Hydroxyflutamide is a nonsteroidal antiandrogen that blocks the effects of the male hormone testosterone. It is used to treat prostate cancer by blocking the growth of cancer cells that are dependent on testosterone. It is also used to treat acne and hirsutism (excessive hair growth) in women. Hydroxyflutamide is typically administered orally and can cause side effects such as liver damage, gynecomastia (breast enlargement in men), and hot flashes. Researchers continue to study hydroxyflutamide to investigate its potential for other applications, including the treatment of other types of cancer and the prevention of hair loss.'
| ID Source | ID |
|---|---|
| PubMed CID | 91649 |
| CHEMBL ID | 491 |
| SCHEMBL ID | 3079778 |
| SCHEMBL ID | 19117358 |
| MeSH ID | M0062732 |
| Synonym |
|---|
| BIDD:ER0519 |
| hydroxy flutamide |
| gtpl2862 |
| 52806-53-8 |
| hydroxyflutamide |
| propanamide, 2-hydroxy-2-methyl-n-(4-nitro-3-(trifluoromethyl)phenyl)- |
| alpha,alpha,alpha-trifluoro-2-methyl-4'-nitro-m-lactotoluidide |
| sch 16423 |
| NCGC00091014-01 |
| 2-hydroxy-2-methyl-n-(4-nitro-3-(trifluoromethyl)phenyl)propanamide |
| hydroxyniphtholide |
| hft , |
| 2-hydroxy-2-methyl-n-[4-nitro-3-(trifluoromethyl)phenyl]propanamide |
| oh-flutamide |
| MLS001061267 |
| smr001227196 |
| 2-hydroxyflutamide |
| 2-hydroxy-flutamide |
| 2-hydroxy-2-methyl-n-(4-nitro-3-trifluoromethyl-phenyl)-propionamide(hydroxyflutamide) |
| chembl491 , |
| hydroxy-flutamide |
| bdbm35909 |
| 2-hydroxy-2-methyl-n-(4-nitro-3-trifluoromethyl-phenyl)-propionamide (hydroxy flutamide) |
| cid_91649 |
| .alpha.-hydroxyflutamide |
| A21118 |
| A1728 |
| NCGC00091014-04 |
| NCGC00091014-03 |
| NCGC00091014-02 |
| AKOS007930906 |
| HMS3039A05 |
| cas-52806-53-8 |
| dtxcid6013562 |
| NCGC00257382-01 |
| tox21_303659 |
| dtxsid8033562 , |
| tox21_201204 |
| NCGC00258756-01 |
| unii-31d90ukp5y |
| 31d90ukp5y , |
| liproca depot |
| FT-0627147 |
| NCGC00091014-06 |
| 2AX6 |
| S10360 |
| SCHEMBL3079778 |
| H1600 |
| MLS006011954 |
| propanamide, 2-hydroxy-2-methyl-n-[4-nitro-3-(trifluoromethyl)phenyl]- |
| mfcd00563126 |
| hydroxyflutamide, >=98% (hplc) |
| 2-hydroxy-2-methyl-n-[4-nitro-3-(trifluoromethyl)phenyl]propanamide (2-hydroxyflutamide) |
| 2-hydroxy-2-methyl-n-[4-nitro-3-(trifluoromethyl)phenyl]propanamide; 2-hydroxyflutamide |
| 2-hydroxy-2-methyl-n-(4-nitro-3-(trifluoromethyl)-phenyl)propanamide |
| 2-hydroxy-2-methyl-n-(4-nitro-3-(trifluoromethyl)phenyl)propanamide; hydroxyniphtholide |
| Z1603855929 |
| SCHEMBL19117358 |
| hydroxyflutamide (hydroxyniphtholide) |
| CS-W013988 |
| BS-17460 |
| 2-hydroxy-2-methyl-n-[4-nitro-3-(trifluoromethyl)phenyl]propionamide |
| 2-hydroxy-4'-nitro-3'-(trifluoromethyl)isobutyranilide |
| BCP12495 |
| 2-hof |
| Q15633976 |
| SB17029 |
| 2-hydroxy flutamide |
| HY-W013272 |
| EN300-127735 |
| SY234851 |
Hydroxyflutamide is a potent nonsteroidal anti-androgenic drug extensively used in laboratory investigations.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Hydroxyflutamide is a potent nonsteroidal anti-androgenic drug extensively used in laboratory investigations. " | ( Influence of the anti-androgen hydroxyflutamide on in vitro development of mouse embryos. Nagamani, M; Osuamkpe, C; Yallampalli, C, 1993) | 2.01 |
Hydroxyflutamide treatment significantly (P less than 0.003) reduced the serum LH values in rats receiving 0-1 mg progesterone. Treatment with hydroxy flutamide, either alone or in combination with hCG, had no effect on the mRNA for these enzymes.
