Biomarker & Intervention Discovery

Prostate Cancer

This page lists 11 druggable gene targets, 47 approved or trial-tested drug candidates and 15 recent clinical trials for Prostate Cancer, with each agent ranked by the strength of its evidence (clinical, mechanistic or correlative). Candidates include existing drugs that could be repurposed. Sources are linked so you can check every claim.

US DALYs837.7KWHO GHE 2021 · all ages
Global DALYs7.74MWHO GHE 2021 · worldwide
US mortality37.3K deaths/yrWHO GHE 2021
Global mortality393.9K deaths/yrWHO GHE 2021 · worldwide
NIH funding$314MFY2025 · RCDC estimate
Funding levelModerate
Spontaneous remissionLow-grade (Gleason 6/Grade Group 1): active surveillance appropriate in 40-50% — many will never need treatment…
Best-intervention remissionLocalised: surgery (radical prostatectomy) or radiotherapy — 90-95% disease-specific survival at 10 years; mCSPC:…
Gap sizeLarge — active surveillance underused in low-risk disease (overtreatment); ADT monotherapy still used where…
Primary barrierpractice
Full remission profile →

Remission & chronicity

Spontaneous remission
Low-grade (Gleason 6/Grade Group 1): active surveillance appropriate in 40-50% — many will never need treatment; high-grade: lethal without treatment within 5-10 years
Best-intervention remission
Localised: surgery (radical prostatectomy) or radiotherapy — 90-95% disease-specific survival at 10 years; mCSPC: darolutamide + docetaxel + ADT (ARASENS): 32% OS improvement; enzalutamide/abiraterone + ADT as standard 2019-2021; PARP inhibitors for BRCA-mutant: olaparib — 34% OS benefit (PROfound)
Gap size
Large — active surveillance underused in low-risk disease (overtreatment); ADT monotherapy still used where combination therapy is standard
Primary barrier
practice
Active surveillance in low-risk PCa is guideline-endorsed but only 50-60% of eligible patients are managed this way (radical treatment used unnecessarily with significant sexual/urinary side effects); intensified ADT combinations are standard of care for mHSPC but ADT monotherapy still prescribed

Biomarker Targets & Therapeutic Agents

Gene targets queried against DGIdb, Open Targets, ChEMBL, PubMed, and Europe PMC. Agents ranked: Clinical > Mechanistic > Correlative.

AKT1 248AR 994BRCA1 283BRCA2 19CYP17A1 124FOLH1 188KLK3 208PARP1 207PTEN 155SRD5A2 145TMPRSS2 69
Therapeutic Agent Effect Direction Evidence Tier Potency Source
FASUDIL ? unclear Mechanistic
TOPOTECAN HYDROCHLORIDE ? unclear Mechanistic
5-METHOXYCANTHINONE ? unclear Mechanistic
IPATASERTIB ↓ inhibits Mechanistic
MS15 ↓ inhibits Mechanistic
NELFINAVIR ↓ inhibits Mechanistic
XL418 ? unclear Mechanistic
ENZASTAURIN ? unclear Mechanistic
TRICIRIBINE ↓ inhibits Mechanistic
PERIFOSINE ↓ inhibits Mechanistic
M-2698 ↓ inhibits Mechanistic
UPROSERTIB ↓ inhibits Mechanistic
CANTHIN-6-ONE ? unclear Mechanistic
CAPIVASERTIB ↓ inhibits Mechanistic
CI-1040 ? unclear Mechanistic
CHEMBL:CHEMBL480356 ? unclear Mechanistic
ANDROGRAPHOLIDE ? unclear Mechanistic
SR-13668 ↓ inhibits Mechanistic
LAUROGUADINE ? unclear Mechanistic
DABRAFENIB ? unclear Mechanistic
GEFITINIB ? unclear Mechanistic
EVEROLIMUS ↓ inhibits Mechanistic
GIGANTOL ? unclear Mechanistic
GSK690693 ↓ inhibits Mechanistic
VAD-044 ~ modulates Mechanistic
HU7691 ↓ inhibits Mechanistic
LY-2780301 ↓ inhibits Mechanistic
GAMBOGIC AMIDE ? unclear Mechanistic
MIRANSERTIB ? unclear Mechanistic
GEDATOLISIB ? unclear Mechanistic
EUPALININ A ? unclear Mechanistic
NINTEDANIB ESYLATE ? unclear Mechanistic
GSK269962A ? unclear Mechanistic
ERLOTINIB ? unclear Mechanistic
CEP-11981 ? unclear Mechanistic
OMIPALISIB ↓ inhibits Mechanistic
A-674563 ↓ inhibits Mechanistic
ARCHEXIN ? unclear Mechanistic
CANERTINIB DIHYDROCHLORIDE ? unclear Mechanistic
BARDOXOLONE METHYL ? unclear Mechanistic

