Biomarker & Intervention Discovery

Benign Prostatic Hyperplasia (BPH)

This page lists 10 druggable gene targets, 52 approved or trial-tested drug candidates and 15 recent clinical trials for Benign Prostatic Hyperplasia (BPH), 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.

Spontaneous remissionProgressive natural history; symptoms worsen in 50-60% over 5 years without treatment; spontaneous improvement in…
Best-intervention remissionCombination alpha-blocker + 5-ARI (tamsulosin + dutasteride): reduces prostate volume 25-30%, acute urinary retention…
Gap sizeModerate — treatment is effective but procedure uptake and pharmacotherapy titration is suboptimal; many patients…
Primary barrierpractice
Full remission profile →
Research Tracker Chronic Disease Interventions Benign Prostatic Hyperplasia (BPH)

Remission & chronicity

Spontaneous remission
Progressive natural history; symptoms worsen in 50-60% over 5 years without treatment; spontaneous improvement in 20-30% (particularly mild symptoms); acute urinary retention risk ~1-2%/year
Best-intervention remission
Combination alpha-blocker + 5-ARI (tamsulosin + dutasteride): reduces prostate volume 25-30%, acute urinary retention risk 67% (CombAT trial); minimally invasive procedures (Rezum, Urolift, Aquablation): IPSS improvement 50-60%, preserving ejaculatory function better than TURP; TURP: gold standard, 70-80% symptom improvement
Gap size
Moderate — treatment is effective but procedure uptake and pharmacotherapy titration is suboptimal; many patients overtreated with TURP when less invasive options appropriate
Primary barrier
practice
Alpha-blockers provide symptomatic relief but do not address prostate volume in large glands (5-ARI needed); TURP remains widely used when Rezum/Urolift preserve sexual function with similar efficacy; pharmacotherapy stepped-up without referral in cases where early MIS procedure would preserve more function

Biomarker Targets & Therapeutic Agents

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

ADRA1A 279ADRA1B 279ADRA1D 279AR 994ESR2 243IGF1 4KLK3 208PDE5A 220SRD5A1 164SRD5A2 145

ADRA1A

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
CARVEDILOL PHOSPHATE ↓ inhibits Mechanistic DGIdb
METHOXAMINE ↑ activates Mechanistic DGIdb
PRAZOSIN ↓ inhibits Mechanistic 0.3162 nM (Ki) DGIdb
PHENOXYBENZAMINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
BUNAZOSIN ? unclear Mechanistic DGIdb
SENREBOTASE ? unclear Mechanistic DGIdb
[125I]HEAT (BE2254) ↓ inhibits Mechanistic DGIdb
PAPAVERINE ? unclear Mechanistic DGIdb
CARVEDILOL ↓ inhibits Mechanistic DGIdb
DOXAZOSIN MESYLATE ↓ inhibits Mechanistic DGIdb
RS-100329 ↓ inhibits Mechanistic DGIdb
LABETALOL ↓ inhibits Mechanistic DGIdb
BETHANIDINE ? unclear Mechanistic DGIdb
NOREPINEPHRINE ↑ activates Mechanistic DGIdb
BUCINDOLOL HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
TRIMAZOSIN ? unclear Mechanistic DGIdb
SILODOSIN ↓ inhibits Mechanistic 1.995 nM (Ki) DGIdb
NIGULDIPINE ↓ inhibits Mechanistic DGIdb
CIRAZOLINE ↑ activates Mechanistic 125.89 nM (EC50) DGIdb
5-METHYLURAPIDIL ↓ inhibits Mechanistic DGIdb
PHENOXYBENZAMINE ↓ inhibits Mechanistic DGIdb
EPINEPHRINE ↑ activates Mechanistic DGIdb
MT-1207 ↓ inhibits Mechanistic DGIdb
TERAZOSIN ↓ inhibits Mechanistic 0.85 nM (Ki) DGIdb
MOXISYLYTE ↓ inhibits Mechanistic DGIdb
NAFTOPIDIL ↓ inhibits Mechanistic DGIdb
PHENYLEPHRINE ↑ activates Mechanistic DGIdb
NOREPINEPHRINE BITARTRATE ↑ activates Mechanistic DGIdb
XYLOMETAZOLINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
TAMSULOSIN HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
A-119637 ↓ inhibits Mechanistic 0.252 nM (Ki) DGIdb
OXYMETAZOLINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
TOLAZOLINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
EPINEPHRINE BITARTRATE ↑ activates Mechanistic DGIdb
DAPIPRAZOLE ↓ inhibits Mechanistic DGIdb
MIDODRINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
NAN 190 ↓ inhibits Mechanistic DGIdb
METARAMINOL BITARTRATE ↑ activates Mechanistic DGIdb
ERGOLOID MESYLATES ↓ inhibits Mechanistic DGIdb
ALFUZOSIN HYDROCHLORIDE ↑ activates Mechanistic DGIdb

