Overview
Formoterol is an inhaled beta-agonist used in the management of COPD and asthma that was first approved for use in the United States in 2001. It acts on bronchial smooth muscle to dilate and relax airways, and is administered as a racemic mixture of its active (R;R)- and inactive (S;S)-enantiomers. A major clinical advantage of formoterol over other inhaled beta-agonists is its rapid onset of action (2-3 minutes), which is at least as fast as salbutamol, combined with a long duration of action (12 hours) - for this reason, treatment guidelines for asthma recommend its use as both a reliever and maintenance medication. It is available as a single-entity product and in several formulations in combination with both inhaled corticosteroids and long-acting muscarinic antagonists.
Indication
Formoterol is indicated in various formulations for the treatment of asthma and COPD. For the treatment of COPD, formoterol is available as a single-entity inhalation solution, in combination with the long-acting muscarinic antagonists (LAMAs) aclidinium and glycopyrronium, and in combination with the corticosteroid budesonide. For the treatment of asthma, formoterol is available in combination with mometasone furoate for patients 5 years and older and with budesonide for patients 6 years and older. Formoterol may also be used on an as-needed basis for prophylaxis against exercise-induced bronchospasm.
Associated Conditions
- Asthma
- Bronchial Asthma
- Bronchoconstriction
- Chronic Obstructive Pulmonary Disease (COPD)
- Exercise-Induced Bronchospasm
- Moderate to Severe Chronic Obstructive Pulmonary Disease (COPD)
Research Report
Formoterol: A Comprehensive Pharmacological and Clinical Monograph
Section 1: Drug Substance Profile
This section establishes the fundamental identity of Formoterol, covering its chemical structure, nomenclature, and key physicochemical properties that influence its formulation and biological activity.
1.1 Identification and Nomenclature
Formoterol, also known by the alternative name eformoterol, is a small molecule drug classified as a selective beta-2 adrenergic receptor agonist.[1] It is identified globally through a standardized set of chemical names and identifiers.
- Drug Name: Formoterol [1]
- Systematic (IUPAC) Names:
- N-[2-hydroxy-5-(1-hydroxy-2-{[2-(4-methoxyphenyl)-1-methylethyl]amino}ethyl)phenyl]formamide [1]
- (RR,SS)-N-[2-hydroxy-5-[1-hydroxy-2-[1-(4-methoxyphenyl) propan-2-ylamino]ethyl] phenyl]formamide [2]
- Identifiers:
- DrugBank ID: DB00983 [1]
- CAS Number: 73573-87-2 (for the racemic free base) [2]
- Related CAS Numbers: 43229-80-7 (for Formoterol Fumarate) [5]
- Synonyms and Development Codes: The drug is known by numerous synonyms reflecting its global development and marketing history, including Formoterolum (the International Nonproprietary Name in Latin), Foradil, Oxis, BD 40A, and CGP-25827A.[1]
- Chemical Classifications: Formoterol belongs to several chemical and therapeutic classes, including Adrenergic Agonists, Selective Beta-2 Adrenergic Receptor Agonists, Phenylethanolamines, Formamides, and Phenols.[1]
1.2 Physicochemical Properties and Formulation Characteristics
The physical and chemical properties of formoterol are integral to its formulation as an inhaled medication and directly influence its unique pharmacological profile.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/06/15 | Phase 2 | Not yet recruiting | |||
2025/03/07 | Not Applicable | Not yet recruiting | |||
2024/05/13 | Phase 4 | Recruiting | SamA Pharmaceutical Co., Ltd | ||
