Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C19H24N2O4.C4H6O6 |
Molecular Weight | 494.4917 |
Optical Activity | ( - ) |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@H]([C@@H](O)C(O)=O)C(O)=O.COC1=CC=C(C[C@@H](C)NC[C@H](O)C2=CC=C(O)C(NC=O)=C2)C=C1
InChI
InChIKey=FCSXYHUNDAXDRH-OKMNHOJOSA-N
InChI=1S/C19H24N2O4.C4H6O6/c1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22;5-1(3(7)8)2(6)4(9)10/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22);1-2,5-6H,(H,7,8)(H,9,10)/t13-,19+;1-,2-/m11/s1
Molecular Formula | C4H6O6 |
Molecular Weight | 150.0868 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | C19H24N2O4 |
Molecular Weight | 344.4049 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/14725487
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/14725487
Sepracor in the US is developing arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral canters and is being developed as an inhaled preparation for the treatment of respiratory disorders. Sepracor believes that arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. The pharmacologic effects of beta2-adrenoceptor agonist drugs, including arformoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3′,5′-adenosine monophosphate (cyclic AMP). Increased intracellular cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL210 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20406080 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Palliative | BROVANA Approved UseBROVANA Inhalation Solution is a long-acting beta2-adrenergic agonist (beta2-agonist) indicated for: Long-term, twice daily (morning and evening) administration in the maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. (1.1) Important limitations of use: BROVANA Inhalation Solution is not indicated to treat acute deteriorations of chronic obstructive pulmonary disease. (1.2, 5.2) BROVANA Inhalation Solution is not indicated to treat asthma. (1.2) 1.1 Maintenance Treatment of COPD BROVANA (arformoterol tartrate) Inhalation Solution is indicated for the long-term, twice daily (morning and evening) maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. BROVANA Inhalation Solution is for use by nebulization only. 1.2 Important Limitations of Use BROVANA Inhalation Solution is not indicated to treat acute deteriorations of chronic obstructive pulmonary disease [see WARNINGS AND PRECAUTIONS (5.2) Launch Date1.16009284E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4.3 pg/mL |
15 μg 2 times / day steady-state, respiratory dose: 15 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: |
ARFORMOTEROL plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
26.65 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24746942 |
24 μg single, respiratory dose: 24 μg route of administration: Respiratory experiment type: SINGLE co-administered: BECLOMETHASONE 17-MONOPROPIONATE |
FORMOTEROL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
22.3 nM |
10 μg single, respiratory dose: 10 μg route of administration: Respiratory experiment type: SINGLE co-administered: MOMETASONE FUROATE |
FORMOTEROL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
34.5 pg × h/mL |
15 μg 2 times / day steady-state, respiratory dose: 15 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: |
ARFORMOTEROL plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
104.52 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24746942 |
24 μg single, respiratory dose: 24 μg route of administration: Respiratory experiment type: SINGLE co-administered: BECLOMETHASONE 17-MONOPROPIONATE |
FORMOTEROL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
33.7 pM × h |
10 μg single, respiratory dose: 10 μg route of administration: Respiratory experiment type: SINGLE co-administered: MOMETASONE FUROATE |
FORMOTEROL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
26 h |
15 μg 2 times / day steady-state, respiratory dose: 15 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: |
ARFORMOTEROL plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
4.71 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/24746942 |
24 μg single, respiratory dose: 24 μg route of administration: Respiratory experiment type: SINGLE co-administered: BECLOMETHASONE 17-MONOPROPIONATE |
FORMOTEROL plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
48% |
15 μg 2 times / day steady-state, respiratory dose: 15 μg route of administration: Respiratory experiment type: STEADY-STATE co-administered: |
ARFORMOTEROL plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
37.5% |
FORMOTEROL plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Other AEs: Diarrhea, Nausea... Other AEs: Diarrhea (6%) Sources: Nausea (6%) Nasopharyngitis (4%) Dry mouth (4%) Vomiting (3%) Dizziness (3%) Insomnia (3%) |
25 ug 2 times / day multiple, respiratory Highest studied dose Dose: 25 ug, 2 times / day Route: respiratory Route: multiple Dose: 25 ug, 2 times / day Sources: Page: p.21 |
unhealthy, 63.8 n = 147 Health Status: unhealthy Condition: Chronic obstructive pulmonary disease Age Group: 63.8 Sex: M+F Population Size: 147 Sources: Page: p.21 |
|
30 ug 2 times / day multiple, respiratory (total) Recommended Dose: 30 ug, 2 times / day Route: respiratory Route: multiple Dose: 30 ug, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Chronic obstructive pulmonary disease Sources: Page: p.1 |
