Formoterol

Summary

Formoterol (CHEMBL1256786) is an approved small molecule (ATC R03AC13) targeting ADRB1 and ADRB2; indicated across 11 conditions including obstructive lung disease and chronic obstructive pulmonary disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: R03AC13 (+1 more)
• Targets: 2 (ADRB1, ADRB2)
• Indications: 11 conditions
• Clinical trials: 151
• Chemistry: 344.4 Da · C19H24N2O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1256786
Name	Formoterol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3410
ChEBI	CHEBI:63082
ATC	R03AC13, R03CC15
Molecular formula	C19H24N2O4
Molecular weight	344.4
InChIKey	BPZSYCZIITTYBL-UHFFFAOYSA-N

SMILES: CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O

IUPAC name: N-[2-hydroxy-5-[1-hydroxy-2-[1-(4-methoxyphenyl)propan-2-ylamino]ethyl]phenyl]formamide

ChEBI definition: A phenylethanoloamine having 4-hydroxy and 3-formamido substituents on the phenyl ring and an N-(4-methoxyphenyl)propan-2-yl substituent.

Also known as: Formoterol, Oxis, formoterol, SID11114088, (R,R)-formoterol, SID50125837, rel-Formoterol, Rel-formoterol, Rel-Formoterol, FORMOTEROL

Parent form; salt/anhydrous children: CHEMBL1893395, CHEMBL2133469, CHEMBL3989798

Patent coverage: 227 distinct patent families (480 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 416 (87%) 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
ADRB1	β1-adrenoceptor	Agonist	6.5	0%	P08588
ADRB2	β2-adrenoceptor	Agonist	10.08	0.4%	P07550

Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Thyrotropin receptor, Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, D(2) dopamine receptor, D(3) dopamine receptor, Beta-3 adrenergic receptor, Cytochrome P450 2D6, Cytochrome P450 1A2, Cytochrome P450 3A4, Cytochrome P450 2C19.

Bioactivity

ChEMBL activities: 49 potent at pChembl ≥ 5 of 55 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ADRB2	9.72	EC50	0.19	nM	CHEMBL_ACT_5238455
ADRB2	9.7	EC50	0.2	nM	CHEMBL_ACT_14710605
ADRB2	9.7	EC50	0.2	nM	CHEMBL_ACT_15030926
Q8K4Z4	9.5	EC50	0.32	nM	CHEMBL_ACT_6308495
Q8K4Z4	9.4	IC50	0.4	nM	CHEMBL_ACT_15051898
ADRB2	9.4	EC50	0.4	nM	CHEMBL_ACT_2934647
ADRB2	9.4	EC50	0.4	nM	CHEMBL_ACT_3015405
Q8K4Z4	9.4	IC50	0.4	nM	CHEMBL_ACT_3294061
ADRB2	9.3	EC50	0.5	nM	CHEMBL_ACT_2420456
ADRB2	9.3	EC50	0.5	nM	CHEMBL_ACT_6284211
ADRB2	9.3	EC50	0.5	nM	CHEMBL_ACT_6308429
ADRB2	9	EC50	1	nM	CHEMBL_ACT_6292043
ADRB2	9	EC50	1	nM	CHEMBL_ACT_8022175
ADRB2	8.89	EC50	1.3	nM	CHEMBL_ACT_3294062
TSHR	8.89	Potency	1.3	nM	CHEMBL_ACT_3921860
TSHR	8.89	Potency	1.3	nM	CHEMBL_ACT_4618025
Q8K4Z4	8.8	EC50	1.58	nM	CHEMBL_ACT_14712797
MAPK1	8.7	Potency	2	nM	CHEMBL_ACT_4524459
ADRB2	8.6	Kd	2.51	nM	CHEMBL_ACT_13449572
ADRB2	8.6	EC50	2.51	nM	CHEMBL_ACT_14657237
ADRB2	8.6	EC50	2.51	nM	CHEMBL_ACT_14712825
ADRB2	8.6	EC50	2.51	nM	CHEMBL_ACT_15030966
ADRB2	8.59	Ki	2.6	nM	CHEMBL_ACT_1447614
ADRB2	8.59	Ki	2.6	nM	CHEMBL_ACT_15051973
ADRB2	8.59	Ki	2.6	nM	CHEMBL_ACT_3423531
ADRB2	8.1	EC50	7.94	nM	CHEMBL_ACT_3423601
ADRB1	7.9	EC50	12.59	nM	CHEMBL_ACT_14712805
ADRB1	7.9	EC50	12.59	nM	CHEMBL_ACT_15030906
ADRB2	7.64	Ki	23	nM	CHEMBL_ACT_3294063
ADRB3	7.6	EC50	25.12	nM	CHEMBL_ACT_14712810

Target pathways

Aggregated over 2 target gene(s): ADRB1, ADRB2.

