II, n=79, 70, 69, 72, 73BL S IIIv to W12 S IIa, n=79, 70, 69, 72, 73BL S IIIv to W12 S III, n=79, 70, 69, 72, 73BL S IIIv to W12 S IIIa, n=79, 70, 69, 72, 73BL S IIIv to W12 S IIIv, n=79, 70, 69, 72, 73BL S IIIv to W12 S IV, n=79, 70, 69, 72, 73BL S IIIv to W12 S IVa, n=79, 70, 69, 72, 73BL S IIIv to W12 S V, n=79, 70, 69, 72, 73BL S IIIv to W12 S Va, n=79, 70, 69, 72, 73BL S IIIv to W12 S VI, n=79, 70, 69, 72, 73BL S IV to W12 S II, n=52, 59, 58, 56, 53BL S IV to W12 S IIa, n=52, 59, 58, 56, 53BL S IV to W12 S III, n=52, 59, 58, 56, 53BL S IV to W12 S IIIa, n=52, 59, 58, 56, 53BL S IV to W12 S IIIv, n=52, 59, 58, 56, 53BL S IV to W12 S IV, n=52, 59, 58, 56, 53BL S IV to W12 S IVa, n=52, 59, 58, 56, 53BL S IV to W12 S V, n=52, 59, 58, 56, 53BL S IV to W12 S Va, n=52, 59, 58, 56, 53BL S IV to W12 S VI, n=52, 59, 58, 56, 53BL S V to W12 S II, n=41, 46, 46, 41, 35BL S V to W12 S IIa, n=41, 46, 46, 41, 35BL S V to W12 S III, n=41, 46, 46, 41, 35BL S V to W12 S IIIa, n=41, 46, 46, 41, 35BL S V to W12 S IIIv, n=41, 46, 46, 41, 35BL S V to W12 S IV, n=41, 46, 46, 41, 35BL S V to W12 S IVa, n=41, 46, 46, 41, 35BL S V to W12 S V, n=41, 46, 46, 41, 35BL S V to W12 S Va, n=41, 46, 46, 41, 35BL S V to W12 S VI, n=41, 46, 46, 41, 35
Dutasteride 0.02 mg108059101000040350020000101404000
Dutasteride 0.1 mg0011155200000010844140000003503800
Dutasteride 0.5 mg1010059200000040547000000101503301
Finasteride 1 mg0011062000000010545020000000203300
Placebo104071201000020245120000200403500

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Change From Baseline in Target Area Hair Width Within a 2.54 cm (1 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT

The target area hair width was the sum of all nonvellus hairs (>=30 µm in width; thick and noticeable hair) within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). For the MT, hair was clipped before each photograph. A cosmetic ink dot was placed by tattoo at Baseline so that the same area could be identified at Baseline and post-Baseline. If the ink dot faded, it was re-done in exactly the same location to ensure it was visible for subsequent photographs. Change from Baseline was calculated as the Week 12 or Week 24 value minus the Baseline value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24

,,,,
Interventionmillimeters (Least Squares Mean)
Week 12, n=147, 144, 151, 145, 131Week 24, n=148, 155, 158, 150, 141
Dutasteride 0.02 mg0.3-0.0
Dutasteride 0.1 mg3.13.9
Dutasteride 0.5 mg4.75.8
Finasteride 1 mg3.24.0
Placebo-0.7-0.9

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Number of Participants With the Indicated Change From Baseline (BL) in the Stage (S) of Androgenic Alopecia (AGA) According to the Norwood-Hamilton Scale at Week 24

"The investigator/designee assessed the stage (Stage I to Stage VII) of AGA (i.e., male pattern baldness [MPB]) by utilizing the Norwood-Hamilton scale, used to measure the progression of MPB. Stage VII indicates worse balding than stage I. Assessment was made by direct visual examination (aided by pictures) of the participant at Baseline and Week 24 (W24). v, vertex; most of the hair loss (commonly seen with advancing age) is on the vertex. a, type a variant; major features are (1) the entire anterior hairline border recedes in unison; (2) there is no simultaneous balding of the vertex." (NCT01231607)
Timeframe: Baseline and Week 24

