bicalutamide profile

bicalutamide: approved for treatment of advanced prostate cancer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group. [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]

bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism. [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]

ID Source	ID
PubMed CID	2375
CHEMBL ID	409
CHEBI ID	144093
CHEBI ID	91617
SCHEMBL ID	3611
MeSH ID	M0151653

Synonym
AC-4232
HMS3393B13
AB00639963-08
AB00639963-09
gtpl2863
raffolutil
nsc-722665
nsc722665
propanamide,
casodex
ici 176334
brn 5364666
ici-176334
(+-)-4'-cyano-alpha,alpha,alpha-trifluoro-3-((p-fluorophenyl)sulfonyl)-2-methyl-m-lactotoluidide
propanamide, n-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-, (+-)-
MLS001424047
90357-06-5
bicalutamide
C08160
smr000466329
MLS000759437
cpd000466329
DB01128
bicalutamide (jan/usp/inn)
casodex (tn)
D00961
NCGC00167977-01
4'-cyano-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methyl-3'-(trifluoromethyl)propionanilide
cosudex
chembl409 ,
bdbm18525
n-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorobenzene)sulfonyl]-2-hydroxy-2-methylpropanamide
HMS2089N12
HMS2051B13
NCGC00167977-02
ici 176,334
nsc-759816
ici176,334-1
FT-0663100
n-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide
CHEBI:144093
n-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
A803039
n-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-methyl-2-oxidanyl-propanamide
A843528
n-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-n-phenylpropanamide
NCGC00167977-03
HMS3263M13
propanamide, n-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-
ccris 8728
hsdb 7655
bicalutamide [usan:usp:inn:ban]
nsc 759816
unii-a0z3nau9dp
a0z3nau9dp ,
dtxcid00209197
dtxsid2022678 ,
cas-90357-06-5
tox21_303560
NCGC00257459-01
tox21_112488
nsc759816
pharmakon1600-01504827
BCP9000408
BICALUTAMIDE - CASODEX
kalumid
calutide
HMS2232H03
CCG-100951
HY-14249
CS-1296
BCPP000337
FT-0631069
FT-0618286
bicalutamide (cdx)
LP01026
4-cyano-3-trifluoromethyl-n-(3-p-fluorophenylsulfonyl-2-hydroxy-2-methylpropionyl)aniline
S1190
AKOS015895073
HMS3372K05
bicalutamide [usp monograph]
bicalutamide [usan]
bicalutamide [ep monograph]
bicalutamide [mi]
bicalutamide [usp-rs]
bicalutamide [who-dd]
propanamide, n-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-, (+/-)-
bicalutamide [usp impurity]
bicalutamide [hsdb]
bicalutamide [jan]
(+/-)-4'-cyano-.alpha.,.alpha.,.alpha.-trifluoro-3-((p-fluorophenyl)sulfonyl)-2-methyl-m-lactotoluidide
bicalutamide [inn]
bicalutamide [orange book]
bicalutamide [vandf]
bicalutamide [mart.]
CCG-222330
CCG-220876
AB00639963-06
n-[4-cyano-3-trifluoromethyl-phenyl]-3-[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methyl-propionamide
4'-cyano-3-[(4- fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3'-trifluoromethylpropionanilide
4'-cyano-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3'-trifluoromethylpropionanilide
n-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropionamide
B3206
NC00201
SCHEMBL3611
KS-1161 ,
NCGC00261711-01
tox21_501026
n-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
AB00639963_10
mfcd00869971
bicalutamide (cdx), >=98% (hplc), powder
EX-A962
SR-01000759410-5
SR-01000759410-4
sr-01000759410
bicalutamide, united states pharmacopeia (usp) reference standard
CHEBI:91617
HMS3654K18
bicalutamide, european pharmacopoeia (ep) reference standard
bicalutamide for system suitability, european pharmacopoeia (ep) reference standard
bicalutamide, pharmaceutical secondary standard; certified reference material
HMS3714P13
NCGC00167977-09
bicalutamide, british pharmacopoeia (bp) reference standard
SW197581-4
n-(4-cyano-3-(trifluoromethyl)phenyl)
-2-hydroxy-2-methylpropanamide
-3-(4-fluorophenylsulfonyl)
n-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropanamide
bicalutamide (casodex)
BCP02110
Q1988832
BRD-A29485665-001-03-7
SB17301
SDCCGSBI-0633779.P001
NCGC00167977-20
AMY33430
racemic bicalutamide
4'-cyano-alpha,alpha,alpha-trifuloro-3-((p-fluorophenyl)sulfonyl)-2-methyl-m-lactotoluidide
binabic
(rs)-bicalutamide
bicalutamide (ep monograph)
bicalutamidum
rac-n-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
bicatlon
bicalutamida
(+-)-4'-cyano-alpha,alpha,alpha-trifluoro-3-((p- fluorophenyl)sulfonyl)-2-methyl-m-lactotoluidide
bicalox
(rs)-4'-cyano-alpha',alpha',alpha',-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2-methylpropiono-m-toluidide
l02bb03
bicamide
bicadex
calutol
bical
bicusan
(+-)-bicalutamide
ormandyl
calumid
(+/-)-n-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
bicalutamide (usp-rs)
bicalutamide (usp impurity)
bicalutamide (mart.)
bicalutamide (usp monograph)
bypro
n-(4-cyano-3-(trifluoromethyl)phenyl)3-3((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-propanamide
EN300-1715981
n-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorobenzenesulfonyl)-2-hydroxy-2-methylpropanamide
Z2108698963

Excerpt	Reference	Relevance
"R-bicalutamide is a first-line therapy used to treat prostate cancer (PCa) inhibiting the androgen receptor (AR) which plays an important role in the development and the progression of PCa. "	( An insight about the mechanism of action (MoA) of R-bicalutamide on the androgen receptor homodimer using molecular dynamic. Cavaliere, F; Cozzini, P, 2022)	1.69
"Bicalutamide is a nonsteroidal antiandrogen widely used as a first-line clinical treatment for advanced prostate cancer (PCa). "	( The ERα-NRF2 signalling axis promotes bicalutamide resistance in prostate cancer. Cao, J; Du, X; Liang, Z; Peng, Y; Shi, J; Tian, L; Yang, K; Zhang, J, 2022)	2.44
"Bicalutamide (Casodex(®) ) is a non-steroidal pure anti-androgen used in the treatment of localized prostate cancer. "	( Enantiomer selective glucuronidation of the non-steroidal pure anti-androgen bicalutamide by human liver and kidney: role of the human UDP-glucuronosyltransferase (UGT)1A9 enzyme. Barbier, O; Campeau, AS; Caron, P; Caron, S; Grosse, L; Meunier, K; Morin, FA; Trottier, J; Verreault, M, 2013)	2.06
"Bicalutamide (Casodex®) is a non-steroidal anti-androgen drug used in the treatment of prostate cancer, which represents the second most common malignancy diagnosed in men worldwide. "	( Optical biosensor analysis in studying new synthesized bicalutamide analogs binding to androgen receptor. Bertucci, C; Carrupt, PA; Fortugno, C; Guerrini, A; Varchi, G, 2014)	2.09
"Bicalutamide (BCM) is an anti-androgen drug used to treat prostate cancer. "	( Box-Behnken study design for optimization of bicalutamide-loaded nanostructured lipid carrier: stability assessment. Belgamwar, VS; Dhas, NL; Ige, PP; Kudarha, R; Pandey, A, 2015)	2.12
"Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer. "	( Effects of the ABCG2 and ABCB1 drug transporter polymorphisms on the pharmacokinetics of bicalutamide in humans. Cha, YJ; Joo, HJ; Kim, KA; Lee, HM; Park, JY, 2015)	2.08
"Bicalutamide is a widely used, relatively non-toxic anti-androgen, particularly when used in combination with androgen deprivation. "	( An open-label, phase 2 trial of bicalutamide dose escalation from 50 mg to 150 mg in men with CAB and castration resistance. A Canadian Urology Research Consortium Study. Aprikian, A; Chin, J; Drachenberg, D; Fradet, Y; Kebabdjian, M; Klotz, L; Singal, R; Zarenda, M, 2014)	2.13
"Bicalutamide is a non-steroidal anti-androgen drug used for the treatment of androgen-dependent prostate cancer. "	( Validation of RP-HPLC Method for Simultaneous Quantification of Bicalutamide and Hesperetin in Polycaprolactone-Bicalutamide-Hesperetin-Chitosan Nanoparticles. Agrawal, S; Ahmad, H; Arya, A; Dwivedi, AK; Khandelwal, K; Khatik, R; Mittapelly, N; Singh, A, 2015)	2.1
"R-Bicalutamide is a first generation antiandrogen used to treat prostate cancer, which inhibits androgen action by competitively binding to the androgen receptor (AR). "	( Interaction mechanism exploration of R-bicalutamide/S-1 with WT/W741L AR using molecular dynamics simulations. An, X; Li, J; Li, S; Liu, H; Wang, Y, 2015)	1.41
"Bicalutamide is a non-steroidal anti-androgen, used during the initiation of androgen deprivation therapy along with a luteinizing hormone-releasing hormone agonist to reduce the symptoms of tumor-related flares in patients with advanced prostate cancer."	( Atypical onset of bicalutamide-induced liver injury. Joo, JS; Kang, SH; Kim, JS; Kim, KH; Kim, SH; Kim, SW; Lee, BS; Lee, ES; Lee, HY; Moon, HS; Sung, JK; Yun, GY, 2016)	1.49
"Bicalutamide is a non-steroidal antiandrogen and is an oral medication that is used for treating prostate cancer. "	( High performance liquid chromatography method for the pharmacokinetic study of bicalutamide SMEDDS and suspension formulations after oral administration to rats. Asati, D; Awasthi, A; Chaurasiya, A; Jain, GK; Khar, RK; Mishra, G; Mukherjee, R; Singh, AK, 2009)	2.02
"Bicalutamide monotherapy is a valuable option for prostate cancer (PCa) patients who wish to avoid the consequences of androgen deprivation; however, this treatment induces gynaecomastia and mastalgia in most patients. "	( An open, randomised, multicentre, phase 3 trial comparing the efficacy of two tamoxifen schedules in preventing gynaecomastia induced by bicalutamide monotherapy in prostate cancer patients. Aragona, F; Bedognetti, D; Boccardo, F; Canclini, L; Conti, G; Cortellini, P; De Cobelli, O; Di Tonno, P; Francesca, F; Gallucci, M; Lapini, A; Martorana, G; Rubagotti, A, 2010)	2.01
"Bicalutamide is an oral nonsteroidal antiandrogen drug used during hormone ablation therapy for prostate cancer. "	( Comparative pharmacokinetic evaluation of two formulations of bicalutamide 50-mg tablets: an open-label, randomized-sequence, single-dose, two-period crossover study in healthy Korean male volunteers. Chung, YJ; Jang, IJ; Kim, BH; Lee, S; Shim, JH; Shin, SG; Yoon, SH; Yu, KS, 2009)	2.04
"Bicalutamide is an oral nonsteroidal antiandrogenic drug used in the treatment of prostate cancer. "	( Relative bioavailability and tolerability of two formulations of bicalutamide 50-mg tablets: a randomized-sequence, open-label, two-period crossover study in healthy Korean male subjects. Cho, JY; Jang, IJ; Lee, S; Shin, SG; Yoon, SH; Yu, KS, 2010)	2.04
"Bicalutamide (BCT) is an antiandrogenic compound belonging to Biopharmaceutics Classification System (BCS) class II drug. "	( Bicalutamide nanocrystals with improved oral bioavailability: in vitro and in vivo evaluation. Malhi, T; Mandpe, L; Pokharkar, VB, )	3.02
"Bicalutamide is an anti-androgen that is used worldwide to treat prostate cancer (CaP). "	( A study of plasma bicalutamide concentrations in hemodialysis patients. Goya, N; Ito, F; Kihara, T; Kubo, K; Nakazawa, H; Suzuki, K; Suzuki, T, 2012)	2.16
"Bicalutamide (BIC) is an alternative treatment to castration for advanced prostate cancer. "	( Effects of bicalutamide and 4OH-tamoxifen on androgen-regulated gene expression in the LNCaP cell line. Argellati, F; Boccardo, F; Mangerini, R; Pfeffer, U, 2012)	2.21
"Bicalutamide is an oral, once-daily nonsteroidal antiandrogen. "	( Bicalutamide: in early-stage prostate cancer. Carswell, CI; Figgitt, DP, 2002)	3.2
"Bicalutamide (BCLT) is a well-known non-steroidal antiandrogenic agent able to interfere with androgen receptor (AR)."	( Bicalutamide dose-dependently inhibits proliferation in human prostatic carcinoma cell lines and primary cultures. Angelucci, A; Bologna, M; Eleuterio, E; Festuccia, C; Gravina, GL; Marronaro, A; Miano, R; Muzi, P; Tubaro, A; Vicentini, C, )	2.3
"Bicalutamide is a nonsteroidal pure antiandrogen given at a dosage of 150 mg once daily as monotherapy for the treatment of early (localised or locally advanced) nonmetastatic prostate cancer. "	( Bicalutamide: clinical pharmacokinetics and metabolism. Cockshott, ID, 2004)	3.21
"Bicalutamide is a non-steroidal anti-androgen commonly used in the treatment of prostate carcinoma. "	( Microarray analysis of bicalutamide action on telomerase activity, p53 pathway and viability of prostate carcinoma cell lines. Baumforth, KR; Bouchal, J; Kolár, Z; Murray, PG; Sváchová, M; von Angerer, E, 2005)	2.08
"Bicalutamide (Casodex) is a competitive androgen receptor antagonist that inactivates androgen-regulated prostate cell growth and function, leading to cell apoptosis and inhibition of prostate cancer growth. "	( Bicalutamide 150mg: a review of its use in the treatment of locally advanced prostate cancer. Keam, SJ; Wellington, K, 2006)	3.22
"Bicalutamide (Casodex) is a competitive androgen receptor antagonist that inactivates androgen-regulated prostate cell growth and function, leading to cell apoptosis and inhibition of prostate cancer growth. "	( Spotlight on bicalutamide 150mg in the treatment of locally advanced prostate cancer. Keam, SJ; Wellington, K, 2007)	2.15
"Bicalutamide is a competitive nonsteroidal androgen receptor antagonist. "	( Treatment of bicalutamide-induced breast events. Sieber, PR, 2007)	2.15
"Bicalutamide is a non-steroidal antiandrogen used in the treatment of prostate cancer. "	( Differential mechanisms of bicalutamide-induced apoptosis in prostate cell lines. Fitzpatrick, JM; Floyd, MS; Teahan, SJ; Watson, RW, 2009)	2.09
"Bicalutamide is a pure antiandrogen that binds to rat, dog, and human prostate; the affinity compared with the natural ligand 5 alpha-dihydrotestosterone is low, but bicalutamide has an affinity for the rat androgen receptor approximately four times higher than hydroxyflutamide, the active metabolite of flutamide."	( The preclinical development of bicalutamide: pharmacodynamics and mechanism of action. Furr, BJ; Tucker, H, 1996)	1.3
"Bicalutamide is a new, potent antiandrogen with potential efficacy in the treatment of men with advanced prostate cancer. "	( A controlled trial of bicalutamide versus castration in patients with advanced prostate cancer. Bales, GT; Chodak, GW, 1996)	2.05
"Bicalutamide is a nonsteroidal competitive inhibitor of androgens at the androgen receptor. "	( High-dose bicalutamide monotherapy for the treatment of prostate cancer. Blackledge, GR, 1996)	2.14
"Bicalutamide is a potent, nonsteroidal antiandrogen with a plasma half-life consistent with a once-daily schedule. "	( Worldwide activity and safety of bicalutamide: a summary review. Blackledge, GR; Kolvenbag, GJ, 1996)	2.02
"Bicalutamide is a new antiandrogen that offers the convenience of once-daily administration, demonstrated activity in prostate cancer, and an excellent safety profile. "	( Worldwide activity and safety of bicalutamide: a summary review. Blackledge, GR; Kolvenbag, GJ, 1996)	2.02
"Bicalutamide is a new, nonsteroidal antiandrogen with a favorable toxicity profile. "	( Fulminant hepatic failure associated with bicalutamide. Chow, E; Dawson, LA; Morton, G, 1997)	2
"Bicalutamide (Casodex) is a new nonsteroidal antiandrogen developed for use in patients with prostate cancer. "	( Bicalutamide (Casodex) in the treatment of prostate cancer: history of clinical development. Blackledge, GR; Gotting-Smith, K; Kolvenbag, GJ, 1998)	3.19
"Bicalutamide, 50-mg daily, is a logical first choice for antiandrogen therapy when used in combination with an LHRH-A for the treatment of patients with advanced prostate cancer."	( Bicalutamide (Casodex) in the treatment of prostate cancer: history of clinical development. Blackledge, GR; Gotting-Smith, K; Kolvenbag, GJ, 1998)	2.46
"Bicalutamide is a nonsteroidal antiandrogen with a long elimination half-life (t1/2) that permits once-daily administration. "	( Bicalutamide in advanced prostate cancer. A review. Goa, KL; Spencer, CM, 1998)	3.19
"Bicalutamide (Casodex) is a new antiandrogen, so far approved for the treatment of prostate cancer in combinations with a GnRH agonist. "	( [Monotherapy with antiandrogens for prostatic cancer]. Sander, S, 1999)	1.75
"Bicalutamide that acts as a pure antagonist in parental LNCaP cells showed agonistic effects on AR transactivation activity in LNCaP-abl cells and was not able to block the effects of androgen in these cells."	( Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system. Bartsch, G; Culig, Z; Eder, IE; Erdel, M; Hittmair, A; Hobisch, A; Hoffmann, J; Klocker, H; Parczyk, K; Schneider, MR; Utermann, G, 1999)	1.27
"bicalutamide is an attractive alternative to castration in patients with locally advanced prostate cancer for whom immediate hormone therapy is indicated."	( Bicalutamide monotherapy compared with castration in patients with nonmetastatic locally advanced prostate cancer: 6.3 years of followup. Anderson, JB; Carroll, K; Chamberlain, M; Iversen, P; Kaisary, AV; Melezinek, I; Tammela, TL; Tyrrell, CJ; Van Poppel, H, 2000)	2.47
"Bicalutamide is an oral antiandrogen with excellent tolerance and preservation of sexual function."	( Survival of patients who had salvage castration after failure on bicalutamide monotherapy for stage (D2) prostate cancer. Blumenfrucht, M; Chang, V; Cogswell, J; Feuerman, M; Hwang, S; Kasimis, B; Kreis, W; Rae, C; Steafather, H; Wilding, G, 2000)	1.27
"Bicalutamide is an effective, non-steroidal antiandrogen, suitable for oral, once daily administration. "	( [The role of bicalutamide in the treatment of prostate cancer]. Segal, G; Stav, SY, 2002)	2.13

Excerpt	Reference	Relevance
"Bicalutamide has a more favourable side-effect profile than the other antiandrogens and is more likely to promote compliance."	( The role of antiandrogen monotherapy in the treatment of prostate cancer. Anderson, J, 2003)	1.04
"Bicalutamide 50 mg has a number of advantages compared with nilutamide and flutamide when used in combination with castration."	( Combined androgen blockade: the case for bicalutamide. Klotz, L; Schellhammer, P, 2005)	1.32
"Bicalutamide has no diuretic effect."	( Bicalutamide and the new perspectives for female pattern hair loss treatment: What dermatologists should know. Acioly, P; Barcaui, CB; Carvalho, RM; Donda, ALV; Frattini, SC; Machado, CJ; Melo, DF; Ramos, PM; Santos, LDN, 2022)	2.89
"Bicalutamide has been identified as an AR antagonist and used for treating AR+/ER- breast cancer in a phase II trial."	( Androgen Receptor Expression and Bicalutamide Antagonize Androgen Receptor Inhibit β-Catenin Transcription Complex in Estrogen Receptor-Negative Breast Cancer. Han, J; Huang, R; Jiang, Y; Li, D; Liang, X; Liu, Q; Niu, M; Panga, D; Song, Y; Sun, S; Wang, S; Wei, W; Xia, B; Zhang, G; Zhang, J; Zheng, W, 2017)	1.46
"Bicalutamide has been ceased, but 21 months later, Mr FD was still on heart failure medications, and passed away months later probably due to complications of prostate cancer."	( Bicalutamide causes heart failure in an elderly patient with prostate cancer. Guirguis, K, 2016)	2.6
"Bicalutamide (Casodex) has been used as an anti-androgen agent for prostate cancer patients during hormone ablation therapy."	( Bicalutamide inhibits androgen-mediated adhesion of prostate cancer cells exposed to ionizing radiation. Alavian, MR; Fitzgerald, TJ; Goel, HL; Languino, LR; Wang, T, 2008)	2.51
"Bicalutamide has been tested in the cell lines mentioned above in the absence and in the presence of MC18, our potent P-glycoprotein/BCRP/MRP1 inhibitor."	( Bicalutamide failure in prostate cancer treatment: involvement of Multi Drug Resistance proteins. Albo, G; Ancona, P; Berardi, F; Colabufo, NA; Contino, M; Inglese, C; Niso, M; Pagliarulo, A; Pagliarulo, V; Perrone, R, 2008)	2.51
"Bicalutamide has a more favourable side-effect profile than the other antiandrogens and is more likely to promote compliance."	( The role of antiandrogen monotherapy in the treatment of prostate cancer. Anderson, J, 2003)	1.04
"Bicalutamide 50 mg has a number of advantages compared with nilutamide and flutamide when used in combination with castration."	( Combined androgen blockade: the case for bicalutamide. Klotz, L; Schellhammer, P, 2005)	1.32
"Bicalutamide has been investigated extensively at daily doses up to 150 mg, and there is evidence of increasing blockade at doses up to this point, as evidenced by increasing suppression of prostate-specific antigen (PSA) and also improvement in response rate, both subjective and objective."	( High-dose bicalutamide monotherapy for the treatment of prostate cancer. Blackledge, GR, 1996)	1.42
"Bicalutamide has not been causally associated with problems such as interstitial pneumonitis and difficulty with light/dark adaptation seen with nilutamide, and in a 50 mg/day dosage causes a lower incidence of diarrhoea than flutamide 750 mg/day."	( Bicalutamide in advanced prostate cancer. A review. Goa, KL; Spencer, CM, 1998)	2.46
"Bicalutamide (Casodex) has been approved as a new option for the treatment of prostate cancer. "	( [A new anti-androgen, bicalutamide (Casodex), for the treatment of prostate cancer--basic clinical aspects]. Akaza, H, 1999)	2.06

Excerpt	Reference	Relevance
"Bicalutamide is able to suppress the initial PSA surge as effectively as cyproterone acetate albeit slightly delayed. "	( Bicalutamide vs cyproterone acetate in preventing flare with LHRH analogue therapy for prostate cancer--a pilot study. Benney, M; Gillatt, DA; Okeke, AA; Sugiono, M; Winkler, MH, 2005)	3.21

Excerpt	Reference	Relevance
"Bicalutamide treatment significantly decreased the PSA concentration relative to the PCa group and reached the normal level."	( The Biochemical Effects of Silver Nanoparticles and Spirulina Extract on Experimentally Induced Prostatic Cancer in Rats. AbdEl-Hamid, OM; El-Magid, ADA; Younes, MA, 2023)	1.63
"Bicalutamide treatment enhanced autophagy in LNCaP cells with increased level of autophagosome coupled with an altered cellular morphology reminiscent of neuroendocrine differentiation. "	( Does androgen-ablation therapy (AAT) associated autophagy have a pro-survival effect in LNCaP human prostate cancer cells? Bennett, HL; Fleming, JT; Leung, HY; Mandal, R; O'Prey, J; Robson, CN; Ryan, KM; Stockley, J, 2013)	1.83
"Bicalutamide-treated and vehicle-only-treated tumours were re-established in vitro, and invasion and sensitivity to docetaxel were measured."	( Androgen deprivation results in time-dependent hypoxia in LNCaP prostate tumours: informed scheduling of the bioreductive drug AQ4N improves treatment response. Byrne, NM; Camac, SN; McKeown, SR; Ming, L; Mitchell, CA; Ward, C; Waugh, DJ; Worthington, J, 2013)	1.11
"Bicalutamide treatment did not influence insulin resistance and CRP level in PCOS, and this ineffectiveness of bicalutamide on CRP levels may be the result of insulin resistance and/or high prolactin levels at this time."	( Serum C-reactive protein (CRP) levels and insulin resistance in non-obese women with polycystic ovarian syndrome, and effect of bicalutamide on hirsutism, CRP levels and insulin resistance. Aslan, C; Bahceci, M; Canoruc, N; Kidir, V; Tuzcu, A; Tuzun, Y, 2004)	1.25
"Bicalutamide treatment induced TrkA and TrkC and reduced p75NTR expression."	( In vitro and in vivo effects of bicalutamide on the expression of TrkA and P75 neurotrophin receptors in prostate carcinoma. Bologna, M; Festuccia, C; Gravina, GL; Muzi, P; Pomante, R; Ricevuto, E; Ventura, L; Vicentini, C, 2007)	1.34
"Treatment with bicalutamide provided a highly significant reduction of 42% in the risk of objective progression compared with standard care alone (9.0% versus 13.8%, hazards ratio 0.58; 95% confidence interval 0.51, 0.66; p <<0.0001)."	( Bicalutamide as immediate therapy either alone or as adjuvant to standard care of patients with localized or locally advanced prostate cancer: first analysis of the early prostate cancer program. Carroll, K; Chodak, G; Delaere, KP; Gleason, D; Iversen, P; Klimberg, I; Kolvenbag, GJ; Lukkarinen, O; McLeod, DG; Montie, J; Persson, BE; See, WA; Tammela, TL; Tyrrell, C; Vaage, S; Wallace, DM; Wirth, MP, 2002)	2.1
"Treatment with bicalutamide began in the 60th week in group 3 rats and continued for 14 weeks."	( Persistence of prostatic intraepithelial neoplasia after effective chemoprevention of microscopic prostate cancer with antiandrogen in a rat model. Akaza, H; Ideyama, Y; Kawai, K; Shirai, T; Tsukamoto, S; Yamauchi, A, 2006)	0.67
"Treatment with bicalutamide plus LHRH-A resulted in longer median survival than treatment with flutamide plus LHRH-A."	( Clinical benefits of bicalutamide compared with flutamide in combined androgen blockade for patients with advanced prostatic carcinoma: final report of a double-blind, randomized, multicenter trial. Casodex Combination Study Group. Block, NL; Kolvenbag, GJ; Patterson, AL; Sarosdy, MF; Schellenger, JJ; Schellhammer, PF; Sharifi, R; Soloway, MS; Venner, PM; Vogelzang, NJ, 1997)	0.96

Excerpt	Reference	Relevance
"001) lower incidence of diarrhea and fewer withdrawals for adverse events among bicalutamide-treated patients."	( Worldwide activity and safety of bicalutamide: a summary review. Blackledge, GR; Kolvenbag, GJ, 1996)	0.8
" This analysis could increase the information related to these adverse reactions mainly available from the published isolated cases."	( Spontaneous reporting of hepatotoxicity associated with antiandrogens: data from the Spanish pharmacovigilance system. Hidalgo, A; Manso, G; Revuelta, P; Salgueiro, E; Thole, Z, 2006)	0.33
"Liver disorders were the most common adverse reactions associated with flutamide and bicalutamide, but not with cyproterone acetate."	( Spontaneous reporting of hepatotoxicity associated with antiandrogens: data from the Spanish pharmacovigilance system. Hidalgo, A; Manso, G; Revuelta, P; Salgueiro, E; Thole, Z, 2006)	0.56
"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
" The most common adverse effects of bicalutamide are induced by its pharmacologic property of competitive androgen receptor blockade and include gynecomastia, hot flashes, fatigue, and decreased libido."	( Bicalutamide-associated fulminant hepatotoxicity. Flaig, TW; O'Bryant, CL; Utz, KJ, 2008)	2.06
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."	( Developing structure-activity relationships for the prediction of hepatotoxicity. Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010)	0.36
" Treatment discontinuation due to adverse events was more common in Arm A compared to Arm B (42 vs."	( A randomized phase II efficacy and safety study of vandetanib (ZD6474) in combination with bicalutamide versus bicalutamide alone in patients with chemotherapy naïve castration-resistant prostate cancer. Azad, AA; Beardsley, EK; Chi, KN; Chin, J; Ellard, SL; Hotte, SJ; Klotz, L; Kollmannsberger, C; Mukherjee, SD, 2014)	0.62
" Of the most common adverse events, those occurring more frequently with enzalutamide than with bicalutamide were fatigue (51 [28%] of 183 patients in the enzalutamide group vs 38 [20%] of 189 in the bicalutamide group), back pain (35 [19%] vs 34 [18%]), and hot flush (27 [15%] vs 21 [11%]); those occurring more frequently with bicalutamide were nausea (26 [14%] vs 33 [17%]), constipation (23 [13%] vs 25 [13%]), and arthralgia (18 [10%] vs 30 [16%])."	( Efficacy and safety of enzalutamide versus bicalutamide for patients with metastatic prostate cancer (TERRAIN): a randomised, double-blind, phase 2 study. Bhattacharya, S; Chowdhury, S; Hasabou, N; Heidenreich, A; Klotz, L; Shore, ND; Siemens, DR; van Os, S; Villers, A; Wang, F, 2016)	0.92
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."	( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016)	0.43
" The adverse event distribution between treatments was similar in each subgroup except for more (5% or greater difference between subgroups) atrial fibrillation, urinary tract infections, falls and decreased appetite as well as less extremity pain and hot flushing in enzalutamide treated patients 75 years old or older, and less back pain and hot flushing in bicalutamide treated patients 75 years old or older."	( Efficacy and Safety of Enzalutamide vs Bicalutamide in Younger and Older Patients with Metastatic Castration Resistant Prostate Cancer in the TERRAIN Trial. Baron, B; Chowdhury, S; Hasabou, N; Heidenreich, A; Klotz, L; Lin, P; Shore, ND; Siemens, DR; van Os, S; Villers, A; Wang, F, 2018)	0.92
"We gathered cases diagnosed with prostate cancer based on the United States Food and Drug Administration Adverse Event Reporting System (FAERS) database from 2004 to 2020."	( Analysis of adverse event of interstitial lung disease in men with prostate cancer receiving hormone therapy using the Food and Drug Administration Adverse Event Reporting System. Chen, C; Li, J; Shen, P; Wu, B; Wu, F; Xu, T; Yin, X; Yu, L, 2023)	0.91
" There is a lack of direct comparison of the therapeutic effects and adverse events between the conventional ARI (bicalutamide) and three second-generation ARIs (enzalutamide, apalutamide and darolutamide)."	( The efficacy and adverse events of conventional and second-generation androgen receptor inhibitors for castration-resistant prostate cancer: A network meta-analysis. Bi, J; Wang, J; Zhang, G; Zhang, X, 2023)	1.12
"Our network meta-analysis evaluated therapeutic effects and adverse events of the conventional ARI (bicalutamide) and the second-generation ARIs in treating CRPC."	( The efficacy and adverse events of conventional and second-generation androgen receptor inhibitors for castration-resistant prostate cancer: A network meta-analysis. Bi, J; Wang, J; Zhang, G; Zhang, X, 2023)	1.13
" Similar adverse events rate were observed among the second-generation ARIs and bicalutamide."	( The efficacy and adverse events of conventional and second-generation androgen receptor inhibitors for castration-resistant prostate cancer: A network meta-analysis. Bi, J; Wang, J; Zhang, G; Zhang, X, 2023)	1.14
" The adverse events of apalutamide were worse than the others, but no statistical significance was observed among these vital AEs."	( The efficacy and adverse events of conventional and second-generation androgen receptor inhibitors for castration-resistant prostate cancer: A network meta-analysis. Bi, J; Wang, J; Zhang, G; Zhang, X, 2023)	0.91