Showing top 40 of 279 agents ranked by evidence tier.

ADRA1B

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
DEBRISOQUIN ? unclear Mechanistic DGIdb
NOREPINEPHRINE ↑ activates Mechanistic DGIdb
KETANSERIN ↓ inhibits Mechanistic DGIdb
COMPOUND 12 [PMID: 26238322] ↓ inhibits Mechanistic DGIdb
CARVEDILOL PHOSPHATE ↓ inhibits Mechanistic DGIdb
EPINEPHRINE ↑ activates Mechanistic DGIdb
DOXAZOSIN MESYLATE ↓ inhibits Mechanistic DGIdb
A61603 ↑ activates Mechanistic DGIdb
ISOPROTERENOL ? unclear Mechanistic DGIdb
MOXISYLYTE ↓ inhibits Mechanistic DGIdb
LABETALOL HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
TAMSULOSIN HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
METHOXAMINE ↑ activates Mechanistic DGIdb
RITANSERIN ↓ inhibits Mechanistic DGIdb
RO-70-0004 ↓ inhibits Mechanistic DGIdb
NEFAZODONE ? unclear Mechanistic DGIdb
MAMBA TOXIN CM-3 ↓ inhibits Mechanistic DGIdb
METARAMINOL BITARTRATE ↑ activates Mechanistic DGIdb
AVIPTADIL ↓ inhibits Mechanistic DGIdb
QUETIAPINE FUMARATE ? unclear Mechanistic DGIdb
MT-1207 ↓ inhibits Mechanistic DGIdb
BUCINDOLOL HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
ISOXSUPRINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
MIANSERIN ↓ inhibits Mechanistic DGIdb
NOREPINEPHRINE BITARTRATE ↑ activates Mechanistic DGIdb
EPHEDRINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
DROXIDOPA ↑ activates Mechanistic DGIdb
CLOZAPINE ↓ inhibits Mechanistic DGIdb
AH 11110 ↓ inhibits Mechanistic DGIdb
METHOTRIMEPRAZINE ? unclear Mechanistic DGIdb
REC 15/2615 ↓ inhibits Mechanistic DGIdb
(+)-ADRENALINE ↑ activates Mechanistic DGIdb
PROMAZINE ? unclear Mechanistic DGIdb
INDORAMIN ↓ inhibits Mechanistic 39.81 nM (Ki) DGIdb
EPINEPHRINE BITARTRATE ↑ activates Mechanistic DGIdb
MIDODRINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
PHENYLEPHRINE ↑ activates Mechanistic DGIdb
LABETALOL ? unclear Mechanistic DGIdb
SPIPERONE ↓ inhibits Mechanistic DGIdb
PHENYLEPHRINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb

Showing top 40 of 279 agents ranked by evidence tier.