Top Reactome pathways

16 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	2	ADRB1, ADRB2
Signaling by GPCR	2	ADRB1, ADRB2
Class A/1 (Rhodopsin-like receptors)	2	ADRB1, ADRB2
Amine ligand-binding receptors	2	ADRB1, ADRB2
GPCR downstream signalling	2	ADRB1, ADRB2
Adrenoceptors	2	ADRB1, ADRB2
G alpha (s) signalling events	2	ADRB1, ADRB2
GPCR ligand binding	2	ADRB1, ADRB2
Membrane Trafficking	1	ADRB2
Metabolism of proteins	1	ADRB2
Vesicle-mediated transport	1	ADRB2
Deubiquitination	1	ADRB2
Ub-specific processing proteases	1	ADRB2
Post-translational protein modification	1	ADRB2
Cargo recognition for clathrin-mediated endocytosis	1	ADRB2
Clathrin-mediated endocytosis	1	ADRB2

Dominant GO biological processes

GO term	Targets
diet induced thermogenesis	2
norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure	2
adenylate cyclase-activating G protein-coupled receptor signaling pathway	2
response to cold	2
positive regulation of cardiac muscle cell apoptotic process	2
heat generation	2
negative regulation of multicellular organism growth	2
positive regulation of MAPK cascade	2
brown fat cell differentiation	2
adenylate cyclase-activating adrenergic receptor signaling pathway	2
positive regulation of cold-induced thermogenesis	2
signal transduction	2
G protein-coupled receptor signaling pathway	2
positive regulation of heart rate by epinephrine-norepinephrine	1
positive regulation of the force of heart contraction by epinephrine-norepinephrine	1

Indications & clinical

Indications

11 indications (1 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
obstructive lung disease	4	MONDO:0002267	HP:0006536
chronic obstructive pulmonary disease	3	MONDO:0005002	EFO:0000341
asthma	3	MONDO:0004979	MONDO:0004979
pulmonary emphysema	3	MONDO:0004849	EFO:0000464
bronchitis	3	MONDO:0003781	EFO:0009661
bronchiectasis	3	MONDO:0004822	HP:0002110
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
bronchiolitis obliterans syndrome	2	MONDO:0015265	EFO:0007183
acute respiratory distress syndrome	2	MONDO:0006502	EFO:1000637
allergic disease	2	MONDO:0005271	MONDO:0005271
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096

Clinical trials

Total trials: 151.