Excerpt	Reference	Relevance
" The S-enantiomer of bicalutamide is rapidly cleared, but the R-enantiomer has a plasma elimination half-life of about 1 week, with a tenfold plasma accumulation at all dose levels, making it suitable for a once-daily administration."	( Pharmacodynamics and pharmacokinetics of bicalutamide: defining an active dosing regimen. Denis, L; Mahler, C, 1996)	0.88
" After fasting, plasma concentrations of (R)-bicalutamide were much higher than those of (S)-bicalutamide; the mean (R)-enantiomer Cmax (734 ng mL-1) was about nine times higher than the (S)-enantiomer value (84 ng mL-1)."	( The effect of food on the pharmacokinetics of the bicalutamide ('Casodex') enantiomers. Cockshott, ID; Cooper, KJ; Oliver, SD; Young, JJ, 1997)	0.81
" Pharmacokinetic samples were taken at various time points up to 3 months, and assayed using an achiral HPLC method."	( Casodex 10-200 mg daily, used as monotherapy for the treatment of patients with advanced prostate cancer. An overview of the efficacy, tolerability and pharmacokinetics from three phase II dose-ranging studies. Casodex Study Group. Channer, K; Cockshott, ID; Denis, L; Newling, D; Soloway, M; Tyrrell, CJ, 1998)	0.3
" Casodex has a half-life of approximately 1 week, enabling once-daily dosing with no effect of age or renal impairment on its pharmacokinetics."	( Casodex 10-200 mg daily, used as monotherapy for the treatment of patients with advanced prostate cancer. An overview of the efficacy, tolerability and pharmacokinetics from three phase II dose-ranging studies. Casodex Study Group. Channer, K; Cockshott, ID; Denis, L; Newling, D; Soloway, M; Tyrrell, CJ, 1998)	0.3
"This article provides a summary of the pharmacodynamic properties of major antiandrogens as well as an extensive review of their tolerability."	( Antiandrogens: a summary review of pharmacodynamic properties and tolerability in prostate cancer therapy. De Angelis, M; De Benedetto, G; Migliari, R; Murru, M; Muscas, G; Verdacchi, T, 1999)	0.3
" The kinetics of (S)-Casodex could not be described in the majority of subjects; in the remainder the mean terminal phase half-life for both groups was less than 1 day."	( The pharmacokinetics of Casodex enantiomers in subjects with impaired liver function. Cockshott, ID; Cooper, KJ; Jones, DC; Sotaniemi, EA, 1993)	0.29
" It has a long plasma elimination half-life (1 week) and accumulates about 10-fold in plasma during daily administration."	( Bicalutamide: clinical pharmacokinetics and metabolism. Cockshott, ID, 2004)	1.77
"Systemic exposure to bicalutamide stabilised at a dose of approximately 300 mg, as determined by pharmacokinetic analysis."	( Tolerability, efficacy and pharmacokinetics of bicalutamide 300 mg, 450 mg or 600 mg as monotherapy for patients with locally advanced or metastatic prostate cancer, compared with castration. Anderson, J; Björk, T; Iversen, P; Kaisary, AV; Morris, T; Tammela, T; Tyrrell, CJ, 2006)	0.91
" ARR2 Pb-Lux mice provide a novel method for rapid pharmacodynamic evaluation of novel pharmacologic compounds designed to inhibit androgen receptor signaling."	( Transgenic mouse model for rapid pharmacodynamic evaluation of antiandrogens. Ellwood-Yen, K; Sawyers, C; Wongvipat, J, 2006)	0.33
" Significant difference was observed in main pharmacokinetic parameters of tmax, Cmax and AUC(0 --> infinity) between SMEDDS and suspension, and a two fold increase in the relative bioavailability of bicalutamide was observed with the SMEDDS compared with suspension formulation."	( High performance liquid chromatography method for the pharmacokinetic study of bicalutamide SMEDDS and suspension formulations after oral administration to rats. Asati, D; Awasthi, A; Chaurasiya, A; Jain, GK; Khar, RK; Mishra, G; Mukherjee, R; Singh, AK, 2009)	0.77
" To this end, the pharmacokinetic properties of the new (test) formulation were compared with those of the currently marketed (reference) formulation."	( Comparative pharmacokinetic evaluation of two formulations of bicalutamide 50-mg tablets: an open-label, randomized-sequence, single-dose, two-period crossover study in healthy Korean male volunteers. Chung, YJ; Jang, IJ; Kim, BH; Lee, S; Shim, JH; Shin, SG; Yoon, SH; Yu, KS, 2009)	0.59
" Serial blood samples for pharmacokinetic analysis were taken over 672 hours after dosing."	( Comparative pharmacokinetic evaluation of two formulations of bicalutamide 50-mg tablets: an open-label, randomized-sequence, single-dose, two-period crossover study in healthy Korean male volunteers. Chung, YJ; Jang, IJ; Kim, BH; Lee, S; Shim, JH; Shin, SG; Yoon, SH; Yu, KS, 2009)	0.59
" The fasting and fed states pharmacokinetic parameters AUC0-576 h, AUC0-∞, Cmax, tmax and t1/2 were determined from plasma concentration-time profile of both formulations."	( The relative bioavailability study and fasting and fed states pharmacokinetics of bicalutamide 50-mg tablets in healthy Chinese volunteers. Lu, HM; Ye, M, 2012)	0.6
" The pharmacokinetic results showed no differences in exposures to ridaforolimus with and without concomitant bicalutamide administration."	( Tolerability, safety and pharmacokinetics of ridaforolimus in combination with bicalutamide in patients with asymptomatic, metastatic castration-resistant prostate cancer (CRPC). de Bono, JS; de Wit, R; Ebbinghaus, SW; Heath, KH; Hudes, GR; Li, X; Meulenbeld, HJ; Tagawa, ST; Whang, YE; Zandvliet, AS, 2013)	0.83
" This novel DBS method has been applied to a pharmacokinetic study in mice."	( Development of an LC-MS/MS method for determination of bicalutamide on dried blood spots: application to pharmacokinetic study in mice. Kumar, A; Mullangi, R; P S, S; Vijay Kumar, S, 2015)	0.66
"After a single oral dose of 150mg bicalutamide was administered, plasma concentrations of bicalutamide were measured, and pharmacokinetic analyses were performed in 27 healthy subjects according to ABCB1 (c."	( Effects of the ABCG2 and ABCB1 drug transporter polymorphisms on the pharmacokinetics of bicalutamide in humans. Cha, YJ; Joo, HJ; Kim, KA; Lee, HM; Park, JY, 2015)	0.92
"ABCB1 polymorphisms did not affect the plasma levels of bicalutamide and the pharmacokinetic parameters did not differ among ABCB1 genotype groups."	( Effects of the ABCG2 and ABCB1 drug transporter polymorphisms on the pharmacokinetics of bicalutamide in humans. Cha, YJ; Joo, HJ; Kim, KA; Lee, HM; Park, JY, 2015)	0.88

Excerpt	Reference	Relevance
"To compare the efficacy and safety of bicalutamide and flutamide, each used in combination with luteinizing hormone-releasing analogue (LHRH-A) therapy, in patients with untreated metastatic (Stage D2) prostate cancer."	( A controlled trial of bicalutamide versus flutamide, each in combination with luteinizing hormone-releasing hormone analogue therapy, in patients with advanced prostate cancer. Casodex Combination Study Group. Block, N; Jones, J; Kolvenbag, G; Patterson, AL; Sarosdy, M; Schellhammer, P; Sharifi, R; Soloway, M; Venner, P; Vogelzang, N, 1995)	0.88
"To review the outcome of therapy with maximal androgen blockade and compare the efficacy and safety of bicalutamide and flutamide, each used in combination with luteinizing hormone-releasing hormone analogue (LHRH-A) therapy, in patients with untreated metastatic (Stage D2) prostate cancer."	( Maximal androgen blockade for patients with metastatic prostate cancer: outcome of a controlled trial of bicalutamide versus flutamide, each in combination with luteinizing hormone-releasing hormone analogue therapy. Casodex Combination Study Group. Block, N; Jones, J; Kolvenbag, G; Patterson, AL; Sarosdy, M; Schellhammer, P; Sharifi, R; Soloway, M; Venner, P; Vogelzang, N, 1996)	0.72
" Because of its efficacy and tolerability profile, together with its convenient once-daily dosing formulation, bicalutamide represents a prime candidate for antiandrogen of first choice in combination with LHRH-A therapy in the treatment of men with metastatic prostate cancer."	( Maximal androgen blockade for patients with metastatic prostate cancer: outcome of a controlled trial of bicalutamide versus flutamide, each in combination with luteinizing hormone-releasing hormone analogue therapy. Casodex Combination Study Group. Block, N; Jones, J; Kolvenbag, G; Patterson, AL; Sarosdy, M; Schellhammer, P; Sharifi, R; Soloway, M; Venner, P; Vogelzang, N, 1996)	0.72
"A randomized, multicenter trial, double-blind for antiandrogen therapy, compared the antiandrogens bicalutamide and flutamide, each combined with luteinizing hormone-releasing hormone analogue therapy (LHRH-A) in 813 patients with Stage D2 prostate carcinoma."	( A controlled trial of bicalutamide versus flutamide, each in combination with luteinizing hormone-releasing hormone analogue therapy, in patients with advanced prostate carcinoma. Analysis of time to progression. CASODEX Combination Study Group. Block, NL; Chen, Y; Kolvenbag, GJ; Patterson, AL; Sarosdy, MF; Schellhammer, PF; Sharifi, R; Soloway, MS; Venner, PM; Vogelzang, NJ, 1996)	0.83
"205 patients with previously untreated stage C/D prostate cancer were randomized (1:1) to receive once-daily bicalutamide 80 mg or placebo, each combined with a luteinizing hormone-releasing hormone (LHRH) agonist."	( Superior anti-tumor efficacy of bicalutamide 80 mg in combination with a luteinizing hormone-releasing hormone (LHRH) agonist versus LHRH agonist monotherapy as first-line treatment for advanced prostate cancer: interim results of a randomized study in Ja Akaza, H; Arai, Y; Igawa, M; Kanetake, H; Kumon, H; Matsuda, T; Naito, S; Ohashi, Y; Soeda, A; Usami, M; Yamaguchi, A, 2004)	0.82
"In Japanese patients with advanced prostate cancer, first-line treatment with bicalutamide 80 mg in combination with an LHRH agonist is superior to LHRH agonist monotherapy in terms of the antitumor response at 12 weeks, and also time to treatment failure and progression, and does not compromise treatment safety."	( Superior anti-tumor efficacy of bicalutamide 80 mg in combination with a luteinizing hormone-releasing hormone (LHRH) agonist versus LHRH agonist monotherapy as first-line treatment for advanced prostate cancer: interim results of a randomized study in Ja Akaza, H; Arai, Y; Igawa, M; Kanetake, H; Kumon, H; Matsuda, T; Naito, S; Ohashi, Y; Soeda, A; Usami, M; Yamaguchi, A, 2004)	0.84
"A total of 151 patients with prostate cancer, who were enrolled into this study from May 2001 to June 2003, were randomized to receive CAB therapy using a luteinizing hormone-releasing hormone agonist (leuprorelin) combined with a steroidal antiandrogen (chlormadinone) or a nonsteroidal antiandrogen (bicalutamide)."	( Hot flashes during androgen deprivation therapy with luteinizing hormone-releasing hormone agonist combined with steroidal or nonsteroidal antiandrogen for prostate cancer. Hakariya, H; Hara, T; Hayashi, M; Igawa, T; Iwasaki, S; Kanetake, H; Kusaba, Y; Sakai, H; Tsurusaki, T; Yura, M, 2009)	0.53
" These results suggest that the up-regulation of IGFBP3 induced by 5-FU plays an important role in the potent anti-tumor effect of 5-FU combined with anti-androgens on CRPC."	( Up-regulation of insulin-like growth factor-binding protein 3 by 5-fluorouracil (5-FU) leads to the potent anti-proliferative effect of androgen deprivation therapy combined with 5-FU in human prostate cancer cell lines. Itoh, K; Kanayama, H; Kawabata, R; Oie, S; Oka, T; Takahashi, M, 2011)	0.37
"The objective of this trial was to evaluate the clinical effects of sorafenib, a multi-targeted kinase inhibitor, in combination with androgen receptor blockade in patients with castration-resistant prostate cancer."	( A phase II study of sorafenib in combination with bicalutamide in patients with chemotherapy-naive castration resistant prostate cancer. Beardsley, EK; Chi, KN; Ellard, SL; Hotte, SJ; Kollmannsberger, C; Mukherjee, SD; North, S; Winquist, E, 2012)	0.63
" Sorafenib 400 mg twice daily was administered with bicalutamide 50 mg once daily on a 28-day cycle."	( A phase II study of sorafenib in combination with bicalutamide in patients with chemotherapy-naive castration resistant prostate cancer. Beardsley, EK; Chi, KN; Ellard, SL; Hotte, SJ; Kollmannsberger, C; Mukherjee, SD; North, S; Winquist, E, 2012)	0.88
" We report here the results of a phase I trial evaluating a humanized monoclonal antibody targeting CTLA-4, CP-675,206 (tremelimumab), in combination with androgen deprivation using an antiandrogen."	( Phase I trial of tremelimumab in combination with short-term androgen deprivation in patients with PSA-recurrent prostate cancer. Eickhoff, JC; Lang, JM; Liu, G; McNeel, DG; Smith, HA; Staab, MJ; Wilding, G, 2012)	0.38
" We evaluated safety and tolerability as well as potential drug-drug interaction of ridaforolimus, a mammalian target of rapamycin (mTOR) inhibitor, when combined with the androgen receptor inhibitor bicalutamide in patients with asymptomatic, metastatic castration-resistant prostate cancer."	( Tolerability, safety and pharmacokinetics of ridaforolimus in combination with bicalutamide in patients with asymptomatic, metastatic castration-resistant prostate cancer (CRPC). de Bono, JS; de Wit, R; Ebbinghaus, SW; Heath, KH; Hudes, GR; Li, X; Meulenbeld, HJ; Tagawa, ST; Whang, YE; Zandvliet, AS, 2013)	0.81
"Although there was no evidence of a clinically relevant pharmacological drug-drug interaction, the occurrence of dose-limiting toxicities in 3 of 11 evaluable patients at a reduced dose of ridaforolimus of 30 mg/day suggests that this combination may not be well suited for asymptomatic or minimally symptomatic prostate cancer patients."	( Tolerability, safety and pharmacokinetics of ridaforolimus in combination with bicalutamide in patients with asymptomatic, metastatic castration-resistant prostate cancer (CRPC). de Bono, JS; de Wit, R; Ebbinghaus, SW; Heath, KH; Hudes, GR; Li, X; Meulenbeld, HJ; Tagawa, ST; Whang, YE; Zandvliet, AS, 2013)	0.62
"The aim of this study was to evaluate acute adverse events and efficacy of three-dimensional intensity- modulated radiotherapy (IMRT) combined with endocrine therapy for intermediate and advanced prostate cancer."	( Intensity-modulated radiotherapy combined with endocrine therapy for intermediate and advanced prostate cancer: long-term outcome of Chinese patients. Cheng, HH; Fu, ZC; Li, DS; Lin, GS; Luo, HC, 2013)	0.39
"Sixty-seven patients were treated with three-dimensional IMRT combined with maximum androgen blockade."	( Intensity-modulated radiotherapy combined with endocrine therapy for intermediate and advanced prostate cancer: long-term outcome of Chinese patients. Cheng, HH; Fu, ZC; Li, DS; Lin, GS; Luo, HC, 2013)	0.39
"IMRT combined with endocrine therapy demonstrated promising efficacy and was well tolerated in patients with intermediate and advanced prostate cancer."	( Intensity-modulated radiotherapy combined with endocrine therapy for intermediate and advanced prostate cancer: long-term outcome of Chinese patients. Cheng, HH; Fu, ZC; Li, DS; Lin, GS; Luo, HC, 2013)	0.39
"To observe the clinical effect of tashinone IIA combined with endocrine therapy in treating advanced-stage prostate cancer."	( Clinical research of Tashinone IIA combined with endocrine therapy in treating advanced-stage prostate cancer. Li, F; Song, L; Tang, L; Tian, F; Wang, Z; Yang, J; Yu, Z, 2014)	0.4
" The aim of this study was to evaluate changes in health-related QOL in patients with locally advanced prostate cancer after intensity-modulated radiotherapy (IMRT) combined with androgen deprivation therapy."	( Long-term quality of life outcomes in patients with locally advanced prostate cancer after intensity-modulated radiotherapy combined with androgen deprivation. Cheng, HH; Cheng, LP; Fu, ZC; Li, DS; Liao, SG; Lin, GS; Luo, HC; Xu, JF; Yin, Q; Yu, QY; Zheng, WF; Zhu, JF, 2014)	0.4
" These are of particular interest since anti-androgenic biological activity has been identified in the aquatic environment and is potentially implicated in sexual disruption alone and in combination with steroid oestrogens."	( Environmental concentrations of anti-androgenic pharmaceuticals do not impact sexual disruption in fish alone or in combination with steroid oestrogens. Brian, J; Green, C; Jobling, S; Kanda, R; Scholze, M; Williams, R, 2015)	0.42
"To compare the efficacy of enzalutamide vs bicalutamide in combination with ADT in men with mHSPC, with a subset analysis of Black patients."	( Clinical Efficacy of Enzalutamide vs Bicalutamide Combined With Androgen Deprivation Therapy in Men With Metastatic Hormone-Sensitive Prostate Cancer: A Randomized Clinical Trial. Cher, ML; Chinni, S; Dickow, B; Dobson, K; Fontana, JA; Heath, EI; Heilbrun, LK; Hwang, C; Jasti, P; Monk, P; Semaan, L; Smith, D; Sonpavde, G; Tejwani, S; Vaishampayan, UN, 2021)	1.16
"The objective of this study was to compare the efficacy of abiraterone acetate with that of bicalutamide in combination with gonadotropin-releasing hormone (GnRH) antagonist treatment for patients with high-risk metastatic hormone-sensitive prostate cancer (mHSPC)."	( Abiraterone acetate versus bicalutamide in combination with gonadotropin releasing hormone antagonist therapy for high risk metastatic hormone sensitive prostate cancer. Fujihara, A; Hongo, F; Ito, S; Matsugasumi, T; Ohashi, M; Okihara, K; Shiraishi, T; Ueda, T; Ukimura, O; Yamada, Y, 2021)	1.14
"To investigate the effect of bicalutamide combined with docetaxel on the levels of prostate-specific antigen (PSA) in serum and vascular endothelial growth factor (VEGF) in patients with advanced prostate carcinoma (PCa)."	( Effect of Bicalutamide Combined with Docetaxel on Serum PSA and VEGF Levels in Patients with Advanced Prostate Carcinoma. Guo, Z; Hu, X; Liu, Z; Lv, R; Meng, L; Yan, L; Zhang, Y, 2022)	1.41
"The implementation of bicalutamide combined with docetaxel in patients with advanced PCa is effective in reducing the inflammatory expression and improving quality of life and has a higher safety profile."	( Effect of Bicalutamide Combined with Docetaxel on Serum PSA and VEGF Levels in Patients with Advanced Prostate Carcinoma. Guo, Z; Hu, X; Liu, Z; Lv, R; Meng, L; Yan, L; Zhang, Y, 2022)	1.44
" In this study, we aimed to evaluate the efficacy and safety of rezvilutamide versus bicalutamide in combination with androgen-deprivation therapy (ADT) for high-volume, metastatic, hormone-sensitive prostate cancer."	( Rezvilutamide versus bicalutamide in combination with androgen-deprivation therapy in patients with high-volume, metastatic, hormone-sensitive prostate cancer (CHART): a randomised, open-label, phase 3 trial. Chen, C; Chen, Z; Chong, T; Dong, Q; Gu, W; Guo, H; Han, W; He, D; Huang, J; Jiang, J; Jin, C; Li, H; Li, J; Liang, C; Luo, H; Ma, L; Tian, Y; Wang, Y; Xiao, J; Yang, X; Ye, D; Zhang, X; Zhou, F; Zhu, S; Zou, Q, 2022)	1.26

Excerpt	Reference	Relevance
" Casodex has been shown to be orally bioavailable and well absorbed, with a plasma half-life of around 1 week."	( Clinical progress with a new antiandrogen, Casodex (bicalutamide). Blackledge, GR, 1996)	0.54
" Clinical studies indicated that Casodex is orally bioavailable and well absorbed, with a plasma half-life of around 1 week."	( Casodex (bicalutamide): overview of a new antiandrogen developed for the treatment of prostate cancer. Blackledge, GR; Cockshott, ID; Furr, BJ, 1997)	0.71
"The oral bioavailability of two investigational formulations of bicalutamide was compared with the current clinical formulation."	( Pharmacokinetics of two novel bicalutamide formulations in healthy male volunteers. Cantarini, M; Fuhr, R; Morris, T, 2006)	0.86
"The concurrent administration of tamoxifen and bicalutamide reduces the synthesis and bioavailability of IGF-1."	( Influence of bicalutamide with or without tamoxifen or anastrozole on insulin-like growth factor 1 and binding proteins in prostate cancer patients. Battaglia, M; Bertaccini, A; Boccardo, F; Conti, G; Romagnoli, A; Rubagotti, A; Zattoni, F, )	0.76
"These data suggest that GCP, an isoflavone-enriched compound with minimal side-effects and far superior intestinal absorption rate of genistein, has significant clinical potential in combination with docetaxel, bicalutamide or targeted agents for the treatment of advanced CaP."	( Genistein combined polysaccharide enhances activity of docetaxel, bicalutamide and Src kinase inhibition in androgen-dependent and independent prostate cancer cell lines. Burich, RA; Holland, WS; Mack, PC; Tepper, C; Vinall, RL; White, RW, 2008)	0.77
" To evaluate the bioavailability of bicalutamide from bicalutamide self-microemulsifying drug delivery systems (SMEDDS) and bicalutamide suspension formulations, a sensitive, specific reversed-phase high performance liquid chromatographic (HPLC) method using ultraviolet detection was developed and validated for the analysis of bicalutamide (BCT) in rat blood plasma."	( High performance liquid chromatography method for the pharmacokinetic study of bicalutamide SMEDDS and suspension formulations after oral administration to rats. Asati, D; Awasthi, A; Chaurasiya, A; Jain, GK; Khar, RK; Mishra, G; Mukherjee, R; Singh, AK, 2009)	0.86
"This study evaluated the relative bioavailability and tolerability of the new generic formulation of bicalutamide 50-mg tablets (test) and the currently marketed formulation (reference) in healthy Korean male subjects."	( Relative bioavailability and tolerability of two formulations of bicalutamide 50-mg tablets: a randomized-sequence, open-label, two-period crossover study in healthy Korean male subjects. Cho, JY; Jang, IJ; Lee, S; Shin, SG; Yoon, SH; Yu, KS, 2010)	0.81
" It is of particular importance as poor dissolution profiles are considered to be the major limitation in bioavailability of the drug."	( Planetary ball milling and supercritical fluid technology as a way to enhance dissolution of bicalutamide. Antosik, A; Chmiel, K; Jachowicz, R; Knapik-Kowalczuk, J; Kurek, M; Paluch, M; Syrek, K; Szafraniec, J, 2017)	0.67
" Given the dissolution rate-limited absorption combined with the reduced bioavailability of bicalutamide as a BCS class II drug, the assessment of the mechanisms driving the increase in drug dissolution is of particular importance in drug development."	( Enhanced dissolution of solid dispersions containing bicalutamide subjected to mechanical stress. Antosik, A; Chmiel, K; Gawlak, K; Jachowicz, R; Knapik-Kowalczuk, J; Kurek, M; Paluch, M; Szafraniec, J, 2018)	0.95
" The findings for the co-amorphous formulation were in agreement with the pharmacokinetics data, showing a quicker onset in plasma concentration as well as a higher bioavailability for both DTX (15-fold) and BIC (3-fold) compared to the crystalline drugs alone."	( Efflux Inhibitor Bicalutamide Increases Oral Bioavailability of the Poorly Soluble Efflux Substrate Docetaxel in Co-Amorphous Anti-Cancer Combination Therapy. Bohr, A; Grohganz, H; Harmankaya, N; Löbmann, K; Nascimento, TL; Rades, T; Wang, Y; Weisser, JJ, 2019)	0.85
"Bicalutamide (BCT), an anticancer drug, suffers from dissolution rate limited bioavailability and poor micromeritic properties."	( Spherical agglomeration to improve dissolution and micromeritic properties of an anticancer drug, Bicalutamide. Dalvadi, H; Parmar, K; Yadav, S, 2019)	2.17
"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
"The result of the present study show that the method developed is a simple, fast and precise method and is used in bioavailability and bioequivalence studies as well as during routine therapeutic drug monitoring of niclosamide and bicalutamide."	( A simultaneous liquid chromatographic analysis of niclosamide and bicalutamide in rat plasma by protein precipitation extraction. Annegowda, HV; Chaitra, VM; Chetan, IA; Majumder, M; Ramesh, B; Sagheer Ahmed, S, 2022)	1.14

