Tadalafil

Summary

Tadalafil (CHEMBL779) is an approved small-molecule EC 3.1.4.35 (3’,5’-cyclic-GMP phosphodiesterase) inhibitor (ATC G04BE08) targeting PDE5A and PDE11A; indicated across 38 conditions including benign prostatic hyperplasia and erectile dysfunction.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: G04BE08
• Targets: 2 (PDE5A, PDE11A)
• Indications: 38 conditions
• Clinical trials: 210
• Chemistry: 389.4 Da · C22H19N3O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL779
Name	Tadalafil
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	110635
ChEBI	CHEBI:71940
ATC	G04BE08
Molecular formula	C22H19N3O4
Molecular weight	389.4
InChIKey	WOXKDUGGOYFFRN-IIBYNOLFSA-N

SMILES: CN1CC(=O)N2[C@@H](C1=O)CC3=C([C@H]2C4=CC5=C(C=C4)OCO5)NC6=CC=CC=C36

IUPAC name: (2R,8R)-2-(1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione

ChEBI definition: A pyrazinopyridoindole that is 2,3,6,7,12,12a-hexahydropyrazino[1’,2’:1,6]pyrido[3,4-b]indole-1,4-dione substituted at position 2 by a methyl group and at position 6 by a 1,3-benzodioxol-5-yl group (the 6R,12aR-diastereomer). A phosphodiesterase V inhibitor inhibitor, currently marketed in pill form for treating erectile dysfunction under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.

Pharmacological roles (ChEBI): EC 3.1.4.35 (3’,5’-cyclic-GMP phosphodiesterase) inhibitor, vasodilator agent.

Also known as: Adcirca, Adcirca (previously tadalafil lilly), Chewtadzy, Cialis, IC-351, IC351, LY-450190, LY450190, NSC-750236, NSC-759172, Tadalafil, Tadalafil component of entadfi

Patent coverage: 6,012 distinct patent families (23,417 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 22,681 (97%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
PDE5A	phosphodiesterase 5A	Inhibition	8.52	0%	O76074
PDE11A	phosphodiesterase 11A	Inhibition	6.52	0.2%	Q9HCR9

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: cGMP-specific 3’,5’-cyclic phosphodiesterase, Nuclear receptor subfamily 2 group E member 1, Phosphodiesterase 4, Phosphodiesterase 6, Phosphodiesterase 6, Acetylcholinesterase, Sodium-dependent serotonin transporter, Voltage-gated inwardly rectifying potassium channel KCNH2, Dual 3’,5’-cyclic-AMP and -GMP phosphodiesterase 11A, Acetylcholinesterase, Nuclear receptor subfamily 1 group I member 2, cGMP-specific 3’,5’-cyclic phosphodiesterase, Rod cGMP-specific 3’,5’-cyclic phosphodiesterase subunit alpha, Cone cGMP-specific 3’,5’-cyclic phosphodiesterase subunit alpha’, Mitogen-activated protein kinase 1, Dual 3’,5’-cyclic-AMP and -GMP phosphodiesterase 11A, cGMP-specific 3’,5’-cyclic phosphodiesterase.

