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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H22N2O4
Molecular Weight 378.4219
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMBRISENTAN

SMILES

Cc1cc(C)nc(n1)O[C@]([H])(C(=O)O)C(c2ccccc2)(c3ccccc3)OC

InChI

InChIKey=OUJTZYPIHDYQMC-LJQANCHMSA-N
InChI=1S/C22H22N2O4/c1-15-14-16(2)24-21(23-15)28-19(20(25)26)22(27-3,17-10-6-4-7-11-17)18-12-8-5-9-13-18/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1

HIDE SMILES / InChI
Ambrisentan (alternative Names: BSF 208075; GSK 1325760; GSK1325760A; Letairis) is an endothelin receptor antagonist that is selective for the endothelin type-A (ETA) receptor. The chemical name of ambrisentan is (+)-(2S)-2-[(4,6-dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid. Ambrisentan is indicated for the treatment of pulmonary arterial hypertension. It is approved in Europe, Canada and the United States for use as a single agent to improve exercise ability and delay clinical worsening. In addition, it is approved in the United States for use in combination with tadalafil to reduce the risks of disease progression, hospitalization and to improve exercise ability. As an endothelin receptor antagonist, ambrisentan prevents endogenous endothelin peptide from constricting the muscles in blood vessels, allowing them to relax and permit a reduction in blood pressure. Endothelin-1 (ET-1) is a potent autocrine and paracrine peptide. Two receptor subtypes, ETA and ETB, mediate the effects of ET-1 in the vascular smooth muscle and endothelium. The primary actions of ETA are vasoconstriction and cell proliferation, while the predominant actions of ETB are vasodilation, antiproliferation, and ET-1 clearance. In patients with PAH, plasma ET-1 concentrations are increased as much as 10-fold and correlate with increased mean right atrial pressure and disease severity. ET-1 and ET-1 mRNA concentrations are increased as much as 9-fold in the lung tissue of patients with PAH, primarily in the endothelium of pulmonary arteries. These findings suggest that ET-1 may play a critical role in the pathogenesis and progression of PAH. Ambrisentan is a high-affinity (Ki=0.011 nM) ETA receptor antagonist with a high selectivity for the ETA versus ETB receptor (>4000-fold). The clinical impact of high selectivity for ETA is not known.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.011 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
LETAIRIS

Approved Use

Letairis is indicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1): To improve exercise ability and delay clinical worsening. In combination with tadalafil to reduce the risks of disease progression and hospitalization for worsening PAH, and to improve exercise ability [see Clinical Studies (14.2)