Showing top 40 of 248 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
AMI-1 ? unclear Mechanistic
DIBEKACIN ? unclear Mechanistic
CARBONYL CYANIDE M-CHLOROPHENYLHYDRAZONE ? unclear Mechanistic
TRIPARANOL ? unclear Mechanistic
DODINE ? unclear Mechanistic
TANNIC ACID ? unclear Mechanistic
DEFLAZACORT ? unclear Mechanistic
CHEMBL:CHEMBL1235854 ? unclear Mechanistic
ERGONOVINE ? unclear Mechanistic
AMPEROZIDE HYDROCHLORIDE ? unclear Mechanistic
ATROPINE METHYLBROMIDE ? unclear Mechanistic
ESTRADIOL VALERATE ? unclear Mechanistic
BERBERINE CHLORIDE ? unclear Mechanistic
NITRALIN ? unclear Mechanistic
DEVAZEPIDE ? unclear Mechanistic
MOCLOBEMIDE ? unclear Mechanistic
GLPG0492 ~ modulates Mechanistic
DEUTENZALUTAMIDE ↓ inhibits Mechanistic
PRUXELUTAMIDE ↓ inhibits Mechanistic
HEPTANE ? unclear Mechanistic
THONZONIUM BROMIDE ? unclear Mechanistic
FENHEXAMID ? unclear Mechanistic
LEMILDIPINE ? unclear Mechanistic
(R)-BICALUTAMIDE ? unclear Mechanistic
MORICIZINE HYDROCHLORIDE ? unclear Mechanistic
METIPRANOLOL ? unclear Mechanistic
FLUROCHLORIDONE ? unclear Mechanistic
PYRIDOSTIGMINE BROMIDE ? unclear Mechanistic
FLUTAMIDE ↓ inhibits Mechanistic 154.0 nM (IC50)
CHEMBL:CHEMBL224318 ? unclear Mechanistic
CHEMBL:CHEMBL423081 ? unclear Mechanistic
PREDNISOLONE ? unclear Mechanistic 2760.0 nM (Ki)
ORBIFLOXACIN ? unclear Mechanistic
PROGESTERONE ? unclear Mechanistic 8.5 nM (Ki)
FLUDIOXONIL ? unclear Mechanistic
CHEMBL:CHEMBL1784521 ? unclear Mechanistic
FLUMETHASONE ? unclear Mechanistic
SERTRALINE HYDROCHLORIDE ? unclear Mechanistic
MELOXICAM ? unclear Mechanistic
CHEMBL:CHEMBL44011 ? unclear Mechanistic

Showing top 40 of 994 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
7-HYDROXY ISOFLAVONE ? unclear Mechanistic
OLAPARIB ? unclear Mechanistic
PLATINUM COMPOUND ? unclear Mechanistic
DAIDZIN ? unclear Mechanistic
CHEMBL:CHEMBL581929 ? unclear Mechanistic
PIDNARULEX ? unclear Mechanistic
CHEMBL:CHEMBL1481721 ? unclear Mechanistic
CHEMBL:CHEMBL484663 ? unclear Mechanistic
CHEMBL:CHEMBL1214407 ? unclear Mechanistic
2-PHENYLQUINOLINE ? unclear Mechanistic
HARMALOL ? unclear Mechanistic
CHEMBL:CHEMBL1574420 ? unclear Mechanistic
DOXORUBICIN HYDROCHLORIDE ? unclear Mechanistic
MITOMYCIN ? unclear Mechanistic
PACLITAXEL PROTEIN-BOUND ? unclear Mechanistic
RESVERATROL ? unclear Mechanistic
CHEMBL:CHEMBL12658 ? unclear Mechanistic
ONONIN ? unclear Mechanistic
CEDIRANIB ? unclear Mechanistic
PIPERINE ? unclear Mechanistic
CHEMBL:CHEMBL446567 ? unclear Mechanistic
CHEMBL:CHEMBL546649 ? unclear Mechanistic
DEPHOSTATIN ? unclear Mechanistic
SEMUSTINE ? unclear Mechanistic
CISPLATIN ? unclear Mechanistic
CHEMBL:CHEMBL1404865 ? unclear Mechanistic
QUARFLOXIN ? unclear Mechanistic
PARP/TANKYRASE INHIBITOR 2X-121 ? unclear Mechanistic
WISTIN ? unclear Mechanistic
CHRYSIN DIMETHYL ETHER ? unclear Mechanistic
GEMCITABINE ? unclear Mechanistic
CHEMBL:CHEMBL600315 ? unclear Mechanistic
AURINTRICARBOXYLIC ACID ? unclear Mechanistic
MITOXANTRONE HYDROCHLORIDE ? unclear Mechanistic
SACITUZUMAB GOVITECAN ? unclear Mechanistic
CHEMBL:CHEMBL588683 ? unclear Mechanistic
CHEMBL:CHEMBL593254 ? unclear Mechanistic
CHEMBL:CHEMBL588525 ? unclear Mechanistic
PURPURIN ? unclear Mechanistic
CHEMBL:CHEMBL316796 ? unclear Mechanistic