,,,,
Interventionparticipants (Number)
BL S IIIv to W24 S II, n=80, 72, 72, 72, 76BL S IIIv to W24 S IIa, n=80, 72, 72, 72, 76BL S IIIv to W24 S III, n=80, 72, 72, 72, 76BL S IIIv to W24 S IIIa, n=80, 72, 72, 72, 76BL S IIIv to W24 S IIIv, n=80, 72, 72, 72, 76BL S IIIv to W24 S IV, n=80, 72, 72, 72, 76BL S IIIv to W24 S IVa, n=80, 72, 72, 72, 76BL S IIIv to W24 S V, n=80, 72, 72, 72, 76BL S IIIv to W24 S Va, n=80, 72, 72, 72, 76BL S IIIv to W24 S VI, n=80, 72, 72, 72, 76BL S IV to W24 S II, n=52, 59, 59, 56, 54BL S IV to W24 S IIa, n=52, 59, 59, 56, 54BL S IV to W24 S III, n=52, 59, 59, 56, 54BL S IV to W24 S IIIa, n=52, 59, 59, 56, 54BL S IV to W24 S IIIv, n=52, 59, 59, 56, 54BL S IV to W24 S IV, n=52, 59, 59, 56, 54BL S IV to W24 S IVa, n=52, 59, 59, 56, 54BL S IV to W24 S V, n=52, 59, 59, 56, 54BL S IV to W24 S Va, n=52, 59, 59, 56, 54BL S IV to W24 S VI, n=52, 59, 59, 56, 54BL S V to W24 S II, n=41, 46, 46, 41, 35BL S V to W12 S IIa, n=41, 46, 46, 41, 35BL S V to W24 S III, n=41, 46, 46, 41, 35BL S V to W24 S IIIa, n=41, 46, 46, 41, 35BL S V to W24 S IIIv, n=41, 46, 46, 41, 35BL S V to W24 S IV, n=41, 46, 46, 41, 35BL S V to W24 S IVa, n=41, 46, 46, 41, 35BL S V to W24 S V, n=41, 46, 46, 41, 35BL S V to W24 S Va, n=41, 46, 46, 41, 35BL S V to W24 S VI, n=41, 46, 46, 41, 35
Dutasteride 0.02 mg2080611000010307460200101011003300
Dutasteride 0.1 mg20110581000010401139040000104803300
Dutasteride 0.5 mg311305410000105210371000003031002500
Finasteride 1 mg21130591000000401336010000101812400
Placebo306067400000020444020000203702900

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Serum Concentration of Dutasteride at Week 12, Week 24, and Follow-up (Week 26)

Serum concentrations of dutasteride were measured after 12 weeks and 24 weeks of study treatment and at follow-up (approximately 2 weeks after the last dose of study treatment). (NCT01231607)
Timeframe: Week 12, Week 24, and Week 26

,,
Interventionnanograms per milliliter (ng/mL) (Mean)
Week 12, n=172, 172, 165Week 24, n=158, 158, 153Week 26, n=156, 154, 152
Dutasteride 0.02 mg0.20.00.1
Dutasteride 0.1 mg2.12.00.3
Dutasteride 0.5 mg33.236.121.1

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Serum Dihydrotestosterone (DHT) at Week 12, Week 24, and Follow-up (Week 26)

Serum concentrations of DHT were measured after 12 weeks and 24 weeks of study treatment and at follow-up (approximately 2 weeks after the last dose of study treatment). (NCT01231607)
Timeframe: Week 12, Week 24, and Week 26

,,,,
Interventionnanomoles per liter (nmol/L) (Mean)
Week 12, n=172, 174, 172, 170, 161Week 24, n=173, 177, 176, 170, 165Week 26, n=173, 177, 177, 171, 165
Dutasteride 0.02 mg0.881.011.11
Dutasteride 0.1 mg0.390.490.77
Dutasteride 0.5 mg0.310.310.37
Finasteride 1 mg0.450.491.03
Placebo1.171.161.21

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Change From Baseline in Terminal Hair Count (THC) Within a 2.54 cm (1 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT

The THC (thick, long, and dark hair) was the sum of all nonvellus hairs (>=60 μm in width; thick and noticeable hair) within a target 2.54 cm (1 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on the hair follicles in the photographs. Change from BL=Week 12/Week 24 value minus BL value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24

,,,,
InterventionHair count (Least Squares Mean)
Week 12, n=147, 144, 151, 145, 131Week 24, n=148, 155, 158, 150, 141
Dutasteride 0.02 mg-13.4-15.7
Dutasteride 0.1 mg18.329.4
Dutasteride 0.5 mg29.346
Finasteride 1 mg24.236.3
Placebo-11.5-17.5

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Change From Baseline in Terminal Hair Count Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT

The THC (thick, long, and dark hair) was the sum of all nonvellus hairs (>=60 μm in width; thick and noticeable hair) within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). A cosmetic ink dot was placed by tattoo at BL so that the same area could be identified at BL and post-BL. If the ink dot faded, it was re-done in exactly the same location to ensure visibility for subsequent photographs. For the MT, hair was clipped before each photograph; HC was based on hair follicles in the photographs. Change from BL=Week 12/Week 24 value minus BL value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24

,,,,
InterventionHair count (Least Squares Mean)
Week 12, n=152, 154, 155, 149, 134Week 24, n=152, 158, 159, 152, 142
Dutasteride 0.02 mg-2.7-2.8
Dutasteride 0.1 mg4.06.0
Dutasteride 0.5 mg5.99.3
Finasteride 1 mg4.57.2
Placebo-1.1-3.0

