Procaterol

drug
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Also known as MeptinSID11113915SID26752069rel-ProcaterolSID144204492SID170465820

Summary

Procaterol (CHEMBL160519) is a phase-3 clinical-stage small molecule (ATC R03AC16) targeting ADRB2; indicated across 2 conditions including obstructive lung disease and asthma.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • ATC class: R03AC16 (+1 more)
  • Targets: 1 (ADRB2)
  • Indications: 2 conditions
  • Clinical trials: 10
  • Chemistry: 290.36 Da · C16H22N2O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL160519
NameProcaterol
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID4916
ATCR03AC16, R03CC08
Molecular formulaC16H22N2O3
Molecular weight290.36
InChIKeyFKNXQNWAXFXVNW-UHFFFAOYSA-N

SMILES: CCC(C(C1=C2C=CC(=O)NC2=C(C=C1)O)O)NC(C)C

IUPAC name: 8-hydroxy-5-[1-hydroxy-2-(propan-2-ylamino)butyl]-1H-quinolin-2-one

Also known as: Meptin, Procaterol, SID11113915, SID26752069, rel-Procaterol, SID144204492, SID170465820, PROCATEROL, procaterol

Parent form; salt/anhydrous children: CHEMBL1322218

Patent coverage: 2,434 distinct patent families (10,101 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 10,095 (100%) 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
ADRB2β2-adrenoceptorAgonist7.10.4%P07550

Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Lysine-specific demethylase 4E, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Thyrotropin receptor, Menin/Histone-lysine N-methyltransferase MLL, Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, D(2) dopamine receptor, Prostaglandin G/H synthase 2, Cytochrome P450 2D6.

Bioactivity

ChEMBL activities: 7 potent at pChembl ≥ 5 of 19 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
TSHR7.9Potency12.6nMCHEMBL_ACT_3911050
TSHR7.9Potency12.6nMCHEMBL_ACT_4617006
ADRB27.48Ki33nMCHEMBL_ACT_16581631
ADRB27.1Kd79.43nMCHEMBL_ACT_13449575
ADRB26.7AC50200nMCHEMBL_ACT_25123343
LMNA6.05Potency891.3nMCHEMBL_ACT_3628026
PTGS25.06AC508800nMCHEMBL_ACT_25166759

Target pathways

Aggregated over 1 target gene(s): ADRB2.

Top Reactome pathways

16 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction1ADRB2
Membrane Trafficking1ADRB2
Signaling by GPCR1ADRB2
Class A/1 (Rhodopsin-like receptors)1ADRB2
Amine ligand-binding receptors1ADRB2
GPCR downstream signalling1ADRB2
Adrenoceptors1ADRB2
Metabolism of proteins1ADRB2
G alpha (s) signalling events1ADRB2
GPCR ligand binding1ADRB2
Vesicle-mediated transport1ADRB2
Deubiquitination1ADRB2
Ub-specific processing proteases1ADRB2
Post-translational protein modification1ADRB2
Cargo recognition for clathrin-mediated endocytosis1ADRB2
Clathrin-mediated endocytosis1ADRB2

Dominant GO biological processes

GO termTargets
diet induced thermogenesis1
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure1
regulation of sodium ion transport1
transcription by RNA polymerase II1
receptor-mediated endocytosis1
smooth muscle contraction1
cell surface receptor signaling pathway1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway1
endosome to lysosome transport1
response to cold1
positive regulation of cardiac muscle cell apoptotic process1
negative regulation of cardiac muscle cell apoptotic process1
positive regulation of bone mineralization1
heat generation1
negative regulation of multicellular organism growth1

Indications & clinical

Indications

2 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).

IndicationTrial phaseMONDOEFO
obstructive lung disease3MONDO:0002267HP:0006536
asthma3MONDO:0004979MONDO:0004979

Clinical trials

Total trials: 10.

Phase distribution

PhaseTrials
PHASE44
PHASE32
PHASE12
PHASE21
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00394485PHASE4TERMINATEDTiotropium + Procaterol vs Tiotropium + Placebo in COPD Patients
NCT01091337PHASE4COMPLETEDComparative Study on the Efficacy and Safety of Procaterol Versus Salbutamol Given Via Metered Dose Inhaler With Spacer in the Management of Acute Asthma Attack in the Emergency Room
NCT01170429PHASE4UNKNOWNEfficacy and Safety Study of Procaterol Hydrochloride to Treat Patients With Cough Variant Asthma (CVA)
NCT06346691PHASE4COMPLETEDEffects of Oral Doxofylline and Procaterol on Chronic Obstructive Pulmonary Disease
NCT00990847PHASE3COMPLETEDNebulized Procaterol Versus Nebule Salbutamol for the Treatment of Moderate Acute Asthma
NCT01095016PHASE3COMPLETEDA Study to Evaluate the Efficacy and Safety of Meptin® Swinghaler and Berotec N® Metered Aerosol in Mild to Moderate Stable Asthma Patients
NCT02162784PHASE2COMPLETEDEfficacy Study of SYN006 HFA MDI in Asthma Patients
NCT02165033PHASE1COMPLETEDMultiple-dose Pharmacokinetics Study of SYN006 HFA MDI Administered Orally to Healthy Volunteers
NCT02165046PHASE1COMPLETEDBioavailability Study of SYN006, Pulmicort pMDI and Meptin Air in Healthy Adult.
NCT02349919Not specifiedUNKNOWNEffect of Oral Procaterol on Postinfectious Persistent Cough