Excerpt	Relevance	Reference
" doses and during daily oral dosing to male and female rats and male dogs."	( The pharmacokinetics of Casodex in laboratory animals. Cockshott, ID; Cooper, KJ; Plummer, GF; Warwick, MJ, 1991)	0.28
"Although a dosage of 50 mg of bicalutamide once daily was not as effective as castration, the favorable quality of life outcomes and the low incidence of nonhormonal adverse events provide reasons to evaluate bicalutamide, as a single therapeutic agent, at higher doses."	( Single-agent therapy with bicalutamide: a comparison with medical or surgical castration in the treatment of advanced prostate carcinoma. Block, NL; Chodak, G; Kasimis, B; Kennealey, GT; Macramalla, E; Sharifi, R, 1995)	0.88
"Casodex, a new nonsteroidal antiandrogen, was investigated in this double-blind, randomized, placebo-controlled study comprising 28 evaluable patients with benign prostatic hyperplasia, who received Casodex at a dosage of 50 mg daily or a placebo for 24 weeks."	( Safety, side effects and patient acceptance of the antiandrogen Casodex in the treatment of benign prostatic hyperplasia. Eri, LM; Tveter, KJ, 1994)	0.29
"The effect of the nonsteroidal antiandrogen Casodex (176334) on a number of risk factors for cardiovascular diseases was investigated in a double-blind, randomized, placebo-controlled study comprising 27 evaluable patients with benign prostatic hyperplasia who received either placebo or Casodex at a dosage of 50 mg daily for 24 weeks."	( Effects of the nonsteroidal antiandrogen Casodex on lipoproteins, fibrinogen and plasminogen activator inhibitor in patients with benign prostatic hyperplasia. Eri, LM; Urdal, P, 1995)	0.29
" The safety and efficacy of Casodex at a dosage of 50 mg."	( A prospective, placebo-controlled study of the antiandrogen Casodex as treatment for patients with benign prostatic hyperplasia. Eri, LM; Tveter, KJ, 1993)	0.29
" Because of its efficacy and tolerability profile, together with its convenient once-daily dosing formulation, bicalutamide represents a prime candidate for antiandrogen of first choice in combination with LHRH-A therapy in the treatment of men with metastatic prostate cancer."	( Maximal androgen blockade for patients with metastatic prostate cancer: outcome of a controlled trial of bicalutamide versus flutamide, each in combination with luteinizing hormone-releasing hormone analogue therapy. Casodex Combination Study Group. Block, N; Jones, J; Kolvenbag, G; Patterson, AL; Sarosdy, M; Schellhammer, P; Sharifi, R; Soloway, M; Venner, P; Vogelzang, N, 1996)	0.72
" The specific aim was to demonstrate pharmacological activity, which would translate into clinical efficacy, good tolerability in the context of its use, oral availability, a convenient and forgiving dosing regimen, and clinical acceptability."	( Clinical progress with a new antiandrogen, Casodex (bicalutamide). Blackledge, GR, 1996)	0.54
" The statistically significant changes were small in absolute terms and showed no dose-response relationship."	( Absence of hepatic enzyme induction in prostate cancer patients receiving 'Casodex' (bicalutamide). Kaisary, A; Klarskov, P; McKillop, D, 1996)	0.52
"The toxicological profile of bicalutamide in animals following acute and chronic dosing is closely associated with the drug's non-steroidal anti-androgenic pharmacological activity."	( An overview of animal toxicology studies with bicalutamide (ICI 176,334). Betton, GR; Imai, M; Iswaran, TJ; Siddall, RA, 1997)	0.85
" The observed slightly higher values of Cmax for (R)-bicalutamide (14%) and (S)-bicalutamide (19%), when dosing with food, achieved statistical significance."	( The effect of food on the pharmacokinetics of the bicalutamide ('Casodex') enantiomers. Cockshott, ID; Cooper, KJ; Oliver, SD; Young, JJ, 1997)	0.8
"For both flutamide and Casodex, no consistent difference was found between the effects of once daily and thrice daily oral dosing in the rat."	( Daily dosing with flutamide or Casodex exerts maximal antiandrogenic activity. Candas, B; Chen, C; Labrie, C; Labrie, F; Luo, S; Martel, C; Singh, SM, 1997)	0.3
" Another finding is that once daily dosing with flutamide exhibits an effectiveness comparable to thrice daily dosing; such data may have potential significance in facilitating compliance by administration of flutamide once daily instead of the current thrice daily schedule in men."	( Daily dosing with flutamide or Casodex exerts maximal antiandrogenic activity. Candas, B; Chen, C; Labrie, C; Labrie, F; Luo, S; Martel, C; Singh, SM, 1997)	0.3
"To evaluate the efficacy, tolerability, endocrinological effects and the pharmacokinetics of Casodex, when given as monotherapy during daily dosing of 10-200 mg to patients with advanced prostate cancer."	( Casodex 10-200 mg daily, used as monotherapy for the treatment of patients with advanced prostate cancer. An overview of the efficacy, tolerability and pharmacokinetics from three phase II dose-ranging studies. Casodex Study Group. Channer, K; Cockshott, ID; Denis, L; Newling, D; Soloway, M; Tyrrell, CJ, 1998)	0.3
" Casodex has a half-life of approximately 1 week, enabling once-daily dosing with no effect of age or renal impairment on its pharmacokinetics."	( Casodex 10-200 mg daily, used as monotherapy for the treatment of patients with advanced prostate cancer. An overview of the efficacy, tolerability and pharmacokinetics from three phase II dose-ranging studies. Casodex Study Group. Channer, K; Cockshott, ID; Denis, L; Newling, D; Soloway, M; Tyrrell, CJ, 1998)	0.3
" Although early trials demonstrated clinical benefits with bicalutamide 50 mg/day as monotherapy, the drug in this dosage is less effective than castration."	( Bicalutamide in advanced prostate cancer. A review. Goa, KL; Spencer, CM, 1998)	1.99
" Assuming that each modality is equally effective, emphasis should be placed on increasing patient tolerance and compliance by the use of long-acting, nontoxic treatments with simple dosing regimens and minimal side effects."	( Androgen deprivation for prostatic carcinoma: a rationale for choosing components. Chatelain, C; Fourcade, RO, 1998)	0.3
" Bicalutamide is available in a convenient one tablet, once-a-day dosing regimen, is at least as effective as flutamide and is better tolerated in terms of diarrhea."	( Which is the optimal antiandrogen for use in combined androgen blockade of advanced prostate cancer? The transition from a first- to second-generation antiandrogen. Sarosdy, MF, 1999)	1.21
" Bicalutamide is also a nonsteroidal anti-androgen that offers the advantages of reduced dosage amounts and reduction in side effects."	( Anti-androgens and other hormonal therapies for prostate cancer. Richie, JP, 1999)	1.21
" Bicalutamide is not associated with interstitial pneumonitis and difficulty with light/dark adaptation seen with nilutamide, and in 50 mg/day dosage causes a lower incidence of diarrhea than flutamide 750 mg/day."	( [The role of bicalutamide in the treatment of prostate cancer]. Segal, G; Stav, SY, 2002)	1.59
"The overall results indicate that bicalutamide administered as a 50-mg daily dosage in combination with castration is a well-tolerated therapy for the treatment of patients with advanced prostate cancer."	( Tolerability assessment of maximal androgen blockade with 50 mg daily of bicalutamide and castration in patients with advanced prostate cancer. Chiang, YJ; Chu, SH; Chuang, CK; Lin, MH; Lin, SJ; Wei, TY; Wu, CT, 2002)	0.83
"Bicalutamide is a nonsteroidal pure antiandrogen given at a dosage of 150 mg once daily as monotherapy for the treatment of early (localised or locally advanced) nonmetastatic prostate cancer."	( Bicalutamide: clinical pharmacokinetics and metabolism. Cockshott, ID, 2004)	3.21
"A macro-simulation model was developed to compare the cost-effectiveness of 2 interventions for stage D2 prostate cancer, 1) CAB with bicalutamide 50 mg per day and monthly dosing of an LH-RHa or 2) monthly LH-RH agonist therapy."	( The cost-effectiveness of combined androgen blockade with bicalutamide and luteinizing hormone releasing hormone agonist in men with metastatic prostate cancer. Clarke, L; Gandhi, S; Hirsch, M; Penson, DF; Ramsey, S; Veenstra, D, 2005)	0.78
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."	( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, )	0.13
" 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
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."	( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011)	0.37
" The plasma R-bicalutamide levels on the non-dialysis day were measured in 2 patients (patients 1 and 2) immediately before dosing and 8 and 24 h after dosing."	( A study of plasma bicalutamide concentrations in hemodialysis patients. Goya, N; Ito, F; Kihara, T; Kubo, K; Nakazawa, H; Suzuki, K; Suzuki, T, 2012)	1.07
" Using a daily dosing regimen with lead-in, concurrent, and post-XRT therapy, the recommended phase 2 dose of sunitinib is 25 mg daily."	( Sunitinib plus androgen deprivation and radiation therapy for patients with localized high-risk prostate cancer: results from a multi-institutional phase 1 study. Corn, PG; DePetrillo, TA; Heath, E; Kuban, D; Maier, J; Mathew, P; Meyn, R; Song, DY, 2013)	0.39
" After decreasing his anti-androgen dosage and starting a specified regimen of phosphodiesterase type 5 inhibitor therapy, his serum PSA levels were found to be elevated."	( Prostate cancer risk after anti-androgen treatment for priapism. Burnett, AL; Goetz, T, 2014)	0.4
" In dose-response F2H experiments, we compared the potencies of abiraterone, bicalutamide, enzalutamide, flutamide, and galeterone/TOK-001 to prevent the dihydrotestosterone-induced N/C interaction in wt AR."	( The fluorescent two-hybrid assay for live-cell profiling of androgen receptor modulators. Bogner, J; Hickson, I; Romer, T; Yurlova, L; Zolghadr, K, 2017)	0.68
"Many anti-cancer drugs are difficult to formulate into an oral dosage form because they are both poorly water-soluble and show poor permeability, the latter often as a result of being an intestinal efflux pump substrate."	( Efflux Inhibitor Bicalutamide Increases Oral Bioavailability of the Poorly Soluble Efflux Substrate Docetaxel in Co-Amorphous Anti-Cancer Combination Therapy. Bohr, A; Grohganz, H; Harmankaya, N; Löbmann, K; Nascimento, TL; Rades, T; Wang, Y; Weisser, JJ, 2019)	0.85
" This approach gives the opportunity to modify tablet properties in a wide range, especially the dissolution rate, by producing dosage forms with a complex design."	( Speed it up, slow it down…An issue of bicalutamide release from 3D printed tablets. Czech, A; Gawlak, K; Jachowicz, R; Jamróz, W; Knapik-Kowalczuk, J; Kurek, M; Leszczyński, B; Paluch, M; Szafraniec-Szczęsny, J; Wróbel, A, 2020)	0.83
" These include the use of multifactorial data analysis identifying correlations between the components and dosage form properties, laboratory and production process parameters with respect to the API liberation Example of such API is bicalutamide."	( Multivariate analysis in the development of bioequivalent tablets containing bicalutamide. Doležel, P; Farkaš, P; Franc, A; Goněc, R; Sova, P, 2021)	1.03
"Radiation dose-response viability and clonogenic assays showed that apalutamide had a stronger radio-sensitising activity for all three cell lines."	( Apalutamide radio-sensitisation of prostate cancer. Giatromanolaki, A; Kakouratos, C; Kalamida, D; Koukourakis, MI; Lamprou, I; Nanos, C; Xanthopoulou, E, 2021)	0.62
"05) were significantly decreased after two different dosage of Bicalutamide treatment."	( Bicalutamide, an androgen receptor antagonist, effectively alleviate allergic rhinitis via suppression of PI3K-PKB activity. Cheng, L; Ma, X; Wu, G; Wu, X; Zhang, Q; Zhang, Y, 2023)	2.59