ADRA1D

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
CARVEDILOL PHOSPHATE ↓ inhibits Mechanistic DGIdb
METHOXAMINE ↑ activates Mechanistic DGIdb
PRAZOSIN ↓ inhibits Mechanistic 0.3162 nM (Ki) DGIdb
PHENOXYBENZAMINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
BUNAZOSIN ? unclear Mechanistic DGIdb
SENREBOTASE ? unclear Mechanistic DGIdb
[125I]HEAT (BE2254) ↓ inhibits Mechanistic DGIdb
PAPAVERINE ? unclear Mechanistic DGIdb
CARVEDILOL ↓ inhibits Mechanistic DGIdb
DOXAZOSIN MESYLATE ↓ inhibits Mechanistic DGIdb
RS-100329 ↓ inhibits Mechanistic DGIdb
LABETALOL ↓ inhibits Mechanistic DGIdb
BETHANIDINE ? unclear Mechanistic DGIdb
NOREPINEPHRINE ↑ activates Mechanistic DGIdb
BUCINDOLOL HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
TRIMAZOSIN ? unclear Mechanistic DGIdb
SILODOSIN ↓ inhibits Mechanistic 1.995 nM (Ki) DGIdb
NIGULDIPINE ↓ inhibits Mechanistic DGIdb
CIRAZOLINE ↑ activates Mechanistic 125.89 nM (EC50) DGIdb
5-METHYLURAPIDIL ↓ inhibits Mechanistic DGIdb
PHENOXYBENZAMINE ↓ inhibits Mechanistic DGIdb
EPINEPHRINE ↑ activates Mechanistic DGIdb
MT-1207 ↓ inhibits Mechanistic DGIdb
TERAZOSIN ↓ inhibits Mechanistic 0.85 nM (Ki) DGIdb
MOXISYLYTE ↓ inhibits Mechanistic DGIdb
NAFTOPIDIL ↓ inhibits Mechanistic DGIdb
PHENYLEPHRINE ↑ activates Mechanistic DGIdb
NOREPINEPHRINE BITARTRATE ↑ activates Mechanistic DGIdb
XYLOMETAZOLINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
TAMSULOSIN HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
A-119637 ↓ inhibits Mechanistic 0.252 nM (Ki) DGIdb
OXYMETAZOLINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
TOLAZOLINE HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
EPINEPHRINE BITARTRATE ↑ activates Mechanistic DGIdb
DAPIPRAZOLE ↓ inhibits Mechanistic DGIdb
MIDODRINE HYDROCHLORIDE ↑ activates Mechanistic DGIdb
NAN 190 ↓ inhibits Mechanistic DGIdb
METARAMINOL BITARTRATE ↑ activates Mechanistic DGIdb
ERGOLOID MESYLATES ↓ inhibits Mechanistic DGIdb
ALFUZOSIN HYDROCHLORIDE ↑ activates Mechanistic DGIdb

Showing top 40 of 279 agents ranked by evidence tier.

AR

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

Showing top 40 of 994 agents ranked by evidence tier.