Phase distribution

Phase	Trials
PHASE3	51
PHASE4	34
PHASE2	32
Not specified	23
PHASE1	9
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06571942	PHASE4	RECRUITING	Effect of the Inhaled Triple Therapies Over the Small Airway in Biomass Exposure
NCT00134979	PHASE4	COMPLETED	Formoterol Certihaler, Tiotropium HandiHaler and Tiotropium HandiHaler in Combination With Formoterol Certihaler in Patients With Stable Chronic Obstructive Pulmonary Disease
NCT00272753	PHASE4	COMPLETED	Effect of Budesonide / Formoterol Combination in Repeated AMP Provocations
NCT00327353	PHASE4	COMPLETED	Influence Of Different Airflow Resistances On Drug Effect Of 50μg Salmeterol And 6 μg Formoterol
NCT00460577	PHASE4	COMPLETED	Efficacy of Formoterol vs Ipatropioum Bromide Plus Fenoterol in Children (5-<12 Years) With Acute Bronchial Obstruction
NCT00463866	PHASE4	COMPLETED	Local Phase 4 Pan-European SMART Study
NCT00490243	PHASE4	COMPLETED	Effect of Different Anti-Asthmatic Treatments on Lung Function and on Exercise-Induced Bronchoconstriction in Children With Asthma
NCT00561886	PHASE4	COMPLETED	Change of Inspiratory Peak Flow in COPD
NCT00900874	PHASE4	UNKNOWN	Rapid Onset Action of Salbutamol Versus Formoterol
NCT00914654	PHASE4	UNKNOWN	Concentrations of Formoterol in Blood and Urine
NCT01070888	PHASE4	TERMINATED	Trial on the Effect of Budesonide/Formoterol and Inhaled Budesonide Alone on Exercise-Induced Asthma
NCT01186653	PHASE4	COMPLETED	Effect on Adrenal Function of Budesonide Versus Fluticasone in Chronic Obstructive Pulmonary Disease (COPD)
NCT01253473	PHASE4	COMPLETED	Symbicort in Airway Predominant Chronic Obstructive Pulmonary Disease (COPD)
NCT01377428	PHASE4	WITHDRAWN	Efficacy of Indacaterol 150 µg Versus Formoterol
NCT01656005	PHASE4	COMPLETED	Beta Blocker Therapy in Moderate to Severe COPD
NCT01748279	PHASE4	COMPLETED	The Effects of Atorvastatin Treatment in COPD Patients
NCT01760304	PHASE4	TERMINATED	Changes in Cardiac Function in COPD Patients After Administration of Budesonide/Formoterol (Symbicort®) Versus Placebo
NCT01787097	PHASE4	COMPLETED	Effect of Symbicort ® on GR in Sputum in COPD
NCT01794780	PHASE4	COMPLETED	A 1-year Multi-center, Prospective, Cohort Study in Patients With Chronic Obstructive Pulmonary Disease Treated With Long-acting Bronchodilator
NCT01845025	PHASE4	TERMINATED	Study of Safety of Foradil in Patients With Persistent Asthma
NCT01892787	PHASE4	COMPLETED	Effects of Particle Size in Small Airways Dysfunction
NCT01912872	PHASE4	TERMINATED	Study to Assess the Efficacy and Safety of Omalizumab Treatment on ICS Reduction for Severe IgE-mediated Asthma
NCT02424344	PHASE4	COMPLETED	Effect of Aclidinium/Formoterol on Lung Hyperinflation, Exercise Capacity and Physical Activity in Moderate to Severe COPD Patients
NCT02491970	PHASE4	TERMINATED	Small Airway Function of Fluticasone/Formoterol (Flutiform®) and Fluticasone/Salmeterol
NCT02526758	PHASE4	UNKNOWN	Small Airways Evaluation and Treatment
NCT02574975	PHASE4	UNKNOWN	Assessment of Airway Responsiveness and Treatment Efficacy in Asthmatics
NCT02988869	PHASE4	COMPLETED	Tiotropium/Formoterol Via Discair® vs Tiotropium Monotherapy or Tiotropium + Formoterol Free Combination Treatment
NCT03028701	PHASE4	COMPLETED	Assessment of Bronchodilator Efficacy of Formoterol/Budesonide 12/400 mcg Via Discair in COPD
NCT03478683	PHASE4	COMPLETED	A Randomized Study, Comparing Fluticasone Furoate/Umeclidinium/Vilanterol (FF/UMEC/VI) Single Inhaler Triple Therapy, Versus Multiple Inhaler Therapy (Budesonide/Formoterol Plus Tiotropium) in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
NCT03478696	PHASE4	COMPLETED	A Randomized Study, Comparing Fluticasone Furoate/Umeclidinium/Vilanterol (FF/UMEC /VI) Single Inhaler Triple Therapy, Versus Multiple Inhaler Therapy (Budesonide/Formoterol Plus Tiotropium) in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
NCT04171180	PHASE4	UNKNOWN	The Efficacy of Budesonide/Formoterol in Cough Variant Asthma
NCT04520230	PHASE4	COMPLETED	Three Treatment of Chronic Obstructive Pulmonary Disease Patients
NCT06282861	PHASE4	TERMINATED	ANTES B+ Clinical Trial
NCT06869382	PHASE4	COMPLETED	ICS+LABA Vs. ICS+LABA+Omalizumab: Impact on Asthma Control and Gene Expression
NCT06429475	PHASE3	RECRUITING	Anti-Inflammatory Reliever South Africa
NCT06473779	PHASE3	ACTIVE_NOT_RECRUITING	Open-label Study to Assess Reduction of Background Asthma Medication While Sustaining Asthma Control and Clinical Remission With Tezepelumab in Patients 12-80yrs With Severe Asthma.
NCT06895460	PHASE3	NOT_YET_RECRUITING	A Trial on the Treatment of Bronchial Asthma With Budesonide Formoterol Combined With Immune Modulators (Staphylococcus and Neisseria Tablets)
NCT00130351	PHASE3	COMPLETED	A 3-week Study Investigating Patient Use and Functionality of Formoterol in a Novel Inhalation Device in Patients With Asthma
NCT00206154	PHASE3	COMPLETED	A Comparison of Symbicort® pMDI 2 x 160/4.5 μg Bid and Symbicort® pMDI 2 x 80/4.5 μg Bid With Formoterol Turbuhaler®, Budesonide pMDI, the Combination of Formoterol Turbuhaler® and Budesonide pMDI, and Placebo in COPD Patients
NCT00206167	PHASE3	COMPLETED	A Comparison of Symbicort® pMDI 2 x 160/4.5 μg Bid and 2 x 80/4.5 μg Bid With Formoterol Turbuhaler® 2 x 4.5 μg Bid and Placebo in Patients With COPD

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

Molecule	Source	Status	Shared targets
Desloratadine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Dihydroergotamine	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
OLODATEROL	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
Pramipexole	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
TAMSULOSIN	ChEMBL + PubChem	Phase 4 (approved)	ADRB1, ADRB2
ACEBUTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ALBUTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARFORMOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ARIPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ATENOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BENPERIDOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BETAXOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BISOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BREXPIPRAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
BROMOCRIPTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CANDESARTAN CILEXETIL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARTEOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CARVEDILOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CELIPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CHLORHEXIDINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLEMASTINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
CLOTRIMAZOLE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DARIFENACIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOBUTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
DOMPERIDONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
EPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ERGOTAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ESMOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FENOTEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
FLUSPIRILENE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
INDACATEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
ISOPROTERENOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LABETALOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
LEVOBUNOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
METOPROLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
MONTELUKAST	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NADOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NEBIVOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NITAZOXANIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NOREPINEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
OXPRENOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PHENYLEPHRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PIMOZIDE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PINDOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRACTOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRENYLAMINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PRIMAQUINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPAFENONE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
PROPRANOLOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RANOLAZINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAMPIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RIFAXIMIN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
RITODRINE	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SALMETEROL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SOTALOL	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
SUNITINIB	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2
TAMOXIFEN	ChEMBL	Phase 4 (approved)	ADRB1, ADRB2