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Change From Baseline in Target Area Hair Width Within a 1.13 cm (0.44 Inch) Diameter Circle at the Vertex at Week 12 and Week 24, as Assessed by MT

The target area hair width was the sum of all nonvellus hairs (>=30 µm in width; thick and noticeable hair) within a target 1.13 cm (0.44 inch) diameter circle at the vertex (crown, topmost part of the head). For the MT, hair was clipped before each photograph. A cosmetic ink dot was placed by tattoo at Baseline so that the same area could be identified at Baseline and post-Baseline. If the ink dot faded, it was re-done in exactly the same location to ensure it was visible for subsequent photographs. Change from Baseline was calculated as the Week 12 or Week 24 value minus the Baseline value. (NCT01231607)
Timeframe: Baseline, Week 12, and Week 24

,,,,
Interventionmillimeters (Least Squares Mean)
Week 12, n=152, 154, 155, 149, 134Week 24, n=152, 158, 159, 152, 142
Dutasteride 0.02 mg0.10.1
Dutasteride 0.1 mg0.70.8
Dutasteride 0.5 mg0.91.2
Finasteride 1 mg0.60.8
Placebo-0.1-0.2

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Pre/Post Ratio PSA Area Under the Curve (AUC)

Pre/Post Ratio prediction area under the receiver operating characteristics curve (AUC) for subjects taking finasteride 5mg every day for 3 months. Measurements of PSA are measured from Baseline until 3 months. (NCT01296672)
Timeframe: Reported at 90-days: assessment at baseline, 1 month, 2 months and 3 months

InterventionRatio (Number)
Finasteride0.57
Placebo0.61

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PCA3 (Prostate Cancer Antigen 3)Score AUC

Area under the Receiver Operating Characteristic Curve (ROC-AUC) of the PCA3 (Prostate Cancer Antigen 3) to detect difference in PSA decline between cases and controls (non-cases) (NCT01296672)
Timeframe: Reported at 90 days: assessed at baseline, 30 days, 60 days and 90-day

Interventionratio (Number)
Finasteride0.65
Placebo0.84

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Number of Participants With Risk of Acute Urinary Retention and Surgery Based on an MPR Threshold of 70%

Claims-based definition of acute urinary retention (AUR) and surgery based on the presence of an ICD-9-CM code of 599.6x, 788.20, or 788.29 and CPT procedure codes, respectively. For this analysis, we evaluated the association between compliance with 5-ARI therapy (measured by medication possession ratio [MPR]) and risk of AUR or surgery. MPR was calculated as the number of days that 5-ARI therapy was taken divided by the total number of follow-up days. For this analysis, the threshold for compliance was set at MPR = 70%. (NCT01334723)
Timeframe: The 5 and a half year period from January 1, 2000 to June 30, 2006

,,,
Interventionparticipants (Number)
Number of Participants with AUR and SurgeryNumber of Participants without AUR and Surgery
Acute Urinary Retention Outcomes Cohort, MPR <=70%21405511
Acute Urinary Retention Outcomes Cohort, MPR >70%15878055
Prostate Surgery Outcomes Cohort, MPR <=70%4816905
Prostate Surgery Outocomes Cohort, MPR >70%33110022

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Number of Participants With Risk of Acute Urinary Retention and Surgery Based on an MPR Threshold of 75%

Claims-based definition of AUR and surgery based on the presence of an ICD-9-CM code of 599.6x, 788.20, or 788.29 and CPT procedure codes, respectively. For this analysis, we evaluated the association between compliance with 5-ARI therapy (measured by medication possession ratio [MPR]) and risk of AUR and surgery. MPR was calculated as the number of days that 5-ARI therapy was taken divided by the total number of follow-up days. For this analysis, the threshold for compliance was set at MPR = 75%. (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006

,,,
Interventionparticipants (Number)
Number of Participants with AUR and surgeryNumber of Participants without AUR and surgery
Acute Urinary Retention Outcomes Cohort, MPR <=75%27557658
Acute Urinary Retention Outcomes Cohort, MPR >75%12775603
Prostate Surgery Outcomes Cohort, MPR <=75%62710480
Prostate Surgery Outcomes Cohort, MPR >75%1856447

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Number of Participants With Risk of Acute Urinary Retention and Surgery Based on an MPR Threshold of 80%

Claims-based definition of AUR and surgery based on the presence of an ICD-9-CM code of 599.6x, 788.20, or 788.29 and CPT procedure codes, respectively. For this analysis, we evaluated the association between compliance with 5-ARI therapy (measured by medication possession ratio [MPR]) and risk of AUR and surgery. MPR was calculated as the number of days that 5-ARI therapy was taken divided by the total number of follow-up days. For this analysis, the threshold for compliance was set at MPR = 80%. (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006