ESR2

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
OSPEMIFENE ↓ inhibits Mechanistic DGIdb
ESTRONE ↑ activates Mechanistic 1135.0 nM (EC50) DGIdb
LAPATINIB ? unclear Mechanistic DGIdb
ESTRADIOL VALERATE ↑ activates Mechanistic DGIdb
FULVESTRANT ↓ inhibits Mechanistic 7.0 nM (IC50) DGIdb
DIETHYLSTILBESTROL ↑ activates Mechanistic 9.0 nM (EC50) DGIdb
RIBOCICLIB ? unclear Mechanistic DGIdb
PERTUZUMAB ? unclear Mechanistic DGIdb
CHEMBL:CHEMBL1222035 ? unclear Mechanistic DGIdb
ALENDRONATE SODIUM ? unclear Mechanistic DGIdb
LASOFOXIFENE TARTRATE ~ modulates Mechanistic DGIdb
LASOFOXIFENE ↑ activates Mechanistic DGIdb
TAMOXIFEN ↓ inhibits Mechanistic DGIdb
BAZEDOXIFENE ACETATE ~ modulates Mechanistic DGIdb
RALOXIFEN ? unclear Mechanistic DGIdb
FERB 033 ↑ activates Mechanistic DGIdb
ERTEBEREL ? unclear Mechanistic DGIdb
ABEMACICLIB ? unclear Mechanistic DGIdb
ESTRIOL ↑ activates Mechanistic DGIdb
GEMCITABINE ? unclear Mechanistic DGIdb
ALLYLESTRENOL ↑ activates Mechanistic DGIdb
R,R-THC ↓ inhibits Mechanistic DGIdb
IXABEPILONE ? unclear Mechanistic DGIdb
4-HYDROXYTAMOXIFEN ↓ inhibits Mechanistic DGIdb
NORENDOXIFEN ↑ activates Mechanistic DGIdb
PRINABEREL ↑ activates Mechanistic DGIdb
WAY200070 ↑ activates Mechanistic DGIdb
(S)-LIQUIRITIGENIN ↑ activates Mechanistic DGIdb
EVEROLIMUS ? unclear Mechanistic DGIdb
GOSERELIN ? unclear Mechanistic DGIdb
TRASTUZUMAB ? unclear Mechanistic DGIdb
OLAPARIB ? unclear Mechanistic DGIdb
MF101 ↑ activates Mechanistic DGIdb
ESTETROL ↑ activates Mechanistic DGIdb
FAM-TRASTUZUMAB DERUXTECAN-NXKI ? unclear Mechanistic DGIdb
CHLOROTRIANISENE ~ modulates Mechanistic DGIdb
NARINGENIN ? unclear Mechanistic DGIdb
CAPIVASERTIB ? unclear Mechanistic DGIdb
INAVOLISIB ? unclear Mechanistic DGIdb
RALOXIFENE HYDROCHLORIDE ~ modulates Mechanistic 43.0 nM (IC50) DGIdb

Showing top 40 of 243 agents ranked by evidence tier.

IGF1

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
XENTUZUMAB ↓ inhibits Mechanistic DGIdb
MECASERMIN ? unclear Mechanistic DGIdb
DUSIGITUMAB ↓ inhibits Mechanistic DGIdb
TROFINETIDE ? unclear Mechanistic DGIdb

KLK3

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

Showing top 40 of 208 agents ranked by evidence tier.

