U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H22N2O4
Molecular Weight 378.4211
Optical Activity ( + )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMBRISENTAN

SMILES

COC([C@H](OC1=NC(C)=CC(C)=N1)C(O)=O)(C2=CC=CC=C2)C3=CC=CC=C3

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

Molecular Formula C22H22N2O4
Molecular Weight 378.4211
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

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

2007
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
Endothelin A-receptor blockade in experimental diabetes improves glucose balance and gastrointestinal function.
2002 Aug
Effect of the novel endothelin(A) receptor antagonist LU 208075 on contraction and relaxation of isolated rat basilar artery.
2002 Aug
Ambrisentan (Myogen).
2002 Oct
Endothelin-A receptor blockade improves postischemic hepatic microhemodynamics.
2004 Nov
Changes of vasoregulatory gene expression following hepatic ischemia/reperfusion and treatment with endothelin-A receptor blockade.
2004 Nov
Gateways to clinical trials.
2004 Oct
Improvement of postischemic hepatic microcirculation after endothelinA receptor blockade--endothelin antagonism influences platelet-endothelium interactions.
2005 Feb
Ambrisentan for pulmonary arterial hypertension.
2005 Jul
[Emerging therapies for the treatment of pulmonary arterial hypertension].
2005 Jun
Endothelin receptor antagonism in pulmonary arterial hypertension--a role for selective ET(A) inhibition?
2006 Dec
Attenuation of proinflammatory gene expression and microcirculatory disturbances by endothelin A receptor blockade after orthotopic liver transplantation in pigs.
2006 Jan
Review of bosentan in the management of pulmonary arterial hypertension.
2007
Gateways to clinical trials.
2007 Apr
EndothelinA receptor antagonist BSF-208075 causes immune modulation and neuroprotection after stroke in gerbils.
2007 Jul 9
Gateways to clinical trials.
2007 Mar
Endothelin receptor antagonists in the treatment of pulmonary arterial hypertension.
2007 Mar
Expert opinion on available options treating pulmonary arterial hypertension.
2007 Oct
Therapeutic challenges for systemic sclerosis: facts and future targets.
2007 Sep
Optimizing endothelin receptor antagonist use in the management of pulmonary arterial hypertension.
2008
Ambrisentan.
2008
Endothelin receptor antagonism: role in the treatment of pulmonary arterial hypertension related to scleroderma.
2008
[Treatment of pulmonary arterial hypertension by endothelin receptor antagonists in 2008].
2008 Apr
[Current treatment of systemic sclerosis. Part II. Vascular and antifibrotic treatment].
2008 Aug
Ambrisentan and its role in the management of pulmonary arterial hypertension.
2008 Dec
Pharmacokinetics and safety of ambrisentan in combination with sildenafil in healthy volunteers.
2008 Dec
Endothelin receptor antagonists in pulmonary arterial hypertension.
2008 Feb
[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
Cost-utility of treatments for pulmonary arterial hypertension: a Markov state-transition decision analysis model.
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
Review of inhaled iloprost for the control of pulmonary artery hypertension in children.
2009
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
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
Long-term ambrisentan therapy for the treatment of pulmonary arterial hypertension.
2009 Nov 17
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.
Substance Class Chemical
Created
by admin
on Sat Dec 16 17:32:57 GMT 2023
Edited
by admin
on Sat Dec 16 17:32:57 GMT 2023
Record UNII
HW6NV07QEC
Record Status Validated (UNII)
Record Version
  • Download
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 [INN]
Common Name English
AMBRISENTAN [EMA EPAR]
Common Name English
Ambrisentan [WHO-DD]
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 Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
LIVERTOX NBK548675
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
WHO-VATC QC02KX02
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
WHO-ATC C02KX02
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
EMA ASSESSMENT REPORTS VOLIBRIS (AUTHORIZED: HYPERTENSION, PULMONARY)
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
NCI_THESAURUS C270
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
EU-Orphan Drug EU/3/05/273
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
NDF-RT N0000175581
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
NDF-RT N0000175364
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
Code System Code Type Description
MERCK INDEX
m1648
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY Merck Index
RXCUI
358274
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY RxNorm
CAS
177036-94-1
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
PUBCHEM
6918493
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
ChEMBL
CHEMBL1111
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
SMS_ID
100000089441
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
DRUG CENTRAL
4337
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
IUPHAR
3951
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
DRUG BANK
DB06403
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
DAILYMED
HW6NV07QEC
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
NCI_THESAURUS
C72694
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
FDA UNII
HW6NV07QEC
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
EPA CompTox
DTXSID4046282
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
MESH
C467894
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
INN
8128
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
EVMPD
SUB25424
Created by admin on Sat Dec 16 17:32:58 GMT 2023 , Edited by admin on Sat Dec 16 17:32:58 GMT 2023
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
BINDER->LIGAND
BINDING
TRANSPORTER -> SUBSTRATE
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
ANTAGONIST
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
METABOLITE -> PARENT
PARENT -> METABOLITE
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC