Alfuzosin

drug
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Also known as AlfuzosinaAlfuzosineNSC-760065SID26719847SID26749009SID90341616SID26749010SID50107503SID50107504ALFUSOZINESID174007387UroxatralC0164756

Summary

Alfuzosin (CHEMBL709) is an approved small-molecule antineoplastic agent (ATC G04CA01) targeting ADRA1A, ADRA1B, and ADRA1D; indicated across 7 conditions including benign prostatic hyperplasia and prostatitis.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: G04CA01
  • Targets: 3 (ADRA1A, ADRA1B, ADRA1D)
  • Indications: 7 conditions
  • Clinical trials: 34
  • Chemistry: 389.4 Da · C19H27N5O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL709
NameAlfuzosin
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID2092
ChEBICHEBI:51141
ATCG04CA01
Molecular formulaC19H27N5O4
Molecular weight389.4
InChIKeyWNMJYKCGWZFFKR-UHFFFAOYSA-N

SMILES: CN(CCCNC(=O)C1CCCO1)C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC

IUPAC name: N-[3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]propyl]oxolane-2-carboxamide

Pharmacological roles (ChEBI): antineoplastic agent, antihypertensive agent, α-adrenergic antagonist.

Also known as: Alfuzosin, Alfuzosina, Alfuzosine, NSC-760065, SID26719847, SID26749009, SID90341616, SID26749010, SID50107503, SID50107504, alfuzosin, ALFUSOZINE

Parent form; salt/anhydrous children: CHEMBL1723

Patent coverage: 1,924 distinct patent families (6,601 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 6,547 (99%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
ADRA1Aα1A-adrenoceptorAntagonist8.1P35348
ADRA1Bα1B-adrenoceptorAntagonist8.60%P35368
ADRA1Dα1D-adrenoceptorAntagonist8.40.2%P25100

Broader ChEMBL bioactivity targets: 22 (assay-derived). Sample: Lysine-specific demethylase 4E, 15-hydroxyprostaglandin dehydrogenase [NAD(+)], Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Alpha-2B adrenergic receptor, Adrenergic receptor alpha-1, Acetylcholinesterase, Sodium-dependent noradrenaline transporter, Alpha-1D adrenergic receptor, Alpha-1A adrenergic receptor, Alpha-1B adrenergic receptor, D(3) dopamine receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Alpha-galactosidase A, Lysosomal alpha-glucosidase, Alpha-1B adrenergic receptor, Alpha-1A adrenergic receptor, Alpha-1D adrenergic receptor, Aldehyde dehydrogenase 1A1, 3-hydroxyacyl-CoA dehydrogenase type-2.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 36 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ADRA1B8.55Ki2.8nMCHEMBL_ACT_323086
ADRA1D8.5Ki3.16nMCHEMBL_ACT_300803
P239448.46Ki3.5nMCHEMBL_ACT_323085
ADRA1D8.44Ki3.6nMCHEMBL_ACT_323084
P158238.31Kd4.9nMCHEMBL_ACT_860949
ADRA1A8.09Ki8.2nMCHEMBL_ACT_323088
ADRA1A8Ki10nMCHEMBL_ACT_300801
ADRA1B8Ki10nMCHEMBL_ACT_300802
ADRA1B7.92Ki12nMCHEMBL_ACT_323087
ACHE7.75IC5018nMCHEMBL_ACT_18570057
ADRA1D7.64IC5023nMCHEMBL_ACT_24959137
P181307.64Ki23nMCHEMBL_ACT_323089
P431407.61Kd24.55nMCHEMBL_ACT_860948
ADRA1A7.42AC5038nMCHEMBL_ACT_25218096
ADRA1A7.1AC5079.7nMCHEMBL_ACT_25137951
ADRA1A6.66Kd218.8nMCHEMBL_ACT_860950
ADRA2C6.09AC50810nMCHEMBL_ACT_25147912
ADRA2A5.17AC506800nMCHEMBL_ACT_25219928
ADRA2B5.05AC508900nMCHEMBL_ACT_25143737

Target pathways

Aggregated over 3 target gene(s): ADRA1A, ADRA1B, ADRA1D.

Top Reactome pathways

9 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction3ADRA1A, ADRA1B, ADRA1D
Signaling by GPCR3ADRA1A, ADRA1B, ADRA1D
Class A/1 (Rhodopsin-like receptors)3ADRA1A, ADRA1B, ADRA1D
Amine ligand-binding receptors3ADRA1A, ADRA1B, ADRA1D
GPCR downstream signalling3ADRA1A, ADRA1B, ADRA1D
Adrenoceptors3ADRA1A, ADRA1B, ADRA1D
G alpha (q) signalling events3ADRA1A, ADRA1B, ADRA1D
G alpha (12/13) signalling events3ADRA1A, ADRA1B, ADRA1D
GPCR ligand binding3ADRA1A, ADRA1B, ADRA1D