PDE5A

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
IBUDILAST ↓ inhibits Mechanistic DGIdb
SILDENAFIL ↓ inhibits Mechanistic 8.7 nM (EC50) DGIdb
GISADENAFIL ↓ inhibits Mechanistic DGIdb
AVANAFIL ↓ inhibits Mechanistic DGIdb
COMPOUND 3M [PMID: 32603117] ↓ inhibits Mechanistic DGIdb
DIPYRIDAMOLE ↓ inhibits Mechanistic DGIdb
T0156 ↓ inhibits Mechanistic DGIdb
TADALAFIL ↓ inhibits Mechanistic 6.7 nM (IC50) DGIdb
PF-03049423 ↓ inhibits Mechanistic DGIdb
SCH51866 ↓ inhibits Mechanistic DGIdb
PENTOXIFYLLINE ↓ inhibits Mechanistic DGIdb
MIRODENAFIL ↓ inhibits Mechanistic DGIdb
THEOPHYLLINE ? unclear Mechanistic DGIdb
ZAPRINAST ↓ inhibits Mechanistic 900.0 nM (IC50) DGIdb
PAPAVERINE ? unclear Mechanistic DGIdb
ICARIIN ↓ inhibits Mechanistic DGIdb
ROLIPRAM ? unclear Mechanistic DGIdb
SLX-2101 ? unclear Mechanistic DGIdb
VARDENAFIL ↓ inhibits Mechanistic DGIdb
PF-00489791 ↓ inhibits Mechanistic DGIdb
SILDENAFIL CITRATE ↓ inhibits Mechanistic DGIdb
ENALAPRIL MALEATE ? unclear Mechanistic DGIdb
NITROSOPRODENAFIL ↓ inhibits Mechanistic DGIdb
OSI-461 ? unclear Mechanistic DGIdb
SIMENAFIL ↓ inhibits Mechanistic DGIdb
C1 ESTERASE INHIBITOR (RECOMBINANT) ? unclear Mechanistic DGIdb
VARDENAFIL HYDROCHLORIDE ↓ inhibits Mechanistic DGIdb
MILRINONE ↓ inhibits Mechanistic DGIdb
LORNEIC ACID A ? unclear Mechanistic DGIdb
EXISULIND ? unclear Mechanistic DGIdb
UDENAFIL ↓ inhibits Mechanistic DGIdb
COMPOUND 53 [PMID: 19631533] ↓ inhibits Mechanistic DGIdb
TUNODAFIL ↓ inhibits Mechanistic DGIdb
CHEMBL90164 ↓ inhibits Mechanistic 11.0 nM (IC50) ChEMBL
CHEMBL87901 ↓ inhibits Mechanistic 60.0 nM (IC50) ChEMBL
CHEMBL313197 ↓ inhibits Mechanistic 24.0 nM (IC50) ChEMBL
CHEMBL86578 ↓ inhibits Mechanistic 93.0 nM (IC50) ChEMBL
CHEMBL313561 ↓ inhibits Mechanistic 130.0 nM (IC50) ChEMBL
CHEMBL87202 ↓ inhibits Mechanistic 10.0 nM (IC50) ChEMBL
CHEMBL87954 ↓ inhibits Mechanistic 135.0 nM (IC50) ChEMBL

Showing top 40 of 220 agents ranked by evidence tier.