Class	Description
(trifluoromethyl)benzenes	An organofluorine compound that is (trifluoromethyl)benzene and derivatives arising from substitution of one or more of the phenyl hydrogens.
monocarboxylic acid amide	A carboxamide derived from a monocarboxylic acid.
monofluorobenzenes	Any member of the class of fluorobenzenes containing a mono- or poly-substituted benzene ring carrying a single fluorine substitutent.
nitrile	A compound having the structure RC#N; thus a C-substituted derivative of hydrocyanic acid, HC#N. In systematic nomenclature, the suffix nitrile denotes the triply bound #N atom, not the carbon atom attached to it.
sulfone	An organosulfur compound having the structure RS(=O)2R (R =/= H).
tertiary alcohol	A tertiary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has three other carbon atoms attached to it.
[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	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Beta-lactamase	Escherichia coli K-12	Potency	89.1251	0.0447	17.8581	100.0000	AID485294
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	0.3981	0.1000	20.8793	79.4328	AID588453
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	25.9956	0.0060	38.0041	19,952.5996	AID1159521; AID1159523
ATAD5 protein, partial	Homo sapiens (human)	Potency	20.5878	0.0041	10.8903	31.5287	AID493106
TDP1 protein	Homo sapiens (human)	Potency	12.7781	0.0008	11.3822	44.6684	AID686978; AID686979
GLI family zinc finger 3	Homo sapiens (human)	Potency	15.1054	0.0007	14.5928	83.7951	AID1259369; AID1259392
AR protein	Homo sapiens (human)	Potency	11.8812	0.0002	21.2231	8,912.5098	AID1259243; AID1259247; AID1259381; AID743035; AID743040; AID743042; AID743054; AID743063
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	50.3755	0.0006	57.9133	22,387.1992	AID1259378
progesterone receptor	Homo sapiens (human)	Potency	1.1278	0.0004	17.9460	75.1148	AID1346795
EWS/FLI fusion protein	Homo sapiens (human)	Potency	2.3239	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	28.5787	0.0008	17.5051	59.3239	AID1159527
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	22.9261	0.0015	30.6073	15,848.9004	AID1224819; AID1224820; AID1224821; AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptor	Homo sapiens (human)	Potency	31.7848	0.0054	28.0263	1,258.9301	AID1346982
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	29.5346	0.0002	29.3054	16,493.5996	AID1259244; AID1259248; AID743069; AID743075; AID743078; AID743079; AID743080; AID743091
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	15.6793	0.0010	19.4141	70.9645	AID743140
arylsulfatase A	Homo sapiens (human)	Potency	4.7755	1.0691	13.9551	37.9330	AID720538
aryl hydrocarbon receptor	Homo sapiens (human)	Potency	29.8493	0.0007	23.0674	1,258.9301	AID743085
activating transcription factor 6	Homo sapiens (human)	Potency	32.0659	0.1434	27.6121	59.8106	AID1159516
nuclear receptor subfamily 1, group I, member 2	Rattus norvegicus (Norway rat)	Potency	10.0000	0.1000	9.1916	31.6228	AID1346983
chromobox protein homolog 1	Homo sapiens (human)	Potency	0.0377	0.0060	26.1688	89.1251	AID488953
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	27.8230	0.0003	23.4451	159.6830	AID743065; AID743067
tyrosine-protein kinase Yes	Homo sapiens (human)	Potency	21.7676	0.0000	5.0182	79.2586	AID686947
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	23.6583	0.0006	27.2152	1,122.0200	AID743202; AID743219
nuclear receptor ROR-gamma isoform 1	Mus musculus (house mouse)	Potency	31.6228	0.0079	8.2332	1,122.0200	AID2551
Voltage-dependent calcium channel gamma-2 subunit	Mus musculus (house mouse)	Potency	31.7848	0.0015	57.7890	15,848.9004	AID1259244
Cellular tumor antigen p53	Homo sapiens (human)	Potency	7.4978	0.0023	19.5956	74.0614	AID651631
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Potency	31.7848	0.0015	51.7393	15,848.9004	AID1259244
[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)
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	133.0000	0.6315	4.4531	9.3000	AID1473740
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50 (µMol)	133.0000	0.2000	5.6774	10.0000	AID1473741
Bile salt export pump	Homo sapiens (human)	IC50 (µMol)	54.4500	0.1100	7.1903	10.0000	AID1443986; AID1473738
Estrogen receptor	Homo sapiens (human)	Ki	100.0000	0.0000	0.4229	7.9070	AID257786
Glucocorticoid receptor	Homo sapiens (human)	Ki	100.0000	0.0001	0.3863	7.0010	AID257785
Progesterone receptor	Oryctolagus cuniculus (rabbit)	IC50 (µMol)	5.6000	0.4400	3.0200	5.6000	AID578353; AID626474
Progesterone receptor	Homo sapiens (human)	IC50 (µMol)	1.8190	0.0000	0.5807	10.0000	AID162117
Glucocorticoid receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	320.0000	0.0001	0.3975	6.0000	AID578355; AID626476
Androgen receptor	Homo sapiens (human)	IC50 (µMol)	3.3371	0.0000	0.8753	10.0000	AID1198071; AID1198072; AID1249995; AID1430111; AID1751744; AID1797749; AID1799354; AID1885040; AID1885078; AID1885121; AID241409; AID248278; AID248385; AID248615; AID248616; AID248693; AID248905; AID253471; AID257779; AID284206; AID284208; AID290229; AID301365; AID301367; AID316695; AID319590; AID319592; AID331662; AID38968; AID38975; AID38983; AID38985; AID38992; AID478366; AID478372; AID493501; AID493503; AID515859; AID539142; AID539145; AID639076; AID639077; AID639078; AID639152; AID639153; AID648200; AID648202; AID648203; AID720861; AID731982; AID731983; AID731984; AID731985; AID756280; AID777284; AID777285
Androgen receptor	Homo sapiens (human)	Ki	0.4925	0.0002	0.4240	7.2000	AID1233505; AID1249994; AID1797738; AID1797740; AID1797749; AID1800104; AID1872310; AID238631; AID238934; AID238961; AID239156; AID253455; AID257782; AID290231; AID316694; AID319591; AID331664; AID39001; AID39008; AID39147; AID493500
Androgen receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	53.9307	0.0010	1.9794	14.1600	AID1569748; AID1797749; AID265578; AID276317; AID578352; AID626476
Androgen receptor	Rattus norvegicus (Norway rat)	Ki	1.5512	0.0003	1.2185	8.9270	AID1751743; AID1797749; AID257783
Androgen receptor	Mus musculus (house mouse)	IC50 (µMol)	1.8350	0.0010	0.8750	3.0000	AID527639; AID730424
Mineralocorticoid receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	680.0000	0.0398	0.8652	2.1000	AID578356; AID626477
Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)	IC50 (µMol)	0.1200	0.0026	1.7646	9.3000	AID639077
Progesterone receptor	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.8900	0.8900	0.8900	0.8900	AID1797749
Progesterone receptor	Rattus norvegicus (Norway rat)	Ki	3.6082	0.0140	3.6082	7.2000	AID1797749; AID257784
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	133.0000	2.4100	6.3433	10.0000	AID1473739
ALK tyrosine kinase receptor	Homo sapiens (human)	Ki	0.0700	0.0001	0.2014	3.7000	AID1797738
[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)	EC50 (µMol)	5.9261	0.0000	0.2079	4.3000	AID1199395; AID1199396; AID319588; AID38805; AID639154; AID639155; AID639156; AID648204; AID648205; AID731980; AID731981; AID754108; AID754109
[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)	EC5 (µMol)	0.0850	0.0001	0.0512	0.2000	AID478367; AID478368; AID539141
Androgen receptor	Homo sapiens (human)	FI5	0.4850	0.2000	0.5425	1.0000	AID284207; AID301366
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
prostaglandin secretion	Multidrug resistance-associated protein 4	Homo sapiens (human)
cilium assembly	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet degranulation	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
bile acid and bile salt transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
cAMP transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 4	Homo sapiens (human)
guanine nucleotide transmembrane transport	Multidrug resistance-associated protein 4	Homo sapiens (human)
fatty acid metabolic process	Bile salt export pump	Homo sapiens (human)
bile acid biosynthetic process	Bile salt export pump	Homo sapiens (human)
xenobiotic metabolic process	Bile salt export pump	Homo sapiens (human)
xenobiotic transmembrane transport	Bile salt export pump	Homo sapiens (human)
response to oxidative stress	Bile salt export pump	Homo sapiens (human)
bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
response to organic cyclic compound	Bile salt export pump	Homo sapiens (human)
bile acid and bile salt transport	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transport	Bile salt export pump	Homo sapiens (human)
protein ubiquitination	Bile salt export pump	Homo sapiens (human)
regulation of fatty acid beta-oxidation	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transport	Bile salt export pump	Homo sapiens (human)
bile acid signaling pathway	Bile salt export pump	Homo sapiens (human)
cholesterol homeostasis	Bile salt export pump	Homo sapiens (human)
response to estrogen	Bile salt export pump	Homo sapiens (human)
response to ethanol	Bile salt export pump	Homo sapiens (human)
xenobiotic export from cell	Bile salt export pump	Homo sapiens (human)
lipid homeostasis	Bile salt export pump	Homo sapiens (human)
phospholipid homeostasis	Bile salt export pump	Homo sapiens (human)
positive regulation of bile acid secretion	Bile salt export pump	Homo sapiens (human)
regulation of bile acid metabolic process	Bile salt export pump	Homo sapiens (human)
transmembrane transport	Bile salt export pump	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
antral ovarian follicle growth	Estrogen receptor	Homo sapiens (human)
epithelial cell development	Estrogen receptor	Homo sapiens (human)
chromatin remodeling	Estrogen receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Estrogen receptor	Homo sapiens (human)
signal transduction	Estrogen receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Estrogen receptor	Homo sapiens (human)
androgen metabolic process	Estrogen receptor	Homo sapiens (human)
male gonad development	Estrogen receptor	Homo sapiens (human)
negative regulation of gene expression	Estrogen receptor	Homo sapiens (human)
positive regulation of phospholipase C activity	Estrogen receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
intracellular estrogen receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
response to estradiol	Estrogen receptor	Homo sapiens (human)
regulation of toll-like receptor signaling pathway	Estrogen receptor	Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic process	Estrogen receptor	Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transduction	Estrogen receptor	Homo sapiens (human)
negative regulation of DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
response to estrogen	Estrogen receptor	Homo sapiens (human)
positive regulation of DNA-templated transcription	Estrogen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
fibroblast proliferation	Estrogen receptor	Homo sapiens (human)
positive regulation of fibroblast proliferation	Estrogen receptor	Homo sapiens (human)
stem cell differentiation	Estrogen receptor	Homo sapiens (human)
regulation of inflammatory response	Estrogen receptor	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
RNA polymerase II preinitiation complex assembly	Estrogen receptor	Homo sapiens (human)
uterus development	Estrogen receptor	Homo sapiens (human)
vagina development	Estrogen receptor	Homo sapiens (human)
prostate epithelial cord elongation	Estrogen receptor	Homo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis	Estrogen receptor	Homo sapiens (human)
regulation of branching involved in prostate gland morphogenesis	Estrogen receptor	Homo sapiens (human)
mammary gland branching involved in pregnancy	Estrogen receptor	Homo sapiens (human)
mammary gland alveolus development	Estrogen receptor	Homo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongation	Estrogen receptor	Homo sapiens (human)
protein localization to chromatin	Estrogen receptor	Homo sapiens (human)
cellular response to estradiol stimulus	Estrogen receptor	Homo sapiens (human)
negative regulation of miRNA transcription	Estrogen receptor	Homo sapiens (human)
regulation of epithelial cell apoptotic process	Estrogen receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Estrogen receptor	Homo sapiens (human)
cellular response to estrogen stimulus	Estrogen receptor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Glucocorticoid receptor	Homo sapiens (human)
regulation of gluconeogenesis	Glucocorticoid receptor	Homo sapiens (human)
chromatin organization	Glucocorticoid receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Glucocorticoid receptor	Homo sapiens (human)
apoptotic process	Glucocorticoid receptor	Homo sapiens (human)
chromosome segregation	Glucocorticoid receptor	Homo sapiens (human)
signal transduction	Glucocorticoid receptor	Homo sapiens (human)
glucocorticoid metabolic process	Glucocorticoid receptor	Homo sapiens (human)
gene expression	Glucocorticoid receptor	Homo sapiens (human)
microglia differentiation	Glucocorticoid receptor	Homo sapiens (human)
adrenal gland development	Glucocorticoid receptor	Homo sapiens (human)
regulation of glucocorticoid biosynthetic process	Glucocorticoid receptor	Homo sapiens (human)
synaptic transmission, glutamatergic	Glucocorticoid receptor	Homo sapiens (human)
maternal behavior	Glucocorticoid receptor	Homo sapiens (human)
intracellular glucocorticoid receptor signaling pathway	Glucocorticoid receptor	Homo sapiens (human)
glucocorticoid mediated signaling pathway	Glucocorticoid receptor	Homo sapiens (human)
positive regulation of neuron apoptotic process	Glucocorticoid receptor	Homo sapiens (human)
negative regulation of DNA-templated transcription	Glucocorticoid receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Glucocorticoid receptor	Homo sapiens (human)
astrocyte differentiation	Glucocorticoid receptor	Homo sapiens (human)
cell division	Glucocorticoid receptor	Homo sapiens (human)
mammary gland duct morphogenesis	Glucocorticoid receptor	Homo sapiens (human)
motor behavior	Glucocorticoid receptor	Homo sapiens (human)
cellular response to steroid hormone stimulus	Glucocorticoid receptor	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Glucocorticoid receptor	Homo sapiens (human)
cellular response to dexamethasone stimulus	Glucocorticoid receptor	Homo sapiens (human)
cellular response to transforming growth factor beta stimulus	Glucocorticoid receptor	Homo sapiens (human)
neuroinflammatory response	Glucocorticoid receptor	Homo sapiens (human)
positive regulation of miRNA transcription	Glucocorticoid receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Glucocorticoid receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Glucocorticoid receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle G2/M phase transition	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
ER overload response	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
in utero embryonic development	Cellular tumor antigen p53	Homo sapiens (human)
somitogenesis	Cellular tumor antigen p53	Homo sapiens (human)
release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic progenitor cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
T cell proliferation involved in immune response	Cellular tumor antigen p53	Homo sapiens (human)
B cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
T cell lineage commitment	Cellular tumor antigen p53	Homo sapiens (human)
response to ischemia	Cellular tumor antigen p53	Homo sapiens (human)
nucleotide-excision repair	Cellular tumor antigen p53	Homo sapiens (human)
double-strand break repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
protein import into nucleus	Cellular tumor antigen p53	Homo sapiens (human)
autophagy	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrest	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
Ras protein signal transduction	Cellular tumor antigen p53	Homo sapiens (human)
gastrulation	Cellular tumor antigen p53	Homo sapiens (human)
neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of neuroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
protein localization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA replication	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell population proliferation	Cellular tumor antigen p53	Homo sapiens (human)
determination of adult lifespan	Cellular tumor antigen p53	Homo sapiens (human)
mRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
rRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
response to salt stress	Cellular tumor antigen p53	Homo sapiens (human)
response to inorganic substance	Cellular tumor antigen p53	Homo sapiens (human)
response to X-ray	Cellular tumor antigen p53	Homo sapiens (human)
response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of gene expression	Cellular tumor antigen p53	Homo sapiens (human)
cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
viral process	Cellular tumor antigen p53	Homo sapiens (human)
glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
cerebellum development	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of cell growth	Cellular tumor antigen p53	Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
mitotic G1 DNA damage checkpoint signaling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of telomere maintenance via telomerase	Cellular tumor antigen p53	Homo sapiens (human)
T cell differentiation in thymus	Cellular tumor antigen p53	Homo sapiens (human)
tumor necrosis factor-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
regulation of tissue remodeling	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV	Cellular tumor antigen p53	Homo sapiens (human)
multicellular organism growth	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of mitochondrial membrane permeability	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to glucose starvation	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
entrainment of circadian clock by photoperiod	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial DNA repair	Cellular tumor antigen p53	Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
transcription initiation-coupled chromatin remodeling	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of proteolysis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of DNA-templated transcription	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Cellular tumor antigen p53	Homo sapiens (human)
response to antibiotic	Cellular tumor antigen p53	Homo sapiens (human)
fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of fibroblast proliferation	Cellular tumor antigen p53	Homo sapiens (human)
circadian behavior	Cellular tumor antigen p53	Homo sapiens (human)
bone marrow development	Cellular tumor antigen p53	Homo sapiens (human)
embryonic organ development	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Cellular tumor antigen p53	Homo sapiens (human)
protein stabilization	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of helicase activity	Cellular tumor antigen p53	Homo sapiens (human)
protein tetramerization	Cellular tumor antigen p53	Homo sapiens (human)
chromosome organization	Cellular tumor antigen p53	Homo sapiens (human)
neuron apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of cell cycle	Cellular tumor antigen p53	Homo sapiens (human)
hematopoietic stem cell differentiation	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glial cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
type II interferon-mediated signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
cardiac septum morphogenesis	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of programmed necrotic cell death	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex assembly	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stress	Cellular tumor antigen p53	Homo sapiens (human)
thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of thymocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
necroptotic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to xenobiotic stimulus	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to ionizing radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to gamma radiation	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to UV-C	Cellular tumor antigen p53	Homo sapiens (human)
stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
signal transduction by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
cellular response to actinomycin D	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondria	Cellular tumor antigen p53	Homo sapiens (human)
cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
replicative senescence	Cellular tumor antigen p53	Homo sapiens (human)
oxidative stress-induced premature senescence	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
oligodendrocyte apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of execution phase of apoptosis	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of mitophagy	Cellular tumor antigen p53	Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediator	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of miRNA transcription	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of G1 to G0 transition	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of miRNA processing	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvate	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of pentose-phosphate shunt	Cellular tumor antigen p53	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxia	Cellular tumor antigen p53	Homo sapiens (human)
regulation of fibroblast apoptotic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Cellular tumor antigen p53	Homo sapiens (human)
negative regulation of stem cell proliferation	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of cellular senescence	Cellular tumor antigen p53	Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathway	Cellular tumor antigen p53	Homo sapiens (human)
ovulation from ovarian follicle	Progesterone receptor	Homo sapiens (human)
glandular epithelial cell maturation	Progesterone receptor	Homo sapiens (human)
regulation of DNA-templated transcription	Progesterone receptor	Homo sapiens (human)
signal transduction	Progesterone receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Progesterone receptor	Homo sapiens (human)
cell-cell signaling	Progesterone receptor	Homo sapiens (human)
positive regulation of gene expression	Progesterone receptor	Homo sapiens (human)
negative regulation of gene expression	Progesterone receptor	Homo sapiens (human)
paracrine signaling	Progesterone receptor	Homo sapiens (human)
negative regulation of phosphorylation	Progesterone receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Progesterone receptor	Homo sapiens (human)
lung alveolus development	Progesterone receptor	Homo sapiens (human)
regulation of epithelial cell proliferation	Progesterone receptor	Homo sapiens (human)
progesterone receptor signaling pathway	Progesterone receptor	Homo sapiens (human)
maintenance of protein location in nucleus	Progesterone receptor	Homo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesis	Progesterone receptor	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Progesterone receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Progesterone receptor	Homo sapiens (human)
negative regulation of transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
MAPK cascade	Androgen receptor	Homo sapiens (human)
in utero embryonic development	Androgen receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure	Androgen receptor	Homo sapiens (human)
epithelial cell morphogenesis	Androgen receptor	Homo sapiens (human)
transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
signal transduction	Androgen receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Androgen receptor	Homo sapiens (human)
cell-cell signaling	Androgen receptor	Homo sapiens (human)
spermatogenesis	Androgen receptor	Homo sapiens (human)
single fertilization	Androgen receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Androgen receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Androgen receptor	Homo sapiens (human)
positive regulation of gene expression	Androgen receptor	Homo sapiens (human)
male somatic sex determination	Androgen receptor	Homo sapiens (human)
intracellular estrogen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
androgen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
intracellular receptor signaling pathway	Androgen receptor	Homo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
Leydig cell differentiation	Androgen receptor	Homo sapiens (human)
multicellular organism growth	Androgen receptor	Homo sapiens (human)
positive regulation of phosphorylation	Androgen receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Androgen receptor	Homo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathway	Androgen receptor	Homo sapiens (human)
positive regulation of cell differentiation	Androgen receptor	Homo sapiens (human)
negative regulation of integrin biosynthetic process	Androgen receptor	Homo sapiens (human)
positive regulation of integrin biosynthetic process	Androgen receptor	Homo sapiens (human)
positive regulation of DNA-templated transcription	Androgen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase III	Androgen receptor	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	Androgen receptor	Homo sapiens (human)
regulation of developmental growth	Androgen receptor	Homo sapiens (human)
animal organ formation	Androgen receptor	Homo sapiens (human)
male genitalia morphogenesis	Androgen receptor	Homo sapiens (human)
epithelial cell proliferation	Androgen receptor	Homo sapiens (human)
negative regulation of epithelial cell proliferation	Androgen receptor	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Androgen receptor	Homo sapiens (human)
activation of prostate induction by androgen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
morphogenesis of an epithelial fold	Androgen receptor	Homo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesis	Androgen receptor	Homo sapiens (human)
prostate gland growth	Androgen receptor	Homo sapiens (human)
prostate gland epithelium morphogenesis	Androgen receptor	Homo sapiens (human)
epithelial cell differentiation involved in prostate gland development	Androgen receptor	Homo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesis	Androgen receptor	Homo sapiens (human)
mammary gland alveolus development	Androgen receptor	Homo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland development	Androgen receptor	Homo sapiens (human)
cellular response to steroid hormone stimulus	Androgen receptor	Homo sapiens (human)
cellular response to estrogen stimulus	Androgen receptor	Homo sapiens (human)
cellular response to testosterone stimulus	Androgen receptor	Homo sapiens (human)
seminiferous tubule development	Androgen receptor	Homo sapiens (human)
non-membrane-bounded organelle assembly	Androgen receptor	Homo sapiens (human)
positive regulation of miRNA transcription	Androgen receptor	Homo sapiens (human)
regulation of protein localization to plasma membrane	Androgen receptor	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway	Androgen receptor	Homo sapiens (human)
male gonad development	Androgen receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Androgen receptor	Homo sapiens (human)
androgen biosynthetic process	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
male genitalia development	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
testosterone biosynthetic process	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
steroid biosynthetic process	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
xenobiotic metabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
negative regulation of gene expression	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bile acid and bile salt transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
heme catabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic export from cell	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transepithelial transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
leukotriene transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
protein autophosphorylation	ALK tyrosine kinase receptor	Homo sapiens (human)
signal transduction	ALK tyrosine kinase receptor	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	ALK tyrosine kinase receptor	Homo sapiens (human)
phosphorylation	ALK tyrosine kinase receptor	Homo sapiens (human)
hippocampus development	ALK tyrosine kinase receptor	Homo sapiens (human)
adult behavior	ALK tyrosine kinase receptor	Homo sapiens (human)
swimming behavior	ALK tyrosine kinase receptor	Homo sapiens (human)
peptidyl-tyrosine autophosphorylation	ALK tyrosine kinase receptor	Homo sapiens (human)
regulation of apoptotic process	ALK tyrosine kinase receptor	Homo sapiens (human)
protein autophosphorylation	ALK tyrosine kinase receptor	Homo sapiens (human)
neuron development	ALK tyrosine kinase receptor	Homo sapiens (human)
negative regulation of lipid catabolic process	ALK tyrosine kinase receptor	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	ALK tyrosine kinase receptor	Homo sapiens (human)
regulation of dopamine receptor signaling pathway	ALK tyrosine kinase receptor	Homo sapiens (human)
response to environmental enrichment	ALK tyrosine kinase receptor	Homo sapiens (human)
energy homeostasis	ALK tyrosine kinase receptor	Homo sapiens (human)
positive regulation of dendrite development	ALK tyrosine kinase receptor	Homo sapiens (human)
regulation of neuron differentiation	ALK tyrosine kinase receptor	Homo sapiens (human)
regulation of cell population proliferation	ALK tyrosine kinase receptor	Homo sapiens (human)
multicellular organism development	ALK tyrosine kinase receptor	Homo sapiens (human)
positive regulation of kinase activity	ALK tyrosine kinase receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
guanine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
urate transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
purine nucleotide transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type bile acid transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 4	Homo sapiens (human)
protein binding	Bile salt export pump	Homo sapiens (human)
ATP binding	Bile salt export pump	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Bile salt export pump	Homo sapiens (human)
bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
canalicular bile acid transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
carbohydrate transmembrane transporter activity	Bile salt export pump	Homo sapiens (human)
ABC-type bile acid transporter activity	Bile salt export pump	Homo sapiens (human)
ATP hydrolysis activity	Bile salt export pump	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Estrogen receptor	Homo sapiens (human)
TFIIB-class transcription factor binding	Estrogen receptor	Homo sapiens (human)
transcription coregulator binding	Estrogen receptor	Homo sapiens (human)
transcription corepressor binding	Estrogen receptor	Homo sapiens (human)
transcription coactivator binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Estrogen receptor	Homo sapiens (human)
chromatin binding	Estrogen receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Estrogen receptor	Homo sapiens (human)
nuclear receptor activity	Estrogen receptor	Homo sapiens (human)
steroid binding	Estrogen receptor	Homo sapiens (human)
protein binding	Estrogen receptor	Homo sapiens (human)
calmodulin binding	Estrogen receptor	Homo sapiens (human)
beta-catenin binding	Estrogen receptor	Homo sapiens (human)
zinc ion binding	Estrogen receptor	Homo sapiens (human)
TBP-class protein binding	Estrogen receptor	Homo sapiens (human)
enzyme binding	Estrogen receptor	Homo sapiens (human)
protein kinase binding	Estrogen receptor	Homo sapiens (human)
nitric-oxide synthase regulator activity	Estrogen receptor	Homo sapiens (human)
nuclear estrogen receptor activity	Estrogen receptor	Homo sapiens (human)
nuclear estrogen receptor binding	Estrogen receptor	Homo sapiens (human)
estrogen response element binding	Estrogen receptor	Homo sapiens (human)
identical protein binding	Estrogen receptor	Homo sapiens (human)
ATPase binding	Estrogen receptor	Homo sapiens (human)
14-3-3 protein binding	Estrogen receptor	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Estrogen receptor	Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA binding	Glucocorticoid receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Glucocorticoid receptor	Homo sapiens (human)
core promoter sequence-specific DNA binding	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Glucocorticoid receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Glucocorticoid receptor	Homo sapiens (human)
RNA binding	Glucocorticoid receptor	Homo sapiens (human)
nuclear receptor activity	Glucocorticoid receptor	Homo sapiens (human)
nuclear glucocorticoid receptor activity	Glucocorticoid receptor	Homo sapiens (human)
steroid binding	Glucocorticoid receptor	Homo sapiens (human)
protein binding	Glucocorticoid receptor	Homo sapiens (human)
zinc ion binding	Glucocorticoid receptor	Homo sapiens (human)
TBP-class protein binding	Glucocorticoid receptor	Homo sapiens (human)
protein kinase binding	Glucocorticoid receptor	Homo sapiens (human)
identical protein binding	Glucocorticoid receptor	Homo sapiens (human)
Hsp90 protein binding	Glucocorticoid receptor	Homo sapiens (human)
steroid hormone binding	Glucocorticoid receptor	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Glucocorticoid receptor	Homo sapiens (human)
estrogen response element binding	Glucocorticoid receptor	Homo sapiens (human)
transcription cis-regulatory region binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
cis-regulatory region sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
core promoter sequence-specific DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
TFIID-class transcription factor complex binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Cellular tumor antigen p53	Homo sapiens (human)
protease binding	Cellular tumor antigen p53	Homo sapiens (human)
p53 binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA binding	Cellular tumor antigen p53	Homo sapiens (human)
chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
DNA-binding transcription factor activity	Cellular tumor antigen p53	Homo sapiens (human)
mRNA 3'-UTR binding	Cellular tumor antigen p53	Homo sapiens (human)
copper ion binding	Cellular tumor antigen p53	Homo sapiens (human)
protein binding	Cellular tumor antigen p53	Homo sapiens (human)
zinc ion binding	Cellular tumor antigen p53	Homo sapiens (human)
enzyme binding	Cellular tumor antigen p53	Homo sapiens (human)
receptor tyrosine kinase binding	Cellular tumor antigen p53	Homo sapiens (human)
ubiquitin protein ligase binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase regulator activity	Cellular tumor antigen p53	Homo sapiens (human)
ATP-dependent DNA/DNA annealing activity	Cellular tumor antigen p53	Homo sapiens (human)
identical protein binding	Cellular tumor antigen p53	Homo sapiens (human)
histone deacetylase binding	Cellular tumor antigen p53	Homo sapiens (human)
protein heterodimerization activity	Cellular tumor antigen p53	Homo sapiens (human)
protein-folding chaperone binding	Cellular tumor antigen p53	Homo sapiens (human)
protein phosphatase 2A binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Cellular tumor antigen p53	Homo sapiens (human)
14-3-3 protein binding	Cellular tumor antigen p53	Homo sapiens (human)
MDM2/MDM4 family protein binding	Cellular tumor antigen p53	Homo sapiens (human)
disordered domain specific binding	Cellular tumor antigen p53	Homo sapiens (human)
general transcription initiation factor binding	Cellular tumor antigen p53	Homo sapiens (human)
molecular function activator activity	Cellular tumor antigen p53	Homo sapiens (human)
promoter-specific chromatin binding	Cellular tumor antigen p53	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Progesterone receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Progesterone receptor	Homo sapiens (human)
transcription coactivator binding	Progesterone receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Progesterone receptor	Homo sapiens (human)
DNA binding	Progesterone receptor	Homo sapiens (human)
nuclear steroid receptor activity	Progesterone receptor	Homo sapiens (human)
G protein-coupled receptor activity	Progesterone receptor	Homo sapiens (human)
steroid binding	Progesterone receptor	Homo sapiens (human)
protein binding	Progesterone receptor	Homo sapiens (human)
zinc ion binding	Progesterone receptor	Homo sapiens (human)
enzyme binding	Progesterone receptor	Homo sapiens (human)
identical protein binding	Progesterone receptor	Homo sapiens (human)
ATPase binding	Progesterone receptor	Homo sapiens (human)
estrogen response element binding	Progesterone receptor	Homo sapiens (human)
nuclear receptor activity	Progesterone receptor	Homo sapiens (human)
transcription cis-regulatory region binding	Androgen receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Androgen receptor	Homo sapiens (human)
RNA polymerase II general transcription initiation factor binding	Androgen receptor	Homo sapiens (human)
transcription coactivator binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Androgen receptor	Homo sapiens (human)
chromatin binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Androgen receptor	Homo sapiens (human)
nuclear receptor activity	Androgen receptor	Homo sapiens (human)
G protein-coupled receptor activity	Androgen receptor	Homo sapiens (human)
signaling receptor binding	Androgen receptor	Homo sapiens (human)
steroid binding	Androgen receptor	Homo sapiens (human)
androgen binding	Androgen receptor	Homo sapiens (human)
protein binding	Androgen receptor	Homo sapiens (human)
beta-catenin binding	Androgen receptor	Homo sapiens (human)
zinc ion binding	Androgen receptor	Homo sapiens (human)
enzyme binding	Androgen receptor	Homo sapiens (human)
ATPase binding	Androgen receptor	Homo sapiens (human)
molecular adaptor activity	Androgen receptor	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Androgen receptor	Homo sapiens (human)
POU domain binding	Androgen receptor	Homo sapiens (human)
molecular condensate scaffold activity	Androgen receptor	Homo sapiens (human)
estrogen response element binding	Androgen receptor	Homo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activity	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
testosterone dehydrogenase [NAD(P)] activity	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activity	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
17-beta-hydroxysteroid dehydrogenase (NADP+) activity	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
protein binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP hydrolysis activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
protein tyrosine kinase activity	ALK tyrosine kinase receptor	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	ALK tyrosine kinase receptor	Homo sapiens (human)
protein binding	ALK tyrosine kinase receptor	Homo sapiens (human)
ATP binding	ALK tyrosine kinase receptor	Homo sapiens (human)
heparin binding	ALK tyrosine kinase receptor	Homo sapiens (human)
receptor signaling protein tyrosine kinase activator activity	ALK tyrosine kinase receptor	Homo sapiens (human)
identical protein binding	ALK tyrosine kinase receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
nucleolus	Multidrug resistance-associated protein 4	Homo sapiens (human)
Golgi apparatus	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
platelet dense granule membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
external side of apical plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 4	Homo sapiens (human)
basolateral plasma membrane	Bile salt export pump	Homo sapiens (human)
Golgi membrane	Bile salt export pump	Homo sapiens (human)
endosome	Bile salt export pump	Homo sapiens (human)
plasma membrane	Bile salt export pump	Homo sapiens (human)
cell surface	Bile salt export pump	Homo sapiens (human)
apical plasma membrane	Bile salt export pump	Homo sapiens (human)
intercellular canaliculus	Bile salt export pump	Homo sapiens (human)
intracellular canaliculus	Bile salt export pump	Homo sapiens (human)
recycling endosome	Bile salt export pump	Homo sapiens (human)
recycling endosome membrane	Bile salt export pump	Homo sapiens (human)
extracellular exosome	Bile salt export pump	Homo sapiens (human)
membrane	Bile salt export pump	Homo sapiens (human)
nucleus	Estrogen receptor	Homo sapiens (human)
nucleoplasm	Estrogen receptor	Homo sapiens (human)
transcription regulator complex	Estrogen receptor	Homo sapiens (human)
cytoplasm	Estrogen receptor	Homo sapiens (human)
Golgi apparatus	Estrogen receptor	Homo sapiens (human)
cytosol	Estrogen receptor	Homo sapiens (human)
plasma membrane	Estrogen receptor	Homo sapiens (human)
membrane	Estrogen receptor	Homo sapiens (human)
chromatin	Estrogen receptor	Homo sapiens (human)
euchromatin	Estrogen receptor	Homo sapiens (human)
protein-containing complex	Estrogen receptor	Homo sapiens (human)
nucleus	Estrogen receptor	Homo sapiens (human)
nucleus	Glucocorticoid receptor	Homo sapiens (human)
nucleus	Glucocorticoid receptor	Homo sapiens (human)
nucleoplasm	Glucocorticoid receptor	Homo sapiens (human)
cytoplasm	Glucocorticoid receptor	Homo sapiens (human)
mitochondrial matrix	Glucocorticoid receptor	Homo sapiens (human)
centrosome	Glucocorticoid receptor	Homo sapiens (human)
spindle	Glucocorticoid receptor	Homo sapiens (human)
cytosol	Glucocorticoid receptor	Homo sapiens (human)
membrane	Glucocorticoid receptor	Homo sapiens (human)
nuclear speck	Glucocorticoid receptor	Homo sapiens (human)
synapse	Glucocorticoid receptor	Homo sapiens (human)
chromatin	Glucocorticoid receptor	Homo sapiens (human)
protein-containing complex	Glucocorticoid receptor	Homo sapiens (human)
nuclear body	Cellular tumor antigen p53	Homo sapiens (human)
nucleus	Cellular tumor antigen p53	Homo sapiens (human)
nucleoplasm	Cellular tumor antigen p53	Homo sapiens (human)
replication fork	Cellular tumor antigen p53	Homo sapiens (human)
nucleolus	Cellular tumor antigen p53	Homo sapiens (human)
cytoplasm	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrion	Cellular tumor antigen p53	Homo sapiens (human)
mitochondrial matrix	Cellular tumor antigen p53	Homo sapiens (human)
endoplasmic reticulum	Cellular tumor antigen p53	Homo sapiens (human)
centrosome	Cellular tumor antigen p53	Homo sapiens (human)
cytosol	Cellular tumor antigen p53	Homo sapiens (human)
nuclear matrix	Cellular tumor antigen p53	Homo sapiens (human)
PML body	Cellular tumor antigen p53	Homo sapiens (human)
transcription repressor complex	Cellular tumor antigen p53	Homo sapiens (human)
site of double-strand break	Cellular tumor antigen p53	Homo sapiens (human)
germ cell nucleus	Cellular tumor antigen p53	Homo sapiens (human)
chromatin	Cellular tumor antigen p53	Homo sapiens (human)
transcription regulator complex	Cellular tumor antigen p53	Homo sapiens (human)
protein-containing complex	Cellular tumor antigen p53	Homo sapiens (human)
plasma membrane	Progesterone receptor	Homo sapiens (human)
nucleoplasm	Progesterone receptor	Homo sapiens (human)
mitochondrial outer membrane	Progesterone receptor	Homo sapiens (human)
cytosol	Progesterone receptor	Homo sapiens (human)
chromatin	Progesterone receptor	Homo sapiens (human)
nucleus	Progesterone receptor	Homo sapiens (human)
plasma membrane	Androgen receptor	Homo sapiens (human)
nucleus	Androgen receptor	Homo sapiens (human)
nucleoplasm	Androgen receptor	Homo sapiens (human)
cytoplasm	Androgen receptor	Homo sapiens (human)
cytosol	Androgen receptor	Homo sapiens (human)
nuclear speck	Androgen receptor	Homo sapiens (human)
chromatin	Androgen receptor	Homo sapiens (human)
protein-containing complex	Androgen receptor	Homo sapiens (human)
nucleus	Androgen receptor	Homo sapiens (human)
plasma membrane	Glutamate receptor 2	Rattus norvegicus (Norway rat)
endoplasmic reticulum	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
endoplasmic reticulum membrane	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
intracellular membrane-bounded organelle	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
endoplasmic reticulum	Testosterone 17-beta-dehydrogenase 3	Homo sapiens (human)
plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell surface	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
intercellular canaliculus	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
plasma membrane	ALK tyrosine kinase receptor	Homo sapiens (human)
plasma membrane	ALK tyrosine kinase receptor	Homo sapiens (human)
extracellular exosome	ALK tyrosine kinase receptor	Homo sapiens (human)
protein-containing complex	ALK tyrosine kinase receptor	Homo sapiens (human)
receptor complex	ALK tyrosine kinase receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
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.
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.
AID588349	qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504836	Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation	2002	The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16	Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
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.
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.
AID1347045	Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347050	Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347049	Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378	qHTS for Inhibitors of ATXN expression: Validation