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

188 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
DESLORATADINEChEMBL + PubChemPhase 4 (approved)ADRB2
DIHYDROERGOTAMINEChEMBL + PubChemPhase 4 (approved)ADRB2
OLODATEROLChEMBL + PubChemPhase 4 (approved)ADRB2
PRAMIPEXOLEChEMBL + PubChemPhase 4 (approved)ADRB2
ACEBUTOLOLChEMBLPhase 4 (approved)ADRB2
ADENOSINEChEMBLPhase 4 (approved)ADRB2
ALBUTEROLChEMBLPhase 4 (approved)ADRB2
AMITRIPTYLINEChEMBLPhase 4 (approved)ADRB2
AMLODIPINEChEMBLPhase 4 (approved)ADRB2
AMOXAPINEChEMBLPhase 4 (approved)ADRB2
ARFORMOTEROLChEMBLPhase 4 (approved)ADRB2
ARIPIPRAZOLEChEMBLPhase 4 (approved)ADRB2
ATENOLOLChEMBLPhase 4 (approved)ADRB2
BENPERIDOLChEMBLPhase 4 (approved)ADRB2
BETAXOLOLChEMBLPhase 4 (approved)ADRB2
BISOPROLOLChEMBLPhase 4 (approved)ADRB2
BREXPIPRAZOLEChEMBLPhase 4 (approved)ADRB2
BROMOCRIPTINEChEMBLPhase 4 (approved)ADRB2
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)ADRB2
CARTEOLOLChEMBLPhase 4 (approved)ADRB2
CARVEDILOLChEMBLPhase 4 (approved)ADRB2
CELIPROLOLChEMBLPhase 4 (approved)ADRB2
CHLORHEXIDINEChEMBLPhase 4 (approved)ADRB2
CLEMASTINEChEMBLPhase 4 (approved)ADRB2
CLOMIPRAMINEChEMBLPhase 4 (approved)ADRB2
CLOTRIMAZOLEChEMBLPhase 4 (approved)ADRB2
CLOZAPINEChEMBLPhase 4 (approved)ADRB2
DARIFENACINChEMBLPhase 4 (approved)ADRB2
DEXAMETHASONEChEMBLPhase 4 (approved)ADRB2
DIPIVEFRINChEMBLPhase 4 (approved)ADRB2
DOBUTAMINEChEMBLPhase 4 (approved)ADRB2
DOMPERIDONEChEMBLPhase 4 (approved)ADRB2
DOPAMINEChEMBLPhase 4 (approved)ADRB2
DOXAZOSINChEMBLPhase 4 (approved)ADRB2
ELAGOLIXChEMBLPhase 4 (approved)ADRB2
EPINEPHRINEChEMBLPhase 4 (approved)ADRB2
EPINEPHRINE BITARTRATEChEMBLPhase 4 (approved)ADRB2
ERGOTAMINEChEMBLPhase 4 (approved)ADRB2
ESMOLOLChEMBLPhase 4 (approved)ADRB2
FENOTEROLChEMBLPhase 4 (approved)ADRB2
FLUSPIRILENEChEMBLPhase 4 (approved)ADRB2
FORMOTEROLChEMBLPhase 4 (approved)ADRB2
HALOPERIDOLChEMBLPhase 4 (approved)ADRB2
INDACATEROLChEMBLPhase 4 (approved)ADRB2
ISOETHARINEChEMBLPhase 4 (approved)ADRB2
ISOPROTERENOLChEMBLPhase 4 (approved)ADRB2
LABETALOLChEMBLPhase 4 (approved)ADRB2
LEVOBUNOLOLChEMBLPhase 4 (approved)ADRB2
LEVOSALBUTAMOLChEMBLPhase 4 (approved)ADRB2
LOFEPRAMINEChEMBLPhase 4 (approved)ADRB2
LOPERAMIDEChEMBLPhase 4 (approved)ADRB2
LOXAPINEChEMBLPhase 4 (approved)ADRB2
MEBEVERINEChEMBLPhase 4 (approved)ADRB2
METAPROTERENOLChEMBLPhase 4 (approved)ADRB2
METOPROLOLChEMBLPhase 4 (approved)ADRB2
MIFEPRISTONEChEMBLPhase 4 (approved)ADRB2
MONTELUKASTChEMBLPhase 4 (approved)ADRB2
NADOLOLChEMBLPhase 4 (approved)ADRB2
NEBIVOLOLChEMBLPhase 4 (approved)ADRB2
NITAZOXANIDEChEMBLPhase 4 (approved)ADRB2