,,,
Interventionparticipants (Number)
Number of Participants with AUR and surgeryNumber of Participants without AUR and surgery
Acute Urinary Retention Outcomes Cohort, MPR <=80%28128975
Acute Urinary Retention Outcomes Cohort, MPR >80%9154591
Prostate Surgery Outcomes Cohort, MPR <=80%62711326
Prostate Surgery Outcomes Cohort, MPR >80%1855601

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Mean Length of 5-ARI Therapy

In this analysis, we evaluated the association between 5-ARI length of therapy and risk of acute urinary retention and prostate surgery. (NCT01334723)
Timeframe: Up to one year following the first pharmacy claim for 5ARI therapy or medical encounter for AUR or prostate surgery in the 5 and a half year period from January 1, 2000 to June 30, 2006

Interventiondays (Mean)
Acute Urinary Retention Outcomes Cohort276.8
Prostate Surgery Outcomes Cohort289.5

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Percentage of Participants Free From Biochemical Failure

Increase in prostate-specific antigen (PSA) measured over time. Freedom from biochemical failure (FFBF) was defined from the time of enrollment until PSA failure occurs as defined by the Phoenix definition of a rise to 2 ng/mL above the nadir PSA value. (NCT01342367)
Timeframe: 4 years

Interventionpercentage of participants (Number)
SOC Cohort81
Oral ADT Group88

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Number of Participants With Clinical Progression

Participants with clinical progression are defined as those with acute urinary retention and/or receiving prostate-related surgery. (NCT01386983)
Timeframe: 3 months prior to and 12 months following index date

Interventionparticipants (Number)
Early Cohort14
Delayed Cohort5

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Number of Participants Who Experienced an Adverse Event

An adverse event is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. (NCT01534351)
Timeframe: Up to 54 weeks

InterventionParticipants (Number)
Finasteride0

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Number of Participants Who Discontinued Treatment Due to an Adverse Event

An adverse event is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of the Sponsor's product, whether or not considered related to the use of the product. (NCT01534351)
Timeframe: Up to 52 weeks

InterventionParticipants (Number)
Finasteride0

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Changes in Mean Macular Sensitivity in the Study Eye at Month 3 Compared to Baseline

Microperimetry was used to assess macular sensitivity. (NCT01585441)
Timeframe: Month 3

Interventiondecibels (Mean)
Finasteride 5 mg-2.00
Placebo-1.40

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Changes in Mean Macular Sensitivity in the Study Eye at the Safety Visit Compared to Baseline

Microperimetry was used to assess macular sensitivity. (NCT01585441)
Timeframe: Final Study Visit

Interventiondecibels (Mean)
Finasteride 5 mg-2.03
Placebo-2.45

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Number of Participants Presenting No Change in Autofluorescence Patterns at Month 3 Compared to Baseline

Autofluorescence patterns as observed on Fundus Autofluorescence (FAF) imaging (NCT01585441)
Timeframe: Month 3

Interventionparticipants (Number)
Finasteride 5 mg2
Placebo3

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Number of Participants Presenting No Change in Autofluorescence Patterns at the Safety Visit Compared to Baseline

Autofluorescence patterns as observed on Fundus Autofluorescence (FAF) imaging (NCT01585441)
Timeframe: Final Study Visit

Interventionparticipants (Number)
Finasteride 5 mg3
Placebo2

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Changes in Best-corrected Visual Acuity (BCVA) in the Study Eye at the Safety Visit Compared to Baseline

"Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. Acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters, the equivalent Snellen measurement is 20/20.~A positive change value indicates improvement of the outcome. A negative change value indicates worsening of the outcome." (NCT01585441)
Timeframe: Final Study Visit

InterventionETDRS letters (Mean)
Finasteride 5 mg-3.33
Placebo0.50

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Number of Participants Presenting No Change in Fluid Leakage at Month 3 Compared to Baseline

Changes in leakage as observed on fluorescein angiography (FA) (NCT01585441)
Timeframe: Month 3

Interventionparticipants (Number)
Finasteride 5 mg2
Placebo2

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Number of Participants Presenting No Change in Fluid Leakage at the Safety Visit Compared to Baseline

Changes in leakage as observed on fluorescein angiography (FA) (NCT01585441)
Timeframe: Final Study Visit

Interventionparticipants (Number)
Finasteride 5 mg2
Placebo2

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Number of Participants Presenting No Change in Size of Existing Plaque(s) on Indocyanine Green (ICG) Angiography at Month 3 Compared to Baseline

(NCT01585441)
Timeframe: Month 3

Interventionparticipants (Number)
Finasteride 5 mg2
Placebo3

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Number of Participants Presenting No Change in Size of Existing Plaque(s) on Indocyanine Green (ICG) Angiography at the Safety Visit Compared to Baseline

(NCT01585441)
Timeframe: Final Study Visit

Interventionparticipants (Number)
Finasteride 5 mg3
Placebo2

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Number of Participants Who Withdrew From the Study