Disc. AE: Bronchospasm paradoxical... AEs leading to discontinuation/dose reduction: Bronchospasm paradoxical (grade 4) Sources: Page: p.1 |
15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Other AEs: Angina pectoris, Angina unstable... Other AEs: Angina pectoris (serious, 3 patients) Sources: Angina unstable (serious, 1 patient) Atrial fibrillation (serious, 3 patients) Cardio-respiratory arrest (serious, 2 patients) Cor pulmonale (serious, 1 patient) Coronary artery disease (serious, 3 patients) Myocardial ischaemia (serious, 1 patient) Vertigo (serious, 1 patient) Iridocyclitis (serious, 1 patient) Barrett's oesophagus (serious, 1 patient) Diverticular perforation (serious, 1 patient) Gastric ulcer haemorrhage (serious, 1 patient) Gastritis erosive (serious, 1 patient) Hiatus hernia (serious, 1 patient) Intestinal perforation (serious, 1 patient) Pancreatitis acute (serious, 1 patient) Non-cardiac chest pain (serious, 3 patients) Oedema peripheral (serious, 1 patient) Cholecystitis (serious, 1 patient) Bronchopneumonia (serious, 1 patient) Clostridial infection (serious, 1 patient) Clostridium difficile colitis (serious, 1 patient) Gastroenteritis bacterial (serious, 1 patient) Osteomyelitis (serious, 1 patient) Osteotomy (serious, 1 patient) Osteomyelitis acute (serious, 1 patient) Postoperative wound infection (serious, 1 patient) Sepsis (serious, 3 patients) Urinary tract infection (serious, 1 patient) Accidental overdose (serious, 1 patient) Ankle fracture (serious, 1 patient) Cervical vertebral fracture (serious, 1 patient) Head injury (serious, 1 patient) Incisional hernia (serious, 1 patient) Open wound (serious, 1 patient) Tibia fracture (serious, 1 patient) Muscular weakness (serious, 1 patient) Rotator cuff syndrome (serious, 1 patient) Brain neoplasm (serious, 1 patient) Metastases to lymph nodes (serious, 1 patient) Oesophageal carcinoma (serious, 1 patient) Squamous cell carcinoma (serious, 1 patient) Throat cancer (serious, 1 patient) Carotid artery disease (serious, 1 patient) Headache (serious, 1 patient) Ischaemic stroke (serious, 1 patient) Sensory disturbance (serious, 1 patient) Transient ischaemic attack (serious, 1 patient) Major depression (serious, 2 patients) Mental status changes (serious, 1 patient) Nephropathy (serious, 1 patient) Renal artery stenosis (serious, 1 patient) Renal failure (serious, 1 patient) Acute respiratory distress syndrome (serious, 1 patient) Bronchiectasis (serious, 1 patient) Hypoxia (serious, 1 patient) Respiratory arrest (serious, 1 patient) Urticaria (serious, 1 patient) Aortic aneurysm (serious, 1 patient) Hypertensive crisis (serious, 1 patient) Hypotension (serious, 1 patient) Iliac artery stenosis (serious, 2 patients) Peripheral arterial occlusive disease (serious, 1 patient) Bronchitis (below serious, 43 patients) Nasopharyngitis (below serious, 38 patients) Upper respiratory tract infection (below serious, 22 patients) Headache (below serious, 35 patients) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dizziness | 3% | 20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Insomnia | 3% | 20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Vomiting | 3% | 20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Dry mouth | 4% | 20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Nasopharyngitis | 4% | 20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Diarrhea | 6% | 20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Nausea | 6% | 20 ug 2 times / day steady, respiratory Recommended Dose: 20 ug, 2 times / day Route: respiratory Route: steady Dose: 20 ug, 2 times / day Sources: |
unhealthy, 40-90 years n = 123 Health Status: unhealthy Condition: COPD Age Group: 40-90 years Sex: M+F Population Size: 123 Sources: |
Bronchospasm paradoxical | grade 4 Disc. AE |
30 ug 2 times / day multiple, respiratory (total) Recommended Dose: 30 ug, 2 times / day Route: respiratory Route: multiple Dose: 30 ug, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Chronic obstructive pulmonary disease Sources: Page: p.1 |
Upper respiratory tract infection | below serious, 22 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Headache | below serious, 35 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Nasopharyngitis | below serious, 38 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Bronchitis | below serious, 43 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Accidental overdose | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Acute respiratory distress syndrome | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Angina unstable | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Ankle fracture | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Aortic aneurysm | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Barrett's oesophagus | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Brain neoplasm | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Bronchiectasis | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Bronchopneumonia | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Carotid artery disease | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Cervical vertebral fracture | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Cholecystitis | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Clostridial infection | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Clostridium difficile colitis | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Cor pulmonale | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Diverticular perforation | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Gastric ulcer haemorrhage | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Gastritis erosive | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Gastroenteritis bacterial | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Head injury | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Headache | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Hiatus hernia | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Hypertensive crisis | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Hypotension | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Hypoxia | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Incisional hernia | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Intestinal perforation | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Iridocyclitis | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Ischaemic stroke | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Mental status changes | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Metastases to lymph nodes | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Muscular weakness | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Myocardial ischaemia | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Nephropathy | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Oedema peripheral | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Oesophageal carcinoma | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Open wound | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Osteomyelitis acute | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Osteomyelitis | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Osteotomy | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Pancreatitis acute | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Peripheral arterial occlusive disease | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Postoperative wound infection | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Renal artery stenosis | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Renal failure | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Respiratory arrest | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Rotator cuff syndrome | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Sensory disturbance | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Squamous cell carcinoma | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Throat cancer | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Tibia fracture | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Transient ischaemic attack | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Urinary tract infection | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Urticaria | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Vertigo | serious, 1 patient | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Cardio-respiratory arrest | serious, 2 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Iliac artery stenosis | serious, 2 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Major depression | serious, 2 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Angina pectoris | serious, 3 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Atrial fibrillation | serious, 3 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Coronary artery disease | serious, 3 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Non-cardiac chest pain | serious, 3 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Sepsis | serious, 3 patients | 15 ug 2 times / day steady, respiratory Dose: 15 ug, 2 times / day Route: respiratory Route: steady Dose: 15 ug, 2 times / day Sources: |
unhealthy n = 420 Health Status: unhealthy Condition: COPD Population Size: 420 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 38.0 |
inconclusive | |||
Page: (ClinPharm1) 11, 14, (ClinPharm2) 4-7 |
moderate [Ki 33 uM] | |||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
no [IC50 >133 uM] | ||||
Page: 28.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=4 Page: (ClinPharm2) 4-7 |
no | |||
Page: 37, 52 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=4 Page: (ClinPharm2) 4-7 |
no | |||
Page: 37, 52 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=4 Page: (ClinPharm2) 4-7 |
no | |||
Page: 37, 52 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=4 Page: (ClinPharm2) 4-7 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=4 Page: (ClinPharm2) 4-7 |
no | |||
Page: 37.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=4 Page: (ClinPharm2) 4-7 |
no | |||
Page: 37.0 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=4 Page: (ClinPharm2) 4-7 |
no | |||
Page: 37.0 |
no | |||
Page: 37, 52 |
no | no (co-administration study) Comment: coadministration with paroxetine did not affect exposure to either drug Page: 37, 52 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 38.0 |
inconclusive | |||
Page: (Label1) 4, (Label2) 14, (ClinPharm1) 11, 14, (ClinPharm2) 2-3 |
major | |||
Page: (Label1) 4, (ClinPharm1) 11, 14, (ClinPharm2) 2-3 |
minor | |||
Page: (Label1) 4, (Label2) 14, (ClinPharm1) 11, 14, (ClinPharm2) 2-3 |
minor | |||