AID686947	qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen	2013	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15	Identification of potent Yes1 kinase inhibitors using a library screening approach.
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.
AID588212	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID248693	Inhibition of androgen dependent human prostate cancer cell MDA-MB-PCa2b proliferation	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.
AID670348	Inhibition of actin based pseudopodia formation in androgen-dependent human LNCAP cells at 100 uM after 48 hrs by DAPI staining based fluorescence microscopy assay	2012	Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13	Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens.
AID290231	Binding affinity to human androgen receptor expressed in CV1 cells	2007	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6	Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
AID700052	Antagonist activity at AR co-activator binding domain expressed in african green monkey CV1 cells assessed as decrease in R1881-induced luciferase activity at <=40 uM relative to control	2012	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21	3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding.
AID1635221	Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
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.
AID639156	Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID648214	Anticancer activity against human LNCaP-hr cells xenografted in BALB/c athymic nude mouse assessed as prostate specific antigen level in plasma at 100 mg/kg, po qd after 28 days relative to control	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID478367	Activity at human AR expressed in human HeLa cells after 48 hrs by transient-luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9	Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
AID253471	Inhibition of 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.
AID1199794	Growth inhibition of human CWR22Rv1 cells by MTT assay	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Novel C-4 heteroaryl 13-cis-retinamide Mnk/AR degrading agents inhibit cell proliferation and migration and induce apoptosis in human breast and prostate cancer cells and suppress growth of MDA-MB-231 human breast and CWR22Rv1 human prostate tumor xenogra
AID38829	In vitro agonistic activity against human androgen receptor (hAR) expressed in CV-1 cells; not active	1999	Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7	Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
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.
AID670343	Antiproliferative activity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13	Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens.
AID578355	Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6	Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).
AID700382	Antagonist activity at androgen receptor in human PC3 cells assessed as reduction in DHT-induced PSA expression at 2.5 uM incubated for 24 hrs by RT-PCR	2012	Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2	Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
AID1329831	In vivo antagonist activity at androgen receptor in immature rat prostate weight model assessed as testosterone propionate-induced weight of seminal vesicles over full body weight at 10 mg/kg, po qd administered for 4 days relative to testosterone propion	2016	Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23	[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
AID319588	Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay	2008	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11	Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
AID1569749	Agonist activity at GAL4-DBD fused rat androgen receptor expressed in UAS-bla 293 cells at 10 uM incubated for 16 hrs followed by fluorescence substrate addition and measured after 2 hrs by beta lactamase reporter gene assay relative to control	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1569745	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF
AID1635223	Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID588219	FDA HLAED, gamma-glutamyl transferase (GGT) increase	2004	Current 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.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID257783	Inhibition of rat AR	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID319590	Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay	2008	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11	Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
AID1569744	Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF
AID1473940	AUC in human at 50 mg, po QD after 24 hrs	2013	Toxicological 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.
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current 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.
AID639152	Antagonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID1233505	Antagonist activity at androgen receptor (unknown origin)	2015	European journal of medicinal chemistry, Jun-24, Volume: 99	Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.
AID38809	Agonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cell	1998	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7	New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
AID1199396	Displacement of [3H]R1881 from androgen receptor in human PC3 cells	2015	Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5	Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
AID731973	Antitumor activity against human LNCaP-hr cells in BALB/c mouse xenograft model assessed as inhibition of tumor growth at 100 mg/kg, po qd for 28 days (Rvb = 100%)	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine 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.
AID639078	Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID38968	Antagonistic activity (IC50) against human androgen receptor (hAR) in co-transfected CV-1 cell	1998	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7	New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
AID700053	Activation of AR co-activator binding domain expressed in african green monkey CV1 cells at <=40 uM relative to control	2012	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 22, Issue:21	3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding.
AID292743	Reduction of testosterone-induced prostate weight increase in Sprague-Dawley rat by modified Hersherberger assay relative to control	2007	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1	The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID1249994	Displacement of [3H]-DHT from androgen receptor in human MDA-MB-453 cells after 90 mins by TopCount analysis	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID639077	Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor T877A mutant expressed in HEK293 derived FreeStyle293F cells after 3 hrs	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID482792	Inhibition of prostate specific antigen secretion in human LNCAP cells expressing androgen receptor at 1.25 to 10 uM in presence of charcoal stripped serum	2010	Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7	Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
AID588215	FDA HLAED, alkaline phosphatase increase	2004	Current 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.
AID316705	Drug level in human CWR22R cells xenografted mouse plasma at 50 mg/kg, po after 24 hrs on day 60	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.
AID588213	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1430112	Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents.
AID1885060	Antiproliferative activity against human LNCaP cells	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID639256	Toxicity in BALB/c mouse assessed as body weight at 20 mg/kg, po qd administered for 29 days measured on day 28 (Rvb = 17.6 +/- 0.4g)	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID1473738	Inhibition 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 assay	2013	Toxicological 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.
AID482789	Inhibition of prostate specific antigen expression in human LNCAP cells in presence of fetal bovine serum	2010	Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7	Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
AID540235	Phospholipidosis-negative literature compound
AID1313182	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	2016	Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15	Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
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.
AID1313184	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	2016	Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15	Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
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.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473739	Inhibition 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 assay	2013	Toxicological 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.
AID478372	Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days	2010	Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9	Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
AID1443995	Hepatotoxicity in human assessed as drug-induced liver injury	2014	Hepatology (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.
AID493505	Effect on immature rat prostate weight in rat assessed as ratio of weight of seminal vesicles to full body weight at 10 mg/kg, po qd for 3 days relative to control	2010	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15	Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
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.
AID1079935	Cytolytic 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]
AID1635252	Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID1885040	Binding affinity to Androgen receptor (unknown origin)	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID265578	Inhibition of rat AR-mediated reporter gene expression in COS7 cells	2006	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12	Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands.
AID319592	Activity at androgen receptor in human Saos2 cells assessed as IL6 repression	2008	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11	Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
AID630712	Antitumor activity against human LNCAP cells xenografted in athymic nude Harlan Sprague-Dawley mouse assessed as serum prostate specific antigen suppression at 10 mg/kg, po administered once daily for 5 weeks measured on week 3 by ELISA relative to vehicl	2011	Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21	Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
AID1635222	Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID588210	Human drug-induced liver injury (DILI) modelling dataset from Ekins et al	2010	Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12	A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID588216	FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase	2004	Current 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.
AID482794	Drug level in SCID mouse serum at 10 mg/kg, iv	2010	Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7	Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
AID639155	Agonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID670341	Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13	Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens.
AID1569748	Antagonist activity at GAL4-DBD fused rat androgen receptor expressed in UAS-bla 293 cells assessed as reduction in R1881-induced activation incubated for 16 hrs followed by fluorescence substrate addition and measured after 2 hrs by beta lactamase report	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF
AID244010	Inhibition of [1-beta-2beta-3H]- -testosterone binding to human steroid 5-alpha-reductase type 2 of BPH tissue at 10 uM; - = not determined	2005	Journal 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.
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.
AID257797	Half life in rat hypothalamus at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID639171	Antitumor activity against human JDCaP cells expressing wild type AR xenografted in testosterone propionate-challenged castrated BALB/c nude mouse assessed as decrease in tumor volume at 20 mg/kg, po bid administered for 29 days measured on day 28 (Rvb =	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID1569747	Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF
AID38985	In vitro binding affinity at human androgen receptor transfected into COS cells.	1999	Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7	Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current 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.
AID1473741	Inhibition 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 assay	2013	Toxicological 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.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID639254	Antitumor activity against human LNCaP-FGC cells expressing androgen receptor W741C/T887A mutant xenografted in castrated BALB/c nude mouse assessed as decrease in prostate specific antigen level in plasma at 20 mg/kg, po qd administered for 29 days measu	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID639154	Agonist activity at human androgen receptor expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID1329841	Toxicity in BALB/c athymic mouse xenografted with bicalutamide-resistant human CWR22-BMSLD1 cells at 150 mg/kg, po qd for 20 days	2016	Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23	[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
AID319589	Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay relative to DHT	2008	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11	Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
AID1708708	Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability	2021	Bioorganic & medicinal chemistry letters, 03-15, Volume: 36	Synthesis, biological evaluation and X-ray analysis of bicalutamide sulfoxide analogues for the potential treatment of prostate cancer.
AID648289	Cytotoxicity against human androgen-independent PC3 cells by MTT assay	2012	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5	1,2,4-Oxadiazoles: a new class of anti-prostate cancer agents.
AID257789	Half life in rat plasma at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID331662	Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
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.
AID539157	Antitumor activity against human bicalutamide-resistant LNCAP cells xenografted in SCID mouse assessed as inhibition of tumor growth at 100 mg/kg, po qd for seven cycles of 5 days on, 2 days off	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID700381	Antagonist activity at androgen receptor in human PC3 cells assessed as increase in Maspin expression at 2.5 uM incubated for 24 hrs in presence of DHT by RT-PCR	2012	Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2	Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
AID1408589	Displacement of Fluormone-DHT from rat GST-tagged rat AR LBD expressed in insect cells at 1 to 10 uM after 4 hrs by fluorescence polarization assay	2018	European journal of medicinal chemistry, Sep-05, Volume: 157	Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor.
AID294971	Reduction of prostate weight in orally dosed immature rat	2007	Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9	beta-Alkylthio indolyl carbinols: potent nonsteroidal antiandrogens with oral efficacy in a prostate cancer model.
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.
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.
AID1250035	Antitumor activity against human CWR22 cells in Balb/c athymic (nu/nu) mouse CWR22-BMSLD1 prostate cancer xenograft model assessed as tumor growth inhibition at 150 mg/kg, po qd administered for 35 days measured from day 10 to 35 during compound dosing	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID539145	Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID319591	Binding affinity to human androgen receptor expressed in monkey COS7 cells by whole cell binding assay	2008	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11	Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
AID648205	Agonist activity at androgen receptor T877A mutant expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID731976	Antitumor activity against human LNCaP-hr cells in BALB/c mouse xenograft model assessed as plasma prostate specific antigen level at 100 mg/kg, po qd for 28 days by ELISA (Rvb = 23.8 +/- 6.1 ng/ml)	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
AID316698	AUC (0 to 6 hrs) in BALB/c mouse at 1.0 mmol/kg, po	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.
AID1329839	Antitumor activity against bicalutamide-resistant human CWR22-BMSLD1 cells xenografted in BALB/c athymic mouse assessed as tumor growth inhibition at 150 mg/kg, po qd for 20 days measured on last day of dosing relative to control	2016	Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23	[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current 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.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID588208	Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset	2010	Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5	Predicting phospholipidosis using machine learning.
AID1199793	Growth inhibition of human LNCAP cells by MTT assay	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Novel C-4 heteroaryl 13-cis-retinamide Mnk/AR degrading agents inhibit cell proliferation and migration and induce apoptosis in human breast and prostate cancer cells and suppress growth of MDA-MB-231 human breast and CWR22Rv1 human prostate tumor xenogra
AID630802	Antitumor activity against human LNCAP cells xenografted in athymic nude Harlan Sprague-Dawley mouse assessed as tumor volume inhibition at 10 mg/kg, po administered once daily for 5 weeks measured after 5 weeks relative to vehicle treated control	2011	Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21	Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
AID648200	Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID720861	Inhibition of BF3 site of androgen receptor in enzalutamide-resistant human LNCAP cells assessed as reduction in PSA level after 3 days	2013	Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3	Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives.
AID1636382	Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 14 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NAD	2016	Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16	Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1249996	In vivo antagonist activity at androgen receptor in immature Sprague-Dawley rat prostate weight model assessed as testosterone propionate-induced weight of seminal vesicles over full body weight at 1 mg/kg, po qd administered for 4 days	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID1636494	Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 224.2 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of	2016	Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16	Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID176507	Antiandrogen activity in male rats	1988	Journal of medicinal chemistry, Apr, Volume: 31, Issue:4	Resolution of the nonsteroidal antiandrogen 4'-cyano-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3'- (trifluoromethyl)-propionanilide and the determination of the absolute configuration of the active enantiomer.
AID1443991	Induction 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 assay	2014	Hepatology (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.
AID1313185	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	2016	Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15	Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
AID493503	Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay	2010	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15	Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
AID1168322	Growth inhibition of human PC3 cells	2014	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21	Synthesis and preliminary investigations into novel 1,2,3-triazole-derived androgen receptor antagonists inspired by bicalutamide.
AID38805	In vitro antagonistic activity against human androgen receptor (hAR) expressed in CV-1 cells	1999	Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7	Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
AID539151	Inhibition of human ERG at 10 uM by whole cell patch-clamp technique	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
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.
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.
AID478366	Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting	2010	Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9	Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
AID639250	Antitumor activity against human LNCaP-FGC cells expressing androgen receptor W741C/T887A mutant xenografted in castrated BALB/c nude mouse assessed as effect on tumor volume at 20 mg/kg, po qd administered for 29 days measured on day 28 (Rvb = 402 +/- 47	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID1198074	Agonist activity at pSG5-tagged human androgen receptor T877A mutant expressed in COS1 cells assessed as receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay relative to control	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3	Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.
AID1199795	Growth inhibition of human PC3 cells by MTT assay	2015	Journal of medicinal chemistry, Feb-26, Volume: 58, Issue:4	Novel C-4 heteroaryl 13-cis-retinamide Mnk/AR degrading agents inhibit cell proliferation and migration and induce apoptosis in human breast and prostate cancer cells and suppress growth of MDA-MB-231 human breast and CWR22Rv1 human prostate tumor xenogra
AID257794	Oral clearance in rat ventral prostate at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
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.
AID700379	Antagonist activity at androgen receptor in human LNCaP cells assessed as reduction in DHT-induced PSA expression at 1 uM by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2	Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug 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.
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.
AID626476	Displacement of [3H]Dex from glucocorticoid receptor in Sprague-Dawley rat liver after 2 hrs by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079931	Moderate 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]
AID539149	AUC in mouse at 10 mg/kg, po using 5% arabic gum as vehicle	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
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.
AID244022	Inhibition of [1-beta-3H]-androstenedione binding to human steroid 5-alpha-reductase type I expressed in DU-145 cells at 10 uM; - = not determined	2005	Journal 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.
AID184812	Effect of compound on LH level on 14-day dosing in intact rats 25 mg/kg	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides.
AID756280	Inhibition of androgen receptor in human LNCAP cells after 1 day by luciferase reporter gene assay	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Discovery of non-LBD inhibitor for androgen receptor by structure-guide design.
AID1751743	Inhibition of [3H] MIB binding to rat prostate androgen receptor LBD by competitive binding assay	2021	Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15	Exploration and Biological Evaluation of Basic Heteromonocyclic Propanamide Derivatives as SARDs for the Treatment of Enzalutamide-Resistant Prostate Cancer.
AID276462	Inhibition of seminal vesicle weight in Sprague-Dawley rat at 2 mg/day, po relative to control	2006	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22	Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators.
AID257799	Effect on ventral prostate weight with reference to control in Wistar rat at 100 mg/kg/day	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID1430111	Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced proliferation after 48 hrs by MTT assay	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents.
AID700390	Agonist activity at androgen receptor W741C mutant expressed in human PC3 cells assessed as stimulation of receptor transactivation at 0.1 to 1 uM by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2	Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
AID38983	In vitro agonistic activity against human androgen receptor (hAR) expressed in CV-1 cells; not active	1999	Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7	Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
AID1324636	Agonist activity at AR W741C/T877A double 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
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1313183	Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	2016	Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15	Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
AID539156	Antitumor activity against human bicalutamide-resistant LNCAP cells xenografted in SCID mouse assessed as inhibition of tumor growth at 10 mg/kg, po qd for seven cycles of 5 days on, 2 days off	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID1249998	Plasma concentration in immature Sprague-Dawley rat prostate weight model at 1 mg/kg, po qd administered for 4 days measured 2 hrs post last dose on day 4	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID578356	Displacement of [3H]aldosterone from Sprague-Dawley rat MR by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6	Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).
AID1079933	Acute 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
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.
AID777284	Antagonist activity at androgen receptor H874Y mutant (unknown origin) expressed in human 22Rv1 cells assessed as inhibition of DHT-induced cell growth after 3 days by 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.
AID777285	Antagonist activity at androgen receptor T877A mutant (unknown origin) expressed in human LNCAP cells assessed as inhibition of DHT-induced cell growth after 6 days by 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.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID242071	In vitro inhibitory concentration against Cytochrome P450 17 expressed in E. coli; - = not determined	2005	Journal 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.
AID754109	Displacement of [3H]R1881 from AR in human MDA-MB-453 cells	2013	Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12	Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.
AID276317	Displacement of [3H]R1881 from rat androgen receptor	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	A bioisosteric approach to the discovery of indole carbinol androgen receptor ligands.
AID257787	Cmax in rat plasma at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID257790	Oral clearance in rat at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID626482	Displacement of [3H]testosterone from androgen receptor in Sprague-Dawley rat prostate gland after 2 hrs by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.
AID478371	Agonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days	2010	Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9	Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
AID290229	Antagonist activity at human androgen receptor expressed in CV1 cells	2007	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6	Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
AID331664	Displacement of [3H]DHT from human Androgen receptor in human MDA-MB-453 cells	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1140401	Antagonist activity at androgen receptor in human LNCAP cells assessed as inhibition of androgen-stimulated cell growth at 20 uM measured every 3 days relative to dihydrotestosterone	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Preliminary investigations into triazole derived androgen receptor antagonists.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID1199397	Growth inhibition of human castration-resistant prostate cancer cells	2015	Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5	Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
AID1291240	Antiproliferative activity against human 22Rv1 cells after 96 hrs by Oncotest monolayer assay	2016	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8	7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer.
AID493501	Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assay	2010	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15	Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
AID1635253	Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID539158	Inhibition of prostate specific antigen production in human bicalutamide-resistant LNCAP cells xenografted SCID mouse at 10 mg/kg, po qd for seven cycles of 5 days on and 2 days off measured on day 17	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID1708709	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability	2021	Bioorganic & medicinal chemistry letters, 03-15, Volume: 36	Synthesis, biological evaluation and X-ray analysis of bicalutamide sulfoxide analogues for the potential treatment of prostate cancer.
AID731984	Inhibition of Androgen receptor T877A mutant (unknown origin) expressed in Freestyle293F cells	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
AID257795	Cmax in rat hypothalamus at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID731980	Agonist activity at Androgen receptor T877A mutant in human LNCaP-hr cells assessed as prostate specific antigen secretion measured after 3 days by enzyme-immunoassay	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
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.
AID731982	Antagonist activity at Androgen receptor T877A mutant (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
AID1079938	Chronic 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]
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1250034	Antitumor activity against human CWR22 cells in Balb/c athymic (nu/nu) mouse CWR22-BMSLD1 prostate cancer xenograft model assessed as tumor growth inhibition at 150 mg/kg, po qd measured for 10 days during compound dosing	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID588209	Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset	2010	Chemical research in toxicology, Jul-19, Volume: 23, Issue:7	Developing structure-activity relationships for the prediction of hepatotoxicity.
AID648204	Agonist activity at androgen receptor expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID777282	Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by 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.
AID257780	Effect on ventral prostate weight with reference to control in Wistar rat at 10 mg/kg/day, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID578353	Displacement of [3H]progesterone from rabbit PR by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6	Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID630792	Kinetic solubility of the compound at pH 7.4	2011	Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21	Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
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.
AID756281	Cytotoxicity against human LNCAP cells assessed as cell viability after 2 days by cell counting method	2013	Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13	Discovery of non-LBD inhibitor for androgen receptor by structure-guide design.
AID1329835	Plasma concentration in immature rat prostate weight model at 10 mg/kg, po qd administered for 4 days measured 2 hrs post last dose on day 4	2016	Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23	[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
AID1473941	Drug concentration at steady state in human at 50 mg, po QD after 24 hrs	2013	Toxicological 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.
AID626475	Displacement of [3H]E2 from estrogen receptor in JW rabbit uterus after 2 hrs by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.
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.
AID515859	Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19	20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth.
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.
AID1708706	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability	2021	Bioorganic & medicinal chemistry letters, 03-15, Volume: 36	Synthesis, biological evaluation and X-ray analysis of bicalutamide sulfoxide analogues for the potential treatment of prostate cancer.
AID1313190	Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15	Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID257791	Cmax in rat ventral prostate at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
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.
AID1635220	Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID588211	Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans	2010	Chemical research in toxicology, Jan, Volume: 23, Issue:1	Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID578352	Displacement of [3H]testosterone from Sprague-Dawley rat AR by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6	Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).
AID331663	Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay relative to dihydrotestosterone	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
AID38830	In vitro antagonistic activity against human androgen receptor (hAR) expressed in CV-1 cells	1999	Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7	Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.
AID630709	Agonist activity at human AR overexpressed in human LNCAP cells assessed as fold increase at 1 uM by luciferase reporter gene assay relative to R1881	2011	Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21	Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
AID190320	Effect of compound on testosterone hormone level on 14-day dosing in intact rats at 25 mg/kg.	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides.
AID316696	Cmax in BALB/c mouse at 1.0 mmol/kg, po	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.
AID648207	Anticancer activity against human LNCaP-hr cells assessed as prostate specific antigen level at 10 uM after 3 days by enzyme immunoassay relative to control	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID539147	Membrane permeability by PAMPA assay	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID1473942	Ratio of drug concentration at steady state in human at 50 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells	2013	Toxicological 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.
AID700378	Antagonist activity at androgen receptor in human LNCaP cells assessed as reduction in DHT-induced PSA expression at 2.5 uM by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2	Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
AID601825	Agonist activity at androgen receptor W741L mutant expressed in african green monkey CV1 cells assessed as induction of transcriptional activity at 1 to 1000 nM by luciferase reporter gene assay	2011	Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11	Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
AID257782	Inhibition of human AR	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID178165	Effective dose for antiandrogen activity in rats	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides.
AID1198071	Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3	Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.
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.
AID1635251	Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID39001	Binding affinity against Androgen receptor transfected into COS cells	1998	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7	New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
AID503305	Antiproliferative activity against human PC3 cells at 500 nM after 120 hrs by MTT assay relative to DMSO	2006	Nature chemical biology, Jun, Volume: 2, Issue:6	Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID601820	Displacement of [3H]MIB from GST-tagged wild type recombinant androgen receptor ligand binding domain after 18 hrs by scintillation counting relative to dihydrotestosterone	2011	Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11	Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
AID700387	Antagonist activity at androgen receptor ARv7 mutant lacking ligand binding domain expressed in human PC3 cells assessed as reduction in DHT-induced receptor transactivation at 1 uM by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2	Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
AID257784	Inhibition of rat PR	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
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.
AID655047	Inhibition of R1881-induced androgen receptor nuclear translocation in human LNCAP cells at 10 uM pretreated for 3 hrs before R1881 challenge measured after 3 hrs by Hoechst staining-based immunocytometric analysis	2012	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5	Methoxychalcone inhibitors of androgen receptor translocation and function.
AID1198073	Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as receptor-mediated testosterone-induced transcriptional activity at 10 uM by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3	Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID539141	Agonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID276469	Stimulation of prostate weight in Sprague-Dawley rat relative to testosterone	2006	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22	Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators.
AID257788	AUC (0-72)hrs in rat plasma at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID731983	Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
AID1140402	Antagonist activity at androgen receptor in human LNCAP cells assessed as inhibition of androgen-stimulated cell growth at 40 uM measured every 3 days relative to dihydrotestosterone	2014	Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9	Preliminary investigations into triazole derived androgen receptor antagonists.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID257796	AUC (0-72)hrs in rat hypothalamus at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID493500	Displacement of [3H]DHT from AR in human MDA-MB-453 cells	2010	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15	Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
AID738080	Antiandrogenic activity in immature castrated Hershberger rat model assessed as inhibition of testosterone propionate-induced seminal vesicle growth at 2 mg/kg, po bid for 7 days	2013	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7	Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.
AID539142	Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID1079936	Choleostatic 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]
AID1635250	Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	2016	European journal of medicinal chemistry, Aug-08, Volume: 118	Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID38800	Agonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cell	1998	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7	New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
AID1569746	Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF
AID316702	Drug level in human CWR22R cells xenografted mouse plasma at 50 mg/kg, po after 1 hr on day 60	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.
AID276461	Inhibition of prostate weight in Sprague-Dawley rat at 2 mg/day, po relative to control	2006	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22	Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators.
AID305321	Inhibition of prostate weight in testosterone treated castrated immature Sprague-Dawley rat at 2 mg/day	2007	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3	Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives.
AID700388	Agonist activity at androgen receptor H874Y mutant expressed in human PC3 cells assessed as potentiation of 0.1 nM DHT-induced receptor transactivation at 0.1 to 1 uM by luciferase reporter gene assay	2012	Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2	Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
AID257793	Half life in rat ventral prostate at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
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.
AID639076	Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrs	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID305324	Inhibition of prostate weight in testosterone treated castrated mature Sprague-Dawley rat	2007	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3	Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives.
AID1751744	Antagonist activity at human androgen receptor expressed in HEK-293 cells harboring GRE-LUC and CMV-renilla luciferase assessed as inhibition of transactivation incubated for 24 hrs in presence of R1881 by dual luciferase assay	2021	Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15	Exploration and Biological Evaluation of Basic Heteromonocyclic Propanamide Derivatives as SARDs for the Treatment of Enzalutamide-Resistant Prostate Cancer.
AID38822	Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cell	1998	Bioorganic & medicinal chemistry letters, Apr-07, Volume: 8, Issue:7	New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID670357	Cytotoxicity against androgen-independent human PC3 cells at 100 uM within 48 hrs by SRB assay	2012	Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13	Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens.
AID316697	Tmax in BALB/c mouse at 1.0 mmol/kg, po	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.
AID184813	Effect of compound on LH level on 14-day dosing in intact rats; No statistically significant difference from control	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides.
AID1708707	Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability	2021	Bioorganic & medicinal chemistry letters, 03-15, Volume: 36	Synthesis, biological evaluation and X-ray analysis of bicalutamide sulfoxide analogues for the potential treatment of prostate cancer.
AID539148	Antiandrogenic activity in castrated mouse assessed as reduction in wet weight gain of seminal vesicle	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
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.
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.
AID276468	Stimulation of levator ani muscle weight in Sprague-Dawley rat relative to testosterone	2006	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22	Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators.
AID1569743	Antagonist activity at GAL4-DBD fused rat androgen receptor expressed in UAS-bla 293 cells assessed as reduction in R1881-induced activation at 10 uM incubated for 16 hrs followed by fluorescence substrate addition and measured after 2 hrs by beta lactama	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF
AID670344	Antiproliferative activity against androgen-independent human PC3 cells after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13	Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens.
AID639252	Antitumor activity against human LNCaP-FGC cells expressing androgen receptor W741C/T887A mutant xenografted in castrated BALB/c nude mouse assessed as effect on tumor volume at 20 mg/kg, po qd administered for 29 days measured on day 28 relative to contr	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID293099	Inhibition of testoterone-induced prostate weight in castrated immature Sprague-Dawley rat	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent androgen receptor antagonists.
AID290230	Antagonist activity at human androgen receptor expressed in CV1 cells assessed as inhibition of DHT-induced response	2007	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6	Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
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.
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.
AID257798	Oral clearance in rat hypothalamus at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID248905	Inhibition 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.
AID1198072	Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in COS1 cells assessed as relative binding inhibition	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3	Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.
AID754108	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis	2013	Journal of medicinal chemistry, Jun-27, Volume: 56, Issue:12	Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.