(NCT01585441)
Timeframe: Duration of the study, up to 1.5 years

Interventionparticipants (Number)
Finasteride 5 mg0
Placebo0

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Percent Change in Subretinal Fluid Volume in the Study Eye at Month 3 Compared to Baseline

"Subretinal fluid volume will be determined by manually moving the segmentation lines of the optical coherence tomography (OCT) image using the Edit Segmentation function of the Cirrus™ HD-OCT software. The segmentation lines will be edited to outline the inner and outer borders of the subretinal fluid pocket. This will be done manually for all the individual B-scans of each OCT image, after which the software algorithm automatically calculates the subretinal fluid volume." (NCT01585441)
Timeframe: Month 3

Interventionpercent change (Mean)
Finasteride 5 mg-37.50
Placebo27.78

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Proportion of Participants With a Reduction in Subretinal Fluid Volume ≥ 50% at 3 Months Compared to Baseline

"This is the primary outcome measure for publication of study results. Subretinal fluid volume will be determined by manually moving the segmentation lines of the optical coherence tomography (OCT) image using the Edit Segmentation function of the Cirrus™ HD-OCT software. The segmentation lines will be edited to outline the inner and outer borders of the subretinal fluid pocket. This will be done manually for all the individual B-scans of each OCT image, after which the software algorithm automatically calculates the subretinal fluid volume." (NCT01585441)
Timeframe: Month 3

Interventionparticipants (Number)
Finasteride 5 mg1
Placebo0

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Proportion of Participants With an Improvement in Best-corrected Visual Acuity (BCVA) ≥ 15 Letters at 3 Months Compared to Baseline.

This is the regulatory filing primary outcome measure. Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. Acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters, the equivalent Snellen measurement is 20/20. (NCT01585441)
Timeframe: Month 3

Interventionparticipants (Number)
Finasteride 5 mg0
Placebo0

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Change in Serum Testosterone Concentration at the Safety Visit Compared to Baseline

The mean change is reported in nanograms of testosterone per decaliter of serum. (NCT01585441)
Timeframe: Final Study Visit

Interventionng/dL (Mean)
Finasteride 5 mg-42.00
Placebo33.00

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Change in Serum Testosterone Concentration at Month 3 Compared to Baseline

The mean change is reported in nanograms of testosterone per decaliter of serum. (NCT01585441)
Timeframe: Month 3

Interventionng/dL (Mean)
Finasteride 5 mg-33.50
Placebo-29.67

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Change in Central Retinal Thickness in the Study Eye at Month 3 Compared to Baseline

Central retinal thickness was assessed by spectral-domain optical coherence tomography (SD-OCT). (NCT01585441)
Timeframe: Month 3

Interventionμm (Mean)
Finasteride 5 mg-55.00
Placebo20.33

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Change in Central Retinal Thickness in the Study Eye at the Safety Visit Compared to Baseline

Central retinal thickness was assessed by spectral-domain optical coherence tomography (SD-OCT). (NCT01585441)
Timeframe: Final Study Visit

Interventionμm (Mean)
Finasteride 5 mg-39.67
Placebo50.50

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Change in Serum Dihydrotestosterone (DHT) Concentration at Month 3 Compared to Baseline

The mean change is reported in picograms of DHT per milliliter of serum. (NCT01585441)
Timeframe: Month 3

Interventionpg/mL (Mean)
Finasteride 5 mg-332.00
Placebo-93.67

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Change in Serum Dihydrotestosterone (DHT) Concentration at the Safety Visit Compared to Baseline

The mean change is reported in picograms of DHT per milliliter of serum. (NCT01585441)
Timeframe: Final Study Visit

Interventionpg/mL (Mean)
Finasteride 5 mg-101.67
Placebo-337.50

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Change in Urinary Levels of Cortisol at Month 3 Compared to Baseline

The mean change is reported in micrograms (μg). (NCT01585441)
Timeframe: Month 3

Interventionμg (Mean)
Finasteride 5 mg5.75
Placebo-7.10

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Change in Urinary Levels of Cortisol at the Safety Visit Compared to Baseline

The mean change is reported in micrograms (μg). (NCT01585441)
Timeframe: Final Study Visit

Interventionμg (Mean)
Finasteride 5 mg-0.60
Placebo0.70

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Changes in Best-corrected Visual Acuity (BCVA) in the Study Eye at Month 3 Compared to Baseline

"Visual acuity was measured using the Early Treatment Diabetic Retinopathy Study (ETDRS) protocol. Acuity is measured as letters read on an ETDRS eye chart and the letters read equate to Snellen measurements. For example, if a participant reads between 84 and 88 letters, the equivalent Snellen measurement is 20/20.~A positive change value indicates improvement of the outcome. A negative change value indicates worsening of the outcome." (NCT01585441)
Timeframe: Month 3