SRD5A1

UniProt Ensembl DGIdb Open Targets
Therapeutic Agent Effect Direction Evidence Tier Potency Source
FINASTERIDE ? unclear Mechanistic 911.0 nM (IC50) DGIdb
CHEMBL:CHEMBL29166 ? unclear Mechanistic DGIdb
ABIRATERONE ACETATE ↓ inhibits Mechanistic DGIdb
DUTASTERIDE ↓ inhibits Mechanistic DGIdb
LEVONORGESTREL ? unclear Mechanistic DGIdb
BEXLOSTERIDE ? unclear Mechanistic 8.0 nM (IC50) DGIdb
CHEMBL99448 ↓ inhibits Mechanistic 5130.0 nM (IC50) ChEMBL
CHEMBL417109 ↓ inhibits Mechanistic 9.0 nM (Ki) ChEMBL
CHEMBL25081 ↓ inhibits Mechanistic 1200.0 nM (Ki) ChEMBL
CHEMBL99615 ↓ inhibits Mechanistic 127.0 nM (IC50) ChEMBL
CHEMBL97266 ↓ inhibits Mechanistic 920.0 nM (Ki) ChEMBL
CHEMBL96006 ↓ inhibits Mechanistic 298.0 nM (IC50) ChEMBL
CHEMBL138580 ↓ inhibits Mechanistic 1600.0 nM (IC50) ChEMBL
CHEMBL439910 ↓ inhibits Mechanistic 79.43 nM (IC50) ChEMBL
CHEMBL278957 ↓ inhibits Mechanistic 34.67 nM (IC50) ChEMBL
CHEMBL277091 ↓ inhibits Mechanistic 562.34 nM (IC50) ChEMBL
CHEMBL16494 ↓ inhibits Mechanistic 60.26 nM (IC50) ChEMBL
CHEMBL279417 ↓ inhibits Mechanistic 32.36 nM (IC50) ChEMBL
CHEMBL15917 ↓ inhibits Mechanistic 32.36 nM (IC50) ChEMBL
CHEMBL16152 ↓ inhibits Mechanistic 151.36 nM (IC50) ChEMBL
CHEMBL16456 ↓ inhibits Mechanistic 173.78 nM (IC50) ChEMBL
CHEMBL439908 ↓ inhibits Mechanistic 89.13 nM (IC50) ChEMBL
CHEMBL278049 ↓ inhibits Mechanistic 1000.0 nM (IC50) ChEMBL
CHEMBL16248 ↓ inhibits Mechanistic 1000.0 nM (IC50) ChEMBL
CHEMBL279131 ↓ inhibits Mechanistic 7.943 nM (IC50) ChEMBL
CHEMBL16027 ↓ inhibits Mechanistic 114.82 nM (IC50) ChEMBL
CHEMBL16330 ↓ inhibits Mechanistic 114.82 nM (IC50) ChEMBL
CHEMBL279420 ↓ inhibits Mechanistic 32.36 nM (IC50) ChEMBL
CHEMBL278981 ↓ inhibits Mechanistic 34.67 nM (IC50) ChEMBL
EPRISTERIDE ↓ inhibits Mechanistic 1100.0 nM (IC50) ChEMBL
CHEMBL77650 ↓ inhibits Mechanistic 990.0 nM (IC50) ChEMBL
CHEMBL24464 ↓ inhibits Mechanistic 709.0 nM (IC50) ChEMBL
CHEMBL311624 ↓ inhibits Mechanistic 1300.0 nM (IC50) ChEMBL
CHEMBL76373 ↓ inhibits Mechanistic 8400.0 nM (IC50) ChEMBL
CHEMBL2311155 ↓ inhibits Mechanistic 2700.0 nM (IC50) ChEMBL
CHEMBL311013 ↓ inhibits Mechanistic 50300.0 nM (IC50) ChEMBL
CHEMBL76959 ↓ inhibits Mechanistic 490.0 nM (IC50) ChEMBL
CHEMBL312466 ↓ inhibits Mechanistic 620.0 nM (IC50) ChEMBL
CHEMBL283564 ↓ inhibits Mechanistic 981.0 nM (IC50) ChEMBL
CHEMBL77169 ↓ inhibits Mechanistic 820.0 nM (IC50) ChEMBL

Showing top 40 of 164 agents ranked by evidence tier.

SRD5A2

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

Showing top 40 of 145 agents ranked by evidence tier.

Clinical Trials

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

REZŪM vs. Dual Drug Therapy for Symptomatic Benign Prostatic Hyperplasia in Sexually Active Men Active Not Recruiting
NCT04838769 Phase: N/A Started: 2021-09-15

The study objective is to compare water vapor thermotherapy with the REZŪM™ System to dual drug therapy for the treatment of symptomatic benign prostatic hyperplasia refractory to alpha-blocker monotherapy in sexually active men.

Tranexamic Acid for Bleeding Reduction During TURP Surgery Recruiting
NCT07460518 Phase: 4 Started: 2026-03-30

Transurethral resection of the prostate (TURP) is commonly performed in elderly patients and may be associated with perioperative bleeding leading to postoperative anemia and delayed recovery. Tranexamic acid (TXA), an antifibrinolytic agent, may reduce surgical bleeding by inhibiting fibrin degrada...

Bioequivalence Study of AJU-G721 and G721R in Healthy Adult Volunteers Under Fasting Conditions Completed
NCT07643220 Phase: 1 Started: 2026-06-27

To evaluate and compare the safety and pharmacokinetic profiles of "AJU-G721" (test drug) and "G721R" (reference drug) in healthy adult male subjects.

Standard Versus Double Alpha Blockers Treatment for Symptomatic Benign Prostatic Obstruction Active Not Recruiting
NCT07815379 Phase: 4 Started: 2025-10-12

Failed medical treatment to alleviate LUTS and AUR is an indication for intervention, some trials were published elucidating the possible use of standard dose tamsulosin and silodosin and double dose tamsulosin but to the best of our knowledge, no studies with head-to-head comparison between Tamsulo...