Bioactivity

ChEMBL activities: 59 potent at pChembl ≥ 5 of 71 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PDE5A	8.92	IC50	1.2	nM	CHEMBL_ACT_12680565
PDE5A	8.92	IC50	1.2	nM	CHEMBL_ACT_18527307
PDE5A	8.92	IC50	1.2	nM	CHEMBL_ACT_19400629
PDE5A	8.92	IC50	1.2	nM	CHEMBL_ACT_19400632
PDE5A	8.89	IC50	1.3	nM	CHEMBL_ACT_556410
PDE5A	8.74	IC50	1.8	nM	CHEMBL_ACT_26335818
PDE5A	8.74	IC50	1.8	nM	CHEMBL_ACT_29311697
PDE5A	8.72	Kd	1.9	nM	CHEMBL_ACT_26335820
PDE5A	8.63	IC50	2.35	nM	CHEMBL_ACT_19231667
PDE5A	8.62	Kd	2.4	nM	CHEMBL_ACT_26335819
PDE5A	8.52	IC50	3	nM	CHEMBL_ACT_5187584
PDE5A	8.5	IC50	3.16	nM	CHEMBL_ACT_18528108
Q28156	8.48	IC50	3.3	nM	CHEMBL_ACT_2014651
PDE5A	8.4	IC50	4	nM	CHEMBL_ACT_1520620
PDE5A	8.4	IC50	4	nM	CHEMBL_ACT_19043576
PDE5A	8.4	IC50	4	nM	CHEMBL_ACT_26105958
PDE5A	8.4	IC50	4	nM	CHEMBL_ACT_29231320
PDE5A	8.4	IC50	4	nM	CHEMBL_ACT_3270094
PDE5A	8.33	IC50	4.67	nM	CHEMBL_ACT_18771482
Q28156	8.3	IC50	5	nM	CHEMBL_ACT_10873854
O54735	8.3	Ki	5	nM	CHEMBL_ACT_1400255
PDE5A	8.3	IC50	5	nM	CHEMBL_ACT_20668220
PDE5A	8.3	IC50	5.01	nM	CHEMBL_ACT_2566973
Q28156	8.3	IC50	5	nM	CHEMBL_ACT_602016
Q28156	8.3	IC50	5	nM	CHEMBL_ACT_628345
PDE5A	8.28	Ki	5.2	nM	CHEMBL_ACT_18771537
PDE5A	8.17	IC50	6.7	nM	CHEMBL_ACT_331695
PDE5A	8.15	IC50	7	nM	CHEMBL_ACT_24983026
PDE5A	8.03	IC50	9.4	nM	CHEMBL_ACT_16755422
PDE5A	8.03	IC50	9.4	nM	CHEMBL_ACT_18549361
PDE11A	8	IC50	10	nM	CHEMBL_ACT_12680556
PDE5A	8	Ki	10	nM	CHEMBL_ACT_1506647
Q28156	7.92	IC50	12	nM	CHEMBL_ACT_2591379
Q28156	7.92	IC50	12	nM	CHEMBL_ACT_3079191
PDE11A	7.7	IC50	20	nM	CHEMBL_ACT_29245858
PDE11A	7.66	IC50	22.1	nM	CHEMBL_ACT_19231729
PDE11A	7.6	IC50	25	nM	CHEMBL_ACT_25725000
PDE11A	7.48	IC50	33	nM	CHEMBL_ACT_1520513
PDE11A	7.43	IC50	37	nM	CHEMBL_ACT_331697
PDE11A	7.33	IC50	47	nM	CHEMBL_ACT_18771739
PDE11A	7.3	IC50	50	nM	CHEMBL_ACT_5187604
PDE11A	7.16	IC50	70	nM	CHEMBL_ACT_25724929
O54735	7.11	EC50	78	nM	CHEMBL_ACT_18771782
PDE11A	6.54	IC50	290	nM	CHEMBL_ACT_2591380
PDE11A	6.54	IC50	290	nM	CHEMBL_ACT_3079193
PDE11A	6.52	IC50	300	nM	CHEMBL_ACT_5187600
PDE6C	6.4	IC50	402	nM	CHEMBL_ACT_19231714
PDE6D	6.01	IC50	980	nM	CHEMBL_ACT_1520621
NR1I2	5.99	AC50	1030	nM	CHEMBL_ACT_25187974
PDE6D	5.9	IC50	1260	nM	CHEMBL_ACT_331696
PDE6D	5.7	IC50	2000	nM	CHEMBL_ACT_1506648
P11541	5.52	IC50	3000	nM	CHEMBL_ACT_3079192
MAPK1	5.4	Potency	3981	nM	CHEMBL_ACT_4701476
NR2E1	5.3	EC50	5000	nM	CHEMBL_ACT_24354775
P04972	5.29	IC50	5100	nM	CHEMBL_ACT_628355
PDE6D	5.28	IC50	5200	nM	CHEMBL_ACT_12680561
PDE6D	5.28	IC50	5200	nM	CHEMBL_ACT_24776148
PDE5A	5.24	EC50	5810	nM	CHEMBL_ACT_23143820
PDE4A	5.04	IC50	9200	nM	CHEMBL_ACT_12680562

Target pathways

Aggregated over 2 target gene(s): PDE5A, PDE11A.

Top Reactome pathways

4 total, by targets touching each:

Pathway	Targets	Genes
cGMP effects	2	PDE11A, PDE5A
G alpha (s) signalling events	1	PDE11A
Smooth Muscle Contraction	1	PDE5A
RHOBTB1 GTPase cycle	1	PDE5A

Dominant GO biological processes

GO term	Targets
signal transduction	2
negative regulation of cAMP/PKA signal transduction	2
cGMP catabolic process	1
negative regulation of receptor guanylyl cyclase signaling pathway	1

Indications & clinical

Indications

4 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
benign prostatic hyperplasia	4	MONDO:0010811	EFO:0000284
erectile dysfunction	4	MONDO:0005362	EFO:0004234
pulmonary arterial hypertension	4	MONDO:0015924	EFO:0001361
pulmonary hypertension	4	MONDO:0005149	MONDO:0005149

30 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
interstitial lung disease	3	MONDO:0015925	EFO:0004244
Raynaud disease	3	MONDO:0008364	EFO:1001145
congenital heart disease	3	MONDO:0005453	HP:0030680
glucose intolerance	3	MONDO:0001076	HP:0001952
transposition of the great arteries	3	MONDO:0000153	MONDO:0000153
Duchenne muscular dystrophy	3	MONDO:0010679	MONDO:0010679
premature ejaculation	3	MONDO:0001780	EFO:0803321
systemic sclerosis	2	MONDO:0005100	EFO:0000717
head and neck squamous cell carcinoma	2	MONDO:0010150	EFO:0000181
hypertensive disorder	2	MONDO:0005044	EFO:0000537
obesity disorder	2	MONDO:0011122	EFO:0001073
gastroparesis	2	MONDO:0006769	EFO:1000948
stroke disorder	2	MONDO:0005098	EFO:0000712
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
Cushing syndrome	2	MONDO:0018912	EFO:0003099
vascular dementia	2	MONDO:0004648	EFO:0004718
Eisenmenger syndrome	2	MONDO:0019944	EFO:0009200
priapism	2	MONDO:0004745	HP:0200023
non-small cell lung carcinoma	2	MONDO:0005233	EFO:0003060
exocrine pancreatic carcinoma	2	MONDO:0005192	EFO:0002618
physiological sexual disorder	2	MONDO:0002134	EFO:0004714
essential hypertension	2	MONDO:0001134	MONDO:0001134
type 2 diabetes mellitus	2	MONDO:0005148	MONDO:0005148
congestive heart failure	1	MONDO:0005009	EFO:0000373
neoplasm	1	MONDO:0005070	EFO:0000616
upper aerodigestive tract neoplasm	1	MONDO:0005398	EFO:0004284
glioblastoma	1	MONDO:0018177	EFO:0000519
anaplastic astrocytoma	1	MONDO:0016684	EFO:0002499
major depressive disorder	1	MONDO:0002009	MONDO:0002009
head and neck cancer	1	MONDO:0005627	EFO:0006859

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 210.