InterventionETDRS letters (Mean)
Finasteride 5 mg1.00
Placebo1.67

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Absolute Change in Walking Speed

Absolute change in 10 m walking speed (NCT02248701)
Timeframe: Baseline, 6 months, 12 months

,
Interventionmeters/second (m/s) change (Mean)
6 months12 months
Placebo Treatment0.050.01
Testosterone Enanthate, Finasteride00.10

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Percent Change in Hip Bone Mineral Density

Percent change in total hip bone mineral density of the non-dominant limb assessed via dual-energy X-ray absorptiometry (DXA) (NCT02248701)
Timeframe: Baseline, 6 months, 12 months

,
Interventionpercent change (Mean)
Change at 6 monthsChange at 12 months
Placebo Treatment-0.51.1
Testosterone Enanthate, Finasteride1.71.2

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Percent Change in Neuromuscular Function

Percent change in thigh (knee extensors) peak isometric torque production of the non-dominant limb assessed via dynamometry (NCT02248701)
Timeframe: Baseline, 6 months, 12 months

,
Interventionpercent change (Mean)
6 months12 months
Placebo Treatment-8.60.5
Testosterone Enanthate, Finasteride19.915.5

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Percent Change in Total Body Fat

Percent change in total body fat assessed via dual-energy x-ray absorptiometry (DXA) (NCT02248701)
Timeframe: Baseline, 6 months, 12 months

,
Interventionpercent change (Mean)
6 months12 months
Placebo Treatment-4.7-1.9
Testosterone Enanthate, Finasteride-6.8-8.7

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Percent Change in Visceral Fat

Percent change in visceral (android) fat mass assessed via dual-energy x-ray absorptiometry (DXA) (NCT02248701)
Timeframe: Baseline, 6 months, 12 months

,
Interventionpercent change (Mean)
6 months12 months
Placebo Treatment-3.20.2
Testosterone Enanthate, Finasteride-8.2-13.6

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Percent Changes in Muscle Cross-Sectional Area

Percent Change in thigh (knee extensors) muscle cross-sectional area of the non-dominant limb assessed via MRI (NCT02248701)
Timeframe: Baseline, 6 months, 12 months

,
Interventionpercent change (Mean)
6 months12 months
Placebo Treatment-0.9-1.9
Testosterone Enanthate, Finasteride7.911.4

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Change From Baseline in Target Area Hair Count (TAHC) at Week 24

TAHC was measured using digital imaging analysis and was reported in terminal hairs/centimeters square (cm^2). TAHC is a standardized objective quantification of the number of hairs within a prespecified target area of the scalp at different timepoints, using macrophotography digital images. The total number of terminal hairs (hair width ≥ 30 μm) was calculated from macrophotographs. The target area used to count TAHC was a 1 cm^2 circular area of clipped hair (length approximately 1 mm) located at the anterior leading edge of the vertex thinning area of the scalp and centered with a semi-permanent microdot tattoo to ensure the same target area was reproduced at each visit. A positive change from Baseline indicated improvement (increase in the number of terminal hairs). Missing data are imputed up to Week 24 using last observation carried forward (LOCF) method. (NCT02781311)
Timeframe: Baseline (Day 1) to Week 24

Interventionterminal hairs/cm^2 (Least Squares Mean)
Placebo6.7
Setipiprant7.1

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Subject Self-Assessment (SSA) Score in Hair Growth at Week 24

The SSA consisted of a single-item measure that assesses each participant's perception of change in scalp hair growth. The participant used a standardized global photograph of his scalp taken at the Screening visit presented side by side with a standardized global photograph taken at the postbaseline visit to give a comparative score. The photographs were presented in a blinded and randomized manner to avoid influencing the participant, and response options were on a 7-point ordinal scale (where, -3=Greatly decreased, -2=Moderately decreased, -1=Slightly decreased, 0=No change, +1=Slightly increased, +2=Moderately increased and +3=Greatly increased). The higher the mean SSA value, the more the perception of hair growth from baseline. Missing data are imputed up to Week 24 using LOCF method. (NCT02781311)
Timeframe: Week 24

Interventionscore on a scale (Least Squares Mean)
Placebo-0.2
Setipiprant-0.3

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Adjusted Mean Change From Baseline in Target Area Hair Width (TAHW) in the Vertex at Weeks 12 and 24

The change from baseline in the TAHW within a 1 cm^2 of baldness area at Weeks 12 and 24, were assessed by macro photographic techniques analysis. The Investigator selected a target area in the anterior leading edge of the vertex thinning area. A small dot tattoo was placed in the center of the circle of the clipped hairs. Using the tattoo as a reference point, the circular area was photographed and a 1 cm^2 circular area within the target area was analysed. Change is the adjusted mean of Weeks 12 and 24 minus baseline, respectively.The analysis uses a covariance pattern model adjusted for treatment group, center, visit and treatment-by-visit interaction as fixed effects and baseline hair count as a covariate with an unstructured covariance structure. (NCT03004469)
Timeframe: Baseline, Week 12 and Week 24