Page: (Label1) 4, (Label2) 14, (ClinPharm1) 11, 14, (ClinPharm2) 2-3 |
minor | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=2 Page: (ClinPharm2) 2-3, , (PMDA) 16 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=2 Page: (ClinPharm2) 2-3, (PMDA) 16 |
no | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2001/20831_Foradil_clinphrmr_P2.pdf#page=2 Page: (ClinPharm2) 2-3, (PMDA) 16 |
no | |||
weak | ||||
Page: 17.0 |
yes | |||
yes | ||||
Page: 28.0 |
yes | |||
Page: 28.0 |
yes | |||
yes | ||||
yes | ||||
Page: 28.0 |
yes | |||
yes | ||||
Page: 28.0 |
yes | |||
yes | ||||
Page: 28.0 |
yes | |||
Page: 17, 37 |
yes | no (co-administration study) Comment: coadministration with paroxetine caused a slight increase in paroxetine; dose adjustment is not required when coadministered with therapeutic agents that are potent inhibitors of CYP2D6 Page: 17, 37 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: 25, 29 |
PubMed
Title | Date | PubMed |
---|---|---|
Tachyphylaxis following regular use of formoterol in exercise-induced bronchospasm. | 2001 |
|
The lung as a route for systemic delivery of therapeutic proteins and peptides. | 2001 |
|
Comparison of the anti-bronchoconstrictor activities of inhaled formoterol, its (R,R)- and (S,S)-enantiomers and salmeterol in the rhesus monkey. | 2001 |
|
Inhaled budesonide/formoterol combination. | 2001 |
|
Long-acting asthma medication, new inhaler approved by FDA. | 2001 Apr 1 |
|
Clinical outcome of adding long-acting beta-agonists to inhaled corticosteroids. | 2001 Aug |
|
Development of a lyophilized formulation for (R,R)-formoterol (L)-tartrate. | 2001 Jan |
|
Comparison between formoterol 12 microg b.i.d. and on-demand salbutamol in moderate persistent asthma. | 2001 Jan |
|
A randomized, 12-week, double-blind, placebo-controlled study comparing formoterol dry powder inhaler with albuterol metered-dose inhaler. | 2001 Jan |
|
Comparison of formoterol and terbutaline for as-needed treatment of asthma: a randomised trial. | 2001 Jan 27 |
|
Bronchodilation and bronchoprotection in asthmatic preschool children from formoterol administered by mechanically actuated dry-powder inhaler and spacer. | 2001 Jul 15 |
|
Protection against cold air and exercise-induced bronchoconstriction while on regular treatment with Oxis. | 2001 Jun |
|
Reversing acute bronchoconstriction in asthma: the effect of bronchodilator tolerance after treatment with formoterol. | 2001 Mar |
|
A placebo-controlled clinical trial of regular monotherapy with short-acting and long-acting beta(2)-agonists in allergic asthmatic patients. | 2001 May |
|
Rapid onset of bronchodilation in COPD: a placebo-controlled study comparing formoterol (Foradil Aerolizer) with salbutamol (Ventodisk). | 2001 Oct |
|
[The effect of triamcinolone, montelukast and formoterol on serum levels of il-4, IgE and clinical parameters in children with asthma]. | 2001 Sep |
|
A cost-effectiveness study comparing the as-needed use of formoterol (Oxis) and terbutaline (Bricanyl) in patients with moderate to severe asthma. | 2001 Sep |
|
Effects of budesonide and formoterol on NF-kappaB, adhesion molecules, and cytokines in asthma. | 2001 Sep 15 |
|
Long-acting inhaled beta(2)-agonist therapy in asthma. | 2001 Sep 15 |
|
Biological actions of formoterol isomers. | 2002 |
|
A post-marketing surveillance study of formoterol (Foradil): its use in general practice in England. | 2002 |
|
Formoterol as dry powder oral inhalation compared with salbutamol metered-dose inhaler in acute exacerbations of chronic obstructive pulmonary disease. | 2002 Apr |
|
Potential masking effect on dyspnoea perception by short- and long-acting beta2-agonists in asthma. | 2002 Feb |
|
The whole story: treatment outcomes with Symbicort. | 2002 Feb |
Patents
Sample Use Guides
15 ug administered twice a day (morning and evening) by nebulization. A total daily dose greater than 30 ug (15 ug twice daily) is not recommended. BROVANA (arformoterol tartrate) should be administered by the inhaled route via a standard jet nebulizer connected to an air compressor
Route of Administration:
Respiratory
In Vitro Use Guide
Curator's Comment: In vitro tests show that arformoterol is an inhibitor of the release of mast cell mediators, such as histamine and leukotrienes, from the human lung. Arformoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness.
Unknown
Substance Class |
Chemical
Created
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Record UNII |
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C319
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NCI_THESAURUS |
C48149
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200815-49-2
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DBSALT001387
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M5542
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SUB32085
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9827062
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100000124467
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C65240
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668284
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CHEMBL1363
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DTXSID80173903
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |
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