Phase distribution

Phase	Trials
PHASE3	50
PHASE4	49
PHASE2	41
Not specified	30
PHASE1	26
PHASE2/PHASE3	6
EARLY_PHASE1	5
PHASE1/PHASE2	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05051436	PHASE4	RECRUITING	The Effects of Mirabegron and Tadalafil on Glucose Tolerance in Prediabetics
NCT07416968	PHASE4	RECRUITING	Randomized Controlled Trial Comparing Low Dose Tadalafil Versus Solifenacin For Management of Overactive Bladder in Women: Multicenter Egyptian National Study
NCT07499804	PHASE4	RECRUITING	Effect of Tadalafil on Endometrial Thickness and Frozen Embryo Transfer Outcomes
NCT00333281	PHASE4	COMPLETED	A Study of Visual Effects of Erectile Dysfunction Medications Dosed Daily for Six Months
NCT00382135	PHASE4	COMPLETED	A Study of Semen Characteristics After 9 Months of Daily Tadalafil 20 mg
NCT00422578	PHASE4	COMPLETED	Effect of Tadalafil on the Quality of Life and Sexual Life in Erectile Dysfunction
NCT00547092	PHASE4	COMPLETED	Study For Which Treatment, Tadalafil or Sildenafil, is Preferred For Problems Getting or Maintaining an Erection
NCT00547352	PHASE4	COMPLETED	Study to Determine a Preference Between Sildenafil or Tadalafil Treatment for Problems Getting an Erection
NCT00547599	PHASE4	COMPLETED	Determine If the Stress That Comes With Not Developing an Erection Affects Tadalafil Effects
NCT00617305	PHASE4	COMPLETED	Study of Add-on Ambrisentan Therapy to Background Phosphodiesterase Type-5 Inhibitor (PDE5i) Therapy in Pulmonary Arterial Hypertension (ATHENA-1)
NCT00644956	PHASE4	COMPLETED	A Randomized, Open-Label, Crossover, Multicenter, Single Dose Comparator Study Evaluating Onset Of Penile Rigidity In Men With Erectile Dysfunction Who Are Treated With Sildenafil And Tadalafil
NCT00663130	PHASE4	COMPLETED	Evaluating the Efficacy Vardenafil 10 mg vs Tadalafil 10 mg in in Subjects With Erectile Dysfunction (ED)
NCT00705588	PHASE4	UNKNOWN	Long Acting Phosphodiesterase 5 Inhibitors as Add-on Therapy for Patients With Pulmonary Hypertension Treated With Prostanoids.
NCT00833638	PHASE4	COMPLETED	A Study in Erectile Dysfunction
NCT01026818	PHASE4	COMPLETED	A Study of Tadalafil After Radical Prostatectomy
NCT01042158	PHASE4	COMPLETED	A Clinical Trial of Ambrisentan and Tadalafil in Pulmonary Arterial Hypertension Associated With Systemic Sclerosis
NCT01067391	PHASE4	COMPLETED	Effect of Tadalafil (Cialis) on the Cardiovascular System of Spinal Cord Injury (SCI) Males
NCT01070511	PHASE4	COMPLETED	Tadalafil in Becker Muscular Dystrophy
NCT01122264	PHASE4	COMPLETED	A Study in Patients With Erectile Dysfunction
NCT01130532	PHASE4	COMPLETED	A Study in Erectile Dysfunction
NCT01272388	PHASE4	TERMINATED	Aortic Stenosis and PhosphodiEsterase iNhibition With Aortic Valve Replacement (ASPEN-AVR): A Pilot Study
NCT01275339	PHASE4	TERMINATED	Aortic Stenosis and PhosphodiEsterase Type 5 iNhibition (ASPEN): A Pilot Study
NCT01302444	PHASE4	TERMINATED	Treprostinil Combined With Tadalafil for Pulmonary Hypertension
NCT01305252	PHASE4	COMPLETED	A 48-week Study of the Effect of Dual Therapy (Inhaled Treprostinil and Tadafafil) Versus Monotherapy (Tadalafil).
NCT01326117	PHASE4	WITHDRAWN	Daily Tadalafil and Gastric Emptying Time in Diabetic Gastroparesis
NCT01352507	PHASE4	COMPLETED	A Study of Tadalafil and Sildenafil in Men With Erectile Dysfunction in China
NCT01364701	PHASE4	UNKNOWN	Evaluation of Safety and Effectiveness of 2 Lower Dose Combined PDE5i’s Versus Single Maximal Dose PDE5i Treatment
NCT01803828	PHASE4	COMPLETED	REmodelling in Diabetic CardiOmapathy: Gender Response to PDE5i InhibiTOrs
NCT02224846	PHASE4	COMPLETED	A Study of Tadalafil (LY450190) in Chinese Men With Erectile Dysfunction
NCT02225548	PHASE4	UNKNOWN	Sagene 2014 - Parkinson’s Disease and Erectile Dysfunction
NCT02252367	PHASE4	COMPLETED	Effect of 12 Weeks Treatment With Tadalafil vs Placebo on Lower Urinary Tract Symptoms
NCT02431754	PHASE4	COMPLETED	A Study of Tadalafil (LY450190) in Participants With Lower Urinary Tract Symptoms (LUTS) Suggestive of Benign Prostatic Hyperplasia LUTS (BPH-LUTS).
NCT02554045	PHASE4	COMPLETED	Daily Tadalafil on Body Fat and Lean Mass
NCT02595684	PHASE4	COMPLETED	Effect of Tadalafil on Insulin Secretion and Insulin Sensitivity in Obese Men.
NCT02891850	PHASE4	COMPLETED	Riociguat rEplacing PDE-5i Therapy evaLuated Against Continued PDE-5i thErapy
NCT02943356	PHASE4	UNKNOWN	Effect of Tadalafil on Erectile Dysfunction Treatment and QOL Improvement Effect (by SF-12) in Andropause Patients With Erectile Dysfunction