AID1885078	Antagonist activity at Androgen receptor (unknown origin) in African green monkey COS-1 cells	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID190321	Effect of compound on testosterone hormone level on 14-day dosing in intact rats; No statistically significant difference from controls	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides.
AID731985	Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cells	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug 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.
AID626474	Displacement of [3H]progesterone from progesterone receptor in JW rabbit uterus after 2 hrs by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.
AID648203	Antagonist activity at androgen receptor T877A mutant expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID257792	AUC (0-72)hrs in rat ventral prostate at 3 mg/kg, po	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID1885121	Antagonist activity at Androgen receptor in human LNCaP cells assessed as inhibition of Binding Function 3 (BF3) of AR measured by luciferase assay	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID639168	Antiandrogenic activity in ICR mouse assessed as reduction of ventral prostate weight at 100 mg/kg, po qd administered for 7 days relative to control	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID293097	Inhibition of testoterone-induced prostate weight in castrated immature Sprague-Dawley rat at 2 mg/day relative to control	2007	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4	2-(2,2,2-Trifluoroethyl)-5,6-dichlorobenzimidazole derivatives as potent 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.
AID1636439	Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 31.6 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of N	2016	Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16	Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID242448	Displacement of [3H]R-1881 from Androgen receptor of PC3-AR cells; - = not determined	2005	Journal 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.
AID539159	Inhibition of prostate specific antigen production in human bicalutamide-resistant LNCAP cells xenografted SCID mouse at 100 mg/kg, po qd for seven cycles of 5 days on and 2 days off measured on day 17	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID230356	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; 2/0.04	1992	Journal of medicinal chemistry, May-15, Volume: 35, Issue:10	Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles.
AID257779	Inhibition of AR mediated transcriptional activation using reporter assay	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID248385	In vitro antagonistic activity against mutant androgen receptor of LNCap cells	2004	Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24	The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
AID1473740	Inhibition 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 assay	2013	Toxicological 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.
AID257785	Inhibition of human GR	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID648202	Antagonist activity at androgen receptor expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID626477	Displacement of [3H]Aldo from mineralocorticoid receptor in Sprague-Dawley rat kidney after 2 hrs by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21	Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.
AID1872310	Binding affinity to Androgen receptor (unknown origin) assessed as inhibition constant	2022	European journal of medicinal chemistry, Feb-15, Volume: 230	Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).
AID670352	Inhibition of actin based pseudopodia formation in androgen-dependent human PC3 cells at 100 uM after 48 hrs by DAPI staining based fluorescence microscopy assay	2012	Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13	Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens.
AID731981	Agonist activity at wild type Androgen receptor in human LNCaP-hr cells assessed as prostate specific antigen secretion measured after 3 days by enzyme-immunoassay	2013	Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1	Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.
AID1769346	Displacement of FluormoneAL Green from recombinant rat androgen receptor at 10 uM incubated for 4 hrs by fluorescent polarization assay relative to control	2021	Journal of medicinal chemistry, 10-28, Volume: 64, Issue:20	Development of 2-(5,6,7-Trifluoro-1
AID192021	Agonist activity indicated by a statistically significant increase in ventral prostate gland weight compared, to control animals; NA means no statistically significant increase in ventral prostate weight compared to controls.	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides.
AID1430114	Selectivity index, ratio of IC50 for mouse 3T3 cells to IC50 for AR T877A mutant in human LNCAP cells	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID305323	Inhibition of prostate weight in testosterone treated castrated immature Sprague-Dawley rat	2007	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 17, Issue:3	Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives.
AID601824	Antagonist activity at androgen receptor T877A mutant expressed in african green monkey CV1 cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity at 1 to 1000 nM by luciferase reporter gene assay	2011	Journal of medicinal chemistry, Jun-09, Volume: 54, Issue:11	Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
AID648290	Cytotoxicity against human androgen-dependent LNCAP cells by MTT assay	2012	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5	1,2,4-Oxadiazoles: a new class of anti-prostate cancer agents.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1199395	Displacement of [3H]R1881 from androgen receptor in human LNCAP cells	2015	Journal of medicinal chemistry, Mar-12, Volume: 58, Issue:5	Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
AID639153	Antagonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID759311	Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay	2013	Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14	Histone deacetylase inhibitors equipped with estrogen receptor modulation activity.
AID248278	In vitro antagonistic activity against androgen receptor of MDA-453 cells	2004	Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24	The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
AID1269934	Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 4 days by MTT assay in presence of DHT and E2	2016	Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4	Design and synthesis of novel androgen receptor antagonists via molecular modeling.
AID1249999	Plasma concentration in immature Sprague-Dawley rat prostate weight model at 10 mg/kg, po qd administered for 4 days measured 2 hrs post last dose on day 4	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID625276	FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI	2011	Drug discovery today, Aug, Volume: 16, Issue:15-16	FDA-approved drug labeling for the study of drug-induced liver injury.
AID639248	Antitumor activity against human JDCaP cells expressing wild type AR xenografted in testosterone propionate-challenged castrated BALB/c nude mouse assessed as decrease in tumor volume at 20 mg/kg, po qd administered for 29 days measured on day 28 relative	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID648201	Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor T877A mutant expressed in HEK293 cells after 3 hrs	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID294972	Reduction of prostate weight in orally dosed mature rat	2007	Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9	beta-Alkylthio indolyl carbinols: potent nonsteroidal antiandrogens with oral efficacy in a prostate cancer model.
AID630714	Antitumor activity against human LNCAP cells xenografted in athymic nude Harlan Sprague-Dawley mouse assessed as serum prostate specific antigen suppression at 10 mg/kg, po administered once daily for 5 weeks measured after 5 weeks by ELISA relative to ve	2011	Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21	Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
AID1198075	Agonist activity at pSG5-tagged human androgen receptor W741L mutant expressed in COS1 cells assessed as receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay relative to control	2015	Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3	Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.
AID292744	Inhibition of testosterone-induced prostate weight increase in Sprague-Dawley rat by modified Hersherberger assay	2007	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1	The discovery of a potent orally efficacious indole androgen receptor antagonist through in vivo screening.
AID539146	Metabolic stability in human liver microsomes assessed as compound remaining after 15 mins by LC-MS/MS analysis	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID178941	Effective dose required to inhibit 50 percent of androgen hormone activity in intact rat	1988	Journal of medicinal chemistry, May, Volume: 31, Issue:5	Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides.
AID539144	Agonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as effect on cell proliferation after 6 days	2010	Bioorganic & medicinal chemistry, Dec-01, Volume: 18, Issue:23	Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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.
AID1168321	Growth inhibition of human LNCAP cells	2014	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21	Synthesis and preliminary investigations into novel 1,2,3-triazole-derived androgen receptor antagonists inspired by bicalutamide.
AID670342	Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13	Antitumor agents 290. Design, synthesis, and biological evaluation of new LNCaP and PC-3 cytotoxic curcumin analogs conjugated with anti-androgens.
AID1249997	In vivo antagonist activity at androgen receptor in immature Sprague-Dawley rat prostate weight model assessed as testosterone propionate-induced weight of seminal vesicles over full body weight at 10 mg/kg, po qd administered for 4 days	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID578354	Displacement of [3H]17-beta-estradiol from rabbit ER by liquid scintillation counting	2011	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6	Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).
AID1233504	Antiproliferative activity against human LNCAP cells after 3 days	2015	European journal of medicinal chemistry, Jun-24, Volume: 99	Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.
AID257786	Inhibition of human ERalpha	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID527639	Antiandrogen activity against androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell proliferation by WST1 assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Novel selective anti-androgens with a diphenylpentane skeleton.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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.
AID1430113	Selectivity ratio of IC50 for AR negative human PC3 cells to IC50 for AR T877A mutant in human LNCAP cells	2017	Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5	Design, synthesis and biological evaluation of 2-(4-phenylthiazol-2-yl) isoindoline-1,3-dione derivatives as anti-prostate cancer agents.
AID630801	Antagonist activity at human AR overexpressed in human LNCAP cells at 1 uM by luciferase reporter gene assay in the presence of agonist R1881	2011	Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21	Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
AID630715	Toxicity in athymic nude Harlan Sprague-Dawley mouse xenografted with human LNCAP cells assessed as effect on body weight at 10 mg/kg, po administered once daily for 5 weeks	2011	Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21	Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1443986	Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after	2014	Hepatology (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.
AID648288	Cytotoxicity against human androgen-independent DU145 cells by MTT assay	2012	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5	1,2,4-Oxadiazoles: a new class of anti-prostate cancer agents.
AID1249995	Antagonist activity at androgen receptor in human MDA-MB-453 cells assessed as inhibition of DHT-induced PSA expression by alkaline phosphatase reporter gene assay	2015	ACS medicinal chemistry letters, Aug-13, Volume: 6, Issue:8	Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
AID248616	Inhibition of T877A androgen receptor of human prostate cancer 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.
AID648210	Anticancer activity against human LNCaP-hr cells xenografted in BALB/c athymic nude mouse assessed as change in tumor volume at 100 mg/kg, po qd after 28 days relative to control	2012	Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7	Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.
AID639164	Antiandrogenic activity in ICR mouse assessed as ventral prostate weight at 100 mg/kg, po qd administered for 7 days (Rvb = 14.6 +/- 1.6g)	2012	Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1	Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.
AID1443992	Total Cmax in human administered as single dose	2014	Hepatology (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.
AID239156	Displacement of [3H]DHT from androgen receptor of human MDA-453 cells	2004	Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24	The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
AID242058	Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells	2005	Journal 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.
AID478368	Activity at human AR expressed in human HeLa cells after 48 hrs by stable-luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9	Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	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.
AID1347160	Primary screen NINDS Rhodamine 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.
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.
AID1797738	AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm070231h: \\Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.\\	2007	Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21	Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
AID1797740	AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1016/j.bmcl.2007.01.007: \\Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.\\	2007	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6	Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
AID1797749	Luciferase Reporter Assay from Article 10.1021/jm050293c: \\(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal andr	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID1800104	HDAC Activity Assay from Article 10.1021/cb400542w: \\Selectively targeting prostate cancer with antiandrogen equipped histone deacetylase inhibitors.\\	2013	ACS chemical biology, Nov-15, Volume: 8, Issue:11	Selectively targeting prostate cancer with antiandrogen equipped histone deacetylase inhibitors.
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.
AID1347405	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection	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.
AID1347057	CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151	Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	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.
AID1347410	qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library	2019	Cellular signalling, 08, Volume: 60	A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347059	CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058	CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1346888	Human Androgen receptor (3C. 3-Ketosteroid receptors)	2010	Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7	Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
AID1346888	Human Androgen receptor (3C. 3-Ketosteroid receptors)	2006	Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2	(+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.
AID1794808	Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).	2014	Journal of biomolecular screening, Jul, Volume: 19, Issue:6	A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808	Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	11 (0.87)	18.7374
1990's	162 (12.80)	18.2507
2000's	489 (38.63)	29.6817
2010's	490 (38.70)	24.3611
2020's	114 (9.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	212 (16.15%)	5.53%
Reviews	114 (8.68%)	6.00%
Case Studies	125 (9.52%)	4.05%
Observational	6 (0.46%)	0.25%
Other	856 (65.19%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (182)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
The Registry to Observe Clinical Outcomes of Patients With High-risk Metastatic Hormone-naïve Prostate Cancer in Japan [NCT04034095]		979 participants (Actual)	Observational [Patient Registry]	2019-07-08	Active, not recruiting
ATLAS: A Randomized, Double-blind, Placebo-controlled Phase 3 Study of JNJ-56021927 in Subjects With High-risk, Localized or Locally Advanced Prostate Cancer Receiving Treatment With Primary Radiation Therapy [NCT02531516]	Phase 3	1,503 participants (Actual)	Interventional	2015-11-30	Active, not recruiting
A Phase I/II, Single Arm, Non-randomized Study of Ribociclib (LEE011), a CDK 4/6 Inhibitor, in Combination With Bicalutamide, an Androgen Receptor (AR) Inhibitor, in Advanced AR+ Triple-negative Breast Cancer: Big Ten Cancer Research Consortium BRE15-024 [NCT03090165]	Phase 1/Phase 2	37 participants (Anticipated)	Interventional	2018-05-07	Recruiting
A Phase III Trial to Evaluate the Duration of Neoadjuvant Total Androgen Suppression (TAS) and Radiation Therapy (RT) in Intermediate-Risk Prostate Cancer [NCT00005044]	Phase 3	1,579 participants (Actual)	Interventional	2000-02-29	Completed
A Phase III Randomized Prospective Trial of Adjuvant Hormonal Therapy in Surgically Treated Prostate Cancer Patients at High Risk for Recurrence [NCT00003645]	Phase 3	64 participants (Actual)	Interventional	1999-06-14	Terminated(stopped due to Per PI request)
A Canadian Phase II, Placebo-controlled Randomized Trial of Bicalutamide in Patients Receiving Maintenance Avelumab for Metastatic Urothelial Cancer. [NCT06018116]	Phase 2	69 participants (Anticipated)	Interventional	2023-10-31	Not yet recruiting
A PHASE III TRIAL OF RADIATION THERAPY WITH OR WITHOUT CASODEX IN PATIENTS WITH PSA ELEVATION FOLLOWING RADICAL PROSTATECTOMY FOR pT3N0 CARCINOMA OF THE PROSTATE [NCT00002874]	Phase 3	840 participants (Actual)	Interventional	1998-02-28	Completed
[NCT02382094]	Phase 3	110 participants (Actual)	Interventional	2005-06-30	Completed
Neoadjuvant Treatment of Prostate Cancer With Bicalutamide and Raloxifene Prior to Radical Prostatectomy [NCT03147196]	Phase 2	0 participants (Actual)	Interventional	2017-06-27	Withdrawn(stopped due to lack of accrual)
Phase II Study Evaluating HSV-tk + Valacyclovir Gene Therapy in Combination With Androgen Deprivation Therapy, Brachytherapy, External Beam Radiotherapy, and Prostatectomy for High-Risk Prostate Cancer [NCT03541928]	Phase 2	60 participants (Anticipated)	Interventional	2018-08-02	Recruiting
An Open-label, Non-comparative, Multi-centre Study to Assess the Efficacy and Safety of Bicalutamide When Used in Combination With Anastrozole for the Treatment of Gonadotropin-independent Precocious Puberty in Boys With Testotoxicosis [NCT00094328]	Phase 2	14 participants (Actual)	Interventional	2004-11-22	Completed
A Phase 3 Study of Androgen Annihilation in High-Risk Biochemically Relapsed Prostate Cancer [NCT03009981]	Phase 3	504 participants (Anticipated)	Interventional	2017-03-06	Active, not recruiting
A Phase I/II Study of High-Dose-Rate Brachytherapy as Monotherapy for Prostate Cancer [NCT02346253]		163 participants (Anticipated)	Interventional	2015-01-13	Active, not recruiting
Bicalutamide in Treating Patients With AR-positive Metastatic Triple Negative Breast Cancer [NCT02353988]	Phase 2	60 participants (Anticipated)	Interventional	2015-01-31	Not yet recruiting
A Phase III, Multicenter, Randomized, Open Study of SHR3680 Compared to Bicalutamide in the Treatment of Patients With Hormone Sensitive Prostate Cancer [NCT03520478]	Phase 3	654 participants (Actual)	Interventional	2018-05-30	Active, not recruiting
A Phase II Study of PROSTVAC-V (Vaccinia)/TRICOM and PROSTVAC-F (Fowlpox)/TRICOM With GM-CSF in Patients With PSA Progression After Local Therapy for Prostate Cancer [NCT00108732]	Phase 2	50 participants (Actual)	Interventional	2006-02-28	Completed
Bicalutamide Implants (Biolen) With Radiation Therapy in Patients With Localized Prostate Cancer [NCT04943536]	Phase 1	20 participants (Anticipated)	Interventional	2021-10-01	Recruiting
A Randomized, Multicenter,Phase III Study of Bicalutamide Versus Chemotherapy in First Line Treatment of AR Positive Metastatic Triple Negative Breast Cancer [NCT03055312]	Phase 3	36 participants (Actual)	Interventional	2016-12-20	Terminated
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: PRIME [NCT03878524]	Phase 1	2 participants (Actual)	Interventional	2020-04-01	Active, not recruiting
Phase III Trial of Dose Escalated Radiation Therapy and Standard Androgen Deprivation Therapy (ADT) With a GNRH Agonist vs. Dose Escalated Radiation Therapy and Enhanced ADT With a GNRH Agonist and TAK-700 For Men With High Risk Prostate Cancer [NCT01546987]	Phase 3	239 participants (Actual)	Interventional	2012-05-31	Active, not recruiting
Adjuvant Androgen Deprivation Versus Mitoxantrone Plus Prednisone Plus Androgen Deprivation in Selected High-Risk Prostate Cancer Patients Following Radical Prostatectomy [NCT00004124]	Phase 3	983 participants (Actual)	Interventional	1999-10-15	Completed
Radiation Therapy and Androgen Deprivation Therapy in Treating Patients Who Have Undergone Surgery for Prostate Cancer (RADICALS) [NCT00541047]	Phase 3	4,236 participants (Actual)	Interventional	2007-11-30	Completed
Phase II Evaluation of Early Oral Estramustine, Oral Etoposide and Intravenous Paclitaxel in Combination With Hormone Therapy in Patients With High-Risk Metastatic Adenocarinoma of the Prostate [NCT00028769]	Phase 2	41 participants (Actual)	Interventional	2001-12-31	Completed
Intermittent Androgen Deprivation in Patients With Stage D2 Prostate Cancer, Phase III [NCT00002651]	Phase 3	3,040 participants (Actual)	Interventional	1995-05-31	Completed
A Randomized, Double-Blind, Phase II, Efficacy and Safety Study of MDV3100 Versus Bicalutamide in Castrate Men With Metastatic Prostate Cancer [NCT01288911]	Phase 2	375 participants (Actual)	Interventional	2011-03-22	Completed
Temsirolimus, an mTOR Inhibitor, to Reverse Androgen Insensitivity in Patients With Castration-resistant Prostate Cancer [NCT01020305]	Phase 1/Phase 2	5 participants (Actual)	Interventional	2009-10-31	Terminated(stopped due to Decision by funding sponsor due to poor accrual)
A Phase III Study of Neoadjuvant Docetaxel and Androgen Suppression Plus Radiation Therapy Versus Androgen Suppression Alone Plus Radiation Therapy for High-Risk Localized Adenocarcinoma of the Prostate [NCT00651326]	Phase 3	48 participants (Actual)	Interventional	2008-06-02	Terminated(stopped due to Poor accrual)
A Phase 2 Study of Bicalutamide Plus Finasteride in Men With MRI Detectable Prostate Nodules Undergoing Active Surveillance [NCT02146937]	Phase 2	0 participants (Actual)	Interventional	2014-03-31	Withdrawn(stopped due to Due to lack of accrual for this study. PI decided to close the study.)
Phase II Study of Neoadjuvant IMC-A12 Combined With Androgen Deprivation Prior to Prostatectomy [NCT00769795]	Phase 2	29 participants (Actual)	Interventional	2008-10-31	Completed
Randomized Trial of Bicalutamide to Block TMPRSS2 in Males With COVID-19 Infection [NCT04509999]	Phase 3	0 participants (Actual)	Interventional	2020-10-26	Withdrawn(stopped due to No patients enrolled and funding withdrawn)
A Phase II Study of Nivolumab Combined With Bicalutamide and Ipilimumab in Metastatic HER2-negative Breast Cancer [NCT03650894]	Phase 2	30 participants (Actual)	Interventional	2019-04-03	Active, not recruiting
A Phase III Randomized Trial Comparing Androgen Deprivation Therapy + TAK-700 With Androgen Deprivation Therapy + Bicalutamide in Patients With Newly Diagnosed Metastatic Sensitive Prostate Cancer [NCT01809691]	Phase 3	1,313 participants (Actual)	Interventional	2013-03-08	Active, not recruiting
A Randomized Study of Finite Androgen Ablation vs. Finite Androgen Ablation in Combination With Abiraterone Acetate and Prednisone in Patients With Prostate Cancer Who Have PSA Progression After Prostatectomy and/or Radiotherapy [NCT01786265]	Phase 2	310 participants (Anticipated)	Interventional	2013-02-05	Active, not recruiting
A Study to Establish the Feasibility of Biolen for the Local Delivery of Bicalutamide in Patients With Prostate Cancer [NCT04284761]	Phase 1	17 participants (Actual)	Interventional	2020-10-11	Completed
A Phase I Trial to Evaluate Acute and Late Toxicities of Concurrent Treatment With Everolimus (RAD001) and Radio-Hormonotherapy in High-risk Prostate Cancer.(RHOMUS) [NCT00943956]	Phase 1	30 participants (Actual)	Interventional	2009-01-31	Completed
A Randomized, Open Label, Multicenter, Phase III, 2-Arm Study of Androgen Deprivation With Leuprolide, +/- Docetaxel for Clinically Asymptomatic Prostate Cancer Subjects With a Rising PSA Following Definitive Local Therapy [NCT00514917]	Phase 3	413 participants (Actual)	Interventional	2007-07-31	Terminated(stopped due to Company decision to discontinue the study, not due to any safety or efficacy concerns)
Pilot Trial of Bicalutamide Versus Placebo in Reproductive-Aged Women With Nonalcoholic Fatty Liver Disease (NAFLD) and Polycystic Ovary Syndrome (PCOS) [NCT05979389]	Phase 1	50 participants (Anticipated)	Interventional	2023-12-31	Not yet recruiting
Autonomic and Renal Contributions to Hypertension With Androgen Deprivation Therapy [NCT05700903]	Phase 4	228 participants (Anticipated)	Interventional	2023-09-20	Recruiting
Randomized, 1-Way Parallel, Bioequivalence Study of Bicalutamide 50 mg Tablets and Casodex® Administered as 1 x 50 mg Tablet in Healthy Subjects Under Fasting Conditions [NCT00973050]	Phase 1	60 participants (Actual)	Interventional	2003-09-30	Completed
Diagnosing and Monitoring Recurrent Disease in Prostate Cancer Patients Using a Positron Emission Tomography Radiotracer (Axumin™) [NCT03996993]		20 participants (Anticipated)	Observational	2019-07-01	Recruiting
Imperial Prostate 4: Comparative Health Research Outcomes of NOvel Surgery in Prostate Cancer [NCT04049747]		2,450 participants (Anticipated)	Interventional	2019-12-11	Recruiting
A Randomized Phase II Trial on the Addition of Dutasteride to Combined Androgen Blockade Therapy Versus Combined Androgen Blockade Therapy Alone in Patients With Recurrent and/or Metastatic Salivary Duct Carcinoma - DUCT Study [NCT05513365]	Phase 2	98 participants (Anticipated)	Interventional	2022-09-27	Recruiting
Phase II-III Trial of Adjuvant Radiotherapy Following Radical Prostatectomy With or Without Adjuvant Docetaxel [NCT03070886]	Phase 2/Phase 3	175 participants (Actual)	Interventional	2017-01-16	Active, not recruiting
Randomised, Double-blind, Placebo Controlled, Parallel-group, Multicentre Phase II Study to Assess Dose Response Relationship of Nolvadex (Oral Tablet) in Prophylactic Treatment of Gynaecomastia and Breast Pain Associated With CASODEX 150 mg (Oral Tablet) [NCT00637871]	Phase 2	0 participants	Interventional	2002-11-30	Completed
Phase II Randomized Clinical Trial Comparing 3-D Conformal Radiation Therapy (RT) vs. Intensity Modulated Radiation Therapy in Post- Prostatectomy Prostate Cancer Patients [NCT02678520]	Phase 2	0 participants (Actual)	Interventional	2015-12-31	Withdrawn(stopped due to PI no longer at institution. Study terminated prior to enrolling subjects.)
FDHT-PET to Visualize the Effect on the Androgen Receptor Level by Bicalutamide [NCT02697032]	Phase 2	22 participants (Actual)	Interventional	2016-02-29	Completed
Randomized, Open-Label, 1-Way Parallel, Bioequivalence Study of Bicalutamide 50 mg Tablet and Casodex (Reference) Following a 50 mg Dose in Healthy Subjects Under Fasting Conditions. [NCT00959335]	Phase 1	36 participants (Actual)	Interventional	2006-08-31	Completed
A Prospective Multi-center Study to Compare the QOL and Efficacy of Endocrine Therapy With or Without Cryoablation for Stage IV Prostate Cancer. [NCT02615223]		120 participants (Anticipated)	Interventional	2015-11-30	Recruiting
A Randomized, Double-Blind, Parallel-Group Trial Comparing Casodex 150mg Once Daily With Placebo in Patients With Non-Metastatic Prostate Cancer. [NCT00672282]	Phase 3	1,218 participants (Actual)	Interventional	1995-10-31	Completed
Adjuvant 3DCRT/IMRT in Combination With Androgen Suppression and Docetaxel for High Risk Prostate Cancer Patients Post-Prostatectomy: A Phase II Trial [NCT00528866]	Phase 2	80 participants (Actual)	Interventional	2008-04-30	Completed
Randomized, Bioequivalence Study of Bicalutamide 50 mg Tablet and Casodex 50 mg Tablet Following a 50 mg Dose in Healthy Subjects Under Fasting Conditions [NCT01039233]	Phase 1	60 participants (Actual)	Interventional	2005-05-31	Completed
A Randomised, Parallel-arm, Open-label Trial Comparing Degarelix With Goserelin Plus Anti-androgen Flare Protection (Bicalutamide), in Terms of Reduction in International Prostate Symptom Score (IPSS), in Patients With Lower Urinary Tract Symptoms (LUTS) [NCT00831233]	Phase 3	42 participants (Actual)	Interventional	2009-04-30	Terminated(stopped due to Poor recruitment due to rare targeted population)
A Randomised, Parallel-arm, Open-label Trial Comparing Degarelix With Goserelin Plus Anti-androgen Flare Protection (Bicalutamide), in Terms of Volume Reduction of the Prostate in Patients With Prostate Cancer Being Candidates for Medical Castration [NCT00884273]	Phase 3	182 participants (Actual)	Interventional	2009-08-31	Completed
A Randomized, Double-Blind, Parallel-Group Trial Comparing Bicalutamide (Casodex) 150mg Once Daily With Placebo in Patients With Non-metastatic Prostate Cancer [NCT00673205]	Phase 3	3,588 participants (Actual)	Interventional	1995-09-30	Completed
Neoadjuvant Androgen Depletion in Combination With Vorinostat Followed by Radical Prostatectomy for Localized Prostate Cancer: Total Androgen-Receptor Gene Expression Targeted Therapy (TARGET) [NCT00589472]	Phase 2	19 participants (Actual)	Interventional	2007-11-30	Completed
A Prospective Multi-center Study to Compare the QOL and Efficacy of External Beam Radiation Therapy or Cryoablation Therapy for Stage III Prostate Cancer [NCT02605226]		240 participants (Anticipated)	Interventional	2015-11-30	Recruiting
Phase II Interstitial Brachytherapy Combined With Androgen Deprivation Therapy for Locally Recurrent Prostate Cancer After Prior External Beam Irradiation [NCT00684905]	Phase 2	50 participants (Anticipated)	Interventional	2000-04-30	Completed
Rapid Hormonal Cycling as Treatment for Patients With Prostate Cancer: The Men's Cycle [NCT00586898]	Phase 2	36 participants (Actual)	Interventional	2001-07-31	Completed
A Compassionate Use Trial With Bicalutamide (Casodex) 150-mg for Subjects With Prostate Cancer [NCT00636259]		0 participants	Expanded Access		No longer available
Androgen Deprivation and Localized Radiotherapy to Metastases in Patients With Oligometastatic Hormone - Sensitive Prostate Cancer [NCT00544830]	Phase 2	29 participants (Actual)	Interventional	2006-07-18	Active, not recruiting
Utility of Exosomal microRNAs to Predict Response to Androgen Deprivation Therapy in Prostate Cancer Patients [NCT02366494]		60 participants (Anticipated)	Observational	2015-04-29	Active, not recruiting
Phase I Study Evaluating Extended Field Intensity Modulated Radiation Therapy and Docetaxel in Patients With Prostate Cancer Associated With Pelvic Node Metastasis [NCT00482807]	Phase 1	9 participants (Actual)	Interventional	2004-08-31	Completed
Phase II, Randomized Study of Patients With Rising PSA at High-Risk of Progression After Primary Therapy to Assess the Clinical and Molecular Efficacy of the Enzastaurin - Bicalutamide Combination to Suppress the Androgen Receptor Without Testosterone Abl [NCT00685633]	Phase 2	0 participants (Actual)	Interventional	2008-12-31	Withdrawn
Phase III Study of the Comparison of Abarelix Versus Goserelin Plus Bicalutamide in Patients With Advanced or Metastatic Prostate Cancer. A One Year Randomised, Open Label, Multi-Centre Phase III Trial. [NCT00841113]	Phase 3	177 participants (Actual)	Interventional	1999-01-31	Completed
Sunitinib, Hormonal Ablation and External Beam Radiation Therapy for High-Risk and Locally Advanced Prostate Cancer [NCT00631527]	Phase 1	19 participants (Actual)	Interventional	2008-02-29	Completed
A Phase II Randomised Efficacy and Safety Study of Vandetanib (ZD 6474) in Combination With Bicalutamide Versus Bicalutamide Alone in Patients With Chemotherapy Naive Hormone Refractory Prostate Cancer. [NCT00757692]	Phase 2	74 participants (Actual)	Interventional	2009-01-31	Completed
INTREPId (INTermediate Risk Erection PreservatIon Trial): A Randomized Trial of Radiation Therapy and Darolutamide for Prostate Cancer [NCT04025372]	Phase 2	220 participants (Anticipated)	Interventional	2020-06-01	Recruiting
Randomized, Open-Label, 1-Way Parallel, Bioequivalence Study of Bicalutamide 50 mg Tablet and Casodex (Reference) Following a 50 mg Dose in Healthy Subjects Under Fed Conditions. [NCT00960310]	Phase 1	36 participants (Actual)	Interventional	2006-06-30	Completed
Bioequivalence Study of ICI176,334-1 in Japanese Healthy Male Subjects - Evaluation of Bioequivalence of ICI176,334-1 and Casodex 80 mg Tablet - [NCT01415778]	Phase 1	48 participants (Actual)	Interventional	2011-08-31	Completed
Oral Mucosal Absorption of ICI176,334-1 in Japanese Healthy Male Subjects [NCT01415791]	Phase 1	8 participants (Actual)	Interventional	2011-08-31	Completed
A Phase I/II Trial of Post-Prostatectomy Radiation Therapy, Hormonal Therapy and Concurrent Docetaxel for High Risk Pathologic T2-T3NO (Tumor-3, Node-0) Prostate Cancer [NCT00669162]	Phase 1/Phase 2	27 participants (Actual)	Interventional	2012-08-31	Completed
The Impact of Continuous Versus Intermittent Androgen Deprivation Therapy on Bone Mineral Density Change in Prostate Cancer Patients: A Multicenter, Randomized Clinical Trial [NCT04248621]	Phase 4	164 participants (Anticipated)	Interventional	2020-01-23	Recruiting
A Randomised, Parallel Arm, Open-label Trial Comparing Degarelix With Goserelin Plus Anti-androgen Flare Protection (Bicalutamide), in Terms of Prostate Size Reduction in Prostate Cancer Patients of Intermediate-to-high Risk, Who Require Neoadjuvant Hormo [NCT00833248]	Phase 3	246 participants (Actual)	Interventional	2009-04-30	Completed
OMPCa-Shanghai: An Open-label, Randomized Prospective Phase II Trial of Androgen Deprivation Therapy or Androgen Deprivation Therapy Plus Definitive Treatment (Radiation or Surgery) of the Primary Tumor in Oligometastatic Prostate Cancer [NCT02742675]	Phase 2	200 participants (Anticipated)	Interventional	2015-09-30	Active, not recruiting
A Multicenter, Phase IB/II Study of Abemaciclib in Combination With Bicalutamide for Androgen Receptor-positive, HER2-negative Metastatic Breast Cancer [NCT05095207]	Phase 1/Phase 2	60 participants (Anticipated)	Interventional	2021-09-29	Recruiting
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)	Interventional	2010-12-17	Active, not recruiting
Randomized, 1-Way, Parallel, Bioequivalence Study of Bicalutamide 50 mg Tablets and Casodex® Administered as 1 x 50 mg Tablet in Healthy Subjects Under Fed Conditions [NCT00972855]	Phase 1	60 participants (Actual)	Interventional	2003-09-30	Completed
Phase Ib Study of Limited Androgen Ablation and Two Dose Levels of Temsirolimus (NSC#683864) in Patients With Prostate Cancer Who Have a Biochemical Relapse After Prostatectomy and/or Radiotherapy [NCT00512668]	Phase 1	24 participants (Actual)	Interventional	2007-09-30	Terminated
Long Term Changes in Bone Mineral Density and Fracture Risk in Patients Receiving Androgen Deprivation Therapy for Advanced Prostate Cancer, With Stratification of Treatment Based on Presenting Values [NCT00536653]		618 participants (Actual)	Interventional	1999-10-31	Completed
Pilot Trial to Evaluate the Safety and Efficacy of the Administration of Bicalutamide (Casodex TM) Per Day in Combination With Raloxifene (Evista TM) Per Day in Patients With Hormone Refractory Prostate Cancer [NCT01050842]	Early Phase 1	18 participants (Actual)	Interventional	2010-02-28	Completed
COMBO Trial: Camostat With Bicalutamide for COVID-19 [NCT04652765]	Phase 1	6 participants (Actual)	Interventional	2021-02-03	Terminated(stopped due to PI Decision to close/stop the study due to no new accrual.)
An Open Label Randomized Phase 2 Study To Evaluate The Activity, Tolerability, And Toxicity Of Combined Neoadjuvant Anti-angiogenesis and Androgen Ablation Therapy in Men Undergoing Radical Prostatectomy [NCT00244920]	Phase 2	0 participants (Actual)	Interventional	2002-01-31	Withdrawn(stopped due to Sponsor withdrew drug.)
A Randomized, Phase II Trial of Brief Androgen-Ablation Combined With Cell-based CG1940/CG8711 Immunotherapy For Prostate Cancer in Patients With Non-Metastatic, Biochemically Relapsed Prostate Cancer [NCT00771017]	Phase 2	0 participants (Actual)	Interventional	2008-07-31	Withdrawn
Phase II Study of Talazoparib With Androgen Deprivation Therapy and Abiraterone in Castration Sensitive Prostate Cancer [NCT04734730]	Phase 2	70 participants (Anticipated)	Interventional	2021-05-04	Recruiting
An Open Randomised Trial to Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX Monotherapy Induced Gynaecomastia and/or Breast Pain in Prostate Cancer Patients [NCT00590213]	Phase 4	125 participants (Anticipated)	Interventional	2003-06-30	Completed
A Randomized Double-Blind Parallel Group Study Comparing Casodex (or Generic Equivalent) 50mg Plus Placebo to Casodex (or Generic Equivalent) 50mg Plus Dutasteride 3.5mg Administered for 18 Months to Men With Prostate Cancer Who Have Failed First-Line And [NCT00470834]	Phase 4	127 participants (Actual)	Interventional	2007-05-31	Completed
Parallel Phase III Randomized Trials of Genomic-Risk Stratified Unfavorable Intermediate Risk Prostate Cancer: De-Intensification and Intensification Clinical Trial Evaluation (GUIDANCE) [NCT05050084]	Phase 3	2,050 participants (Anticipated)	Interventional	2021-11-03	Recruiting
Parallel Phase III Randomized Trials for High Risk Prostate Cancer Evaluating De-Intensification for Lower Genomic Risk and Intensification of Concurrent Therapy for Higher Genomic Risk With Radiation (PREDICT-RT*) [NCT04513717]	Phase 3	2,478 participants (Anticipated)	Interventional	2020-12-15	Recruiting
A Randomized Phase II Study to Evaluate the Efficacy and Safety of Chemotherapy (CT) vs Androgen Deprivation Therapy (ADT) in Patients With Recurrent and/or Metastatic, Androgen Receptor (AR) Expressing, Salivary Gland Cancer (SGCs) [NCT01969578]	Phase 2	149 participants (Actual)	Interventional	2015-09-24	Active, not recruiting
Cancer Hospital, Chinese Academy of Medical Sciences/National Cancer Center of China [NCT06145308]	Phase 2	30 participants (Anticipated)	Interventional	2023-12-01	Recruiting
A Randomized, Double-blind Phase II Trial to Assess the Efficacy and Safety of Bicalutamide (Casodex® ) Associated to ZD6474 (Zactima™ ) or to Placebo in Patients With Castration-refractory Metastatic Prostate Cancer Without Any Clinical Symptom Related t [NCT00659438]	Phase 2	95 participants (Actual)	Interventional	2008-02-29	Completed
A Randomized Phase II Study of Peripheral Androgen Blockade With Bicalutamide Followed by Placebo or Treatment With the Gamma Secretase Inhibitor RO4929097 in Men With Rising PSA After Definitive Local Therapy for Adenocarcinoma of the Prostate [NCT01200810]	Phase 2	10 participants (Actual)	Interventional	2010-08-31	Terminated(stopped due to Drug was no longer available)
A Randomized Double-Blind Comparative Trial of Bicalutamide (Casodex™) Versus Placebo in Patients With Early Prostate Cancer. [NCT00657904]	Phase 3	3,618 participants (Actual)	Interventional	1995-08-31	Completed
Bioequivalence Study of ICI176,334-1 (Bicalutamide New Formulation) in Japanese Healthy Male Subjects - Evaluation of Bioequivalence of ICI176,334-1 and Casodex Tablet (80mg) [NCT01416870]	Phase 1	102 participants (Actual)	Interventional	2010-07-31	Terminated
Oral Mucosal Absorption Study of ICI176,334-1 (Bicalutamide New Formulation) in Japanese Healthy Male Subjects [NCT01416883]	Phase 1	8 participants (Actual)	Interventional	2010-07-31	Terminated
Bicalutamide Monotherapy Preserves Bone Mineral Density, Muscle Strength and Has Significant Quality of Life Benefits for Men With Advanced Prostate Cancer [NCT00551044]		42 participants (Actual)	Interventional	2003-08-31	Completed
Randomized, Multicentre, Phase III Study in Patients With Intermediate-risk T1 T2 Prostate Adenocarcinomas, to Verify the Role of Six Months of Total Androgen Blockade for Two Dosage Levels of Prostate Radiation Therapy (70 Gy and 76 Gy) Versus Prostate R [NCT00223145]	Phase 3	600 participants (Actual)	Interventional	2000-12-31	Active, not recruiting
A Treatment Protocol to Monitor the Safety of a 200 mg Daily Dose of Bicalutamide (Casodex) in Patients With Advanced Prostate Cancer [NCT00846976]	Phase 3	101 participants (Actual)	Interventional	1994-12-31	Completed
Phase 2 Trial of Maximum Androgen Blockade (MAB) Dose Escalation From 50 mg to 150 mg Bicalutamide (Casodex) for Biochemical Failure in Prostate Cancer Patients [NCT00554086]	Phase 2	65 participants (Actual)	Interventional	2005-11-30	Completed
Veterans Affairs Seamless Phase II/III Randomized Trial of STAndard Systemic theRapy With or Without PET-directed Local Therapy for OligoRecurrenT Prostate Cancer (VA STARPORT) [NCT04787744]	Phase 2/Phase 3	464 participants (Anticipated)	Interventional	2021-07-01	Recruiting
A Multi-centre, Single-arm, Prospective Study to Assess Efficacy and Safety of Neoadjuvant Hormone Therapy Using Zoladex (Goserelin) and Casodex (Bicalutamide) in Patients With Advanced Prostate Cancer Undergoing Radical Prostatectomy. [NCT03971110]	Phase 4	9 participants (Actual)	Interventional	2021-01-28	Terminated(stopped due to Due to the limited potential patients pool, the enrollment goal could not be achieved. After review and communication, the decision to teminate study was made.)
A Phase II Study of the Efficacy and Tolerability of Bicalutamide Plus Aromatase Inhibitors in Estrogen Receptor(+)/Androgen Receptor(+)/HER2(-) Metastatic Breast Cancer [NCT02910050]	Phase 2	58 participants (Anticipated)	Interventional	2016-01-31	Recruiting
A Phase II Trial to Promote Recovery From COVID-19 With Endocrine Therapy [NCT04374279]	Phase 2	0 participants (Actual)	Interventional	2021-04-30	Withdrawn(stopped due to Limited resources.)
A Pilot Study of Hormonal Therapy Combined With Central Memory T Cells (Tcm) for Patients With Advanced Prostate Cancer [NCT03587285]	Phase 1/Phase 2	11 participants (Actual)	Interventional	2018-09-23	Active, not recruiting
A Phase III Prospective Randomized Trial of Dose-Escalated Radiotherapy With or Without Short-Term Androgen Deprivation Therapy for Patients With Intermediate-Risk Prostate Cancer [NCT00936390]	Phase 3	1,538 participants (Actual)	Interventional	2009-09-30	Active, not recruiting
Implant and External Radiation for Prostate Cancer With or Without Hormonal Therapy: A Prospective Randomized Trial [NCT00243646]	Phase 3	6 participants (Actual)	Interventional	2004-08-31	Terminated(stopped due to poor accrual)
Longitudinal, Randomized, Open and Prospective Clinical Trial to Evaluate the Efficacy of Continuous vs Intermittent Maximum Androgen Blockade (CMAB vs IMAB) With Goserelin-Bicalutamide Combination in the Treatment of Hormonal naïve With Metastatic Prosta [NCT00255268]	Phase 4	15 participants (Anticipated)	Interventional	2004-08-31	Withdrawn
A Randomized, Placebo-Controlled Phase IIb Clinical Trial of 2-Difluoromethylornithine (DFMO) Versus Bicalutamide (CASODEX) Alone and in Combination in Patients With Prostate Cancer in the Period Prior to Radical Prostatectomy or Brachytherapy: Modulation [NCT00086736]	Phase 2	34 participants (Actual)	Interventional	2001-11-30	Completed
Phase I Trial of Concurrent Taxotere With Radiation Therapy and Hormonal Therapy For Clinically Localized High Risk Prostate Cancer [NCT00099086]	Phase 1	20 participants (Actual)	Interventional	2007-01-16	Active, not recruiting
A Phase III Trial of Short Term Androgen Deprivation With Pelvic Lymph Node or Prostate Bed Only Radiotherapy (SPPORT) in Prostate Cancer Patients With a Rising PSA After Radical Prostatectomy [NCT00567580]	Phase 3	1,792 participants (Actual)	Interventional	2008-02-29	Active, not recruiting
A Phase 2 Study of GW786034 (Pazopanib) With or Without Bicalutamide in Hormone Refractory Prostate Cancer [NCT00486642]	Phase 2	23 participants (Actual)	Interventional	2007-09-30	Completed
A Phase II Randomized Trial of Bicalutamide in Patients Receiving Intravesical BCG for Non-muscle Invasive Bladder Cancer [NCT05327647]	Phase 2	160 participants (Anticipated)	Interventional	2022-06-23	Recruiting
A Phase II Study of AT101, to Abrogate BCL-2 Mediated Resistance to Androgen Ablation Therapy in Patients With Newly Diagnosed Stage D2 Prostate Cancer [NCT00666666]	Phase 2	55 participants (Actual)	Interventional	2009-07-31	Completed