,,
InterventionMicrometer (Mean)
Week 12Week 24
Oral Finasteride + P-3074 Vehicle-0.69380.7163
P-3074 + Finasteride Placebo-1.1231-0.8052
P-3074 Vehicle + Finasteride Placebo-0.7207-1.5289

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Adjusted Mean Change From Baseline in Participants Hair Growth/Loss at Weeks 12 and 24, Assessed for the Vertex by Blind Assessor

An independent blinded assessor was responsible for evaluating, under blinded conditions, the screening global photographs of the target area for all participants. They evaluated the eligibility of each participants according to the clinical inclusion criteria. The independent blinded assessor assessed the change of the hair growth from Baseline to Week 12 and from Baseline to Week 24, using a 7-point scale: -3 = greatly decreased, -2 = moderately decreased, -1 = slightly decreased, 0 = no change, +1 = slightly increased, +2 = moderately increased, +3 = greatly increased. This assessment was performed by comparing the global photographs obtained at screening visit with those subsequently obtained at Weeks 12 and 24. The analysis uses a covariance pattern model adjusted for treatment group, center, visit and treatment-by-visit interaction as fixed effects with an unstructured covariance structure. (NCT03004469)
Timeframe: Baseline, Week 12 and Week 24

,,
Interventionscore on a scale (Mean)
Week 12Week 24
Oral Finasteride + P-3074 Vehicle0.20.3
P-3074 + Finasteride Placebo0.00.2
P-3074 Vehicle + Finasteride Placebo0.20.1

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Adjusted Mean Change From Baseline in Participants Hair Growth/Loss Assessed for the Vertex by Investigator at Weeks 12 and 24

The local Investigator assessed change in hair growth from Baseline to Week 12 and from Baseline to Week 24, using a 7-point scale. The evaluation was done by the Investigator or designee, by comparing the global vertex view photograph obtained at baseline visit with the participants actual scalp at 12 and 24 weeks. For the purpose of assessment of changes in hair growth by Investigators screening visits (where global photos were taken) were used as Baseline. The change from Baseline in hair growth was assessed using the following 7-point scale: -3 = greatly decreased, -2 = moderately decreased, -1 = slightly decreased, 0 = no change, +1 = slightly increased, +2 = moderately increased, +3 = greatly increased. The analysis uses a covariance pattern model adjusted for treatment group, center, visit and treatment-by-visit interaction as fixed effects with an unstructured covariance structure. (NCT03004469)
Timeframe: Baseline, Week 12 and Week 24

,,
Interventionscore on a scale (Mean)
Week 12Week 24
Oral Finasteride + P-3074 Vehicle0.50.7
P-3074 + Finasteride Placebo0.50.8
P-3074 Vehicle + Finasteride Placebo0.40.3

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Adjusted Mean Change From Baseline in Hair Growth Assessed by Target Area Hair Count (TAHC) in the Vertex at Week 24

The change from baseline in the TAHC within a 1 cm^2 (square centimeter) of baldness area at Week 24, were assessed by macro photographic techniques analysis. The Investigator selected a target area in the anterior leading edge of the vertex thinning area. A small dot tattoo was placed in the center of the circle of the clipped hairs. Using the tattoo as a reference point, the circular area was photographed and a 1 cm^2 circular area within the target area was analysed. Change is the adjusted mean of Week 24 minus baseline.The analysis uses a covariance pattern model adjusted for treatment group, center, visit and treatment-by-visit interaction as fixed effects and baseline hair count as a covariate with an unstructured covariance structure. (NCT03004469)
Timeframe: Baseline and Week 24

InterventionHairs (Mean)
P-3074 + Finasteride Placebo20.2
P-3074 Vehicle + Finasteride Placebo6.7
Oral Finasteride + P-3074 Vehicle21.1

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Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious TEAEs

An Adverse event is defined as any untoward medical occurrence in a participants or clinical investigation patient administered a pharmaceutical product and which does not necessarily have to have a causal relationship with treatment. A serious AE was an AE that results in any of the following outcomes: death; life threatening; persistent/significant disability/incapacity; initial or prolonged inpatient hospitalization; congenital anomaly/birth defect and medically significant event. The Treatment Emergent Adverse Events (TEAEs) is defined as all AEs occurring on or after the first dose of the IMP. (NCT03004469)
Timeframe: From the start of IMP up to 28 weeks

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Interventionparticipants (Number)
TEAEsSerious TEAEs
Oral Finasteride + P-3074 Vehicle411
P-3074 + Finasteride Placebo754
P-3074 Vehicle + Finasteride Placebo765

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Local Tolerability as Assessed by Incidence Rate of Skin Irritation Event Via Severity Score for Skin Irritation Scale

"Local tolerability at the application site was assessed to rate the severity of any skin irritation. The Investigator used the Severity score for skin Irritation scale to assess local tolerability. The dermal response and other effects indicative irritation responses were recorded at time of examination. Anything other than No evidence of irritation under Dermal Response was considered as a Dermal Response Skin Irritation event. Anything other than No other effects under Other Effects was considered as an Other Effects of Skin Irritation event. The event incidence rate is calculated as the number of events interest divided by total personal time in years." (NCT03004469)
Timeframe: Baseline to Week 24

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InterventionEvents per personal years (Number)
Dermal ResponseOther Effects
Oral Finasteride + P-3074 Vehicle0.6610.755
P-3074 + Finasteride Placebo0.3400.368
P-3074 Vehicle + Finasteride Placebo0.2450.463

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Adjusted Mean Change From Baseline in Hair Growth Assessed by TAHC in the Vertex at Week 12

The change from baseline in the TAHC within a 1 cm^2 of baldness area at Week 12, were assessed by macro photographic techniques analysis. The Investigator selected a target area in the anterior leading edge of the vertex thinning area. A small dot tattoo was placed in the center of the circle of the clipped hairs. Using the tattoo as a reference point, the circular area was photographed and a 1 cm^2 circular area within the target area was analysed. Change is the adjusted mean of Week 24 minus baseline.The analysis uses a covariance pattern model adjusted for treatment group, center, visit and treatment-by-visit interaction as fixed effects and baseline hair count as a covariate with an unstructured covariance structure. (NCT03004469)
Timeframe: Baseline and Week 12

InterventionHairs (Mean)
P-3074 + Finasteride Placebo20.4
P-3074 Vehicle + Finasteride Placebo7.6
Oral Finasteride + P-3074 Vehicle22.5

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Adjusted Mean International Index of Erectile Function (IIEF-2) Scores at Weeks 4, 8, 12 and 24

The 15-question IIEF-2 Questionnaire (Sexual Function Questionnaire) was used to evaluate any changes in sexual function and activity, at Weeks 4, 8, 12 and 24. A score of 0-5 is awarded to each of the 15 questions that examine the 4 main domains of male sexual function: erectile function, orgasmic function, sexual desire and intercourse satisfaction. Erectile function domain has 6 questions with the score for domain range from 0-30. Orgasmic function domain has 2 questions with the score for domain range from 0-10. , Sexual desire function domain has 2 questions with the score for domain range from 0-10. Intercourse satisfaction function domain has 3 questions with the score for domain range from 0-15. Overall Satisfaction domain has 2 questions with the score for domain range from 0-10. A higher score indicated a worse outcome in that domain. (NCT03004469)
Timeframe: Weeks 4, 8, 12 and 24

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Interventionscore on a scale (Mean)
Erectile Function Score, Week 4Erectile Function Score, Week 8Erectile Function Score, Week 12Erectile Function Score, Week 24Orgasmic Function Score, Week 4Orgasmic Function Score, Week 8Orgasmic Function Score, Week 12Orgasmic Function Score, Week 24Sexual Desire Score, Week 4Sexual Desire Score, Week 8Sexual Desire Score, Week 12Sexual Desire Score, Week 24Intercourse Satisfaction Score, Week 4Intercourse Satisfaction Score, Week 8Intercourse Satisfaction Score, Week 12Intercourse Satisfaction Score, Week 24Overall Satisfaction Score, Week 4Overall Satisfaction Score, Week 8Overall Satisfaction Score, Week 12Overall Satisfaction Score, Week 24
Oral Finasteride + P-3074 Vehicle23.524.423.624.98.99.19.09.07.17.67.87.88.59.08.38.97.97.87.68.2
P-3074 + Finasteride Placebo24.524.325.325.39.38.79.48.97.37.47.77.79.49.69.99.87.97.98.18.0
P-3074 Vehicle + Finasteride Placebo26.224.925.526.19.08.78.99.17.57.48.07.710.79.910.210.88.07.88.18.1

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Adjusted Mean Overall Male Hair Growth Questionnaire (MHGQ) Score as Assessed by the Participant at Weeks 12 and 24

Participants assessed their scalp hair using a validated, self-administered MHGQ, which was given in their language. The self-administered MHGQ overall score assessed using the following 5-point scale: 1 = very satisfied, 2 = satisfied, 3 = neutral (neither satisfied nor dissatisfied), 4 = dissatisfied, 5 = very dissatisfied. A higher score indicated a worse outcome. The questionnaire was administered to eligible participants to subjectively measure their perception of hair growth. A higher score indicated a worse outcome. (NCT03004469)
Timeframe: Week 12 and Week 24

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Interventionscore on a scale (Mean)
Week 12Week 24
Oral Finasteride + P-3074 Vehicle2.82.9
P-3074 + Finasteride Placebo2.92.8
P-3074 Vehicle + Finasteride Placebo3.03.0

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