The aim of this study was to determine the pharmacokinetic parameters of flutamide. Flutamide is a nonsteroidal antiandrogenic compound, and its pharmacologically active metabolite, hydroxyflutamide, in renal insufficiency.
| Excerpt | Reference | Relevance |
|---|---|---|
| " It was present in the plasma in small and variable concentrations, which precluded quantitative assessment of pharmacokinetic parameters for individual subjects." | ( Single and multiple dose pharmacokinetic evaluation of flutamide in normal geriatric volunteers. Perentesis, G; Radwanski, E; Symchowicz, S; Zampaglione, N, 1989) | 0.28 |
| "The aim of this study was to determine the pharmacokinetic parameters of flutamide, a nonsteroidal antiandrogenic compound, and its pharmacologically active metabolite, hydroxyflutamide, in renal insufficiency." | ( Pharmacokinetics of flutamide in patients with renal insufficiency. Affrime, MB; Anjum, S; Cutler, DL; Halstenson, CE; Lambrecht, LJ; Radwanski, E; Swan, SK, 1999) | 0.5 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " We investigated the effects of the proteasome inhibitors MG115 and PSI alone or in combination with different concentrations of the antiandrogen hydroxyflutamide on the cellular proliferation, apoptosis and viability of 10 prostatic adenocarcinoma cell cultures." | ( Proteasome inhibitors and their combination with antiandrogens: effects on apoptosis, cellular proliferation and viability of prostatic adenocarcinoma cell cultures. Stöckle, M; Tahmatzopoulos, A; Unteregger, G; Wullich, B; Zwergel, T; Zwergel, U, 2004) | 0.52 |
| " The data also suggest a possible drug-drug interaction between flutamide and APAP, resulting in inhibition of flutamide metabolism and increased APAP bioactivation and toxicity." | ( Transport, metabolism, and hepatotoxicity of flutamide, drug-drug interaction with acetaminophen involving phase I and phase II metabolites. Ellis, E; Kostrubsky, SE; Mutlib, AE; Nelson, SD; Strom, SC, 2007) | 0.34 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "A bioavailability study of randomized cross-over design was carried out in eight volunteers who were given a 48-h flutamide treatment consisting of 250-mg tablets three times daily or 400-mg sustained-release tablets twice daily, followed 3 weeks later by the alternative dosage form." | ( Steady-state hydroxyflutamide plasma levels after the administration of two dosage forms of flutamide. Asade, RH; Muiño, JP; Prizont, L; Tessler, J, 1991) | 0.65 |
| " In this study, the pharmacokinetics and bioavailability of flutamide and its main active metabolite, 2-hydroflutamide, were determined in seven healthy mature stallions." | ( Pharmacokinetics of the anti-androgenic drug flutamide in healthy stallions. Buzon-Cuevas, A; Mendoza, FJ; Perez-Ecija, A; Serrano-Rodriguez, JM, 2017) | 0.46 |
| "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 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " To determine the specificity of the HF effect, we measured the DHT/HF index in a single prostate at different concentrations of HF in the presence of fixed concentrations of DHT (2 x 10(-8) M) and noted a dose-response relationship." | ( Measurement of androgen sensitivity in the human prostate in in vitro three-dimensional histoculture. Connors, K; Geller, J; Hoffman, RM; Sionit, LR, 1992) | 0.28 |
| "A bioavailability study of randomized cross-over design was carried out in eight volunteers who were given a 48-h flutamide treatment consisting of 250-mg tablets three times daily or 400-mg sustained-release tablets twice daily, followed 3 weeks later by the alternative dosage form." | ( Steady-state hydroxyflutamide plasma levels after the administration of two dosage forms of flutamide. Asade, RH; Muiño, JP; Prizont, L; Tessler, J, 1991) | 0.65 |
| " Addition of human chorionic gonadotrophin (hCG), as a source of LH activity, to a subthreshold (1 U/day) FSH infusion rate resulted in 20% of rats ovulating at an hCG dosage of 50 mIU/day; increasing the hCG infusion to 200 mIU/day concomitant with the subthreshold FSH infusion rate increased ovulation rate to a mean of 69 +/- 8/rat, with 100% of rats ovulating." | ( Bimodal effects of luteinizing hormone and role of androgens in modifying superovulatory responses of rats to infusion with purified porcine follicle-stimulating hormone. Armstrong, DT; Chandrasekhar, Y; Opavsky, MA; Siuda, A, 1989) | 0.28 |