2024/02/28 | Phase 4 | Recruiting | |||
2023/10/30 | Not Applicable | Completed | Morten Hostrup, PhD | ||
2022/09/23 | Not Applicable | Completed | |||
2021/06/24 | Phase 2 | Completed | UPECLIN HC FM Botucatu Unesp | ||
2021/05/19 | N/A | Completed | |||
2020/11/04 | Not Applicable | UNKNOWN | |||
2020/07/31 | Phase 1 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| RPK Pharmaceuticals, Inc. | 53002-2667 | RESPIRATORY (INHALATION) | 4.5 ug in 1 1 | 7/24/2019 | |
| American Health Packaging | 60687-770 | RESPIRATORY (INHALATION) | 15 ug in 2 mL | 4/1/2024 | |
| A-S Medication Solutions | 50090-1403 | RESPIRATORY (INHALATION) | 4.5 ug in 1 1 | 10/17/2023 | |
| Mylan Pharmaceuticals Inc. | 0378-7502 | RESPIRATORY (INHALATION) | 4.5 ug in 1 1 | 9/24/2020 | |
| A-S Medication Solutions | 50090-6382 | RESPIRATORY (INHALATION) | 4.5 ug in 1 1 | 7/24/2019 | |
| Rhodes Pharmaceuticals L.P. | 42858-094 | RESPIRATORY (INHALATION) | 20 ug in 2 mL | 6/1/2023 | |
| Organon LLC | 78206-126 | RESPIRATORY (INHALATION) | 5 ug in 1 1 | 6/5/2025 | |
| Ritedose Pharmaceuticals, LLC | 76204-026 | RESPIRATORY (INHALATION) | 15 ug in 2 mL | 12/20/2023 | |
| AstraZeneca Pharmaceuticals LP | 0310-4600 | RESPIRATORY (INHALATION) | 4.8 ug in 1 1 | 3/24/2023 | |
| RPK Pharmaceuticals, Inc. | 53002-2666 | RESPIRATORY (INHALATION) | 4.5 ug in 1 1 | 7/24/2019 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| SYMBICORT RAPIHALER SUSPENSION FOR INHALATION 80/4.5 mcg/actuation | SIN14962P | AEROSOL, METERED | 4.5 mcg/actuation | 2/24/2016 | |
| DUORESP® SPIROMAX® DRY POWDER FOR INHALATION 320 MCG/9 MCG | SIN16057P | POWDER, METERED | 9 mcg / inhalation | 12/7/2020 | |
| FOSTER NEXTHALER INHALATION POWDER 100 MCG/6 MCG PER DOSE | SIN15332P | POWDER, METERED | 6mcg/dose | 9/19/2017 | |
| DUORESP® SPIROMAX® DRY POWDER FOR INHALATION 160 MCG/4.5 MCG | SIN16056P | POWDER, METERED | 4.5 mcg / inhalation | 12/7/2020 | |
| SYMBICORT RAPIHALER SUSPENSION FOR INHALATION 80/2.25 mcg/actuation | SIN14963P | AEROSOL, METERED | 2.25 mcg/actuation | 2/24/2016 | |
| SYMBICORT RAPIHALER SUSPENSION FOR INHALATION 40/2.25 mcg/actuation | SIN14964P | AEROSOL, METERED | 2.25 mcg/actuation | 2/24/2016 | |
| SYMBICORT RAPIHALER SUSPENSION FOR INHALATION 160/4.5 mcg/actuation | SIN14961P | AEROSOL, METERED | 4.5 mcg/actuation | 2/24/2016 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| Formoterol Fumarate Powder for Inhalation | 国药准字H20103179 | 化学药品 | 吸入剂 | 4/8/2020 | |
| Formoterol Fumarate Powder for Inhalation | 国药准字HJ20130379 | 化学药品 | 吸入粉雾剂 | 12/28/2022 | |
| Formoterol Fumarate Powder for Inhalation | 国药准字HJ20130378 | 化学药品 | 吸入粉雾剂 | 12/28/2022 | |
| Formoterol Fumarate Tablets | 国药准字H20080780 | 化学药品 | 片剂 | 5/22/2023 | |
| Formoterol Fumarate Tablets | 国药准字H20040943 | 化学药品 | 片剂 | 9/25/2020 | |
| Formoterol fumarate Inhalation Solution | 国药准字H20249786 | 化学药品 | 吸入制剂 | 12/25/2024 | |
| Formoterol fumarate Inhalation Solution | 国药准字H20253076 | 化学药品 | 吸入制剂 | 1/8/2025 | |
| Formoterol fumarate Inhalation Solution | 国药准字H20253077 | 化学药品 | 吸入制剂 | 1/8/2025 | |
| Formoterol fumarate Inhalation Solution | 国药准字H20253128 | 化学药品 | 吸入制剂 | 1/14/2025 | |
| Formoterol fumarate Inhalation Solution | 国药准字H20253219 | 化学药品 | 吸入制剂 | 1/14/2025 |
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| FORADILE formoterol (eformoterol) fumarate 12 microgram per capsule (as dihydrate) powder for inhalation | 58673 | Medicine | A | 1/29/1997 |
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