Arformoterol

Summary

Arformoterol (CHEMBL1363) is an approved small-molecule bronchodilator agent; indicated across 5 conditions including chronic obstructive pulmonary disease and pulmonary emphysema.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 5 conditions
• Clinical trials: 158
• Chemistry: 344.4 Da · C19H24N2O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1363
Name	Arformoterol
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3083544
ChEBI	CHEBI:408174
Molecular formula	C19H24N2O4
Molecular weight	344.4
InChIKey	BPZSYCZIITTYBL-YJYMSZOUSA-N

SMILES: C[C@H](CC1=CC=C(C=C1)OC)NC[C@@H](C2=CC(=C(C=C2)O)NC=O)O

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

ChEBI definition: An N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide in which both of the stereocentres have R configuration. The active enantiomer of formoterol, it is administered by inhalation (generally as the tartrate salt) as a direct-acting sympathomimetic and bronchodilator for the treatment of chronic obstructive pulmonary disease (any progressive respiratory disease that makes it harder to breathe over time, such as chronic bronchitis and emphysema).

Pharmacological roles (ChEBI): bronchodilator agent, anti-asthmatic drug, β-adrenergic agonist.

Also known as: (-)-formoterol, (r,r)-formoterol, Arformoterol, Formoterol r, r-form, (R,R)-Formoterol, ARFORMOTEROL, Formoterol, arformoterol

Parent form; salt/anhydrous children: CHEMBL605993, CHEMBL1200811, CHEMBL1951071, CHEMBL3184383

Patent coverage: 8,896 distinct patent families (35,020 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 34,120 (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

Broader ChEMBL bioactivity targets: 9 (assay-derived). Sample: Progesterone receptor, Beta-2 adrenergic receptor, Beta-1 adrenergic receptor, D(2) dopamine receptor, Sodium-dependent serotonin transporter, Alpha-1A adrenergic receptor, Prostaglandin G/H synthase 2, Sodium-dependent dopamine transporter, Beta-2 adrenergic receptor.

Bioactivity

ChEMBL activities: 11 potent at pChembl ≥ 5 of 14 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q8K4Z4	9.9	EC50	0.13	nM	CHEMBL_ACT_13864586
Q8K4Z4	9.89	EC50	0.13	nM	CHEMBL_ACT_13864604
ADRB2	9.5	EC50	0.32	nM	CHEMBL_ACT_13864598
ADRB2	8.58	EC50	2.63	nM	CHEMBL_ACT_23194855
ADRB2	7.43	AC50	37.5	nM	CHEMBL_ACT_25122929
ADRA1A	7.3	AC50	50	nM	CHEMBL_ACT_25229866
ADRB1	6.96	EC50	109	nM	CHEMBL_ACT_23194852
SLC6A4	6.21	AC50	621.3	nM	CHEMBL_ACT_25150408
ADRB1	5.95	AC50	1125	nM	CHEMBL_ACT_25121850
ADRA1A	5.61	AC50	2461	nM	CHEMBL_ACT_25137980
SLC6A3	5.27	AC50	5425	nM	CHEMBL_ACT_25124025

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

5 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
chronic obstructive pulmonary disease	3	MONDO:0005002	EFO:0000341
pulmonary emphysema	3	MONDO:0004849	EFO:0000464
chronic bronchitis	3	MONDO:0005607	EFO:0006505
bronchitis	3	MONDO:0003781	EFO:0009661
asthma	2	MONDO:0004979	MONDO:0004979

Clinical trials

Total trials: 158.