| " From this study, it has been demonstrated that the pharmacokinetics of F and HF do not change appreciably upon multiple dosing of 250 mg F capsule given three times a day." | ( Single and multiple dose pharmacokinetic evaluation of flutamide in normal geriatric volunteers. Perentesis, G; Radwanski, E; Symchowicz, S; Zampaglione, N, 1989) | 0.28 |
| " The dose-response of DHT was biphasic in the presence and absence of FSH, such that progesterone production in the presence of 8 micrograms/ml DHT was similar to basal progesterone production." | ( Comparative effects of androgens and catecholestrogens on progesterone production by porcine granulosa cells. Hammond, JM; Spicer, LJ, 1988) | 0.27 |
| " Dose-response curves were analyzed for 5alpha-dihydrotestosterone, the most active androgen in normal prostate, and androstenedione, a major androgen derived from the adrenals." | ( Functional characterization of mutant androgen receptors from androgen-independent prostate cancer. Balk, SP; Bubley, GJ; Fenton, MA; Fertig, AM; Kolvenbag, G; Shuster, TD; Taplin, ME, 1997) | 0.3 |
| " Dosing adjustments for renal impairment or HD are not indicated for flutamide." | ( Pharmacokinetics of flutamide in patients with renal insufficiency. Affrime, MB; Anjum, S; Cutler, DL; Halstenson, CE; Lambrecht, LJ; Radwanski, E; Swan, SK, 1999) | 0.3 |
| "Experience with dose response and mechanisms of toxicity has shown that multiple mechanisms may exist for a single agent along the continuum of the full dose-response curve." | ( Dose-dependent transitions in mechanisms of toxicity: case studies. Andersen, ME; Bogdanffy, MS; Bus, JS; Cohen, SD; Conolly, RB; David, RM; Doerrer, NG; Dorman, DC; Gaylor, DW; Hattis, D; Rogers, JM; Setzer, RW; Slikker, W; Swenberg, JA; Wallace, K, 2004) | 0.32 |
| " The lead compound [3aS-(3aalpha,4beta,5beta,7beta,7aalpha)]-4-(octahydro-5-hydroxy-4,7-dimethyl-1,3-dioxo-4,7-epoxy-2H-isoindol-2-yl)-2-iodobenzonitrile was shown to have potent in vivo efficacy after oral dosing in the CWR22 human prostate tumor xenograph model." | ( Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists. Attar, RM; Balog, A; Chandrasena, G; Fura, A; Furch, JA; Galella, MA; Geng, J; Giese, S; Gottardis, MM; Gougoutas, J; Jure-Kunkel, M; Krystek, SR; Mitt, T; Obermeier, M; Rampulla, R; Rizzo, CA; Salvati, ME; Shan, W; Vite, GD, 2008) | 0.35 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 21.7695 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 51.3236 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 51.3236 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
| TDP1 protein | Homo sapiens (human) | Potency | 17.5886 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 22.6522 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 8.9084 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID1259381; AID588515; AID588516; AID743035; AID743036; AID743040; AID743042; AID743053; AID743054; AID743063 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 70.4514 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 47.7163 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224839; AID1224893 |
| progesterone receptor | Homo sapiens (human) | Potency | 2.8982 | 0.0004 | 17.9460 | 75.1148 | AID1346795 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 22.0347 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 32.6123 | 0.0002 | 14.3764 | 60.0339 | AID588533; AID720691; AID720692 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 69.9870 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 21.8303 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 49.9925 | 0.3758 | 27.4851 | 61.6524 | AID743220 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 29.4862 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID720659 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 43.1886 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743078; AID743079; AID743080; AID743091 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 47.9516 | 0.0010 | 24.5048 | 61.6448 | AID588534; AID743215 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 45.0550 | 0.0010 | 19.4141 | 70.9645 | AID743191 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 39.8045 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 89.1251 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 52.9661 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 39.1729 | 0.0006 | 27.2152 | 1,122.0200 | AID651741; AID743202; AID743219 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 100.0000 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 25.1189 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 33.3689 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 36.2619 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 33.3689 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 18.8336 | 0.0266 | 22.4482 | 66.8242 | AID651802 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 25.1189 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Progesterone receptor | Homo sapiens (human) | IC50 (µMol) | 2.0130 | 0.0000 | 0.5807 | 10.0000 | AID162117 |