Showing top 40 of 283 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
CARBOPLATIN ? unclear Mechanistic
OLAPARIB ? unclear Mechanistic
TALAZOPARIB ? unclear Mechanistic
NIRAPARIB ? unclear Mechanistic
RUCAPARIB ? unclear Mechanistic
QUARFLOXIN ? unclear Mechanistic
CISPLATIN ? unclear Mechanistic
VELIPARIB ? unclear Mechanistic
BOSUTINIB ? unclear Mechanistic
PLATINUM COMPOUND ? unclear Mechanistic
TEMOZOLOMIDE ? unclear Mechanistic
ENZALUTAMIDE ? unclear Mechanistic
DASATINIB ANHYDROUS ? unclear Mechanistic
GEMCITABINE ? unclear Mechanistic
PIDNARULEX ? unclear Mechanistic
SACITUZUMAB GOVITECAN ? unclear Mechanistic
CEDIRANIB ? unclear Mechanistic
INIPARIB ? unclear Mechanistic
PARP/TANKYRASE INHIBITOR 2X-121 ? unclear Mechanistic
Therapeutic Agent Effect Direction Evidence Tier Potency Source
PACLITAXEL PROTEIN-BOUND ? unclear Mechanistic
ORTERONEL ↓ inhibits Mechanistic
ENZALUTAMIDE ? unclear Mechanistic
GALETERONE ↓ inhibits Mechanistic
ABIRATERONE-C6 OXIME ↓ inhibits Mechanistic
ABIRATERONE ACETATE ↓ inhibits Mechanistic 17.0 nM (IC50)
SEVITERONEL ? unclear Mechanistic
LEVOKETOCONAZOLE ↓ inhibits Mechanistic
LAPITERONEL ? unclear Mechanistic
YXG-158 ↓ inhibits Mechanistic
ABIRATERONE ? unclear Mechanistic 4.0 nM (IC50)
CHEMBL138580 ↓ inhibits Mechanistic 1800.0 nM (IC50)
CHEMBL310690 ↓ inhibits Mechanistic 160.0 nM (IC50)
CHEMBL341591 ↓ inhibits Mechanistic 400.0 nM (IC50)
CHEMBL2111948 ↓ inhibits Mechanistic 1520.0 nM (IC50)
CHEMBL3137965 ↓ inhibits Mechanistic 74.0 nM (IC50)
CHEMBL2112781 ↓ inhibits Mechanistic 1250.0 nM (IC50)
CHEMBL357811 ↓ inhibits Mechanistic 27.0 nM (IC50)
CHEMBL2112888 ↓ inhibits Mechanistic 260.0 nM (IC50)
CHEMBL2111947 ↓ inhibits Mechanistic 540.0 nM (IC50)
CHEMBL3137967 ↓ inhibits Mechanistic 5.0 nM (IC50)
CHEMBL2112782 ↓ inhibits Mechanistic 970.0 nM (IC50)
CHEMBL432751 ↓ inhibits Mechanistic 3.0 nM (IC50)
CHEMBL2112772 ↓ inhibits Mechanistic 1520.0 nM (IC50)
CHEMBL310315 ↓ inhibits Mechanistic 13.0 nM (IC50)
CHEMBL82926 ↓ inhibits Mechanistic 47.0 nM (IC50)
CHEMBL2112775 ↓ inhibits Mechanistic 2500.0 nM (IC50)
KETOCONAZOLE ↓ inhibits Mechanistic 740.0 nM (IC50)
CHEMBL3085257 ↓ inhibits Mechanistic 1800.0 nM (IC50)
CHEMBL2111951 ↓ inhibits Mechanistic 290.0 nM (IC50)
CHEMBL419743 ↓ inhibits Mechanistic 400.0 nM (IC50)
CHEMBL2112522 ↓ inhibits Mechanistic 21.0 nM (IC50)
CHEMBL2112517 ↓ inhibits Mechanistic 42.0 nM (IC50)
CHEMBL2112524 ↓ inhibits Mechanistic 100.0 nM (IC50)
CHEMBL2112526 ↓ inhibits Mechanistic 24.0 nM (IC50)
CHEMBL2112533 ↓ inhibits Mechanistic 400.0 nM (IC50)
CHEMBL2112519 ↓ inhibits Mechanistic 430.0 nM (IC50)
CHEMBL325307 ↓ inhibits Mechanistic 50.0 nM (IC50)
CHEMBL114864 ↓ inhibits Mechanistic 150.0 nM (IC50)
CHEMBL115944 ↓ inhibits Mechanistic 150.0 nM (IC50)

Showing top 40 of 124 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
MERCAPTOPURINE ? unclear Mechanistic
CAPROMAB ? unclear Mechanistic
DIHYDROTESTOSTERONE ? unclear Mechanistic
AUTOLOGOUS PSMA-4SCAR-EXPRESSING T-CELLS 4SCAR-PSMA ? unclear Mechanistic
MLN-2704 ~ modulates Mechanistic
METHOTREXATE ? unclear Mechanistic
APVO-414 ? unclear Mechanistic
J591 177LU ~ modulates Mechanistic
CYT-500 177LU ~ modulates Mechanistic
TECHNETIUM TC 99M TROFOLASTAT ? unclear Mechanistic
MDX-070 ? unclear Mechanistic
HUJ591 177LU ~ modulates Mechanistic
SURAMIN ? unclear Mechanistic
THERAPEUTIC ANDROGEN ? unclear Mechanistic
MIPSAGARGIN ? unclear Mechanistic
MLN-591RL ? unclear Mechanistic
COMPOUND 8D [PMID: 15027864] ↓ inhibits Mechanistic
VIPIVOTIDE TETRAXETAN ↓ inhibits Mechanistic
CAPROMAB PENDETIDE ? unclear Mechanistic
DOCETAXEL ANHYDROUS ↓ inhibits Mechanistic
LUTETIUM LU 177 VIPIVOTIDE TETRAXETAN ? unclear Mechanistic
LUTETIUM LU-177 VIPIVOTIDE TETRAXETAN ~ modulates Mechanistic
YTTRIUM Y 90 CAPROMAB PENDETIDE ~ modulates Mechanistic
HUJ591 111IN ~ modulates Mechanistic
CLAVULANIC ACID ? unclear Mechanistic
THERAPEUTIC CORTICOSTEROID ? unclear Mechanistic
IMMUNOTOXIN ? unclear Mechanistic
CHEMBL51979 ↓ inhibits Mechanistic 43000.0 nM (IC50)
CHEMBL47009 ↓ inhibits Mechanistic 0.3 nM (IC50)
CHEMBL65043 ↓ inhibits Mechanistic 220.0 nM (IC50)
CHEMBL433298 ↓ inhibits Mechanistic 940.0 nM (IC50)
CHEMBL432726 ↓ inhibits Mechanistic 4000.0 nM (IC50)
CHEMBL63454 ↓ inhibits Mechanistic 1200.0 nM (IC50)
CHEMBL303352 ↓ inhibits Mechanistic 90.0 nM (IC50)
CHEMBL64901 ↓ inhibits Mechanistic 82.0 nM (IC50)
CHEMBL65860 ↓ inhibits Mechanistic 20000.0 nM (IC50)
CHEMBL304885 ↓ inhibits Mechanistic 2600.0 nM (IC50)
CHEMBL60317 ↓ inhibits Mechanistic 1100.0 nM (IC50)
CHEMBL61882 ↓ inhibits Mechanistic 6500.0 nM (IC50)
CHEMBL294565 ↓ inhibits Mechanistic 1400.0 nM (IC50)

Showing top 40 of 188 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
MILVEXIAN ↓ inhibits Mechanistic
HUMAN C1-ESTERASE INHIBITOR ↓ inhibits Mechanistic
AVORALSTAT ↓ inhibits Mechanistic
APROTININ ↓ inhibits Mechanistic
SEBETRALSTAT ↓ inhibits Mechanistic
BEROTRALSTAT ↓ inhibits Mechanistic
COMPOUND 11 [PMID: 16413183] ↓ inhibits Mechanistic
BEROTRALSTAT HYDROCHLORIDE ↓ inhibits Mechanistic
ANTITHROMBIN III ? unclear Mechanistic
LANADELUMAB ↓ inhibits Mechanistic
ECALLANTIDE ↓ inhibits Mechanistic
CHEMBL8108 ↓ inhibits Mechanistic 12000.0 nM (IC50)
CHEMBL268367 ↓ inhibits Mechanistic 7200.0 nM (IC50)
CHEMBL559015 ↓ inhibits Mechanistic 61.0 nM (Ki)
CHEMBL289395 ↓ inhibits Mechanistic 5000.0 nM (Ki)
CHEMBL125153 ↓ inhibits Mechanistic 1300.0 nM (Ki)
CHEMBL127909 ↓ inhibits Mechanistic 110.0 nM (Ki)
CHEMBL126707 ↓ inhibits Mechanistic 600.0 nM (Ki)
CHEMBL339902 ↓ inhibits Mechanistic 800.0 nM (Ki)
CHEMBL96433 ↓ inhibits Mechanistic 1.9 nM (Ki)
CHEMBL127407 ↓ inhibits Mechanistic 1300.0 nM (Ki)
CHEMBL127278 ↓ inhibits Mechanistic 4800.0 nM (Ki)
CHEMBL107955 ↓ inhibits Mechanistic 7200.0 nM (Ki)
SEPIMOSTAT MESYLATE ↓ inhibits Mechanistic 570.0 nM (Ki)
CHEMBL107627 ↓ inhibits Mechanistic 7300.0 nM (Ki)
CHEMBL107911 ↓ inhibits Mechanistic 35000.0 nM (Ki)
CHEMBL107282 ↓ inhibits Mechanistic 27000.0 nM (Ki)
CHEMBL319035 ↓ inhibits Mechanistic 22000.0 nM (Ki)
CHEMBL322901 ↓ inhibits Mechanistic 15000.0 nM (Ki)
CHEMBL107743 ↓ inhibits Mechanistic 97000.0 nM (Ki)
CHEMBL322165 ↓ inhibits Mechanistic 3300.0 nM (Ki)
CHEMBL107392 ↓ inhibits Mechanistic 58000.0 nM (Ki)
CHEMBL176243 ↓ inhibits Mechanistic 500.0 nM (IC50)
CHEMBL175130 ↓ inhibits Mechanistic 300.0 nM (IC50)
CHEMBL369086 ↓ inhibits Mechanistic 500.0 nM (IC50)
CHEMBL176671 ↓ inhibits Mechanistic 640.0 nM (IC50)
CHEMBL174558 ↓ inhibits Mechanistic 380.0 nM (IC50)
CHEMBL174499 ↓ inhibits Mechanistic 130.0 nM (IC50)
CHEMBL369681 ↓ inhibits Mechanistic 790.0 nM (IC50)
CHEMBL367953 ↓ inhibits Mechanistic 560.0 nM (IC50)

Showing top 40 of 208 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
NIRAPARIB ↓ inhibits Mechanistic
VELIPARIB ↓ inhibits Mechanistic
4-[3-(1,4-DIAZEPAN-1-YLCARBONYL)-4-FLUOROBENZYL]PHTHALAZIN-1(2H)-ONE ↓ inhibits Mechanistic
PAMIPARIB ↓ inhibits Mechanistic
OLAPARIB ↓ inhibits Mechanistic
COMPOUND 5 [TOMASSI ET AL., 2020] ↓ inhibits Mechanistic
COMPOUND 9 [LIN ET AL., 2023] ↓ inhibits Mechanistic
INIPARIB ↓ inhibits Mechanistic
AZ1366 ↓ inhibits Mechanistic
DUAL VEGFR/PARP INHIBITOR 14B ↓ inhibits Mechanistic
NIACIN ? unclear Mechanistic
2X-121 ↓ inhibits Mechanistic
AMELPARIB DIHYDROCHLORIDE DIHYDRATE ↓ inhibits Mechanistic
CEP-9722 ? unclear Mechanistic
ORAL AZACITIDINE ? unclear Mechanistic
RUCAPARIB PHOSPHATE ↓ inhibits Mechanistic
AG14361 ↓ inhibits Mechanistic
ME0328 ↓ inhibits Mechanistic
SARUPARIB ↓ inhibits Mechanistic
SENAPARIB ↓ inhibits Mechanistic
NIRAPARIB TOSYLATE ? unclear Mechanistic
TALAZOPARIB ↓ inhibits Mechanistic
PJ34 ↓ inhibits Mechanistic
TALAZOPARIB TOSYLATE ↓ inhibits Mechanistic
PARP1 INHIBITOR (S)-G9 ↓ inhibits Mechanistic
NICARAVEN ? unclear Mechanistic
PARP-1/2 INHIBITOR ABT-767 ? unclear Mechanistic
INO-1001 ? unclear Mechanistic
BGP-15 ? unclear Mechanistic
RUCAPARIB ↓ inhibits Mechanistic
TRABECTEDIN ? unclear Mechanistic
VENADAPARIB ↓ inhibits Mechanistic
FLUZOPARIB ↓ inhibits Mechanistic
MC2050 ↓ inhibits Mechanistic
PARP INHIBITOR E7016 ? unclear Mechanistic
LERZEPARIB ↓ inhibits Mechanistic
CICLOPIROX ↓ inhibits Mechanistic
E-7016 ↓ inhibits Mechanistic
RUCAPARIB CAMSYLATE ↓ inhibits Mechanistic
PALACAPARIB ↓ inhibits Mechanistic

Showing top 40 of 207 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
VS-5584 ? unclear Mechanistic
PLX-4720 ? unclear Mechanistic
OSIMERTINIB ? unclear Mechanistic
ERDAFITINIB ? unclear Mechanistic
EVEROLIMUS ? unclear Mechanistic
PEMBROLIZUMAB ? unclear Mechanistic
IPATASERTIB ? unclear Mechanistic
TRASTUZUMAB ? unclear Mechanistic
VISTUSERTIB ? unclear Mechanistic
CHEMBL:CHEMBL4439276 ? unclear Mechanistic
ZSTK474 ? unclear Mechanistic
DORDAVIPRONE ? unclear Mechanistic
PACLITAXEL PROTEIN-BOUND ? unclear Mechanistic
GEDATOLISIB ? unclear Mechanistic
ANTINEOPLASTIC AGENT ? unclear Mechanistic
ERLOTINIB ? unclear Mechanistic
TEMSIROLIMUS ? unclear Mechanistic
NAVITOCLAX ? unclear Mechanistic
NIVOLUMAB ? unclear Mechanistic
OXALIPLATIN ? unclear Mechanistic
EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE INHIBITOR ? unclear Mechanistic
IPILIMUMAB ? unclear Mechanistic
ALPELISIB ? unclear Mechanistic
ABT-737 ? unclear Mechanistic
PILARALISIB ? unclear Mechanistic
FLUOROURACIL ? unclear Mechanistic
CX-6258 ? unclear Mechanistic
PICTILISIB ? unclear Mechanistic
SELUMETINIB ? unclear Mechanistic
TAS0612 ? unclear Mechanistic
TASELISIB ? unclear Mechanistic
LETROZOLE ? unclear Mechanistic
VOXTALISIB ? unclear Mechanistic
FULVESTRANT ? unclear Mechanistic
ATEZOLIZUMAB ? unclear Mechanistic
IZORLISIB ? unclear Mechanistic
CETUXIMAB ? unclear Mechanistic
PI3K/BET INHIBITOR LY294002 ? unclear Mechanistic
SIROLIMUS ? unclear Mechanistic
BEVACIZUMAB ? unclear Mechanistic