Phase II Trial of Bicalutamide and RAD001 in Patients With Hormone-Independent Prostatic Adenocarcinoma (HIPC) After the First-Line Androgen Deprivation Therapy [NCT00814788]	Phase 2	24 participants (Actual)	Interventional	2008-12-31	Completed
Phase I/II Randomized Trial of LBH589 (Panobinostat) at Two Dose Levels Combined With Bicalutamide (Casodex) in Men With Castration-resistant Prostate Cancer [NCT00878436]	Phase 1/Phase 2	52 participants (Actual)	Interventional	2009-06-30	Completed
A Randomized Phase II Study of Androgen Deprivation Combined With IMC-A12 Versus Androgen Deprivation Alone for Patients With New Hormone Sensitive Metastatic Prostate Cancer [NCT01120236]	Phase 2	211 participants (Actual)	Interventional	2010-12-31	Completed
Docetaxel, Estramustine and Short Term Androgen Withdrawal for Patients With a Rising PSA After Definitive Local Treatment [NCT00165399]	Phase 2	62 participants (Actual)	Interventional	2004-03-31	Completed
A Comparative Trial of the Efficacy of Two Different Nolvadex (NDX) Dosing and Scheduling Regimens in Preventing Gynecomastia Induced by Casodex (CDX) 150 Monotherapy in Prostate Cancer Patients. An Open, Multicenter, Phase III Trial. [NCT00233610]	Phase 3	180 participants	Interventional	2003-12-31	Completed
Phase I/II Trial of Palbociclib in Combination With Bicalutamide for the Treatment of AR(+) Metastatic Breast Cancer (MBC) [NCT02605486]	Phase 1/Phase 2	46 participants (Actual)	Interventional	2015-11-11	Active, not recruiting
Pilot Phase II Trial of Bevacizumab in Combination With Hormonal and Radiotherapy in Patients With High-Risk Prostate Cancer [NCT00348998]	Phase 2	18 participants (Anticipated)	Interventional	2006-04-30	Active, not recruiting
Phase II Trial of Abraxane Plus Hormonal Therapy as Initial Treatment of Unresectable or Metastatic Adenocarcinoma of the Prostate [NCT00521781]	Phase 2	14 participants (Actual)	Interventional	2007-08-31	Terminated(stopped due to Sponsor decision)
A Phase I Study Of SU5416 With Androgen Ablation And Radiation In Patients With Intermediate and Advanced Stage Prostate Cancer [NCT00026377]	Phase 1	3 participants (Actual)	Interventional	2001-11-30	Completed
A Phase II Trial Of Oral Bicalutamide With Subcutaneous Goserelin In Patients With Epithelial Ovarian, Fallopian Tube, Or Peritoneal Carcinoma In Second Or Greater Remission [NCT00012090]	Phase 2	0 participants	Interventional	2000-09-30	Completed
Randomized Phase III Step-Up Study On Initial Antiandrogen Monotherapy In Comparison With Watchful Waiting In Asymptomatic T1-3 Any G (Any Gleason) NO or Nx M0 Prostate Cancer Patients Without Local Treatment With Curative Intent [NCT00014586]	Phase 3	110 participants (Actual)	Interventional	2001-01-31	Terminated(stopped due to low accrual)
Phase III Randomized Trial Study Comparing the Outcome of High-Dose IMRT (86.4 GY) Alone With IMRT to 75.6 GY Plus Neoadjuvant/Adjuvant Androgen Deprivation in Patients With High Grade Intermediate Risk and Unfavorable Risk Prostate Cancer [NCT00067015]	Phase 3	3 participants (Actual)	Interventional	2003-05-31	Completed
Three Dimensional Conformal Radiotherapy / Intensity Modulated Radiotherapy Alone Vs Three Dimensional Conformal Therapy / Intensity Modulated Radiotherapy Plus Adjuvant Hormonal Therapy In Localized T1b-c, T2a, N0, M0 Prostatic Carcinoma. A Phase III Ran [NCT00021450]	Phase 3	819 participants (Actual)	Interventional	2001-04-30	Completed
Phase III Randomized Study of Adjuvant Therapy for High Risk pT3N0 Prostate Cancer [NCT00023829]	Phase 3	67 participants (Actual)	Interventional	2001-08-31	Completed
A Phase III Randomized Study of Patients With High Risk, Hormone-Naive Prostate Cancer: Androgen Blockade With 4 Cycles of Immediate Chemotherapy Versus Androgen Blockade With Delayed Chemotherapy [NCT00030654]	Phase 3	21 participants (Actual)	Interventional	2002-10-31	Completed
A Randomized Phase II Trial of Exemestane With and Without Bicalutamide as Second Line Therapy After Failure of Androgen Suppression in Advanced Prostate Cancer [NCT00031889]	Phase 2	5 participants (Actual)	Interventional	2001-08-31	Completed
A Phase 1, Open Label, Non-Randomized, Dose Escalation Study to Evaluate the Safety of CP-675,206 in Combination With Neoadjuvant Androgen Ablation and a Phase 2, Open Label, Randomized Study to Evaluate the Efficacy of CP-675,206 in Combination With Neoa [NCT00075192]	Phase 1/Phase 2	8 participants (Actual)	Interventional	2004-03-31	Completed
A Randomized Phase III Study Comparing Androgen Suppression and Elective Pelvic Nodal Irradiation Followed by High Dose 3-D Conformal Boost Versus Androgen Suppression and Elective Pelvic Nodal Irradiation Followed by 125-Iodine Brachytherapy Implant Boos [NCT00175396]	Phase 3	400 participants (Anticipated)	Interventional	2004-05-31	Active, not recruiting
A Phase II Trial of Avastin, Docetaxel and Androgen Deprivation Followed by Continued Avastin and Androgen Deprivation for Men With a Rising Prostate Specific Antigen (PSA) After Local Therapy [NCT00658697]	Phase 2	42 participants (Actual)	Interventional	2008-06-30	Completed
The Role of HER Receptor Family as Indicator of Prognosis and Drug Responsiveness in Locally Advanced Prostate Cancer [NCT00418080]	Phase 2	86 participants	Interventional	2002-04-30	Completed
A Randomised Pilot Study to Evaluate the Effect(s) of Casodex 150 mg and Zoladex 3.6 mg on Pathological and Genomic Tumour Markers in Subjects Undergoing Radical Prostatectomy for Localised Prostate Carcinoma [NCT00293696]	Phase 4	30 participants (Actual)	Interventional	2004-10-31	Completed
Phase II Randomized Comparative Trial of TAK-700 (Orteronel) Versus Bicalutamide in Metastatic Prostate Cancer Patients Failing 1st Line Treatment With LHRH Agonists or Surgical Castration. [NCT01658527]	Phase 2	0 participants (Actual)	Interventional	2014-01-31	Withdrawn(stopped due to Pharmaceutical company has terminated orteronel (TAK-700) development for Prostate Cancer)
A Phase I Pilot Study of Samarium-153 Combined With Neoadjuvant Hormonal Therapy and Radiation Therapy in Men With Locally Advanced Prostate Cancer [NCT00328614]	Phase 1	32 participants (Actual)	Interventional	2003-03-31	Completed
Feasibility of Cytoreductive Prostatectomy in Men Newly Diagnosed With Metastatic Prostate Cancer [NCT02458716]	Phase 1	26 participants (Actual)	Interventional	2015-03-06	Completed
Phase I/II Study of Sorafenib Concurrent With Androgen Deprivation and Radiotherapy in the Treatment of Intermediate- and High-Risk Localized Prostate Cancer [NCT00924807]	Phase 1/Phase 2	4 participants (Actual)	Interventional	2008-09-30	Terminated(stopped due to Sponsor closed the trial)
A Phase II Trial of RAD001 and Bicalutamide for Androgen Independent Prostate Cancer [NCT00630344]	Phase 2	36 participants (Actual)	Interventional	2008-02-29	Completed
Randomized Phase II Screening Trial of Enzalutamide/MDV-3100 and LHRH Analogue vs Combined Androgen Deprivation (LHRH Analogue + Bicalutamide) in Metastatic Hormone Sensitive Prostate Cancer [NCT02058706]	Phase 2	71 participants (Actual)	Interventional	2014-05-31	Completed
Bicalutamide for the Treatment of Androgen Receptor Positive (AR(+)), Estrogen Receptor Negative, Progesterone Receptor Negative (ER(-)/PR(-)) Metastatic Breast Cancer Patients: A Phase II Feasibility Study [NCT00468715]	Phase 2	28 participants (Actual)	Interventional	2007-03-23	Completed
Androgen Deprivation Therapy With or Without Radium-223 Dichloride in Patients With Newly Diagnosed Metastatic Prostate Cancer With Bone Metastases: Hoosier Cancer Research Network GU13-170 [NCT02582749]	Phase 2	16 participants (Actual)	Interventional	2016-04-30	Terminated(stopped due to Funding withdrawn)
STRIVE: A MULTICENTER PHASE 2, RANDOMIZED, DOUBLE-BLIND, EFFICACY AND SAFETY STUDY OF ENZALUTAMIDE VS. BICALUTAMIDE IN MEN WITH PROSTATE CANCER WHO HAVE FAILED PRIMARY ANDROGEN DEPRIVATION THERAPY [NCT01664923]	Phase 2	396 participants (Actual)	Interventional	2012-08-31	Completed
Androgen Receptor Modulation Phase II, Randomized Study of MK-2206 - Bicalutamide Combination in Patients With Rising PSA at High-Risk of Progression After Primary Therapy [NCT01251861]	Phase 2	108 participants (Actual)	Interventional	2010-12-23	Active, not recruiting
A Phase II Study of Definitive Therapy for Newly Diagnosed Men With Oligometastatic Prostate Cancer [NCT02716974]	Phase 2	26 participants (Actual)	Interventional	2016-06-30	Completed
Phase III Randomized Study Of Adjuvant Hormonal Therapy With And Without Docetaxel And Estramustine In Patients With Advanced Prostate Cancer Or With A High Risk Of Relapse [NCT00055731]	Phase 3	413 participants (Actual)	Interventional	2002-11-14	Completed
Pilot Phase II Trial of Bevacizumab in Combination With Hormonal and Radiotherapy in Patients With High-Risk Prostate Cancer [NCT00349557]	Phase 2	18 participants (Anticipated)	Interventional	2006-04-30	Completed
Long Term Adjuvant Hormonal Treatment With LHRH Analogue Versus No Further Treatment in Locally Advanced Prostatic Carcinoma Treated by External Irradiation and a Six Months Combined Androgen Blockade - A Phase III Study [NCT00003026]	Phase 3	966 participants (Anticipated)	Interventional	1997-04-30	Completed
Phase II Study of Antineoplastons A10 and AS2-1 Capsules With Total Androgen Blockade in Patients With Stage III or IV Adenocarcinoma of the Prostate [NCT00003517]	Phase 2	0 participants (Actual)	Interventional		Withdrawn
An Open-Label, Multicenter, Phase III Study to Assess the Impact of Transient Androgenic Deprivation With Enantone LP 11.25 Mg (Leuprorelin) on the Histological Progression of Indolent Prostate Cancer [NCT02085252]	Phase 3	116 participants (Actual)	Interventional	2013-06-03	Completed
A Randomized Phase II Study of Androgen Deprivation Therapy With or Without Palbociclib in RB-Positive Metastatic Hormone-Sensitive Prostate Cancer [NCT02059213]	Phase 2	72 participants (Actual)	Interventional	2014-06-30	Completed
[NCT00421694]	Phase 2/Phase 3	119 participants	Interventional		Completed
The RolE oF Androgen Excess in MUscle Energy MetaboLism in Women With PolyCystic Ovary Syndrome (REFUEL PCOS) Study 2 [NCT05647356]		16 participants (Anticipated)	Interventional	2023-01-01	Not yet recruiting
A Phase II Study of Definitive Therapy for Newly Diagnosed Men With Oligometastatic Prostate Cancer After Prostatectomy [NCT03043807]	Phase 2	26 participants (Actual)	Interventional	2017-02-22	Completed
Randomized Phase II Study of Salvage XRT + ADT +/- Abiraterone Acetate and Apalutamide (ARN-509) for Rising PSA After Radical Prostatectomy With Adverse Features.(FORMULA-509 Trial) [NCT03141671]	Phase 2	345 participants (Actual)	Interventional	2017-11-24	Active, not recruiting
Neoadjuvant Chemohormonal Therapy Followed by Salvage Surgery for High Risk PSA Failure With Biopsy Proven Local Recurrence After Initial Definitive Radiotherapy [NCT01531205]	Phase 2	2 participants (Actual)	Interventional	2012-05-31	Terminated(stopped due to low accrual)
Maximal Suppression of the Androgen Axis in Clinically Localized Prostate Cancer [NCT00298155]	Phase 2	35 participants (Actual)	Interventional	2006-07-31	Completed
Phase I Dose Escalation Trial of CP-675,206 (Tremelimumab, Anti-CTLA-4 Monoclonal Antibody) in Combination With Short Term Androgen Deprivation in Patients With Stage D0 Prostate Cancer [NCT00702923]	Phase 1	12 participants (Actual)	Interventional	2008-07-31	Terminated(stopped due to Enrollment was halted prematurely due to slow accrual.)
A Prospective, Single Center, Phase II Study of Bicalutamide as A Treatment in Androgen Receptor (AR)-Positive Metastatic Triple-Negative Breast Cancer (mTNBC) Patients [NCT02348281]	Phase 2	1 participants (Actual)	Interventional	2015-01-31	Terminated(stopped due to it's too slow to enroll suitable patients into this study)
Phase III Randomized Trial Comparing Total Androgen Blockade Versus Total Androgen Blockade Plus Pelvic Irradiation in Clinical Stage T3-4, N0, M0 Adenocarcinoma of the Prostate [NCT00002633]	Phase 3	361 participants (Actual)	Interventional	1995-02-08	Completed
Phase III Randomized Trial of Standard Systemic Therapy (SST) Versus Standard Systemic Therapy Plus Definitive Treatment (Surgery or Radiation) of the Primary Tumor in Metastatic Prostate Cancer [NCT03678025]	Phase 3	1,273 participants (Anticipated)	Interventional	2018-09-24	Recruiting
Exploratory Study of Molecular Profile-Associated Evidence Guided Precision Therapy for Salivary Gland Cancer [NCT05087706]		182 participants (Anticipated)	Observational [Patient Registry]	2021-07-30	Recruiting
A Phase III Protocol of Androgen Suppression (AS) and Radiation Therapy (RT) vs AS and RT Followed by Chemotherapy With Paclitaxel, Estramustine, and Etoposide (TEE) for Localized, High-Risk, Prostate Cancer [NCT00004054]	Phase 3	397 participants (Actual)	Interventional	2000-01-31	Completed
Stereotactic Prostate Radiotherapy With or Without Androgen Deprivation Therapy, a Phase III, Multi-institutional Randomized-controlled Trial. The SPA Trial. [NCT05019846]	Phase 3	310 participants (Anticipated)	Interventional	2021-09-30	Recruiting
Signal TrAnsduction Pathway Activity Analysis in OVarian cancER [NCT03458221]	Phase 2/Phase 3	148 participants (Anticipated)	Interventional	2023-01-31	Recruiting
Randomized Trial of External Beam Radiation With or Without Short-Course Hormonal Therapy in Intermediate Risk Prostate Cancer Patients [NCT00388804]	Phase 3	39 participants (Actual)	Interventional	2005-02-28	Terminated(stopped due to Slow accrual.)
Pilot Neoadjuvant Trial of Chemohormonal Therapy Followed by Prostatectomy in Patients With High Risk or Oligometastatic Prostate Cancer [NCT03358563]	Early Phase 1	30 participants (Actual)	Interventional	2018-01-17	Completed
Randomized, Bioequivalence Study of Bicalutamide 50 mg Tablet and Casodex® 50 mg Tablet Following a 50 mg Dose in Healthy Subjects Under Fed Conditions [NCT01044706]	Phase 1	60 participants (Actual)	Interventional	2005-05-31	Completed
Bicalutamide With or Without Metformin for Biochemical Recurrence in Overweight or Obese Prostate Cancer Patients (BIMET-1) [NCT02614859]	Phase 2	29 participants (Actual)	Interventional	2015-12-01	Completed
A Phase 3 Trial of Androgen Ablation Alone vs. Chemo/Hormonal Therapy as Initial Treatment of Unresectable/Metastatic Adenocarcinoma of the Prostate [NCT00002855]	Phase 3	306 participants (Actual)	Interventional	1996-08-31	Completed
A Phase III Randomized Trial Comparing Intermittent Versus Continuous Androgen Suppression for Patients With Prostate-Specific-Antigen Progression in the Clinical Absence of Distant Metastases Following Radiotherapy for Prostate Cancer [NCT00003653]	Phase 3	1,386 participants (Actual)	Interventional	1999-01-05	Completed
Docetaxel Followed by Radical Prostatectomy in Patients With High Risk Localized Prostate Cancer [NCT01250717]	Phase 2	28 participants (Actual)	Interventional	2001-01-31	Completed
Randomized Phase II Trial of Short-Course Androgen Deprivation Therapy +/- Bevacizumab for PSA Recurrence of Prostate Cancer After Definitive Local Therapy [NCT00776594]	Phase 2	102 participants (Actual)	Interventional	2008-10-31	Completed
Whole-Pelvic Radiotherapy With a Stereotactic Body Radiotherapy Boost and Long-Term Androgen Deprivation for Unfavorable-Intermediate and High Risk Localized Adenocarcinoma of the Prostate. [NCT02064036]	Phase 1	17 participants (Actual)	Interventional	2013-06-06	Completed
Phase II Randomized Open Label Study of Neo-Adjuvant Degarelix vs. LHRH Agonist in Prostate Cancer Patients Prior to Radical Prostatectomy [NCT01674270]	Phase 2	35 participants (Actual)	Interventional	2012-08-31	Completed
A Multi-institutional Phase I and Biomarker Study of Everolimus Added to Combined Hormonal and Radiation Therapy for High Risk Prostate Cancer [NCT01642732]	Phase 1	1 participants (Actual)	Interventional	2012-10-31	Terminated(stopped due to Lack of accrual and funding expires in June, 2014.)
STEEL: A Randomized Phase II Trial of Salvage Radiotherapy With Standard vs Enhanced Androgen Deprivation Therapy (With Enzalutamide) in Patients With Post-Prostatectomy PSA Recurrences With Aggressive Disease Features [NCT03809000]	Phase 2	188 participants (Actual)	Interventional	2019-04-15	Active, not recruiting
Phase II Study of Bicalutamide and Dutasteride for Prostate Cytoreduction Prior to Permanent Implant I-125 Prostate Brachytherapy [NCT00866554]	Phase 2	60 participants (Actual)	Interventional	2009-03-31	Completed
Phase Ib Dose Finding Study of BKM 120 in Combination With LH-RH Agonists and Bicalutamide in Men With Non Castrate Metastatic Prostate Cancer [NCT02487823]	Phase 1	6 participants (Actual)	Interventional	2014-10-31	Terminated(stopped due to Defect of recruitment)
PERSONALIZED MEDICINE GROUP / UCBG UC-0105/1304: SAFIR02_Breast - Evaluation of the Efficacy of High Throughput Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer [NCT02299999]	Phase 2	1,460 participants (Actual)	Interventional	2014-04-07	Active, not recruiting
A Phase II Immunotherapeutic Trial: Combination Androgen Ablative Therapy and CTLA-4 Blockade as a Treatment for Advanced Prostate Cancer [NCT00170157]	Phase 2	112 participants (Actual)	Interventional	2004-06-30	Completed
Phase I Trial of Weekly Cabazitaxel With Concurrent Intensity Modulated Radiation Therapy and Androgen Deprivation Therapy for the Treatment of Locally Advanced High Risk Adenocarcinoma of the Prostate [NCT01420250]	Phase 1	20 participants (Anticipated)	Interventional	2011-09-22	Active, not recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00002651 (6) [back to overview]	Emotional Functioning as Measured by the SF-36 Mental Health Inventory
NCT00002651 (6) [back to overview]	Erectile Dysfunction
NCT00002651 (6) [back to overview]	High Libido
NCT00002651 (6) [back to overview]	Overall Survival
NCT00002651 (6) [back to overview]	Physical Functioning as Measured by the SF-36
NCT00002651 (6) [back to overview]	Vitality
NCT00002874 (9) [back to overview]	Non-Prostate Cancer Death (12-year Rates Reported)
NCT00002874 (9) [back to overview]	Grade 3+ Toxicity
NCT00002874 (9) [back to overview]	Progression-free Survival (12-year Rates Reported)
NCT00002874 (9) [back to overview]	Distant Failure (12-year Rates Reported)
NCT00002874 (9) [back to overview]	Overall Survival (12-year Rates Reported)
NCT00002874 (9) [back to overview]	Prostate Cancer Death (12-year Rates Reported)
NCT00002874 (9) [back to overview]	PSA Complete Response at End of Protocol Treatment
NCT00002874 (9) [back to overview]	Second PSA Recurrence (12-year Rates Reported)
NCT00002874 (9) [back to overview]	Third PSA Recurrence (12-year Rates Reported)
NCT00003645 (2) [back to overview]	"Number of Wives of the Participants Having Better Than or Equal to a Good Quality of Life"
NCT00003645 (2) [back to overview]	Quality of Life for Participants
NCT00004054 (5) [back to overview]	Rate of Biochemical Failure at 5 Years
NCT00004054 (5) [back to overview]	Overall Survival (5-year Rate Reported)
NCT00004054 (5) [back to overview]	Disease-free Survival Rate at 5 Years
NCT00004054 (5) [back to overview]	Rate of Local Progression at 5 Years
NCT00004054 (5) [back to overview]	Rate of Distant Metastasis at Five Years
NCT00004124 (3) [back to overview]	Overall Survival
NCT00004124 (3) [back to overview]	Compare Qualitative and Quantitative Toxicities of These Regimens in These Patients
NCT00004124 (3) [back to overview]	Disease Free Survival
NCT00005044 (7) [back to overview]	Disease-specific Survival (DSS) (10-year Rates Reported)
NCT00005044 (7) [back to overview]	Overall Survival (OS) (10-year Rates Reported)
NCT00005044 (7) [back to overview]	Time to Second Biochemical Failure (SBF) (10-year Rates Reported)
NCT00005044 (7) [back to overview]	Clinical Patterns of Tumor Recurrence: Time to Locoregional Progression (LRP) and Time to Distant Metastasis (DM) (10 Year Rates Reported)
NCT00005044 (7) [back to overview]	Time to First Biochemical Failure (BF) (10-year Rates Reported)
NCT00005044 (7) [back to overview]	Treatment-induced Morbidity (Highest Grade Toxicity Reported Per Patient)
NCT00005044 (7) [back to overview]	Disease-free Survival (DFS) (10-year Rates Reported)
NCT00028769 (3) [back to overview]	Number of Patients With Grade 3 Through Grade 5 Adverse Events That Are Related to Study Drug
NCT00028769 (3) [back to overview]	Progression-free Survival
NCT00028769 (3) [back to overview]	Overall Survival (OS)
NCT00094328 (9) [back to overview]	Change in Average Testicular Volume
NCT00094328 (9) [back to overview]	Change in Predicted Adult Height (PAH)
NCT00094328 (9) [back to overview]	Change in Growth Rate (SD Units)
NCT00094328 (9) [back to overview]	Change in Growth Rate (SD Units)
NCT00094328 (9) [back to overview]	Change in Growth Rate (cm/Year)
NCT00094328 (9) [back to overview]	Change in Growth Rate (cm/Year)
NCT00094328 (9) [back to overview]	Change in Bone Age Maturation Rate (cm/Year)
NCT00094328 (9) [back to overview]	Change in Bone Age to Chronological Age Ratio
NCT00094328 (9) [back to overview]	Number of Patients With Height Between 5th and 95th Percentile
NCT00108732 (4) [back to overview]	Proportion of Patients With PSA Response
NCT00108732 (4) [back to overview]	The Difference Between PSA Slopes Before and After Treatment
NCT00108732 (4) [back to overview]	Difference Between Day 4 PSA Level and Day 15 PSA Level
NCT00108732 (4) [back to overview]	Proportion of Patients Free of PSA Progression at 6 Months (Prior to the Start of Androgen Ablation)
NCT00170157 (2) [back to overview]	Percent of Participants With Undetectable Prostate-specific Antigen (PSA) Response
NCT00170157 (2) [back to overview]	Number of Participants Progression-free at 18 Months
NCT00298155 (2) [back to overview]	To Determine the Effects of Different Modes of Androgen Deprivation on Serum DHT
NCT00298155 (2) [back to overview]	Prostate Tissue DHT
NCT00328614 (1) [back to overview]	Maximum Tolerated Dose of Samarium-153
NCT00388804 (1) [back to overview]	Prostate Specific Antigen (PSA) Failures
NCT00468715 (1) [back to overview]	Number of Participants Evaluated for Toxicity
NCT00470834 (5) [back to overview]	Time to Disease Progression
NCT00470834 (5) [back to overview]	Change From Baseline in Total PSA at Months 6, 12, 18, 21, and 42
NCT00470834 (5) [back to overview]	Number of Participants With Metastatic Disease
NCT00470834 (5) [back to overview]	Number of Participants With PSA Response
NCT00470834 (5) [back to overview]	Time to Treatment Failure
NCT00486642 (7) [back to overview]	PSA Response Rate
NCT00486642 (7) [back to overview]	Progression-free Survival
NCT00486642 (7) [back to overview]	Objective Tumor Response Rate as Assessed by RECIST Criteria
NCT00486642 (7) [back to overview]	Toxicity
NCT00486642 (7) [back to overview]	Median Duration of PSA-Response
NCT00486642 (7) [back to overview]	Time to Disease Progression
NCT00486642 (7) [back to overview]	Stable Disease Rate as Assessed by RECIST Criteria
NCT00514917 (11) [back to overview]	Change From Baseline in Functional Assessment of Cancer Therapy-Prostate (FACT-P) Trial Outcome Index (TOI) Score at EOT
NCT00514917 (11) [back to overview]	Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT00514917 (11) [back to overview]	Change From Baseline in Multidimensional Assessment of Fatigue (MAF) Index Score at EOT
NCT00514917 (11) [back to overview]	Change From Baseline in Functional Assessment of Cancer Therapy-Prostate (FACT-P) Total Score at End of Treatment (EOT)
NCT00514917 (11) [back to overview]	Cancer-Specific Survival: Number of Participants Who Died (Cancer-Specific)
NCT00514917 (11) [back to overview]	Median Progression-Free Survival (PFS) in Intent-to-treat (ITT) Population
NCT00514917 (11) [back to overview]	Median Progression-Free Survival (PFS) in Testosterone Specific Evaluable Population
NCT00514917 (11) [back to overview]	Overall Survival (OS): Number of Participants Who Died (All Cause)
NCT00514917 (11) [back to overview]	Progression-Free Survival (PFS) Rate at Month 36 in ITT Population
NCT00514917 (11) [back to overview]	Progression-Free Survival (PFS) Rate at Month 36 in Testosterone Specific Evaluable Population
NCT00514917 (11) [back to overview]	Change From Baseline in Erectile Function Domain of International Index of Erectile Function (EF-IIEF) Total Score at EOT
NCT00528866 (9) [back to overview]	Overall Survival (3-year Rate)
NCT00528866 (9) [back to overview]	Number of Participants Free From Progression at 3 Years
NCT00528866 (9) [back to overview]	Prostate Cancer Death (3-year Rate)
NCT00528866 (9) [back to overview]	Non-prostate Cancer Death (3-year Rate)
NCT00528866 (9) [back to overview]	"Number of Patients With Acute Adverse Events (Based on CTCAE, v3.0)"
NCT00528866 (9) [back to overview]	"Time to Late Grade 3+ Adverse Events (Based on CTCAE, v3.0)"
NCT00528866 (9) [back to overview]	Distant Metastasis (3-year Rate)
NCT00528866 (9) [back to overview]	Local-regional Progression (3 Year Rate)
NCT00528866 (9) [back to overview]	Time to Biochemical (PSA) Failure (3-year Rate)
NCT00544830 (7) [back to overview]	CR Without ADT in Patients With Metastases Limited to Pelvic Lymph Nodes.
NCT00544830 (7) [back to overview]	Follow-up of the 8 Patients With Metastases Limited to Pelvic Lymph Nodes.
NCT00544830 (7) [back to overview]	Length of Follow-up
NCT00544830 (7) [back to overview]	Patients Who Achieved PSA Nadir of < 0.2 at 36 Weeks.
NCT00544830 (7) [back to overview]	Time to Prostate-specific Antigen (PSA) Relapse
NCT00544830 (7) [back to overview]	Rate of Treatment Failure (no PSA Threshold Below 4 ng/dl, or no PSA Below Baseline Level Before LHRH Treatment).
NCT00544830 (7) [back to overview]	Count of Patients Remaining Off of Therapy
NCT00567580 (9) [back to overview]	Percentage of Participants Who Died Due to Prostate Cancer (Cause-specific Mortality)
NCT00567580 (9) [back to overview]	Percentage of Participants Free From Progression (FFP) at 5 Years
NCT00567580 (9) [back to overview]	Percentage of Participants Free From Hormone-refractory Disease (Castrate-resistant Disease)
NCT00567580 (9) [back to overview]	Percentage of Participants Alive (Overall Mortality)
NCT00567580 (9) [back to overview]	Percentage of Participants With Distant Metastasis
NCT00567580 (9) [back to overview]	Percentage of Participants Experiencing Grade 2+ and 3+ Adverse Events ≤ 90 Days of the Completion of Radiotherapy (RT)
NCT00567580 (9) [back to overview]	Percentage of Participants With Local Failure
NCT00567580 (9) [back to overview]	Percentage of Participants With Secondary Biochemical Failure (Alternative Biochemical Failure)
NCT00567580 (9) [back to overview]	Percentage of Participants Experiencing Late Grade 2+ and 3+ Adverse Events > 90 Days From the Completion of Radiotherapy (RT)
NCT00586898 (1) [back to overview]	Response
NCT00589472 (6) [back to overview]	Levels of DHEA-S in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]	Levels of Testosterone in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]	Levels of PSA in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]	Gleason Score
NCT00589472 (6) [back to overview]	Levels of DHEA in Blood From Radical Prostatectomy Specimens
NCT00589472 (6) [back to overview]	Levels of DHT in Blood From Radical Prostatectomy Specimens
NCT00630344 (6) [back to overview]	Time to Progression (TTP)
NCT00630344 (6) [back to overview]	Overall Response Rate
NCT00630344 (6) [back to overview]	Incidence of Grade 4 Treatment-Related Toxicity
NCT00630344 (6) [back to overview]	Incidence of Grade 1-3 Treatment-Related Rash Toxicity
NCT00630344 (6) [back to overview]	Incidence of Grade 1-3 Treatment-Related Mucositis Toxicity
NCT00630344 (6) [back to overview]	Incidence of Grade 1-3 Treatment-Related Fatigue Toxicity
NCT00658697 (5) [back to overview]	Time to PSA Progression (TTP)
NCT00658697 (5) [back to overview]	Prostate-Specific Antigen (PSA) Progression at 1 Year After Completing Androgen Deprivation Therapy (ADT)
NCT00658697 (5) [back to overview]	Toxicity
NCT00658697 (5) [back to overview]	Testosterone Recovery
NCT00658697 (5) [back to overview]	Proportion of Patients With PSA Responses at One Year After the Completion of ADT
NCT00659438 (6) [back to overview]	PSA Response Rate
NCT00659438 (6) [back to overview]	Prostate Specific Antigen (PSA) Progression Free Rate at 4 Months
NCT00659438 (6) [back to overview]	Progression Rate From the Radionuclide Bone Scanning
NCT00659438 (6) [back to overview]	Progression Free Survival (PFS) at 4 Months (Instead of Time to PSA Progression)
NCT00659438 (6) [back to overview]	Overall Survival (OS)
NCT00659438 (6) [back to overview]	Progression Free Survival (PFS) at 4 Months (Instead of Time to Onset of Cancer-related Symptoms)
NCT00666666 (3) [back to overview]	Percentage of Patients With Overall PSA < 4.0 ng/mL
NCT00666666 (3) [back to overview]	Percentage of Patients With PSA ≥ 0.2 ng/mL But < 4.0 ng/mL
NCT00666666 (3) [back to overview]	Percentage of Patients With Undetectable Prostate-specific Antigen (PSA) (< 0.2 ng/mL) at End of 7 Cycles
NCT00669162 (1) [back to overview]	Percentage of Patients Who Can Safely Tolerate and Complete Adjuvant Hormonal Therapy, Radiation Therapy and Docetaxel After a Radical Prostatectomy
NCT00702923 (3) [back to overview]	The Number of Participants With an Increase in PSA Doubling Time
NCT00702923 (3) [back to overview]	Number of Participants With PSA Recurrence.
NCT00702923 (3) [back to overview]	The Number of Participants Who Developed Cancer Antigen-specific Immune Responses
NCT00776594 (4) [back to overview]	Analysis of Cytokines and Angiogenic Factors in Plasma/Serum
NCT00776594 (4) [back to overview]	Cardiovascular Safety Including Measurement of Blood Pressure During Treatment Period (6 Months).
NCT00776594 (4) [back to overview]	Relapse-free Survival
NCT00776594 (4) [back to overview]	Number of Participants With PSA <0.2 ng/ml at Six Months
NCT00814788 (3) [back to overview]	PSA Response Rate
NCT00814788 (3) [back to overview]	Progression-free Survival
NCT00814788 (3) [back to overview]	Overall Survival
NCT00831233 (10) [back to overview]	Number of Participants With Markedly Abnormal Values in Vital Signs and Body Weight
NCT00831233 (10) [back to overview]	Number of Participants With Testosterone <=0.5 Nanograms/Milliliter at Each Visit
NCT00831233 (10) [back to overview]	Percentage Change From Baseline in Prostate-specific Antigen (PSA) Concentration at Each Visit
NCT00831233 (10) [back to overview]	Number of Participants With Markedly Abnormal Values in Safety Laboratory Variables
NCT00831233 (10) [back to overview]	Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 12
NCT00831233 (10) [back to overview]	Change From Baseline in Total IPSS at Weeks 4 and 8
NCT00831233 (10) [back to overview]	Change From Baseline in Residual Volume (Vresidual) at Each Visit
NCT00831233 (10) [back to overview]	Change From Baseline in Quality of Life (QoL) Related to Urinary Symptoms at Each Visit
NCT00831233 (10) [back to overview]	Change From Baseline in Maximum Urine Flow (Qmax) at Each Visit
NCT00831233 (10) [back to overview]	Change From Baseline in Prostate Size Based on Trans Rectal Ultra Sound (TRUS) at Week 12
NCT00833248 (9) [back to overview]	Change From Baseline in Quality of Life (QoL) Related to Urinary Symptoms at Each Visit
NCT00833248 (9) [back to overview]	Change From Baseline in Serum Oestradiol Levels During the Study
NCT00833248 (9) [back to overview]	Change From Baseline in Serum Prostate-Specific Antigen (PSA) Levels During the Study
NCT00833248 (9) [back to overview]	Number of Participants With Markedly Abnormal Values in Vital Signs and Body Weight
NCT00833248 (9) [back to overview]	Number of Participants With Markedly Abnormal Values in Safety Laboratory Variables
NCT00833248 (9) [back to overview]	Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 4, 8, and 12
NCT00833248 (9) [back to overview]	Change From Baseline in Serum Testosterone Levels During the Study
NCT00833248 (9) [back to overview]	Change From Baseline in Prostate Size Based on Trans Rectal Ultra Sound (TRUS) at Week 12 (Full Analysis Set)
NCT00833248 (9) [back to overview]	Change From Baseline in Prostate Size Based on Trans Rectal Ultra Sound (TRUS) at Week 12 (Per Protocol Analysis Set)
NCT00878436 (2) [back to overview]	Percentage of Patients Free of Progression and Without Symptomatic Deterioration
NCT00878436 (2) [back to overview]	Percentage of Patients Free of Progression and Without Symptomatic Deterioration
NCT00884273 (10) [back to overview]	Change From Baseline in Total International Prostate Symptom Score (IPSS) at Week 4, 8, and 12
NCT00884273 (10) [back to overview]	Number of Participants With Markedly Abnormal Values in Vital Signs and Body Weight
NCT00884273 (10) [back to overview]	Number of Participants With Markedly Abnormal Values in Safety Laboratory Variables
NCT00884273 (10) [back to overview]	Change in Serum Testosterone Levels During the Study
NCT00884273 (10) [back to overview]	Change in Serum Prostate-Specific Antigen (PSA) Levels During the Study
NCT00884273 (10) [back to overview]	Change From Baseline in Prostate Size Based on TRUS at Week 4 and 8
NCT00884273 (10) [back to overview]	Change From Baseline in Quality of Life (QoL) Related to Urinary Symptoms at Each Visit
NCT00884273 (10) [back to overview]	Change From Baseline in Burden of Urinary Symptoms Based on the Benign Prostatic Hyperplasia Impact Index (BPHII)
NCT00884273 (10) [back to overview]	Change From Baseline in Prostate Size Based on Trans Rectal Ultra Sound (TRUS) at Week 12 (Per Protocol Analysis Set)
NCT00884273 (10) [back to overview]	Change From Baseline in Prostate Size Based on Trans Rectal Ultra Sound (TRUS) at Week 12 (Full Analysis Set)
NCT00936390 (16) [back to overview]	Percentage of Participants With Distant Metastasis
NCT00936390 (16) [back to overview]	Change From Baseline in Expanded Prostate Cancer Index Composite (EPIC) Bowel Domain Score
NCT00936390 (16) [back to overview]	Percentage of Participants With Local Recurrence
NCT00936390 (16) [back to overview]	Percentage of Participants With Late Grade 3+ Adverse Events
NCT00936390 (16) [back to overview]	Number of Participants With Acute Adverse Events
NCT00936390 (16) [back to overview]	Percentage of Participants Alive (Overall Survival)
NCT00936390 (16) [back to overview]	Percentage of Participants Dead Due to Cause Other Than Prostate Cancer (Non-Prostate Cancer-specific Mortality)
NCT00936390 (16) [back to overview]	Percentage of Participants Dead Due to Prostate Cancer (Prostate Cancer-specific Mortality)
NCT00936390 (16) [back to overview]	Percentage of Participants Failed (Freedom From Failure)
NCT00936390 (16) [back to overview]	Percentage of Participants With Biochemical Failure
NCT00936390 (16) [back to overview]	Change From Baseline in Expanded Prostate Cancer Index Composite (EPIC) Hormonal Domain Score
NCT00936390 (16) [back to overview]	Change From Baseline in Expanded Prostate Cancer Index Composite (EPIC) Sexual Domain Score
NCT00936390 (16) [back to overview]	Change From Baseline in Expanded Prostate Cancer Index Composite (EPIC) Urinary Domain Score
NCT00936390 (16) [back to overview]	Change From Baseline in Patient Reported Outcome Measurement Information System (PROMIS) Fatigue Domain Score
NCT00936390 (16) [back to overview]	Percentage of Participants Alive (Overall Survival) by Radiation Therapy Modality
NCT00936390 (16) [back to overview]	Percentage of Participants Receiving Salvage Androgen Deprivation Therapy (ADT)
NCT01020305 (1) [back to overview]	Reduction in Serum PSA
NCT01044706 (2) [back to overview]	Cmax (Maximum Observed Concentration of Drug Substance in Plasma)
NCT01044706 (2) [back to overview]	AUC0-144 (Area Under the Concentration-time Curve From Time Zero to 144 Hour Post-dose)
NCT01120236 (8) [back to overview]	Correlation of microRNA Measures With 28-week PSA Response
NCT01120236 (8) [back to overview]	Toxicity
NCT01120236 (8) [back to overview]	Correlation of microRNA Measures With Baseline Circulating Tumor Cell (CTC) Counts
NCT01120236 (8) [back to overview]	Change in Level of Insulin
NCT01120236 (8) [back to overview]	Proportion of Patients Who do Not Achieve a Partial PSA Response
NCT01120236 (8) [back to overview]	Undetectable PSA Rate
NCT01120236 (8) [back to overview]	Change in Level of IGF-I, Free IGF-I and C-peptide
NCT01120236 (8) [back to overview]	Change in Level of IGFBP2, IGFBP3 and Growth Hormone
NCT01200810 (1) [back to overview]	Safety and Tolerability Assessed Using NCI CTCAE Version 4.0
NCT01250717 (1) [back to overview]	Pathologic Complete Response Was Assessed by Rigorous Pathological Examination by One of Two Pathologists
NCT01251861 (11) [back to overview]	Time to PSA Nadir
NCT01251861 (11) [back to overview]	Time to PSA Progression
NCT01251861 (11) [back to overview]	The Association Between Gleason Score and PSA Response
NCT01251861 (11) [back to overview]	The Association Between Prior Hormonal Therapy and PSA Response
NCT01251861 (11) [back to overview]	Proportion of Patients With PSA Response
NCT01251861 (11) [back to overview]	Duration of PSA Response
NCT01251861 (11) [back to overview]	PSA Slope After Starting Bicalutamide Treatment
NCT01251861 (11) [back to overview]	PSA Slope Prior to Randomization
NCT01251861 (11) [back to overview]	Proportion of Patients With PSA Decline > 85% at 44 Weeks
NCT01251861 (11) [back to overview]	The Proportion of Patients With Undetectable PSA Level (< 0.2 ng/mL) at 44 Weeks
NCT01251861 (11) [back to overview]	PSA Slope After Randomization and Before Starting Bicalutamide
NCT01288911 (12) [back to overview]	Best PSA Response
NCT01288911 (12) [back to overview]	Percentage of Participants With an Objective Response
NCT01288911 (12) [back to overview]	PFS Based on Investigator Assessment
NCT01288911 (12) [back to overview]	Progression Free Survival (PFS) Based on Independent Central Review (ICR) Assessment
NCT01288911 (12) [back to overview]	Prostate-specific Antigen (PSA) Response by Week 13
NCT01288911 (12) [back to overview]	Radiographic PFS Based on ICR Assessment
NCT01288911 (12) [back to overview]	Time to ≥ 30% PSA Decline From Baseline
NCT01288911 (12) [back to overview]	Time to ≥ 50% PSA Decline From Baseline
NCT01288911 (12) [back to overview]	Time to ≥ 90% PSA Decline From Baseline
NCT01288911 (12) [back to overview]	Time to PSA ≤ 4 ng/mL
NCT01288911 (12) [back to overview]	Time to PSA Progression
NCT01288911 (12) [back to overview]	Percentage of Participants With Adverse Events
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
NCT01531205 (5) [back to overview]	Incidence of PSA Progression Free Survival (PFS)
NCT01531205 (5) [back to overview]	Surgical Margin Negative Rate (SM Rate)
NCT01531205 (5) [back to overview]	Incidence of Detecting Circulating Tumor Cells (CTC)
NCT01531205 (5) [back to overview]	Incidence of Complete Response (CR)
NCT01531205 (5) [back to overview]	Incidence of Perioperative and Postoperative Morbidity
NCT01546987 (20) [back to overview]	Testosterone Recovery at 12 and 24 Months
NCT01546987 (20) [back to overview]	Change in Patient-reported Quality of Life as Measured by Expanded Prostate Cancer Index Composite (EPIC) Short Form at One Year
NCT01546987 (20) [back to overview]	Percentage of Participants With Distant Metastases
NCT01546987 (20) [back to overview]	Percentage of Participants With General Clinical Treatment Failure
NCT01546987 (20) [back to overview]	Percentage of Participants With Local Progression
NCT01546987 (20) [back to overview]	Percentage of Patients Alive [Overall Survival] (Primary Endpoint of Original Protocol)
NCT01546987 (20) [back to overview]	Hemoglobin A1c
NCT01546987 (20) [back to overview]	Change From Baseline in Body Mass Index (BMI)
NCT01546987 (20) [back to overview]	Percentage of Participants With Death Due to Prostate Cancer
NCT01546987 (20) [back to overview]	Percentage of Participants With Biochemical Failure (Primary Endpoint of Revised Protocol)
NCT01546987 (20) [back to overview]	Change in Patient-Reported Outcome Measurement Information System (PROMIS) Fatigue Short Form at One Year
NCT01546987 (20) [back to overview]	Percentage of Participants With Grade 3 or Higher Adverse Events
NCT01546987 (20) [back to overview]	Serum Testosterone
NCT01546987 (20) [back to overview]	Serum High-density Lipoprotein (LDL)
NCT01546987 (20) [back to overview]	Serum High-density Lipoprotein (HDL)
NCT01546987 (20) [back to overview]	Number of Patients With Clinical Survivorship Events
NCT01546987 (20) [back to overview]	Number of Participants by Highest Grade Adverse Event
NCT01546987 (20) [back to overview]	Median Testosterone Recovery Time
NCT01546987 (20) [back to overview]	Fasting Total Cholesterol
NCT01546987 (20) [back to overview]	Fasting Plasma Glucose
NCT01664923 (7) [back to overview]	Best Overall Soft Tissue Response
NCT01664923 (7) [back to overview]	Quality of Life: Time to Degradation of Functional Assessment of Cancer Therapy - Prostate (FACT-P)
NCT01664923 (7) [back to overview]	Progression Free Survival (PFS)
NCT01664923 (7) [back to overview]	Percentage of Participants With Treatment Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT01664923 (7) [back to overview]	Percentage of Participants With a PSA Response ≥ 50%
NCT01664923 (7) [back to overview]	Time to PSA Progression
NCT01664923 (7) [back to overview]	Duration of Radiographic PFS
NCT01809691 (4) [back to overview]	Progression Free Survival
NCT01809691 (4) [back to overview]	Overall Survival
NCT01809691 (4) [back to overview]	PSA Response Rates
NCT01809691 (4) [back to overview]	Number of Participants With Gr 3 Through 5 Adverse Events That Are Related to Study Drugs
NCT02058706 (10) [back to overview]	Number of Participants With PSA Remission Assessed Using the Prostate Cancer Clinical Trials Working Group (PCWG2) Criteria
NCT02058706 (10) [back to overview]	Overall Survival at 2 Years
NCT02058706 (10) [back to overview]	Percentage of Patients Progression-free at 6 Months
NCT02058706 (10) [back to overview]	Percentage of Patients With Bone Metastases Progression Free at Six Months
NCT02058706 (10) [back to overview]	The Percentage of Patients Responding
NCT02058706 (10) [back to overview]	Time to Treatment Failure
NCT02058706 (10) [back to overview]	Percentage of Patients Progression Free at One Year
NCT02058706 (10) [back to overview]	Achievement of PSA Response Assessed Using PCWG2 Criteria
NCT02058706 (10) [back to overview]	The Number of Participants With a CTC Response
NCT02058706 (10) [back to overview]	Achievement of Measurable Disease Response
NCT02059213 (8) [back to overview]	Proportion of Patients Who Achieve Undetectable PSA (<0.2ng/mL)
NCT02059213 (8) [back to overview]	Biochemical Progression-free Survival Rate
NCT02059213 (8) [back to overview]	Number of Participants With Grade >=3 Adverse Events That Are Possibly, Probably or Definitely Related to Study Treatment
NCT02059213 (8) [back to overview]	Clinical Progression-free Survival Rate
NCT02059213 (8) [back to overview]	Frequency of Dose Modification
NCT02059213 (8) [back to overview]	Frequency of Treatment Delay
NCT02059213 (8) [back to overview]	Duration of Therapy
NCT02059213 (8) [back to overview]	Number of Patients Who Achieve a PSA ≤ 4ng/mL After Seven Months of Protocol Treatment in Each Arm
NCT02085252 (8) [back to overview]	Prostatic Volume as a Measure of Tumor Radiologic Progression Using Dynamic Magnetic Resonance Imaging (MRI)
NCT02085252 (8) [back to overview]	Highest Diameter of the Lesion as a Measure of Tumor Radiologic Progression Using Dynamic MRI
NCT02085252 (8) [back to overview]	Change From Baseline in the International Prostate Symptom Score (I-PSS) Total Symptom (S) Score
NCT02085252 (8) [back to overview]	Change From Baseline in the International Index of Erectile Function (IIEF-5) Questionnaire Score
NCT02085252 (8) [back to overview]	Change From Baseline in Prostate-specific Antigen (PSA) Levels
NCT02085252 (8) [back to overview]	Change From Baseline in Hospital Anxiety and Depression Scale (HADS) Score
NCT02085252 (8) [back to overview]	Number of Participants With Negative Biopsies at Month 12
NCT02085252 (8) [back to overview]	Number of Participants With Gleason Score ≥ 7
NCT02614859 (5) [back to overview]	Biochemical Response Rate Based on PSA
NCT02614859 (5) [back to overview]	BMI Decline After 32 Weeks
NCT02614859 (5) [back to overview]	PSA Decline
NCT02614859 (5) [back to overview]	PSA Decline ≥ 85% at 32 Weeks
NCT02614859 (5) [back to overview]	Median PSA Decline
NCT02716974 (3) [back to overview]	Safety of the Multimodality Therapy as Assessed by Number of Participants With Neutropenia and Surgical or Radiation Toxicities
NCT02716974 (3) [back to overview]	Efficacy as Assessed by 2-year PSA Progression-free Survival Rate
NCT02716974 (3) [back to overview]	Time to Prostate-specific Antigen Recurrence
NCT03043807 (1) [back to overview]	Time to Prostate-specific Antigen Recurrence
NCT04652765 (5) [back to overview]	Number of Participants Requiring Hospitalization
NCT04652765 (5) [back to overview]	Number of Participants Experiencing Symptoms
NCT04652765 (5) [back to overview]	Number of Drug-related Serious Adverse Events
NCT04652765 (5) [back to overview]	Number of Drug-related Adverse Events
NCT04652765 (5) [back to overview]	All-cause Mortality