| Androgen receptor | Homo sapiens (human) | IC50 (µMol) | 2.6192 | 0.0000 | 0.8753 | 10.0000 | AID1250202; AID1250204; AID1661980; AID1799354; AID241409; AID248615; AID284206; AID284208; AID301365; AID301367; AID316695; AID339521; AID365468; AID38975; AID38992; AID469714; AID694143; AID730427; AID777287 |
| Androgen receptor | Homo sapiens (human) | Ki | 0.0697 | 0.0002 | 0.4240 | 7.2000 | AID238631; AID238934; AID238961; AID253455; AID316694; AID339517; AID339523; AID39008; AID39147 |
| Androgen receptor | Mus musculus (house mouse) | IC50 (µMol) | 0.6073 | 0.0010 | 0.8750 | 3.0000 | AID201917; AID730424; AID777288 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| ORF73 | Human gammaherpesvirus 8 | EC50 (µMol) | 75.0000 | 0.0600 | 8.1346 | 32.1400 | AID435023 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Androgen receptor | Homo sapiens (human) | FI5 | 0.6000 | 0.2000 | 0.5425 | 1.0000 | AID284207; AID301366 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID491348 | Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. |
| AID694141 | Antagonist activity at wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 assessed as testosterone induced luciferase activity at 10 uM after 18 hrs relative untreated control | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. |
| AID241409 | Inhibition of androgen receptor in human MDA-453 cells | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. |
| AID284207 | Agonist activity at androgen receptor expressed in HeLa cells assessed as effect on dihydrotestosterone-induced transcriptional activity by reporter gene assay | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships. |
| AID468984 | Inhibition 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 hrs | 2009 | Journal 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. |
| AID39147 | Binding affinity for human androgen receptor in transiently-transfected COS-1 cells. | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. |
| AID1323713 | Antagonist activity at AR in mouse SC3 cells assessed as inhibition of dihydrotestosterone-induced cell growth 10'-5 to 10'-7 M measured after 3 days by CCK8 assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Development of 6-arylcoumarins as nonsteroidal progesterone antagonists. Structure-activity relationships and fluorescence properties. |
| AID248615 | Inhibition of human androgen receptor of breast carcinoma MDA-453 cells in reporter gene assay | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. |
| AID1885058 | Antiproliferative activity against androgen-sensitive mouse SEM-107 cells | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13 | Therapeutic Strategies to Target the Androgen Receptor. |
| AID1250201 | Agonist activity at wild type AR expressed in human SC cells assessed as effect on cell proliferation by WST-8 assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists. |
| AID238934 | Inhibition of [3H]DHT binding to androgen receptor of MDA-453 cells | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. |
| AID39294 | In vivo binding affinity for rat ventral prostate androgen receptor by displacement of [3H]R-1881 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. |
| AID301370 | Inhibition of testosterone propionate-stimulated seminal vesicle weight gain in castrated mouse at 10 mg/body, sc | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. |
| AID230355 | In vivo relative binding affinity (1h/18h) as ratio of binding affinities for R1881 and compound against rat ventral prostate androgen receptor using [3H]- R1881 as radioligand; 2.6/0.1 | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. |
| AID339521 | Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
| AID39323 | Relative binding affinity against rat ventral prostate androgen receptor using competition assay after 18 hours. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiandrogenic steroidal sulfonylpyrazoles. |
| AID162117 | Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. |
| AID284208 | Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships. |