Showing top 40 of 155 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
FINASTERIDE ↓ inhibits Mechanistic 1.2 nM (IC50)
DUTASTERIDE ↓ inhibits Mechanistic
ABIRATERONE ACETATE ↓ inhibits Mechanistic
CHEMBL25081 ↓ inhibits Mechanistic 260.0 nM (Ki)
CHEMBL99615 ↓ inhibits Mechanistic 122.0 nM (IC50)
CHEMBL97266 ↓ inhibits Mechanistic 20000.0 nM (Ki)
CHEMBL138580 ↓ inhibits Mechanistic 9000.0 nM (IC50)
CHEMBL2111948 ↓ inhibits Mechanistic 16000.0 nM (IC50)
CHEMBL2111947 ↓ inhibits Mechanistic 10000.0 nM (IC50)
EPRISTERIDE ↓ inhibits Mechanistic 3.0 nM (IC50)
CHEMBL24464 ↓ inhibits Mechanistic 437.0 nM (IC50)
CHEMBL2311155 ↓ inhibits Mechanistic 83.9 nM (IC50)
CHEMBL277403 ↓ inhibits Mechanistic 192.0 nM (IC50)
CHEMBL36573 ↓ inhibits Mechanistic 172.0 nM (IC50)
CHEMBL283564 ↓ inhibits Mechanistic 387.0 nM (IC50)
TUROSTERIDE ↓ inhibits Mechanistic 55.0 nM (IC50)
CHEMBL24191 ↓ inhibits Mechanistic 25.2 nM (IC50)
CHEMBL24958 ↓ inhibits Mechanistic 1390.0 nM (IC50)
CHEMBL24470 ↓ inhibits Mechanistic 256.0 nM (IC50)
CHEMBL2298601 ↓ inhibits Mechanistic 1.9 nM (IC50)
CHEMBL285599 ↓ inhibits Mechanistic 0.2 nM (IC50)
CHEMBL262635 ↓ inhibits Mechanistic 41.0 nM (IC50)
CHEMBL25196 ↓ inhibits Mechanistic 2.9 nM (IC50)
CHEMBL24291 ↓ inhibits Mechanistic 7.1 nM (IC50)
CHEMBL284645 ↓ inhibits Mechanistic 1553.0 nM (IC50)
CHEMBL25083 ↓ inhibits Mechanistic 36.0 nM (IC50)
CHEMBL25282 ↓ inhibits Mechanistic 212.0 nM (IC50)
CHEMBL280954 ↓ inhibits Mechanistic 69.0 nM (IC50)
CHEMBL25193 ↓ inhibits Mechanistic 4.0 nM (IC50)
CHEMBL24193 ↓ inhibits Mechanistic 218.0 nM (IC50)
CHEMBL280387 ↓ inhibits Mechanistic 428.0 nM (IC50)
CHEMBL25072 ↓ inhibits Mechanistic 0.2 nM (IC50)
CHEMBL24465 ↓ inhibits Mechanistic 0.4 nM (IC50)
CHEMBL279206 ↓ inhibits Mechanistic 23.0 nM (IC50)
CHEMBL25593 ↓ inhibits Mechanistic 1218.0 nM (IC50)
CHEMBL25093 ↓ inhibits Mechanistic 10.0 nM (Ki)
CHEMBL278860 ↓ inhibits Mechanistic 381.0 nM (IC50)
CHEMBL25448 ↓ inhibits Mechanistic 154.0 nM (IC50)
CHEMBL285439 ↓ inhibits Mechanistic 6300.0 nM (IC50)
CHEMBL412425 ↓ inhibits Mechanistic 0.12 nM (IC50)

Showing top 40 of 145 agents ranked by evidence tier.