NCT02968901	PHASE4	TERMINATED	Clinical Study Evaluating the Effects of First-line Oral cOmbination theraPy of maciTentan and tadalafIl in Patients With Newly Diagnosed pulMonary Arterial Hypertension (OPTIMA)
NCT03229889	PHASE4	COMPLETED	Trial of Tadalafil, Tamsulosin and Combination for Access Sheath Deployment
NCT03309592	PHASE4	WITHDRAWN	Efficacy and Safety of Combination Ambrisentan and Tadalafil in Patients With Portopulmonary Hypertension
NCT04946162	PHASE4	WITHDRAWN	The Use of Tadalafil in Confirmed COVID-19 Pneumonia.
NCT05446493	PHASE4	COMPLETED	Serum YKL-40 Level and Platelets Indices Among Patients With Diabetic Erectile Dysfunction
NCT05494567	PHASE4	UNKNOWN	Efficacy of Tadalafil/Solifenacin VS Tamsulosin/Solifenacin Combination Therapy for BPH/OAB
NCT05537272	PHASE4	UNKNOWN	The Efficacy of Tamsulosin and Tadalafil Compared to Placebo in the Treatment and Prevention of Urinary Disorders After Transperineal Prostate Biopsy
NCT05818670	PHASE4	COMPLETED	Comparison Between Tamsulosin and Tadalafil in Management of Benign Prostatic Hyperplasia Long Term Study
NCT06809205	PHASE4	COMPLETED	Efficacy and Safety of Tadalafil, Tamsulosin, and Their Combinations in Treating Lower Urinary Tract Symptoms in BPH Patients With Prostate Volumes ≤ 40 ml: A Prospective Comparative Study
NCT06947265	PHASE4	COMPLETED	Safety And Efficacy Of L-Arginine Monotherapy Versus Tadalafil Monotherapy Versus Their Combination In Men With Erectile Dysfunction; A Prospective Randomized Study
NCT07563647	PHASE4	COMPLETED	Association Between Diastolic Dysfunction and Erectile Dysfunction and the Effect of Tadalafil and SGLT2 Inhibitors on Them in Men With Metabolic Syndrome
NCT07574268	PHASE4	COMPLETED	Efficacy of Transcutaneous Electrical Neural Stimulation and Tadalafil in Men With Erectile Dysfunction: A Randomized, Double-Blind, Bi-centric, Placebo- and Sham-Controlled Trial
NCT07602608	PHASE4	COMPLETED	Platelet-Rich Plasma With or Without Tadalafil for Erectile Dysfunction
NCT05052879	PHASE3	NOT_YET_RECRUITING	Efficacy and Safety of Toronto Association in the Treatment of Erectile Dysfunction and Premature Ejaculation
NCT05195775	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	Tadalafil as Adjuvant Therapy for DMD
NCT05206955	PHASE3	RECRUITING	Study of Tadalafil vs. Placebo for Improving Hemodynamics and End-Organ Dysfunction in Fontan Physiology
NCT05844462	PHASE3	RECRUITING	Tadalafil for Severe Pulmonary Hypertension Due to Chronic Obstructive Pulmonary Disease
NCT06520839	PHASE3	RECRUITING	Genetic Factors of Erectile Dysfunction Degree and Response to Tadalafil Treatment in Patients With Diabetes
NCT06583590	PHASE2/PHASE3	RECRUITING	Evaluation of Efficacy of Botulinum Toxin A Plus Oral Tadalafil 5 mg in Diabetic Men With Erectile Dysfunction
NCT07177326	PHASE3	NOT_YET_RECRUITING	Combination Therapy of Tadalafil 2.5mg Plus Sildenafil 25mg Versus Tadalafil 5 mg Monotherapy for Treatment of Erectile Dysfunction: A Randomized, Placebo-Controlled Double-Blinded Cross-Over Study
NCT07245680	PHASE3	RECRUITING	COMMODITIES Trial: Initial Dual Oral Therapy vs Monotherapy in PAH With Cardiovascular Comorbidities
NCT00122499	PHASE3	COMPLETED	A Study to Assess the Efficacy of Tadalafil to Treat Erectile Dysfunction After Radiotherapy of Prostate Cancer
NCT00125918	PHASE3	COMPLETED	PHIRST-1: Tadalafil in the Treatment of Pulmonary Arterial Hypertension
NCT00215631	PHASE3	TERMINATED	Can Tadalafil Maintain Erectile Function In Patients Treated With Radiotherapy For Prostate Cancer?
NCT00381732	PHASE3	COMPLETED	A Study to Evaluate the Efficacy and Safety of 2.5mg and 5mg Tadalafil Given Once a Day to Men With Erectile Dysfunction
NCT00384930	PHASE2/PHASE3	COMPLETED	Study of Tadalafil Once-a Day for 12 Weeks in Men With Signs and Symptoms of Benign Prostatic Hyperplasia
NCT00421083	PHASE3	COMPLETED	Efficacy and Safety of Tadalafil in Subjects With Erectile Dysfunction Caused by Spinal Cord Injury
NCT00422734	PHASE3	COMPLETED	Tadalafil Taken Daily Compared to Placebo on Improvement of Getting and Maintaining an Erection and Sexual Quality of Life
NCT00547183	PHASE3	COMPLETED	Study the Safety and Effectiveness of Tadalafil in Men With Diabetes Who Have Problems Getting and Keeping an Erection
NCT00547287	PHASE3	COMPLETED	Studying the Preference of Tadalafil to Sildenafil in Men With Problems Getting an Erection Across Nations