Dominant GO biological processes

GO termTargets
signal transduction3
G protein-coupled receptor signaling pathway3
phospholipase C-activating G protein-coupled receptor signaling pathway3
positive regulation of cytosolic calcium ion concentration3
cell-cell signaling3
positive regulation of MAPK cascade3
adenylate cyclase-activating adrenergic receptor signaling pathway3
neuron-glial cell signaling3
adrenergic receptor signaling pathway3
positive regulation of cardiac muscle hypertrophy2
intracellular signal transduction2
positive regulation of vasoconstriction2
regulation of muscle contraction2
regulation of vasoconstriction2
regulation of cardiac muscle contraction2

Indications & clinical

Indications

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

IndicationPhaseMONDOEFO
benign prostatic hyperplasia4MONDO:0010811EFO:0000284

4 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)PhaseMONDOEFO
prostatitis3MONDO:0005280EFO:0003830
nephrolithiasis3MONDO:0008171EFO:0004253
constipation disorder2MONDO:0002203HP:0002019
multiple sclerosis2MONDO:0005301MONDO:0005301

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

Clinical trials

Total trials: 34.

Phase distribution

PhaseTrials
PHASE314
PHASE411
PHASE23
Not specified3
PHASE12
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00280605PHASE4COMPLETEDALF-ONE : ALFuzosin ONcE Daily
NCT00401661PHASE4COMPLETEDSexuality And Management of Benign Prostatic Hyperplasia With Alfuzosin
NCT00427882PHASE4COMPLETEDMale Sexual Health Questionnaire (MSHQ) - Sexual Function Study
NCT00451061PHASE4UNKNOWNThe Efficacy of Alpha-blockers for Expulsion of Distal Ureteral Stones
NCT00486785PHASE4COMPLETEDSAMBA: Sexuality And Management of Benign Prostatic Hyperplasia With Alfuzosin
NCT00542165PHASE4COMPLETEDMulticenter Prospective Study on the Changes of Sexual Function Following Treatment With Alfuzosin (Xatral XL®) in Patients With Benign Prostate Hypertrophy
NCT00575913PHASE4COMPLETEDAlfuzosin XL Lower Urinary Tract Symptoms Efficacy and Sexuality Study
NCT00637715PHASE4COMPLETEDOnce Daily Given Alfuzosin in the Treatment of BPH
NCT00696761PHASE4COMPLETEDThe Long Term Effects of Alfuzosin(Xatral XL) in Lower Urinary Tract Symptoms(LUTS)/BPH Patients
NCT00836823PHASE4COMPLETEDEvaluation of Symptom-specific Goal Achievement
NCT03144596PHASE4COMPLETEDThe Effects of α-adrenergic Receptor Antagonists on Choroid and Pupil
NCT00029822PHASE3COMPLETEDClinical Trial in Males With BPH (Enlarged Prostate)
NCT00064649PHASE3TERMINATEDMinimally Invasive Surgical Therapy for BPH
NCT00103402PHASE3COMPLETEDTrial to Compare Alfuzosin Versus Placebo in the Treatment of Chronic Prostatitis/Chronic Pelvic Pain Syndrome
NCT00290030PHASE3COMPLETEDALFAURUS : A DB Randomized Parallel Group Study of Alfuzosin 10mg OD vs Placebo in the Management of AUR in Patients With a 1st Episode Due to BPH
NCT00388271PHASE3WITHDRAWNUse of Alfuzosin in Stone Treatment With ESWL
NCT00399464PHASE3COMPLETEDEfficacy and Safety of SL77.0499-10 (Alfuzosin) Versus Placebo and Tamsulosin in Japanese Patients With Benign Prostatic Hyperplasia
NCT00453908PHASE3TERMINATEDAlfuzosin Versus Placebo in Acute Urinary Retention
NCT00454402PHASE3TERMINATEDALF-STONE: Alfuzosin in Uretheric Stones
NCT00540891PHASE3COMPLETEDThe Efficacy, Onset of Effect, and Safety of Alfuzosin Once Daily in the Treatment of Lower Urinary Tract Symptoms of Benign Prostatic Hyperplasia: A Randomized, Placebo-Controlled Trial Using an Acute International Prostate Score
NCT00549939PHASE3COMPLETEDAlfuzosin Treatment in Children and Adolescents With Neurogenic Urinary Bladder Dysfunction
NCT00576823PHASE3COMPLETEDAlfuzosin Treatment in Children and Adolescents With Hydronephrosis of Neuropathic Etiology
NCT00629720PHASE3COMPLETEDPharmacokinetics and Safety Study With Alfuzosin in Children and Adolescents With Elevated Detrusor Leak Point Pressure of Neuropathic Etiology
NCT00688948PHASE2/PHASE3TERMINATEDAlfuzosin for Voiding Dysfunction in Multiple Sclerosis (MS)
NCT00713739PHASE3UNKNOWNAlfuzosin for Medical Expulsion Therapy of Ureteral Stones
NCT00893113PHASE3COMPLETEDAn Efficacy Study to Evaluate Alfuzosin to Treat Men With Erectile Dysfunction and Mild Lower Urinary Tract Symptoms
NCT00336921PHASE2COMPLETEDAlfuzosin for Treating Acute Urinary Retention
NCT00679315PHASE2COMPLETEDEfficacy and Safety of Alfuzosin for the Treatment of Voiding Dysfunction in Female
NCT01834729PHASE2COMPLETEDEffects of Alpha-1 Antagonist, Stress and Relaxation on Anorectal Functions
NCT02266537PHASE1COMPLETEDStudy to Assess the Influence of Three Different α-antagonists and Placebo on the Extent of Weekly Phenylephrine-induced Mydriasis at Three Different Concentrations of Phenylephrine in Healthy Male Volunteers
NCT06316336PHASE1UNKNOWNMultiple Dose, Bioequivalence Study of Generic Alfuzosin Hydrochloride 10 mg Prolonged-release Tablets Under Fed Conditions
NCT00256399Not specifiedCOMPLETEDUroxatral in Men With Benign Prostate Hypertrophy (BPH) and Erectile Dysfunction (ED)
NCT00583258Not specifiedWITHDRAWNA Randomized Study of Whether Alfuzosin(Xatral) Helps in the Passage of Kidney Stones
NCT02977832Not specifiedCOMPLETEDClinical Results of Odyliresin (Iresine Celosia) in Symptomatic Benign Prostatic Hyperplasia