Phase distribution

Phase	Trials
PHASE3	53
PHASE4	37
PHASE2	33
Not specified	24
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
NCT00424528	PHASE4	COMPLETED	Efficacy Safety Study of Arformoterol/Tiotropium Combination Versus Either Therapy Alone in Chronic Obstructive Pulmonary Disease (COPD)
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
NCT00773786	PHASE4	COMPLETED	Effect of Brovana and Tiotropium in Chronic Obstructive Pulmonary Disease (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)
NCT01361984	PHASE4	UNKNOWN	Sunovion Brovana Versus Serevent Inspiratory Capacity High Resolution Computed Tomography
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)
NCT00064415	PHASE3	COMPLETED	To Evaluate the Long-term Safety of (R,R)-Formoterol in Subjects With COPD
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
NCT00250679	PHASE3	COMPLETED	Safety and Efficacy of Arformoterol Tartrate Inhalation Solution in Subjects With Chronic Obstructive Pulmonary Disease
NCT00252785	PHASE3	COMPLETED	Efficacy & Safety of Symbicort® TURBUHALER® 160/4.5 µg Twice Daily & Pulmicort® TURBUHALER® 200 µg Twice Daily + Theolong® Tablet 200 mg Twice Daily in Japanese Asthmatic Patients
NCT00255255	PHASE3	COMPLETED	Safety & Efficacy of Symbicort® Turbuhaler® (1, 2, and 4 x 160/4.5 µg Twice Daily) in Japanese Patients With Asthma
NCT00259766	PHASE3	COMPLETED	SHARE - Symbicort and Health Economics in a Real Life Evaluation
NCT00259779	PHASE3	COMPLETED	Comparison Between Symbicort® and Prednisolone in COPD
NCT00288379	PHASE3	COMPLETED	SMILDA - Symbicort®Turbuhaler® Allergan Challenge Study in Allergic Patients With Mild Asthma
NCT00290264	PHASE3	COMPLETED	SALTO - Symbicort Single Inhaler Therapy Use in Adolescent Adults and Adults With Persistent Asthma
NCT00319306	PHASE3	COMPLETED	Real Life Effectiveness in Asthma of Symbicort Single Inhaler Therapy
NCT00326053	PHASE3	COMPLETED	Prevention of Asthma Relapse After Discharge From Emergency
NCT00393458	PHASE3	COMPLETED	Efficacy, Safety, and Tolerability of Once Daily Indacaterol in Chronic Obstructive Pulmonary Disease (COPD) Using Formoterol Twice Daily as Active Control
NCT00419744	PHASE3	COMPLETED	A Comparison of SYMBICORT® pMDI With Formoterol Turbuhaler® in Subjects With COPD
NCT00463567	PHASE2/PHASE3	COMPLETED	26 Week Efficacy, Safety and Tolerability Study of Indacaterol in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT00476099	PHASE3	COMPLETED	Efficacy and Safety Study of Beclometasone/Formoterol Single Inhaler in Patients With COPD
NCT00476268	PHASE3	COMPLETED	Efficacy and Tolerability of Beclometasone/Formoterol Single Inhaler in Patients With Moderate to Severe Persistent Asthma
NCT00646009	PHASE3	COMPLETED	Symbicort Onset of Action 2
NCT00651547	PHASE3	COMPLETED	Symbicort in Asthmatic Children - SEEDLING
NCT00651651	PHASE3	COMPLETED	Efficacy of Symbicort Versus Its Monocomponents - SPRUCE 80/4.5
NCT00651768	PHASE3	COMPLETED	Titratable Dosing in Moderate to Severe Asthmatics
NCT00652002	PHASE3	COMPLETED	Efficacy of Symbicort Versus Its Monocomponents - SPRUCE 160/4.5
NCT00652392	PHASE3	COMPLETED	Efficacy of Symbicort pMDI Administered Once Daily in Adolescents and Adults During 12 Weeks - STEM
NCT00662779	PHASE3	WITHDRAWN	Bronchoprotective Effect of Arformoterol in Children With Exercise-Induced Bronchospasm (EIB)
NCT00691951	PHASE3	COMPLETED	Effects of Budesonide & Budesonide/Formoterol on Smoking Asthmatic Subjects
NCT00793624	PHASE3	COMPLETED	Safety and Efficacy of BI 1744 CL in Patients With Chronic Obstructive Pulmonary Disease I
NCT00796653	PHASE3	COMPLETED	Safety and Efficacy of BI 1744 CL in Patients With Chronic Obstructive Pulmonary Disease II
NCT00861926	PHASE3	COMPLETED	Study on Foster Efficacy Maintenance and Reliever vs Foster Maintenance + Salbutamol Reliever in Asthmatics (MART2)
NCT00909779	PHASE3	COMPLETED	Safety Study of Arformoterol Tartrate Inhalation Solution in Chronic Obstructive Pulmonary Disease (COPD) Subjects
NCT00972140	PHASE3	COMPLETED	Formoterol-HFA 3-month Study in Chronic Obstructive Pulmonary Disease (COPD) Patients