NCT00547417	PHASE3	COMPLETED	To Determine Effect and Safety of Tadalafil Taken by Men of Different Races and With Different Diseases When Needed for Erections
NCT00547495	PHASE3	COMPLETED	Study the Safety and Effectiveness of Tadalafil in Men With Problems Getting or Maintaining an Erection When Taken Prior to Desiring an Erection
NCT00547508	PHASE3	COMPLETED	To Determine How Different Doses of Tadalafil Work on Getting and Keeping an Erection 26 or 36 Hours After Taking
NCT00547573	PHASE3	COMPLETED	Determine Safety and Effectiveness of Tadalafil in Asian Men When Taken as Needed for Getting and Keeping an Erection
NCT00549302	PHASE3	COMPLETED	Study the Safety and Effectiveness of Tadalafil on High Blood Pressure in the Blood Vessel Going From the Heart to the Lungs
NCT00626665	PHASE3	COMPLETED	Randomised Control Trial to Assess the Efficacy of Tadalafil in Raynaud’s Phenomenon in Scleroderma
NCT00668109	PHASE3	COMPLETED	Assessment of Efficacy of Vardenafil in Subjects With Erectile Dysfunction and Diabetes, Hypertension or Hyperlipidemia
NCT00827242	PHASE3	COMPLETED	Study to Treat Patients Who Have Signs and Symptoms of Benign Prostatic Hyperplasia (BPH) With Tadalafil Daily
NCT00836693	PHASE3	COMPLETED	Effect of Tadalafil Once a Day in Men With Erectile Dysfunction
NCT00848081	PHASE3	COMPLETED	A Study of Tadalafil in Men With Benign Prostatic Hyperplasia Symptoms Who Are Being Treated With Alpha Blockers
NCT00855582	PHASE3	COMPLETED	A Study in the Treatment of Erectile Dysfunction and Benign Prostate Hyperplasia
NCT00861757	PHASE3	COMPLETED	Multinational Study to Evaluate Tadalafil in Asian Men With Signs and Symptoms of Benign Prostatic Hyperplasia
NCT00931528	PHASE3	COMPLETED	Tadalafil in Preventing Erectile Dysfunction in Patients With Prostate Cancer Treated With Radiation Therapy
NCT00970632	PHASE3	COMPLETED	A Study of Tadalafil in Men With Benign Prostatic Hyperplasia
NCT01117298	PHASE3	COMPLETED	A Randomized Control Trial to Assess the Efficacy of Tadalafil in Raynaud’s Phenomenon in Scleroderma
NCT01139762	PHASE3	COMPLETED	A Study of Tadalafil Use With Finasteride in Men With Enlarged Prostates and Urinary Symptoms
NCT01152190	PHASE3	COMPLETED	A Study in Benign Prostatic Hyperplasia
NCT01178073	PHASE3	COMPLETED	A Study of First-Line Ambrisentan and Tadalafil Combination Therapy in Subjects With Pulmonary Arterial Hypertension (PAH)
NCT01324999	PHASE2/PHASE3	COMPLETED	Tadalafil for Sarcoidosis Associated Pulmonary Hypertension
NCT01444651	PHASE3	COMPLETED	A Trial of Tadalafil and Glycemic Traits
NCT01460342	PHASE3	COMPLETED	Phase 3 Study of Tadalafil Once-Daily in Asian Men With Benign Prostatic Hyperplasia (BPH)
NCT01553981	PHASE3	COMPLETED	A Trial of Tadalafil in Interstitial Lung Disease of Scleroderma
NCT01824290	PHASE3	COMPLETED	A Study of Tadalafil in Pediatric Participants With Pulmonary Arterial Hypertension (PAH)
NCT01865084	PHASE3	TERMINATED	A Study of Tadalafil for Duchenne Muscular Dystrophy
NCT01910389	PHASE3	TERMINATED	Phosphodiesterase Type 5 Inhibition With Tadalafil Changes Outcomes in Heart Failure
NCT01937871	PHASE3	COMPLETED	A Study of Tadalafil in Men With Benign Prostatic Hyperplasia (BPH) and Erectile Dysfunction (ED)
NCT01960153	PHASE3	WITHDRAWN	Phosphodiesterase Type 5 Inhibition With Tadalafil Changes Outcomes in Heart Failure: Extent of Renal Damage
NCT02558231	PHASE3	COMPLETED	The Efficacy and Safety of Initial Triple Versus Initial Dual Oral Combination Therapy in Patients With Newly Diagnosed Pulmonary Arterial Hypertension
NCT02862483	PHASE3	UNKNOWN	The Efficacy and Safety of the Combination of Tamsulosin and Tadalafil in Men With Lower Urinary Tract Symptoms Due to Benign Prostatic Hyperplasia and Erectile Dysfunction
NCT03049540	PHASE3	COMPLETED	Effect of Phosphodiesterase-5 Inhibition With Tadalafil on SystEmic Right VEntricular Size and Function
NCT03246880	PHASE3	COMPLETED	Clinical Trial To Evaluate the Efficacy and Safety of CKD-397 in Benign Prostatic Hyperplasia Patients
NCT03904693	PHASE3	COMPLETED	Clinical Study to Compare the Efficacy and Safety of Macitentan and Tadalafil Monotherapies With the Corresponding Fixed-dose Combination Therapy in Subjects With Pulmonary Arterial Hypertension (PAH)
NCT03905018	PHASE3	UNKNOWN	Effect of Tadalafil Administration on Vasodilatation Mediated by Flow in Patients With Obesity Grade I-II
NCT04361305	PHASE3	UNKNOWN	Observational Study of Pharmacological Treatment for Premature Ejaculation Concurrent With Erectile Dysfunction