| AID612450 | Activation of androgen receptor in androgen-sensitive (AR+) mouse Shionogi cells assessed as stimulation of cell proliferation after 10 days relative to control | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15 | Development of 3-substituted-androsterone derivatives as potent inhibitors of 17β-hydroxysteroid dehydrogenase type 3. |
| AID238631 | Binding affinity for androgen receptor in human MDA-453 cells | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. |
| AID445837 | Binding affinity to androgen receptor in hamster DDT cells by scintillation counting | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. |
| AID1885059 | Antiproliferative activity against human T47D cells | 2022 | Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13 | Therapeutic Strategies to Target the Androgen Receptor. |
| AID445838 | Binding affinity to androgen receptor LBD T877A mutant in hamster DDT cells by scintillation counting | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. |
| AID38827 | Efficacy as a function of maximal inhibition against human androgen receptor. | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. |
| AID1661980 | Antagonistic activity at AR in human 22Rv1 cells assessed as reduction in cell number by CCK8 assay | 2020 | Journal of medicinal chemistry, 09-24, Volume: 63, Issue:18 | Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer. |
| AID183961 | Androgenic activity as percent increase in rat ventral prostate (castrated immature rat) weight caused by 100 mg/kg per day x 10 oral dose; Not significant | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiandrogenic steroidal sulfonylpyrazoles. |
| AID730424 | Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange. |
| AID445834 | Agonist activity at androgen receptor in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transformation by R-SAT assay relative to dihydrotestosterone | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. |
| AID445836 | Agonist activity at androgen receptor LBD T877A mutant in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transformation by R-SAT assay relative to dihydrotestosterone | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. |
| AID301367 | Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. |
| AID431977 | Activity in human PC3 cells expressing androgen receptor T877A mutant assessed as ARE-dependent transactivation at 1 uM after 24 hrs by luciferase reporter gene assay in absence of DHT | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17 | Design and synthesis of androgen receptor antagonists with bulky side chains for overcoming antiandrogen resistance. |
| AID39322 | Relative binding affinity against rat ventral prostate androgen receptor using competition assay after 1 hour. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiandrogenic steroidal sulfonylpyrazoles. |
| AID1324635 | Agonist activity at AR T877A mutant (unknown origin) expressed in human PC3 cells assessed as receptor transactivation at 5 uM after 24 hrs by PSA-luciferase reporter gene assay | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12 | Identification of Triptophenolide from |
| AID176903 | Peroral dose inhibiting testosterone propionate (subcutaneous administration) induced rat ventral prostate weight gain by 50% | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. |
| AID38832 | Percent maximal inhibition against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines. |
| AID201917 | In vitro inhibition of DHT (dihydrotestosterone) on proliferation of androgen-sensitive cancer Schionogi (SC-3) cells | 1995 | Journal 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. |
| AID23700 | Partition coefficient (logP) | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Non-steroidal antiandrogens. Design of novel compounds based on an infrared study of the dominant conformation and hydrogen-bonding properties of a series of anilide antiandrogens. |
| AID207442 | In vitro inhibition of human Steroid 5-alpha-reductase type 2 in transfected SW-13 cells using [3H]- delta4-Androstenedione as substrate; NA is not active | 1995 | Journal 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. |
| AID491350 | Growth stimulatory activity of human LNCAP cells | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. |
| AID339524 | Agonist activity at wild type human recombinant androgen receptor assessed as induction of prostate specific antigen production in human LNCaP cells by ELISA | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