NCT01001364	PHASE3	COMPLETED	A Comparative Study Between Foraseq and Formoterol/Budesonide Inhalation Capsules in Patients with Asthma
NCT01047553	PHASE3	COMPLETED	Study to Evaluate the Safety and Efficacy of Formoterol in a Daily Dose of 18 µg (9 µg Twice Daily) in Japanese Chronic Obstructive Pulmonary Disease (COPD) Patients
NCT01167010	PHASE3	COMPLETED	A Non-inferiority, Comparative Study Between Foraseq®, Eurofarma´s Formoterol/Budesonide and Alenia® in Asthma
NCT01202084	PHASE3	COMPLETED	A Study Comparative of Formoterol/Fluticasone Foraseq® and Fluticasone in Asthma Patients
NCT01290874	PHASE3	COMPLETED	Blacks and Exacerbations on Long Acting Beta Agonists (LABA) vs. Tiotropium (BELT)
NCT01393145	PHASE3	WITHDRAWN	Efficacy and Safety Study of Formoterol/Fluticasone and Salmeterol/Fluticasone in Patients With Moderate-to-severe COPD
NCT01574651	PHASE3	COMPLETED	The Effect of QVA149 on Health Related Quality of Life in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT01602523	PHASE3	UNKNOWN	Effect of Symbicort on Sleep Quality in Patients With Emphysema
NCT01676987	PHASE3	COMPLETED	Evaluation of the Efficacy and Safety of a Fixed-dose, Single-capsule Budesonide-formoterol Combination in Uncontrolled Asthma
NCT01917331	PHASE3	COMPLETED	Efficacy of Fixed Combination of Beclometasone + Formoterol + Glycopyrrolate Versus Foster® in COPD
NCT01946620	PHASE3	COMPLETED	A Study to Show That Flutiform is Well Tolerated and Effective in the Treatment of COPD
NCT02157935	PHASE3	COMPLETED	Comparing the Efficacy of Symbicort® pMDI and Formoterol Turbuhaler in Reducing Exacerbations in Patients With Cronic Obstructive Pulmonary Disease
NCT02345161	PHASE3	COMPLETED	A Comparison Study Between the Fixed Dose Triple Combination of Fluticasone Furoate/ Umeclidinium/ Vilanterol Trifenatate (FF/UMEC/VI) With Budesonide/Formoterol in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
NCT02477397	PHASE3	UNKNOWN	Symptom-driven Maintenance and Reliever Treatment to Prevent Exacerbations in COPD
NCT02725242	PHASE3	COMPLETED	Efficacy of Once-daily Budesonide/Formoterol Turbuhaler 4.5/160 µg in Step Down Asthma
NCT03387241	PHASE3	UNKNOWN	Efficacy of FLUTIFORM ® vs Seretide® in Moderate to Severe Persistent Asthma in Subjects Aged ≥12 Years
NCT03573817	PHASE3	COMPLETED	A 42-day Parallel Group Safety Study of Revefenacin and Formoterol, Administered in Sequence and as a Combination, in Participants With COPD
NCT04191434	PHASE3	UNKNOWN	Efficacy and Safety of Flamboyant 125/12 Association in the Treatment of Adults With Moderate Asthma
NCT04191447	PHASE3	UNKNOWN	Efficacy and Safety of Flamboyant 200/12 Association in the Treatment of Adults With Severe Asthma
NCT04193878	PHASE3	TERMINATED	ARrest RESpiraTory Failure From PNEUMONIA
NCT06676319	PHASE2	RECRUITING	Study of Lunsekimig (SAR443765) Compared With Placebo in Adults With High-risk Asthma
NCT00443482	PHASE2	COMPLETED	Study to Demonstrate Equivalence of Formoterol 12 and 24 µg Delivered Via Two Types of Single Dose Dry Powder Inhalers (Concept1 and Aerolizer)
NCT00545272	PHASE2	COMPLETED	A Dose Ranging Trial of 4 Doses of Indacaterol Delivered Via TWISTHALER® Device in Adult and Adolescent Patients With Persistent Asthma
NCT00557466	PHASE2	COMPLETED	A Dose Ranging Trial of 4 Doses of Indacaterol Delivered Via the TWISTHALER® Device in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT00583947	PHASE2	COMPLETED	A Safety and Tolerability Study of Arformoterol Tartrate Inhalation Solution in Pediatric Subjects
NCT00624754	PHASE2	COMPLETED	Prospective Evaluation of the Efficacy of Budesonide/Formoterol in Bronchiolitis Obliterans in AHSCT
NCT00626522	PHASE2	COMPLETED	Aclidinium/Formoterol Fixed Combination Dose Finding Study
NCT00635882	PHASE2	COMPLETED	Asthma Study Comparing Anti-Inflammatory Effects of 3 Doses of Mometasone Furoate/Formoterol Fumarate and Medium Dose Mometasone Furoate (Study P05122 AM1)(COMPLETED)
NCT00658255	PHASE2	COMPLETED	Relative Bronchodilating Effects of Formoterol When Administered Via Symbicort Pressurized Metered-dose Inhaler (pMDI) or Oxis Turbuhaler

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

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).