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

27 molecules share ≥1 primary target. Top 27 by shared-target count:

Molecule	Source	Status	Shared targets
DIPYRIDAMOLE	ChEMBL + PubChem	Phase 4 (approved)	PDE11A, PDE5A
SILDENAFIL	ChEMBL + PubChem	Phase 4 (approved)	PDE11A, PDE5A
VARDENAFIL	ChEMBL + PubChem	Phase 4 (approved)	PDE11A, PDE5A
ZAPRINAST	ChEMBL	Phase 2	PDE11A, PDE5A
AVANAFIL	ChEMBL	Phase 4 (approved)	PDE5A
CELECOXIB	ChEMBL	Phase 4 (approved)	PDE5A
DONEPEZIL	ChEMBL	Phase 4 (approved)	PDE5A
IBUDILAST	ChEMBL	Phase 4 (approved)	PDE5A
MILRINONE	ChEMBL	Phase 4 (approved)	PDE5A
PALBOCICLIB	ChEMBL	Phase 4 (approved)	PDE5A
TANNIC ACID	ChEMBL	Phase 4 (approved)	PDE5A
ICARIIN	ChEMBL	Phase 3	PDE5A
ICARITIN	ChEMBL	Phase 3	PDE5A
PAPAVERINE	ChEMBL	Phase 3	PDE5A
UDENAFIL	ChEMBL	Phase 3	PDE5A
CARTAZOLATE	ChEMBL	Phase 2	PDE5A
CILOSTAMIDE	ChEMBL	Phase 2	PDE5A
CIPAMFYLLINE	ChEMBL	Phase 2	PDE5A
GISADENAFIL	ChEMBL	Phase 2	PDE5A
ISOMAZOLE	ChEMBL	Phase 2	PDE5A
MIRODENAFIL	ChEMBL	Phase 2	PDE5A
PF-00489791	ChEMBL	Phase 2	PDE5A
PF-03049423	ChEMBL	Phase 2	PDE5A
ROLIPRAM	ChEMBL	Phase 2	PDE5A
SULMAZOLE	ChEMBL	Phase 2	PDE5A
Crisaborole	PubChem	Approved	PDE11A
Roflumilast	PubChem	Approved	PDE11A