Udenafil

Summary

Udenafil (CHEMBL2103849) is a phase-3 clinical-stage small molecule (ATC G04BE11) targeting PDE5A; indicated across 9 conditions including erectile dysfunction and pulmonary arterial hypertension.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• ATC class: G04BE11
• Targets: 1 (PDE5A)
• Indications: 9 conditions
• Clinical trials: 31
• Chemistry: 516.7 Da · C25H36N6O4S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2103849
Name	Udenafil
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	135413547
ATC	G04BE11
Molecular formula	C25H36N6O4S
Molecular weight	516.7
InChIKey	IYFNEFQTYQPVOC-UHFFFAOYSA-N

SMILES: CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)NCCC4CCCN4C)OCCC)C

IUPAC name: 3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,5-d]pyrimidin-5-yl)-N-[2-(1-methylpyrrolidin-2-yl)ethyl]-4-propoxybenzenesulfonamide

Also known as: DA-8159, Udenafil, Udenafilo, Zydena, UDENAFIL

Patent coverage: 283 distinct patent families (962 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 876 (91%) 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	8.08	0%	O76074

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: cGMP-specific 3’,5’-cyclic phosphodiesterase.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
PDE5A	8.08	IC50	8.25	nM	CHEMBL_ACT_24872434

Target pathways

Aggregated over 1 target gene(s): PDE5A.

Top Reactome pathways

3 total, by targets touching each:

Pathway	Targets	Genes
cGMP effects	1	PDE5A
Smooth Muscle Contraction	1	PDE5A
RHOBTB1 GTPase cycle	1	PDE5A

Dominant GO biological processes

GO term	Targets
signal transduction	1
cGMP catabolic process	1
negative regulation of cAMP/PKA signal transduction	1

Indications & clinical

Indications

9 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
erectile dysfunction	3	MONDO:0005362	EFO:0004234
pulmonary arterial hypertension	3	MONDO:0015924	EFO:0001361
diastolic heart failure	3	MONDO:0006727	EFO:1000899
heart disorder	3	MONDO:0005267	EFO:0003777
systolic heart failure	3	MONDO:0006993	EFO:1001207
Alzheimer disease	3	MONDO:0004975	MONDO:0004975
vascular dementia	2	MONDO:0004648	EFO:0004718
Raynaud disease	2	MONDO:0008364	EFO:1001145
liver disorder	1	MONDO:0005154	EFO:0001421

Clinical trials

Total trials: 31.