Therapeutic Agent Effect Direction Evidence Tier Potency Source
MM3122 ↓ inhibits Mechanistic
CAMOSTAT ↓ inhibits Mechanistic 1000.0 nM (EC50)
OTAMIXABAN ↓ inhibits Mechanistic 620.0 nM (IC50)
I-432 ↓ inhibits Mechanistic
N-0385 ↓ inhibits Mechanistic
NAFAMOSTAT ↓ inhibits Mechanistic 1.0 nM (IC50)
COMPOUND 5 [PMID: 21741839] ↓ inhibits Mechanistic
N-0920 ↓ inhibits Mechanistic
CHEMBL1229259 ↓ inhibits Mechanistic 20.0 nM (Ki)
CHEMBL1809250 ↓ inhibits Mechanistic 53.0 nM (Ki)
CHEMBL1809251 ↓ inhibits Mechanistic 68.0 nM (Ki)
CHEMBL3219102 ↓ inhibits Mechanistic 3.0 nM (Ki)
CHEMBL3219101 ↓ inhibits Mechanistic 3.0 nM (Ki)
CHEMBL3219100 ↓ inhibits Mechanistic 3.0 nM (Ki)
CHEMBL3219103 ↓ inhibits Mechanistic 3.0 nM (Ki)
CHEMBL3219079 ↓ inhibits Mechanistic 0.9 nM (Ki)
CHEMBL3219087 ↓ inhibits Mechanistic 1.0 nM (Ki)
PROPAMIDINE ↓ inhibits Mechanistic 9000.0 nM (IC50)
PENTAMIDINE ↓ inhibits Mechanistic 1200.0 nM (IC50)
DEBRISOQUIN ↓ inhibits Mechanistic 70000.0 nM (IC50)
CHEMBL5270157 ↓ inhibits Mechanistic 4000.0 nM (IC50)
CHEMBL5271456 ↓ inhibits Mechanistic 9000.0 nM (IC50)
CHEMBL5275059 ↓ inhibits Mechanistic 20000.0 nM (IC50)
CHEMBL5270536 ↓ inhibits Mechanistic 20000.0 nM (IC50)
CHEMBL5285196 ↓ inhibits Mechanistic 3400.0 nM (IC50)
CHEMBL5266850 ↓ inhibits Mechanistic 4000.0 nM (IC50)
CHEMBL5275526 ↓ inhibits Mechanistic 20000.0 nM (IC50)
CHEMBL5287275 ↓ inhibits Mechanistic 12000.0 nM (IC50)
TANNIC ACID ↓ inhibits Mechanistic 2310.0 nM (IC50)
DIMINAZENE ↓ inhibits Mechanistic 1350.0 nM (IC50)
CHEMBL1185793 ↓ inhibits Mechanistic 70.0 nM (IC50)
GABEXATE ↓ inhibits Mechanistic 130.0 nM (IC50)
CHEMBL147503 ↓ inhibits Mechanistic 1240.0 nM (IC50)
CHEMBL5561725 ↓ inhibits Mechanistic 22.0 nM (IC50)
CHEMBL5555448 ↓ inhibits Mechanistic 2.5 nM (IC50)
CHEMBL5562350 ↓ inhibits Mechanistic 14.0 nM (IC50)
CHEMBL5558547 ↓ inhibits Mechanistic 1.2 nM (IC50)
CHEMBL5560759 ↓ inhibits Mechanistic 9.8 nM (IC50)
CHEMBL5564865 ↓ inhibits Mechanistic 16.0 nM (IC50)
CHEMBL5557087 ↓ inhibits Mechanistic 16.0 nM (IC50)

Showing top 40 of 69 agents ranked by evidence tier.


Clinical Trials

Drug, biologic and supplement trials (treatment or prevention) from ClinicalTrials.gov whose main condition is Prostate Cancer: recruiting, active or completed, most recently updated first. Data retrieved 2026-10-28.

NCT07365423 Phase: 2 Started: 2026-04-24

TerbinaPro is a phase II drug-repurposing study evaluating oral Terbinafine in patients with biochemical recurrence of prostate cancer after prior local treatment with curative intent. When local salvage strategies have been exhausted, recurrence usually reflects micro-metastatic disease without cle...

NCT07310433 Phase: 2 Started: 2026-05-01

Dapagliflozin is a well-established medication being marketed and used for treatment Type 2 diabetes mellitus (T2DM). In retrospective cohort studies done by our team, we found that metastatic prostate cancer patients who received Dapagliflozin together with standard anti-cancer treatment, androgen ...

NCT04597125 Phase: 4 Started: 2020-11-09

Researchers in this study want to compare how well drug radium-223 dichloride (Xofigo) and androgen receptor pathway inhibitor (ARPI) therapy work in participants with prostate gland cancer which has spread to the bone and progressed on or after one line of ARPI therapy. Meanwhile researchers want t...

NCT04015622 Phase: 2 Started: 2020-10-07

The purpose of this study is to assess the strategy in treatment selection using ctDNA fraction as a predictive biomarker to direct treatment decision (ctDNA fraction \<2% receives enzalutamide, and ctDNA fraction ≥2% receives docetaxel) versus clinician's choice of enzalutamide or docetaxel, in sub...

NCT05997615 Phase: 1 Started: 2023-08-10

There are many treatment options for men with various stages of prostate cancer. Some treatments work well for a while but can cause medical problems in some men. Also, the cancer may come back after treatment. This is an early development study of VIR-5500 in men with prostate cancer. In this study...

NCT07562438 Phase: 2 Started: 2026-04-29

PSMA is an ideal target for precision diagnosis and treatment of prostate cancer. P17-088 is a novel albumin-binding PSMA-targeted radioligand. This study aims to explore the safety and efficacy of 177Lu-labeled P17-088 for treating patients with PSMA-positive metastatic androgen pathway modulation ...

NCT07339267 Phase: 1 Started: 2026-01-20

In this study, ASP5541 will be given to Chinese men with prostate cancer. It will be given together with prednisone and androgen deprivation therapy (ADT). Prednisone is a steroid, and ADT is already given to the men as their standard of care for prostate cancer. The main aims of the study are to ch...

NCT05515978 Phase: Early 1 Started: 2022-10-10

Metformin is used widely in the treatment of type 2 diabetes. It has off-label indications for use in the prevention of diabetes and in hyperinsulinar obesity. In medical practices, the implementation of metformin for these off-label indications is variable, often at the level of the provider. Multi...

NCT07244341 Phase: 1 Started: 2025-12-03

This study will assess the safety and tolerability of valemetostat in combination with darolutamide in participants with Metastatic Castration Resistant Prostate Cancer (mCRPC).