The Efficacy and Safety of Silodosin in the Treatment of Benign Prostatic Hyperplasia Completed
NCT05551221 Phase: 4 Started: 2022-09-21

Objective: To evaluate the efficacy and safety of Silodosin Capsules in the treatment of Benign Prostatic Hyperplasia (BPH) with Lower Urinary Tract Symptoms (LUTS) compared with Tamsulosin Hydrochloride Sustained Release Capsules. Study design: A multicenter, prospective, randomized, investigator-b...

A Clinical Trial to Evaluate the Safety and the Pharmacokinetics of AD-116 Compared to AD-1161 in Healthy Adult Male Volunteers Completed
NCT07103278 Phase: 1 Started: 2026-01-22

The study compare and evaluate the safety and pharmacokinetic characteristics between the administration of AD-116 and the administration of AD-1161 in healthy adult male volunteers

A Clinical Trial to Compare and Evaluate Evaluate the Pharmacokinetics and Safety of CKD-846 Completed
NCT07404735 Phase: 1 Started: 2026-02-23

A Clinical trial to compare and evaluate evaluate the pharmacokinetics and safety of CKD-846

BOTOX Injection Technique for LUTS Due to BPH Completed
NCT07645456 Phase: 1 Started: 2025-10-01

his prospective, randomized comparative study evaluated whether a combined Botulinum Toxin Type A (BOTOX) injection technique provides superior outcomes compared to injecting the prostatic parenchyma alone for patients with benign prostatic hyperplasia (BPH) and a prostate volume of 30-60 grams. Six...

The Evaluation of Banana Flower Stamens Extract on Prevention of Benign Prostatic Hyperplasia in Adults Completed
NCT04266418 Phase: N/A Started: 2023-03-01

To assess the evaluation of banana flower stamens extract on prevention of benign prostatic hyperplasia in adults

New Treatment Strategies and Epigenetic Biomarker for Management of Benign Prostatic Hyperplasia Recruiting
NCT06944145 Phase: 2 Started: 2025-12-03

SRD5A2 is a critical enzyme for prostatic development and growth, and the SRD5A2 inhibitor, finasteride, is used to treat benign prostatic hyperplasia (BPH). SRD5A2 is absent in 30% of normal adult men, which explains the resistance of a subset of patients to this commonly prescribed drug. This proj...

A Study to Evaluate the Safety and Pharmacokinetics of AD-116 and AD-1161 in Healthy Adult Male Subjects Recruiting
NCT07444385 Phase: 1 Started: 2026-02-26

A Study to Evaluate the Safety and Pharmacokinetics of AD-116 and AD-1161 Under Fed Conditions in Healthy Adult Male Subjects

A Clinical Observation Study of a Chinese Patent Medicine Combined With Tamsulosin in Improving Sleep and Nocturia Symptoms After Enucleation of the Prostate Recruiting
NCT07357324 Phase: 4 Started: 2024-12-01

This study will test whether a traditional Chinese medicine called Lingze tablets, when added to the standard drug tamsulosin, can better improve sleep and nighttime urination problems in men after prostate surgery. Who can participate? Men aged 50 years or older who have had transurethral holmium l...

A Clinical Trial to Compare and Evaluate Evaluate the Pharmacokinetics and Safety of CKD-846 Completed
NCT06110923 Phase: 1 Started: 2023-11-13

A Clinical trial to compare and evaluate evaluate the pharmacokinetics and safety of CKD-846

Optilume™ BPH Prostatic Drug Coated Balloon Dilation Catheter Completed
NCT03423979 Phase: 2 Started: 2017-12-19

A prospective, non-randomized study. The subjects will be enrolled and treated with the Optilume BPH Prostatic DCB Dilation Catheter System at up to 8 clinical sites. The post-treatment follow-up visit can be up to 5 years. The objective of the study is to evaluate the safety and efficacy of the Opt...