Phase distribution

Phase	Trials
PHASE3	14
PHASE1	7
PHASE2	5
PHASE4	3
PHASE2/PHASE3	1
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01421940	PHASE4	COMPLETED	The Efficacy of Penile Rehabilitation Using Udenafil After Total Mesorectal Excision of Rectal Cancer
NCT01769482	PHASE4	UNKNOWN	Understanding of Chest Pain in Microvascular Disease Proved by Cardiac Magnetic Resonance Image
NCT03142542	PHASE4	UNKNOWN	The Efficacy and Safety of Udenafil in Patients With Erectile Dysfunction After Bilateral Nerve-sparing Radical Prostatectomy
NCT05918211	PHASE3	RECRUITING	Fontan Udenafil Exercise Longitudinal Assessment Trial - 2
NCT01037218	PHASE3	COMPLETED	Treatment of Erectile Dysfunction II
NCT01037244	PHASE3	COMPLETED	Treatment of Erectile Dysfunction I
NCT01065012	PHASE3	COMPLETED	Treatment of Erectile Dysfunction - Long Term Safety and Efficacy
NCT01305083	PHASE3	COMPLETED	Efficacy and Safety Study of Udenafil Tablets in Erectile Dysfunction.
NCT01364181	PHASE3	COMPLETED	The Impact of Udenafil on Exercise Capacity in Severe Chronic Obstructive Pulmonary Disease (COPD) Patients
NCT01599117	PHASE3	UNKNOWN	A Randomized Trial of Udenafil Therapy in Patients With Heart Failure With Preserved Ejection Fraction [ULTIMATE-HFpEF]
NCT01646515	PHASE3	TERMINATED	Udenafil Therapy to Improve Symptomatology, Exercise Tolerance and Hemodynamics in Patients With Chronic Systolic Heart Failure
NCT01696240	PHASE3	UNKNOWN	A Randomized Trial of Udenafil Therapy in Patients With Mild Pulmonary Hypertension [ULTIMATE-Mild PHT]
NCT01774864	PHASE3	COMPLETED	Efficacy and Safety Study of Udenafil to Treat Erectile Dysfunction
NCT01901640	PHASE3	COMPLETED	Safety Study of Once-a-Day Dosing of Udenafil to Treat Erectile Dysfunction
NCT02304198	PHASE2/PHASE3	COMPLETED	Clinical Trial to Evaluate the Long-term Safety of Udenafil in Patient With PAH
NCT02741115	PHASE3	COMPLETED	Fontan Udenafil Exercise Longitudinal Assessment Trial
NCT03013751	PHASE3	COMPLETED	A Extension Study of Udenafil in Adolescents
NCT03430583	PHASE3	COMPLETED	Evaluation of Fontan-associated Hepatic Stiffness and the Efficacy of Udenafil in Reducing Liver Stiffness
NCT00282607	PHASE2	COMPLETED	A Study of DA-8159 in Subjects With Erectile Dysfunction
NCT00607282	PHASE2	COMPLETED	Efficacy of Udenafil After Radical Resection for Sigmoid Colon and Rectal Cancer
NCT01466543	PHASE2	UNKNOWN	Effect of Zydena (Udenafil) on Cerebral Blood Flow and Peripheral Blood Viscosity
NCT01553721	PHASE2	COMPLETED	Efficacy and Safety Study of Udenafil in Patient With Pulmonary Arterial Hypertension(PAH)
NCT01967251	PHASE2	WITHDRAWN	Efficacy, Safety and Dose-response of Udenafil in Patients With Benign Prostatic Hyperplasia and Erectile Dysfunction
NCT02201342	PHASE1/PHASE2	COMPLETED	Pharmacokinetic/Pharmacodynamic Study of Udenafil in Adolescents
NCT00956306	PHASE1	COMPLETED	A Pharmacokinetic Study of Udenafil in Adult Subjects With or Without Impaired Hepatic Function
NCT01230541	PHASE1	COMPLETED	Effect of Udenafil on Spermatogenesis
NCT01231997	PHASE1	COMPLETED	Clinical Study to Investigate the Safety and Pharmacokinetics of Udenafil Tablet in Renal Impaired Male Patients
NCT01241032	PHASE1	COMPLETED	Phase I Study to Investigate the Alcohol Interaction of DA8159
NCT01928563	PHASE1	UNKNOWN	Clinical Trial to Investigate the Pharmacokinetic Drug Interaction Between Udenafil and Dapoxetine
NCT01929213	PHASE1	UNKNOWN	Clinical Trial to Investigate the Pharmacokinetic Drug Interaction Between Udenafil and Bosentan After Oral Administration
NCT01967264	PHASE1	COMPLETED	Safety and Pharmacokinetic Profile of Udenafil in Healthy Mexican Adults

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

25 molecules share ≥1 primary target. Top 25 by shared-target count:

Molecule	Source	Status	Shared targets
SILDENAFIL	ChEMBL + PubChem	Phase 4 (approved)	PDE5A
TADALAFIL	ChEMBL + PubChem	Phase 4 (approved)	PDE5A
VARDENAFIL	ChEMBL + PubChem	Phase 4 (approved)	PDE5A
AVANAFIL	ChEMBL	Phase 4 (approved)	PDE5A
CELECOXIB	ChEMBL	Phase 4 (approved)	PDE5A
DIPYRIDAMOLE	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
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
ZAPRINAST	ChEMBL	Phase 2	PDE5A