Launch Date

1.18186561E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
838.3 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMBRISENTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
6976.5 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMBRISENTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
18.9 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AMBRISENTAN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9 h
steady-state, oral
AMBRISENTAN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
10 mg 1 times / day multiple, oral
Highest studied dose
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 45.6 years
n = 17
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: 45.6 years
Sex: M+F
Population Size: 17
Sources:
100 mg single, oral
Highest studied dose
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, adult
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
pregnant, adult
Health Status: pregnant
Condition: pulmonary arterial hypertension
Age Group: adult
Sex: F
Sources:
Other AEs: Fetal damage...
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: adult
Sex: M+F
Sources:
Other AEs: Liver injury...
5 mg 1 times / day multiple, oral (max)
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
unhealthy, children
n = 13
Health Status: unhealthy
Condition: heart defects
Age Group: children
Population Size: 13
Sources:
Other AEs: Anemia, Hypertension...
Other AEs:
Anemia (below serious, 2 patients)
Hypertension (below serious, 1 patient)
Sources:
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Other AEs: Anaemia, Acute myocardial infarction...
Other AEs:
Anaemia (serious, 1 patient)
Acute myocardial infarction (serious, 3 patients)
Angina pectoris (serious, 1 patient)
Angina unstable (serious, 1 patient)
Atrial fibrillation (serious, 2 patients)
Sinus tachycardia (serious, 1 patient)
Cardiac failure congestive (serious, 4 patients)
Cardiomegaly (serious, 1 patient)
Dilatation atrial (serious, 1 patient)
Tricuspid valve incompetence (serious, 1 patient)
Palpitations (serious, 1 patient)
Extrasystoles (serious, 1 patient)
Electromechanical dissociation (serious, 1 patient)
Acute vestibular syndrome (serious, 1 patient)
Visual impairment (serious, 1 patient)
Constipation (serious, 4 patients)
Nausea (serious, 2 patients)
Colonic polyp (serious, 1 patient)
Small intestinal obstruction (serious, 1 patient)
Upper gastrointestinal haemorrhage (serious, 1 patient)
Oedema peripheral (serious, 4 patients)
Oedema (serious, 1 patient)
Pain (serious, 2 patients)
Pyrexia (serious, 2 patients)
Fatigue (serious, 2 patients)
Catheter site haemorrhage (serious, 1 patient)
Influenza like illness (serious, 1 patient)
Hyperthermia (serious, 1 patient)
Pharyngitis (serious, 1 patient)
Sinusitis (serious, 1 patient)
Pneumonia (serious, 9 patients)
Bronchitis (serious, 3 patients)
Bronchopneumonia (serious, 1 patient)
Infection (serious, 1 patient)
Cellulitis (serious, 2 patients)
Sepsis (serious, 2 patients)
Influenza (serious, 2 patients)
Urinary tract infection (serious, 1 patient)
Oral candidiasis (serious, 1 patient)
Conjunctivitis viral (serious, 1 patient)
Road traffic accident (serious, 1 patient)
Fracture rib (serious, 1 patient)
Electrocardiogram ST-T segment abnormal (serious, 1 patient)
Electrocardiogram T wave inversion (serious, 1 patient)
Computerised tomogram thorax abnormal (serious, 1 patient)
Hyperkalaemia (serious, 4 patients)
Hypokalaemia (serious, 2 patients)
Hyperglycaemia (serious, 2 patients)
Anorexia (serious, 1 patient)
Diabetic ketoacidosis (serious, 1 patient)
Hypophosphataemia (serious, 1 patient)
Back pain (serious, 1 patient)
Musculoskeletal pain (serious, 1 patient)
Clubbing (serious, 1 patient)
Pain in jaw (serious, 1 patient)
Myalgia (serious, 1 patient)
Squamous cell carcinoma (serious, 1 patient)
Prostate cancer (serious, 1 patient)
Prostate cancer metastatic (serious, 1 patient)
Lung neoplasm malignant (serious, 1 patient)
Headache (serious, 5 patients)
Cerebrovascular accident (serious, 1 patient)
Ischaemic stroke (serious, 1 patient)
Somnolence (serious, 1 patient)
Carotid artery stenosis (serious, 1 patient)
Coma (serious, 1 patient)
Grand mal convulsion (serious, 1 patient)
Nerve compression (serious, 1 patient)
Hypoaesthesia (serious, 1 patient)
Anxiety (serious, 3 patients)
Delirium (serious, 1 patient)
Insomnia (serious, 1 patient)
Renal failure acute (serious, 2 patients)
Renal failure (serious, 1 patient)
Benign prostatic hyperplasia (serious, 1 patient)
Idiopathic pulmonary fibrosis (serious, 20 patients)
Emphysema (serious, 2 patients)
Pulmonary fibrosis (serious, 2 patients)
Pulmonary alveolar haemorrhage (serious, 1 patient)
Dyspnoea (serious, 17 patients)
Respiratory arrest (serious, 1 patient)
Cough (serious, 4 patients)
Haemoptysis (serious, 4 patients)
Productive cough (serious, 1 patient)
Acute respiratory failure (serious, 5 patients)
Respiratory failure (serious, 4 patients)
Nasal congestion (serious, 4 patients)
Allergic rhinitis (serious, 1 patient)
Choking (serious, 1 patient)
Rhinorrhoea (serious, 1 patient)
Hypoxia (serious, 1 patient)
Pneumothorax (serious, 1 patient)
Pneumonitis (serious, 1 patient)
Hiccups (serious, 1 patient)
Pleurisy (serious, 1 patient)
Hypotension (serious, 4 patients)
Hypertension (serious, 3 patients)
Subclavian vein thrombosis (serious, 1 patient)
Flushing (serious, 1 patient)
Hot flush (serious, 1 patient)
Cardiac ventricular disorder (serious, 1 patient)
Peripheral ischaemia (serious, 1 patient)
Oedema peripheral (below serious, 73 patients)
Upper respiratory tract infection (below serious, 47 patients)
Headache (below serious, 47 patients)
Dyspnoea (below serious, 40 patients)
Nasopharyngitis (below serious, 37 patients)
Idiopathic pulmonary fibrosis (below serious, 19 patients)
Nasal congestion (below serious, 27 patients)
Diarrhoea (below serious, 20 patients)
Sinusitis (below serious, 20 patients)
Back pain (below serious, 18 patients)
Dizziness (below serious, 20 patients)
Sources:
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Arterial Hypertension
Population Size: 19
Sources:
Other AEs: Jaw fracture, Edema...
Other AEs:
Jaw fracture (serious, 1 patient)
Edema (below serious, 8 patients)
Diarrhea (below serious, 4 patients)
Paraesthesia (below serious, 4 patients)
Epistaxis (below serious, 3 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Fetal damage grade 5
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
pregnant, adult
Health Status: pregnant
Condition: pulmonary arterial hypertension
Age Group: adult
Sex: F
Sources:
Liver injury serious
5 mg 1 times / day multiple, oral
Recommended
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
unhealthy, adult
Health Status: unhealthy
Condition: pulmonary arterial hypertension
Age Group: adult
Sex: M+F
Sources:
Hypertension below serious, 1 patient
5 mg 1 times / day multiple, oral (max)
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
unhealthy, children
n = 13
Health Status: unhealthy
Condition: heart defects
Age Group: children
Population Size: 13
Sources:
Anemia below serious, 2 patients
5 mg 1 times / day multiple, oral (max)
Dose: 5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 5 mg, 1 times / day
Sources:
unhealthy, children
n = 13
Health Status: unhealthy
Condition: heart defects
Age Group: children
Population Size: 13
Sources:
Back pain below serious, 18 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Idiopathic pulmonary fibrosis below serious, 19 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Diarrhoea below serious, 20 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Dizziness below serious, 20 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Sinusitis below serious, 20 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Nasal congestion below serious, 27 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Nasopharyngitis below serious, 37 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Dyspnoea below serious, 40 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Headache below serious, 47 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Upper respiratory tract infection below serious, 47 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Oedema peripheral below serious, 73 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Acute vestibular syndrome serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Allergic rhinitis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Anaemia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Angina pectoris serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Angina unstable serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Anorexia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Back pain serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Benign prostatic hyperplasia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Bronchopneumonia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Cardiac ventricular disorder serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Cardiomegaly serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Carotid artery stenosis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Catheter site haemorrhage serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Cerebrovascular accident serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Choking serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Clubbing serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Colonic polyp serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Coma serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Computerised tomogram thorax abnormal serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Conjunctivitis viral serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Delirium serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Diabetic ketoacidosis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Dilatation atrial serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Electrocardiogram ST-T segment abnormal serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Electrocardiogram T wave inversion serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Electromechanical dissociation serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Extrasystoles serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Flushing serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Fracture rib serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Grand mal convulsion serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hiccups serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hot flush serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hyperthermia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hypoaesthesia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hypophosphataemia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hypoxia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Infection serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Influenza like illness serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Insomnia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Ischaemic stroke serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Lung neoplasm malignant serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Musculoskeletal pain serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Myalgia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Nerve compression serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Oedema serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Oral candidiasis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pain in jaw serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Palpitations serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Peripheral ischaemia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pharyngitis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pleurisy serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pneumonitis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pneumothorax serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Productive cough serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Prostate cancer metastatic serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Prostate cancer serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pulmonary alveolar haemorrhage serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Renal failure serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Respiratory arrest serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Rhinorrhoea serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Road traffic accident serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Sinus tachycardia serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Sinusitis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Small intestinal obstruction serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Somnolence serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Squamous cell carcinoma serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Subclavian vein thrombosis serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Tricuspid valve incompetence serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Upper gastrointestinal haemorrhage serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Urinary tract infection serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Visual impairment serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Dyspnoea serious, 17 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Atrial fibrillation serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Cellulitis serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Emphysema serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Fatigue serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hyperglycaemia serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hypokalaemia serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Influenza serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Nausea serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pain serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pulmonary fibrosis serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pyrexia serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Renal failure acute serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Sepsis serious, 2 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Idiopathic pulmonary fibrosis serious, 20 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Acute myocardial infarction serious, 3 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Anxiety serious, 3 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Bronchitis serious, 3 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hypertension serious, 3 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Cardiac failure congestive serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Constipation serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Cough serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Haemoptysis serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hyperkalaemia serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Hypotension serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Nasal congestion serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Oedema peripheral serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Respiratory failure serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Acute respiratory failure serious, 5 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Headache serious, 5 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Pneumonia serious, 9 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 329
Health Status: unhealthy
Condition: Early Idiopathic Pulmonary Fibrosis
Population Size: 329
Sources:
Epistaxis below serious, 3 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Arterial Hypertension
Population Size: 19
Sources:
Diarrhea below serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Arterial Hypertension
Population Size: 19
Sources:
Paraesthesia below serious, 4 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Arterial Hypertension
Population Size: 19
Sources:
Edema below serious, 8 patients
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Arterial Hypertension
Population Size: 19
Sources:
Jaw fracture serious, 1 patient
10 mg 1 times / day steady, oral (max)
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy
n = 19
Health Status: unhealthy
Condition: Arterial Hypertension
Population Size: 19
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG


Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no (co-administration study)
Comment: ambrisentan had no inhibitory effect on the P-gp efflux of digoxin
Page: 36, 61
weak [IC50 100 uM]
weak [IC50 45 uM]
weak [IC50 47 uM]
weak [Inhibition 300 uM]
weak [Inhibition 300 uM]
weak [Inhibition 300 uM]
weak [Inhibition 300 uM]
weak
weak
weak
Drug as victim
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Ambrisentan for pulmonary arterial hypertension.
2005 Jul
Management of pulmonary arterial hypertension associated with congenital heart disease.
2007
[Pulmonary hypertension and right ventricular failure. Part XI. Endothelin receptor blockers in the treatment of primary pulmonary arterial hypertension].
2007
Review of bosentan in the management of pulmonary arterial hypertension.
2007
Therapeutic targets in systemic sclerosis.
2007
New drug approved for pulmonary arterial hypertension.
2007 Aug 1
Ambrisentan (Letairis) for pulmonary arterial hypertension.
2007 Oct 22
Therapeutic challenges for systemic sclerosis: facts and future targets.
2007 Sep
Ambrisentan.
2007 Sep
New drugs: ambrisentan, temsirolimus, and eculizumab.
2007 Sep-Oct
Ambrisentan.
2008
Endothelin receptor antagonism: role in the treatment of pulmonary arterial hypertension related to scleroderma.
2008
Effects of selective and unselective endothelin-receptor antagonists on prostacyclin synthase gene expression in experimental pulmonary hypertension.
2008
Endothelin receptor antagonists for pulmonary arterial hypertension: rationale and place in therapy.
2008
[Treatment of pulmonary arterial hypertension by endothelin receptor antagonists in 2008].
2008 Apr
Inhibition of endothelin receptors in the treatment of pulmonary arterial hypertension: does selectivity matter?
2008 Aug
Ambrisentan and its role in the management of pulmonary arterial hypertension.
2008 Dec
Acute right ventricular failure in the setting of acute pulmonary embolism or chronic pulmonary hypertension: a detailed review of the pathophysiology, diagnosis, and management.
2008 Feb
Endothelin receptor antagonists in pulmonary arterial hypertension.
2008 Feb
Pulmonary hypertension: past, present and future.
2008 Jan
The management of pulmonary hypertension in children.
2008 Jul
The status of pulmonary arterial hypertension in 2008.
2008 Jun 10
Ambrisentan for the treatment of pulmonary arterial hypertension: results of the ambrisentan in pulmonary arterial hypertension, randomized, double-blind, placebo-controlled, multicenter, efficacy (ARIES) study 1 and 2.
2008 Jun 10
Gateways to clinical trials.
2008 Mar
The endothelin system as a therapeutic target in cardiovascular disease: great expectations or bleak house?
2008 Mar
Ambrisentan for the management of pulmonary arterial hypertension.
2008 May
[Systemic sclerosis].
2008 May
[Specific drugs for the treatment of pulmonary arterial hypertension - current status].
2008 Oct
Pulmonary arterial hypertension: on the way to a manageable disease.
2008 Sep
Therapeutic methods used in patients with Eisenmenger syndrome.
2009
Bosentan in the treatment of pulmonary arterial hypertension with the focus on the mildly symptomatic patient.
2009
Oral therapies for the treatment of pulmonary arterial hypertension: a population-based cost-minimization analysis.
2009
Endothelin-1 inhibition by ambrisentan as a potential treatment adjunct after debulking surgery in epithelial ovarian cancer.
2009
Ambrisentan: new drug. Too risky in mildly symptomatic pulmonary hypertension.
2009 Apr
Gateways to clinical trials.
2009 Apr
Use of inhaled iloprost in an infant with bronchopulmonary dysplasia and pulmonary artery hypertension.
2009 Aug
Ambrisentan, an endothelin receptor type A-selective endothelin receptor antagonist, for the treatment of pulmonary arterial hypertension.
2009 Aug
Endothelin receptor antagonists for pulmonary hypertension in adult patients with sickle cell disease.
2009 Dec
A meta-analysis of randomized controlled trials in pulmonary arterial hypertension.
2009 Feb
Pulmonary arterial hypertension in children: a medical update.
2009 Jan
Ambrisentan therapy in patients with pulmonary arterial hypertension who discontinued bosentan or sitaxsentan due to liver function test abnormalities.
2009 Jan
Gateways to clinical trials.
2009 Jun
Small-molecule endothelin receptor antagonists: a review of patenting activity across therapeutic areas.
2009 Jun
Effect of ketoconazole on the pharmacokinetic profile of ambrisentan.
2009 Jun
New concepts in the invasive and non invasive evaluation of remodelling of the right ventricle and pulmonary vasculature in pulmonary arterial hypertension.
2009 Mar 12
The pharmacokinetics and pharmacodynamics of warfarin in combination with ambrisentan in healthy volunteers.
2009 May
Gateways to clinical trials.
2009 Nov
Gateways to clinical trials.
2009 Sep
Safety and tolerability of bosentan in the management of pulmonary arterial hypertension.
2009 Sep 21
Pharmacotherapy in pulmonary arterial hypertension: a systematic review and meta-analysis.
2010 Jan 29
Patents