| AID253472 | Inhibition of mutant T877A Androgen receptor in human LNCaP cells; Ag means agonist | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. |
| AID38992 | Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines. |
| AID730427 | Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange. |
| AID339517 | Displacement of [3H]testosterone from wild type human androgen receptor | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
| AID694142 | Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay relative to untreated control | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. |
| AID301365 | Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cells | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. |
| AID694143 | Displacement of [3H]R1881 from wild type human androgen receptor expressed in COS-1 cells co-transfected with pSG5 after 15 mins by scintillation assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators. |
| AID1250203 | Antagonist activity at wild type AR expressed in human SC cells assessed as inhibition of 0.3 to 10 nM DHT-induced cell proliferation after 3 days by WST-8 assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists. |
| AID777287 | Displacement of [3H]-DHT from human GST-tagged androgen receptor LBD (627 to 919) expressed in Escherichia coli HB-101 after 15 hrs by liquid scintillation counting analysis | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10 | Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists. |
| AID39301 | In vitro relative binding affinity for rat androgen receptor | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Non-steroidal antiandrogens. Design of novel compounds based on an infrared study of the dominant conformation and hydrogen-bonding properties of a series of anilide antiandrogens. |
| AID777286 | Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity at 10 uM after 24 hrs by chemiluminescence assay relative to control | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10 | Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists. |
| AID468985 | Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 3 uM after 7 hrs | 2009 | Journal 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. |
| AID248865 | Inhibition of androgen dependent human prostate cancer cell MDA-MB-PCa2b proliferation; Ag means agonist | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. |
| AID316695 | Antagonist activity at human androgen receptor in MDA453 cells by alkaline phosphatase reporter gene assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists. |
| AID238961 | Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cells | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. |
| AID248943 | Activation of T877A androgen receptor of human prostate cancer LNCap cells in reporter gene assay | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. |
| AID1250204 | Displacement of [3H]-DHT from human GST fused AR-LBD (627 to 919 amino acids) transfected in Escherichia coli HB 101 after 15 hrs by liquid scintillation counting assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists. |
| AID287852 | Binding affinity to human androgen receptor expressed in HEK293 cells at 0.1 uM relative to R1881 | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Chemical synthesis and biological activities of 16alpha-derivatives of 5alpha-androstane-3alpha,17beta-diol as antiandrogens. |
| AID431978 | Activity in human PC3 cells expressing androgen receptor W741C mutant assessed as ARE-dependent transactivation at 1 uM after 24 hrs by luciferase reporter gene assay in absence of DHT | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17 | Design and synthesis of androgen receptor antagonists with bulky side chains for overcoming antiandrogen resistance. |
| AID301366 | Agonist activity at human androgen receptor expressed in HeLa cells assessed as five times increase in transcriptional activity by reporter gene assay | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. |
| AID339527 | Antiproliferative activity against human LNCaP cells | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
| AID777288 | Antagonist activity at androgen receptor in mouse SC3 cells assessed as inhibition of DHT-induced cell growth after 3 days by CCK-8/WST-8 assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10 | Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists. |
| AID287848 | Inhibition of DHT-stimulated proliferation of androgen sensitive AR+ Shionogi cells at 0.1 uM | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Chemical synthesis and biological activities of 16alpha-derivatives of 5alpha-androstane-3alpha,17beta-diol as antiandrogens. |
| AID417704 | Antiandrogenic activity in mouse SC115 cells expressing androgen receptor assessed as inhibition of DHT-induced cell proliferation at 1 uM after 10 days relative to DHT | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities. |
| AID287853 | Binding affinity to human androgen receptor expressed in HEK293 cells at 1 uM relative to R1881 | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Chemical synthesis and biological activities of 16alpha-derivatives of 5alpha-androstane-3alpha,17beta-diol as antiandrogens. |
| AID730431 | Agonist activity at CMX-GAL4 tagged human VDR expressed in HEK293 cells assessed as increase in transcriptional activity by luciferase reporter gene assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange. |
| AID207455 | In vitro inhibition of human Steroid 5-alpha-reductase type I in transfected 293 cells using [3H]- delta4-Androstenedione as substrate; NA is not active | 1995 | Journal 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. |
| AID1288976 | Plasma protein binding in healthy geriatric volunteer by equilibrium dialysis method | 1999 | British journal of clinical pharmacology, Jan, Volume: 47, Issue:1 | Pharmacokinetics of flutamide in patients with renal insufficiency. |
| AID316694 | Displacement of [3H]DHT from human androgen receptor in MDA453 cells | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists. |
| AID365467 | Displacement of [3H]DHT from GST-tagged human AR-LBD transfected in Escherichia coli HB-101 at 10 uM | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring. |
| AID177269 | Anti-androgenic activity in vivo on groups of five rats treated with seven daily subcutaneous doses of testosterone propionate at 200 ug/kg | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Non-steroidal antiandrogens. Design of novel compounds based on an infrared study of the dominant conformation and hydrogen-bonding properties of a series of anilide antiandrogens. |
| AID417703 | Androgenic activity in mouse SC115 cells expressing androgen receptor assessed as DHT-induced cell proliferation at 1 uM after 10 days relative to DHT | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities. |
| AID38975 | Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. |
| AID365468 | Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17 | Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring. |
| AID176392 | Antiandrogenic activity as the dose required to inhibit testosterone propionate-induced rat ventral prostate weight gain in castrated immature rat by 50%. | 1990 | Journal of medicinal chemistry, Aug, Volume: 33, Issue:8 | Antiandrogenic steroidal sulfonylpyrazoles. |
| AID287850 | Proliferative activity on androgen sensitive AR+ Shionogi cells at 0.1 uM relative to DHT | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Chemical synthesis and biological activities of 16alpha-derivatives of 5alpha-androstane-3alpha,17beta-diol as antiandrogens. |
| AID280723 | Displacement of [3H]R1881 from rat AR relative to R1881 | 2007 | Journal of medicinal chemistry, Mar-08, Volume: 50, Issue:5 | Synthesis and biological evaluation of [18F]bicalutamide, 4-[76Br]bromobicalutamide, and 4-[76Br]bromo-thiobicalutamide as non-steroidal androgens for prostate cancer imaging. |
| AID39008 | Binding affinity for human androgen receptor transfected into mammalian COS-1 cells | 2000 | Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5 | Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines. |
| AID469714 | Antagonist activity at androgen receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay | 2009 | Journal of natural products, Nov, Volume: 72, Issue:11 | The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. |
| AID253455 | Binding affinity for mutant T877A Androgen receptor in human LNCaP cells | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. |
| AID301369 | Inhibition of testosterone propionate-stimulated seminal vesicle weight gain in castrated mouse at 3 mg/body, sc | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. |
| AID417702 | Androgenic activity in mouse SC115 cells expressing androgen receptor assessed as DHT-induced cell proliferation at 0.1 uM after 10 days relative to DHT | 2009 | European journal of medicinal chemistry, Feb, Volume: 44, Issue:2 | Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities. |