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.

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.

571 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
AMLODIPINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
APRACLONIDINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
ASENAPINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
ATENOLOLChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
AZELASTINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
BREXPIPRAZOLEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
BRIMONIDINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
BUSPIRONEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
CARIPRAZINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
CISAPRIDEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
CLONIDINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
CLOZAPINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
DEXMEDETOMIDINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
DOPAMINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
DOXAZOSINChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
EBASTINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
EPINEPHRINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
FENOLDOPAMChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
HALOPERIDOLChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
INDACATEROLChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
INDORAMINChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
ISOPROTERENOLChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
LABETALOLChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
MOXISYLYTEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
NAFTOPIDILChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
NEFAZODONEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
NOREPINEPHRINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
OLANZAPINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
OXYMETAZOLINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
PHENTOLAMINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
PRAZOSINChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
QUETIAPINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
RISPERIDONEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
SERTINDOLEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
SILODOSINChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
TAMSULOSINChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
TEGASERODChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
TERAZOSINChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
TERFENADINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
TOLAZOLINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
VERAPAMILChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
VILAZODONEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
XYLOMETAZOLINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
ZIPRASIDONEChEMBLPhase 4 (approved)ADRA1A, ADRA1B, ADRA1D
BUNAZOSINChEMBLPhase 3ADRA1A, ADRA1B, ADRA1D
IDAZOXANChEMBLPhase 3ADRA1A, ADRA1B, ADRA1D
LATREPIRDINEChEMBLPhase 3ADRA1A, ADRA1B, ADRA1D
MEDETOMIDINEChEMBLPhase 3ADRA1A, ADRA1B, ADRA1D
YOHIMBINEChEMBLPhase 3ADRA1A, ADRA1B, ADRA1D
ABANOQUILChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
CIRAZOLINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
DEXNIGULDIPINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
IPSAPIRONEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
MAZAPERTINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
NIGULDIPINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
PIPEROXANChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
PIZOTYLINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
SPIRAMIDEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
SPIROXATRINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
TASIPIMIDINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
UPIDOSINChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
ZOTEPINEChEMBLPhase 2ADRA1A, ADRA1B, ADRA1D
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRA1D
PRAMIPEXOLEChEMBL + PubChemPhase 4 (approved)ADRA1A, ADRA1D
AMITRIPTYLINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
AMOXAPINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
APOMORPHINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
ASTEMIZOLEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
BENZTROPINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
BROMOCRIPTINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
CARVEDILOLChEMBLPhase 4 (approved)ADRA1A, ADRA1D
CHLORPROMAZINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
CINNARIZINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
CITALOPRAMChEMBLPhase 4 (approved)ADRA1A, ADRA1D
CLEMASTINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
CLOMIPRAMINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
CYPROHEPTADINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
DAPIPRAZOLEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)ADRA1A, ADRA1D
DOBUTAMINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
DOMPERIDONEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
DOXEPINChEMBLPhase 4 (approved)ADRA1A, ADRA1D
ERGOTAMINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
FENTANYLChEMBLPhase 4 (approved)ADRA1A, ADRA1B
FLUPHENAZINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
GUANABENZChEMBLPhase 4 (approved)ADRA1A, ADRA1D
GUANFACINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
IMIQUIMODChEMBLPhase 4 (approved)ADRA1A, ADRA1D
KETOTIFENChEMBLPhase 4 (approved)ADRA1A, ADRA1D
LOPERAMIDEChEMBLPhase 4 (approved)ADRA1A, ADRA1B
LUMATEPERONE TOSYLATEChEMBLPhase 4 (approved)ADRA1A, ADRA1B
MAPROTILINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
MEPAZINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
MIANSERINChEMBLPhase 4 (approved)ADRA1A, ADRA1D
NORTRIPTYLINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
PERGOLIDEChEMBLPhase 4 (approved)ADRA1A, ADRA1D
PHENYLEPHRINEChEMBLPhase 4 (approved)ADRA1A, ADRA1B
PROCHLORPERAZINEChEMBLPhase 4 (approved)ADRA1A, ADRA1D