NCT05593497 Phase: 2 Started: 2024-05-31

The purpose of this study is to learn about how an investigational drug intervention completed before doing prostate surgery (specifically, radical prostatectomy with lymph node dissection) may help in treatment of high risk localized prostate cancers that are most resistant to standard treatments. ...

NCT04655365 Phase: 2 Started: 2022-03-22

This study aimed to evaluate the diagnostic performance of 18F-DCFPyL (PyL) PET/CT in subjects presenting not previously treated for castration resistant prostate cancer and showing negative or equivocal findings per institutional standard of care conventional imaging

NCT07609225 Phase: Early 1 Started: 2026-10-16

This study compares two different imaging procedures to each other, one using positron emission tomography (PET) with fluorothymidine F-18 (FLT) (FLT PET for short), and the other using chemical shift-encoded (CSE) magnetic resonance imaging (MRI) or CSE-MRI for short, to determine specifically if C...

NCT07117760 Phase: 2 Started: 2025-04-22

PSMA is an ideal target for precision diagnosis and treatment of prostate cancer. LNC1011 is a novel albumin-binding PSMA-targeted radioligand. This study aims to explore the safety and efficacy of 225Ac-labeled LNC1011 for treating patients with PSMA-positive metastatic castration-resistant prostat...

NCT07570979 Phase: 1 Started: 2026-05-25

The purpose of this study is to assess the safety, tolerability, pharmacokinetics/pharmacodynamics, preliminary anti-tumor activity, and recommended dose of INR731 as a single agent and in combination with standard-of-care androgen receptor pathway inhibitors (ARPIs) in adult patients with metastati...

NCT07181161 Phase: 1/2 Started: 2025-10-01

The main purpose of this study is to assess the safety and tolerability of AZD0516 as monotherapy and/or in combination with other anti-cancer agents for treatment of metastatic prostate cancer.


Agents Found By Disease-Level Search

Searched directly from “Prostate Cancer” via ClinicalTrials.gov interventions and Open Targets' disease→drug data — independent of the 11-gene target panel above. This surfaces agents whose mechanism doesn't route through a curated gene (combination therapies, standard-of-care drugs, targets outside the panel).

47 agents shown (approved or with trial evidence) — 36 not found by the gene-target search above.

DocetaxelNOT in gene-target list

Phase 3 · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT00165399 NCT00004001 NCT00005096

DegarelixNOT in gene-target list

Approved · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT00268892 NCT00268892 NCT00268892

Apalutamide

Approved · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT03371719 NCT03767244 NCT07406282

Abiraterone Acetate

Approved · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT01637402 NCT07198633 NCT07406282

enzalutamide

Approved · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT07198633 NCT07406282 NCT02407054

Radium-223 dichloride (Xofigo, BAY88-8223)NOT in gene-target list

· 3 trials · source: ClinicalTrials.gov
NCT01565746 NCT01565746 NCT01565746

Estramustine

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT00165399 NCT00004001

Immunotherapy allogeneic GM-CSF secreting cellular vaccineNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT00140387 NCT00140348

68Ga-PSMA-11NOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT05670106 NCT02673151

Bone scanNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT03493945 NCT07200830

Computed TomographyNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT07200830 NCT07164027

Darolutamide

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT05762536 NCT07406282

prednisone

Approved · 2 trials · source: ClinicalTrials.gov, Open Targets
NCT00004001 NCT01637402

SM88 (Cohort 1)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02796898

SM88 (Cohort 2)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02796898

sodium seleniteNOT in gene-target list

Phase 1 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT02184533

Ga-68 PSMA11NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03768349

F-18 PSMA 1007NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03768349

BafetinibNOT in gene-target list

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT01215799

High Dose Rate MonotherapyNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05665738

PEG Hydrogel (SpaceOAR)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02212548

CasodexNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00165399

ZoladexNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00165399

Dose increase after injection of biodegradable material A safety study of high-risk prostate cancer patientsNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06461793

recombinant interferon alfaNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00005847

estramustine phosphate sodium

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00005847

isotretinoin

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00005847

mitoxantrone hydrochloride

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00005847

paclitaxelNOT in gene-target list

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00005847

vinorelbine ditartrateNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00005847

DC-Tn-MUC1: autologous dendritic cells expressing Tn-MUC1NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00852007

JUR-003NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07824349

Leuprorelin SRNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01122121

Flutamide

Approved · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT01122121

Community Health Worker supportNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05301114

bintrafusp alfa (M7824)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03493945

N-803NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03493945

MVA-BN-BrachyuryNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03493945

FPV-BrachyuryNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03493945

EpacadostatNOT in gene-target list

Phase 1/2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT03493945

AcetaminophenNOT in gene-target list

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT03493945

IbuprofenNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03493945

NaproxenNOT in gene-target list

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT03493945

EKGNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03493945

CT chest, abdomen and pelvisNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03493945

Degarelix acetate, Leuprolide acetateNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01344564

Carboplatin

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT04038502

Generated by the Open Source Medicine Foundation Biomarker Pipeline — 2026-10-08. Data sources: DGIdb, Open Targets, ChEMBL, PubMed, ClinicalTrials.gov. Not medical advice.