| AID301368 | Inhibition of testosterone propionate-stimulated seminal vesicle weight gain in castrated mouse at 1 mg/body, sc | 2007 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20 | Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists. |
| AID339523 | Displacement of [3H]testosterone from human recombinant androgen receptor T877A mutant expressed in LNCaP cells | 2008 | Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14 | 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor. |
| AID284206 | Displacement of [3H]mibolerone from androgen receptor expressed in CHOK1 cells | 2007 | Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1 | Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships. |
| AID1250202 | Antagonist activity at wild type AR expressed in human SC cells assessed as inhibition of 1 nM DHT-induced cell proliferation after 3 days by WST-8 assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists. |
| AID248995 | Activation of L701H/T877A mutant androgen receptor of human prostate cancer MDAMB-PCa2b cell proliferation | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. |
| AID161974 | Efficacy as a function of maximal inhibition against human progesterone receptor B (hPR-B). | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. |
| AID445835 | Agonist activity at androgen receptor LBD T877A mutant in mouse NIH3T3 cells transiently transfected with beta-galactosidase reporter gene assessed as cellular transformation by R-SAT assay | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. |
| AID287849 | Inhibition of DHT-stimulated proliferation of androgen sensitive AR+ Shionogi cells at 1 uM | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Chemical synthesis and biological activities of 16alpha-derivatives of 5alpha-androstane-3alpha,17beta-diol as antiandrogens. |
| AID203348 | In vitro inhibition of 5-alpha-dihydrotestosterone stimulated shionogi cell proliferation. | 1995 | Journal 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. |
| AID15475 | Calculated partition coefficient (clogP) | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Non-steroidal antiandrogens. Design of novel compounds based on an infrared study of the dominant conformation and hydrogen-bonding properties of a series of anilide antiandrogens. |
| AID1347411 | qHTS 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) Libary | 2020 | ACS 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. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines. |
| AID1799354 | SPA Binding Assay (IC50) from Article 10.1021/cb900143a: \\Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.\\ | 2009 | ACS chemical biology, Oct-16, Volume: 4, Issue:10 | Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription. |
| AID1346888 | Human Androgen receptor (3C. 3-Ketosteroid receptors) | 1998 | Biochemical pharmacology, May-01, Volume: 55, Issue:9 | Androgen antagonistic effect of estramustine phosphate (EMP) metabolites on wild-type and mutated androgen receptor. |
| AID493017 | Wombat Data for BeliefDocking | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10 | Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 24 (8.66) | 18.7374 |
| 1990's | 104 (37.55) | 18.2507 |
| 2000's | 85 (30.69) | 29.6817 |
| 2010's | 53 (19.13) | 24.3611 |
| 2020's | 11 (3.97) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (26.09) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (1.74%) | 5.53% |
| Reviews | 3 (1.04%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 280 (97.22%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| An Open, Single and Multiple Dose, Efficacy and Safety Proof of Principle Study of Liproca Depot, a Controlled Release Formulation of 2-hydroxyflutamide, Injected Into the Prostate in Patients With Localized Prostate Cancer [NCT00913263] | Phase 1/Phase 2 | 24 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
| An Open, Single Dose, Antitumour Effect Study of 2-hydroxy-flutamide as a Controlled Release Product (Liproca Depot), Injected Into the Prostate in Patients With Localized Prostate Cancer [NCT02341404] | Phase 2 | 23 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
| A Single Blind, Two-Stage Dose Finding Study to Evaluate the Safety, Tolerability and Efficacy of a Single Liproca® Depot Injection Into the Prostate in Patients With Localized Prostate Cancer, Assigned to Active Surveillance Who Are at High Risk for Dise [NCT03348527] | Phase 2 | 61 participants (Actual) | Interventional | 2017-05-12 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||