5-Alpha Reductase 2 as a Marker of Resistance to 5ARI Therapy Recruiting
NCT04288427 Phase: N/A Started: 2020-09-25

The study is being conducted to learn why some patients with Benign Prostatic Hyperplasia (BPH) do not respond to a commonly used treatment drug, Finasteride. The hope is to find ways to predict which patients will not respond to Finasteride so that, in the future, these patients can be identified p...

Agents Found By Disease-Level Search

Searched directly from “Benign Prostatic Hyperplasia (BPH)” via ClinicalTrials.gov interventions and Open Targets' disease→drug data — independent of the 10-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).

52 agents shown (approved or with trial evidence) — 46 not found by the gene-target search above.

Tamsulosin

Approved · 7 trials · source: ClinicalTrials.gov, Open Targets
NCT05818670 NCT04107896 NCT02244320

Tadalafil

Approved · 5 trials · source: ClinicalTrials.gov, Open Targets
NCT05818670 NCT00861757 NCT02239484

dutasteride

Approved · 5 trials · source: ClinicalTrials.gov, Open Targets
NCT01657851 NCT00883909 NCT00368979

Alfuzosin

Approved · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT00290030 NCT00542165 NCT00399464

Silodosin

Approved · 3 trials · source: ClinicalTrials.gov, Open Targets
NCT04107896 NCT01222650 NCT07134907

UK-369,003NOT in gene-target list

· 3 trials · source: ClinicalTrials.gov
NCT00408954 NCT00408954 NCT00814736

NX-1207NOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT01846793 NCT00918983

Reference formulationNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT01262989 NCT01330303

Transurethral Resection of the ProstateNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT01533038 NCT00908427

silodosin (KSO-0400)NOT in gene-target list

Approved · 2 trials · source: ClinicalTrials.gov
NCT01222650 NCT01222650

bTURPNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT07718256 NCT01637701

spinal anesthesiaNOT in gene-target list

· 2 trials · source: ClinicalTrials.gov
NCT01342562 NCT01342562

BONT-A intra-prostatic injectionNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01275521

Optimized medical BPH treatmentNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01275521

the Digital Repetitive Infrapubic Pressure maneuverNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01387893

FLOMAX® capsulesNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02244294

Beacon PlatformNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07741656

tamsulosin capsulesNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02417831

tamsulosin HClNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02417831

Dutasteride plus tamsulosinNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01777269

SpermotrendNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT05222841

talaporfin sodiumNOT in gene-target list

Phase 1 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00918034

Transurethral illumination with light emitting diodesNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00918034

PlacementNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00918034

RezumNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06820606

UroLiftNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06820606

tertomotide (GV1001)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02855892

teverelix TFA 120 mgNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04693507

teverelix TFA 180 mgNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04693507

Nesbit techniqueNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06901115

Corkscrew techniqueNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06901115

HolepNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT04471155

Prostate Artery EmbolizationNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02026908

CKD-846NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06110923

D091NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT06110923

Levofloxacin oral tabletsNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00169585

alpha-adrenergic blockerNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02244307

BOTOXNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01566292

PhytotherapyNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07144709

Embosphere® (Prostatic Arteries Embolization)NOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02869971

Drug therapyNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02869971

INTUPRO ionic fluidNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07381127

OzarelixNOT in gene-target list

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT00427219

dutasteride/tamsulosinNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT01657851

Tamsulosin Oral CapsuleNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03856242

TURPNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT03856242

Naftopidil

Phase 3 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT01922375

MK0906, finasteride / Duration of Treatment: 48 weeksNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT00127179

PuraStat hydrogel and the syringeNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT07789041

AdalimumabNOT in gene-target list

Phase 2 · 1 trial · source: ClinicalTrials.gov, Open Targets
NCT06062875

HCP1303 capsule 5/0.2mgNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02667938

HCP1303 capsule 5/0.4mgNOT in gene-target list

· 1 trial · source: ClinicalTrials.gov
NCT02667938

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