Sample Use Guides

In Vivo Use Guide
Curator's Comment:: Doses higher than 10 mg once daily have not been studied in patients with pulmonary arterial hypertension
5 mg once daily, and consider increasing the dose to 10 mg once daily if 5 mg is tolerated. Tablets may be administered with or without food.
Route of Administration: Oral
The effect of the novel and ET(A) receptor selective antagonist LU 208075 (AMBRISENTAN) was characterized by the contraction and relaxation induced by ET-1 and bigET-1 on rat basilar artery. Concentration-effect curves were constructed by cumulative application of ET-1 or bigET-1 in the presence of LU 208075 (10(-7)M, 10(-6)M, and 10(-5)M). The effect of LU 208075 was determined by the pA(2) value. The contraction by ET-1 and bigET-1 was inhibited by LU 208075 in a dose-dependent manner.
Name Type Language
AMBRISENTAN
EMA EPAR   INN   JAN   MART.   MI   ORANGE BOOK   VANDF   WHO-DD  
INN  
Official Name English
AMBRISENTAN [MI]
Common Name English
(+)-(2S)-2-((4,6-DIMETHYLPYRIMIDIN-2-YL)OXY)-3-METHOXY-3,3-DIPHENYLPROPANOIC ACID
Systematic Name English
AMBRISENTAN [JAN]
Common Name English
GSK1325760
Code English
AMBRISENTAN [ORANGE BOOK]
Common Name English
GSK-1325760
Code English
LU-208075
Code English
LETAIRIS
Brand Name English
VOLIBRIS
Brand Name English
AMBRISENTAN [MART.]
Common Name English
GSK1325760A
Code English
AMBRISENTAN [WHO-DD]
Common Name English
AMBRISENTAN [INN]
Common Name English
AMBRISENTAN [EMA EPAR]
Common Name English
GSK-1325760A
Code English
AMBRISENTAN [VANDF]
Common Name English
AMBRISENTAN, (+)-
Common Name English
Classification Tree Code System Code
WHO-ATC C02KX52
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
LIVERTOX 35
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
WHO-VATC QC02KX02
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
WHO-ATC C02KX02
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
EMA ASSESSMENT REPORTS VOLIBRIS (AUTHORIZED: HYPERTENSION, PULMONARY)
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
NCI_THESAURUS C270
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
EU-Orphan Drug EU/3/05/273
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
NDF-RT N0000175581
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
NDF-RT N0000175364
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
Code System Code Type Description
MERCK INDEX
M1648
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY Merck Index
RXCUI
358274
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY RxNorm
CAS
177036-94-1
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
PUBCHEM
6918493
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
ChEMBL
CHEMBL1111
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
DRUG CENTRAL
4337
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
IUPHAR
3951
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
DRUG BANK
DB06403
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
NCI_THESAURUS
C72694
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
FDA UNII
HW6NV07QEC
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
EPA CompTox
177036-94-1
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
MESH
C467894
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
INN
8128
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY
EVMPD
SUB25424
Created by admin on Sat Jun 26 06:20:00 UTC 2021 , Edited by admin on Sat Jun 26 06:20:00 UTC 2021
PRIMARY