Emotional Functioning as Measured by the SF-36 Mental Health Inventory

This outcome was scored on a scale of 0 to 100, with higher scores indicating better functioning. Change from Baseline in SF-36 Score at 3 Months (NCT00002651)
Timeframe: 3 months

Intervention	units on a scale (Mean)
Continuous Hormonal Therapy	-0.95
Intermittent Hormonal Therapy	1.92

Intervention	units on a scale (Mean)
Continuous Hormonal Therapy	-1.74
Intermittent Hormonal Therapy	0.09

Intervention	units on a scale (Mean)
Continuous Hormonal Therapy	-1.42
Intermittent Hormonal Therapy	-0.11

Intervention	participants (Number)
	Acute radiotherapy toxicity	Hormone therapy and late radiotherapy toxicity
Bicalutamide	8	100
Placebo	17	73

Intervention	score on a scale (Mean)
	Mental	Physical	Sexual Function
Arm I - Leuprolide + Flutamide	55	49	5
Arm II - No Treatment	54	49	28

Intervention	percentage of probability of survival (Number)
Arm I: Bicalutamide + Goserelin	87
Arm II: Mitoxantrone + Prednisone + Bivalutamid + Goserelin	86

Intervention	Participants (Number)
	Abdominal pain/cramping	Abscess	Alkaline phosphatase increase	Allergic reaction	Allergic rhinitis	Alopecia	Anal incontinence	Anemia	Anorexia	Anxiety/agitation	Apnea	Arrhythmia, NOS	Arthralgia	Arthritis	Ataxia (incoordination)	Bilirubin increase	Blurred vision	Bone pain	Bruising	CPK increase	Cardiac ischemia/infarction	Cardiovascular-other	Cataract	Cerebrovascular ischemia	Chest pain,not cardio or pleur	Conduction abnormality/block	Confusion	Conjunctivitis	Constipation/bowel obstruction	Cough	Creatinine increase	Cushingoid appearance	Dehydration	Depression	Diarrhea without colostomy	Dizziness/light headedness	Dry eye	Dry skin	Dysmenorrhea	Dyspepsia/heartburn	Dyspnea	Dysuria	Ear-other	Edema	Endocrine-other	Epistaxis	Erectile impotence	Eryth/rash/eruption/desq, NOS	Esophagitis/dysphagia	Eye-other	Fatigue/malaise/lethargy	Febrile neutropenia	Feminization of male	Fever without neutropenia	Fever, NOS	Flatulence	Flu-like symptoms-other	Flushing	GGT increase	GI Mucositis, NOS	GI-other	GU-other	Gastritis	Gastritis/ulcer, NOS	Glaucoma	Gynecomastia	Headache	Hematologic-other	Hematuria	Hemolysis	Hemoptysis	Hemorrhage-other	Hiccoughs	Hot flashes	Hypercalcemia	Hypercholesterolemia	Hyperglycemia	Hyperkalemia	Hypermagnesemia	Hypernatremia	Hypertension	Hypertriglyceridemia	Hypoalbuminemia	Hypocalcemia	Hypoglycemia	Hypokalemia	Hypomagnesemia	Hyponatremia	Hypotension	Hypothyroidism	Hypoxia	Incontinence	Infection w/o 3-4 neutropenia	Infection with 3-4 neutropenia	Infection, unk ANC	Inner ear-hearing loss	Insomnia	Invol. movement/restlessness	Joint,muscle,bone-other	LVEF decrease/CHF	Leukopenia	Libido loss	Local injection site reaction	Lung-other	Lymphopenia	Male infertility	Melena/ GI bleeding	Memory loss	Metabolic-other	Middle ear-hearing loss/otitis	Mood/consciousness change, NOS	Mouth dryness	Muscle weakness (not neuro)	Myalgia	Myalgia/arthralgia, NOS	Myocarditis	Nail changes	Nausea	Neuro-other	Neuropathic pain	Neutropenia/granulocytopenia	PRBC transfusion	Pain-other	Palpitations	Pelvic pain	Pericar. effusion/pericarditis	Personality/behavioral change	Phlebitis	Pigmentation changes/yellowing	Pleural effusions	Pneumonitis/infiltrates	Proctitis	Proteinuria	Pruritus	RT-GI mucositis, NOS	RT-focal dermatitis, NOS	RT-late bladder morbidity	RT-late intestinal morbidity	RT-pain	Rash/desquamation	Rectal bleeding/hematochezia	Rectal/perirectal pain	Respiratory infect w/o neutrop	Respiratory infection, unk ANC	Rigors/chills	SGOT (AST) increase	SGPT (ALT) increase	Salivary change, NOS	Second primary	Seizures	Sensory neuropathy	Sexual/reproductive-other	Sinus bradycardia	Skin-other	Speech impairment	Stomatitis/pharyngitis	Supraventricular arrhythmia	Surgery-wound infection	Sweating	Syncope	Taste disturbance	Tearing	Thrombocytopenia	Thrombosis/embolism	Tremor	Troponin T (cTnT) increase	Urinary frequency/urgency	Urinary retention	Urinary tr infect w/ neutrop	Urinary tr infect w/o neutrop	Urinary tr infection, unk ANC	Urine color change	Urticaria	Ventricular arrhythmia	Vertigo	Vision,NOS	Voice change/stridor/larynx	Vomiting	Weakness (motor neuropathy)	Weight gain	Weight loss
Arm I: Bicalutamide + Goserelin	19	0	11	1	2	91	2	52	7	52	1	0	43	17	1	5	3	19	1	0	1	0	5	1	11	1	6	0	57	10	7	0	0	80	55	33	1	11	0	7	21	14	0	40	3	0	181	0	2	1	258	0	1	0	1	2	2	5	1	0	12	9	2	0	2	140	37	1	9	0	0	1	0	439	4	5	44	0	0	0	38	2	1	1	0	8	1	3	3	2	0	88	5	0	1	3	79	2	11	0	14	163	11	0	4	2	0	15	0	0	2	10	55	26	1	0	4	26	5	0	11	0	112	1	9	0	12	0	0	0	0	4	3	13	0	3	1	2	1	46	12	7	1	1	7	42	22	0	0	1	37	2	0	11	0	5	0	0	138	0	1	0	3	2	0	0	86	13	0	1	3	3	3	1	1	0	0	10	3	179	12
Arm II: Mitoxantrone + Prednisone + Bivalutamid + Goserelin	41	1	11	5	16	131	2	141	41	62	1	1	64	17	1	20	6	34	14	2	1	5	6	0	19	0	14	4	117	34	17	8	6	85	75	71	5	28	1	44	49	11	2	56	2	2	146	2	13	6	357	2	0	9	6	3	6	4	0	10	20	9	0	1	0	100	82	1	13	1	1	4	4	422	5	2	78	4	1	4	38	0	6	7	1	11	1	2	11	0	4	71	10	2	4	2	92	2	27	8	317	133	17	2	49	3	2	12	1	1	3	13	77	45	12	1	57	205	4	1	239	3	127	6	11	1	11	5	3	1	1	4	1	23	1	1	0	1	0	63	10	5	7	8	24	42	26	1	6	1	57	1	4	11	1	49	2	1	129	3	46	6	35	5	2	1	101	7	1	2	2	44	4	0	1	1	6	51	6	151	29

Intervention	percentage of participants (Number)
	Locoregional progression	Distant metastasis
TAS x 28 Weeks	4	6
TAS x 8 Weeks	6	6

Intervention	percentage of participants (Number)
	Protocol definition	Phoenix definition
TAS x 28 Weeks	59	27
TAS x 8 Weeks	56	27

Intervention	percentage of participants (Number)
	Acute RT and Hormone Toxicity: Grade 1	Acute RT and Hormone Toxicity: Grade 2	Acute RT and Hormone Toxicity: Grade 3	Acute RT and Hormone Toxicity: Grade 4	Acute RT and Hormone Toxicity: Grade 5	Late RT Toxicity: Grade 1	Late RT Toxicity: Grade 2	Late RT Toxicity: Grade 3	Late RT Toxicity: Grade 4	Late RT Toxicity: Grade 5
TAS x 28 Weeks	19.5	49.8	25.7	0.1	0	32.9	22.5	8.0	0.3	0
TAS x 8 Weeks	30.8	41.6	16.1	0	0	34.0	20.5	9.7	0.1	0

Intervention	mL (Mean)
	After 6 months treatment	After 12 months treatment
Open Label Bicalutamide With Anastrozole	1.46	2.69

Intervention	years (Median)
Consolidation Arm I	5.8
Consolidation Arm II	5.1

Intervention	Participants (Count of Participants)
Placebo	259
Bicalutamide	360

Intervention	Participants (Number)
	After 3 months treatment	After 6 months treatment	After 9 months treatment	After 12 months treatment
Open Label Bicalutamide With Anastrozole	3	3	3	3

Intervention	percentage of participants (Number)
Androgen Ablative (AA) Therapy + MDX-010	55
Androgen Ablative (AA) Then AA Therapy + MDX-010	39

Intervention	Days (Mean)
Bicalutamide 50 mg/Placebo	376.9
Bicalutamide 50 mg/Dutasteride 3.5 mg	433.1

Intervention	Nanograms per milliliter (ng/mL) (Median)
	Month 6, n=62, 61	Month 12, n=62, 61	Month 18, n=62, 61	Month 21, n=26, 30	Month 42, n=26, 30
Bicalutamide 50 mg/Dutasteride 3.5 mg	-2.2	-2.1	-1.7	-1.8	0.6
Bicalutamide 50 mg/Placebo	-2.0	-1.7	-1.2	-2.1	-0.1

Intervention	participants (Number)
	Months 1-18, n=65, 62	Months 19-42, n=26, 30	Overall (Months 1-42), n=65, 62
Bicalutamide 50 mg/Dutasteride 3.5 mg	5	1	6
Bicalutamide 50 mg/Placebo	8	1	9

Intervention	participants (Number)
	Months 1-18, n=65, 62	Months 19-42, n=4, 7	Overall (Months 1-42), n=65, 62
Bicalutamide 50 mg/Dutasteride 3.5 mg	38	0	38
Bicalutamide 50 mg/Placebo	37	0	37

Intervention	Days (Mean)
Bicalutamide 50 mg/Placebo	368.4
Bicalutamide 50 mg/Dutasteride 3.5 mg	457.5

Intervention	units on a scale (Mean)
	Baseline (n=206, 206)	Change at EOT (n=187, 187)
Docetaxel+Leuprolide+Bicalutamide	82.1	-5.4
Leuprolide+Bicalutamide	80.4	-3.1

Intervention	participants (Number)
	Any TEAE	Any Serious AE	Any TEAE Resulting in Death	Any TEAE Leading to any Treatment Discontinuation	Any Grade 3-4 TEAE	Docetaxel Related TEAE	Leuprolide Related TEAE	Bicalutamide Related TEAE	Any Treatment Related TEAE	Any Grade 3-4 Serious TEAE	Any TEAE Leading to Interruption of any Treatment
Docetaxel+Leuprolide+Bicalutamide	188	49	0	35	94	183	109	52	184	43	77
Leuprolide+Bicalutamide	163	20	1	1	22	NA	136	74	136	14	1

Intervention	units on a scale (Mean)
	Baseline (n=168, 171)	Change at EOT (n=127, 144)
Docetaxel+Leuprolide+Bicalutamide	16.4	4.0
Leuprolide+Bicalutamide	16.6	2.6

bicalutamide

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Studies (1,266)

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Research Demand Index: 96.47

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Clinical Trials (182)

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Emotional Functioning as Measured by the SF-36 Mental Health Inventory

Erectile Dysfunction

High Libido

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Physical Functioning as Measured by the SF-36

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Non-Prostate Cancer Death (12-year Rates Reported)

Grade 3+ Toxicity

Progression-free Survival (12-year Rates Reported)

Distant Failure (12-year Rates Reported)

Overall Survival (12-year Rates Reported)

Prostate Cancer Death (12-year Rates Reported)

PSA Complete Response at End of Protocol Treatment

Second PSA Recurrence (12-year Rates Reported)

Third PSA Recurrence (12-year Rates Reported)

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Quality of Life for Participants

Rate of Biochemical Failure at 5 Years

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Overall Survival

Compare Qualitative and Quantitative Toxicities of These Regimens in These Patients

Disease Free Survival

Disease-specific Survival (DSS) (10-year Rates Reported)

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Time to Second Biochemical Failure (SBF) (10-year Rates Reported)

Clinical Patterns of Tumor Recurrence: Time to Locoregional Progression (LRP) and Time to Distant Metastasis (DM) (10 Year Rates Reported)

Time to First Biochemical Failure (BF) (10-year Rates Reported)

Treatment-induced Morbidity (Highest Grade Toxicity Reported Per Patient)

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Number of Patients With Grade 3 Through Grade 5 Adverse Events That Are Related to Study Drug

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Change in Average Testicular Volume

Change in Predicted Adult Height (PAH)

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Number of Patients With Height Between 5th and 95th Percentile

Proportion of Patients With PSA Response

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Proportion of Patients Free of PSA Progression at 6 Months (Prior to the Start of Androgen Ablation)

Intervention	units on a scale (Mean)
	Baseline (n=206, 205)	Change at EOT (n=186, 184)
Docetaxel+Leuprolide+Bicalutamide	121.4	-4.9
Leuprolide+Bicalutamide	119.6	-3.4

Intervention	months (Median)
Docetaxel+Leuprolide+Bicalutamide	25.4
Leuprolide+Bicalutamide	23.3

Intervention	percent chance of being progression-free (Number)
Docetaxel+Leuprolide+Bicalutamide	15.5
Leuprolide+Bicalutamide	8.6

Intervention	percent chance of being progression-free (Number)
Docetaxel+Leuprolide+Bicalutamide	15.8
Leuprolide+Bicalutamide	9.1

Intervention	units on a scale (Mean)
	Baseline (n=201, 205)	Change at EOT (n=180, 186)
Docetaxel+Leuprolide+Bicalutamide	6.4	-3.1
Leuprolide+Bicalutamide	6.8	-3.3

Intervention	percentage of participants (Number)
	Grade 2+	Grade 3+
PBRT + STAD	36.3	8.7
PBRT Alone	18.8	4.4
PLNRT + PBRT + STAD	43.6	12.2

Intervention	participants (Number)
	Complete Response (CR)	Partial Response (PR)	Stable Disease (SD)
All Participants	22	4	3

Intervention	participants (Number)
	Grade 3 treatment related AE	Grade 4 treatment related AEs
Docetaxel, Bevacizumab, and ADT	16	5

Intervention	percentage of participants with data (Number)
	Testosterone >=100 ng/mL	Testosterone >=240 ng/mL
Docetaxel, Bevacizumab, and ADT	83	35

Intervention	percentage of participants with data (Number)
	PSA <0.2 ng/mL	PSA <=0.01 ng/mL
Docetaxel, Bevacizumab, and ADT	44	25