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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H17F2N5OS
Molecular Weight 437.467
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ISAVUCONAZOLE

SMILES

C[C@@]([H])(c1nc(cs1)-c2ccc(cc2)C#N)[C@](Cn3cncn3)(c4cc(ccc4F)F)O

InChI

InChIKey=DDFOUSQFMYRUQK-RCDICMHDSA-N
InChI=1S/C22H17F2N5OS/c1-14(21-28-20(10-31-21)16-4-2-15(9-25)3-5-16)22(30,11-29-13-26-12-27-29)18-8-17(23)6-7-19(18)24/h2-8,10,12-14,30H,11H2,1H3/t14-,22+/m0/s1

HIDE SMILES / InChI

Description
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24187505

Isavuconazole is an active form of isavuconazonium, a prodrug which is marketed under the name Cresemba. Isavuconazole inhibits lanosterol 14-alpha demethylase (or CYP51A1) and leads to the accumulation of ergosterol toxic precursors in the fungal cytoplasm. Isavuconazole is indicated for the treatment of invasive aspergillosis and invasive mucormycosis.

CNS Activity

Curator's Comment:: Oral administration of 25 mg/kg isavuconazonium sulfate to rats resulted in isavuconazole brain at levels about twice those detected in the plasma.

Originator

Curator's Comment:: # Hoffmann-La Roche

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
CRESEMBA

Approved Use

Cresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis.

Launch Date

1.42560002E12
Curative
CRESEMBA

Approved Use

Cresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis.

Launch Date

1.42560002E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7499 ng/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
20028 ng/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
121402 ng × h/mL
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
352805 ng × h/mL
600 mg 1 times / day steady-state, oral
dose: 600 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
130 h
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
200 mg 1 times / day steady-state, oral
dose: 200 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ISAVUCONAZOLE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (0.2%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (0.4%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138
Disc. AE: Blood creatinine increased...
AEs leading to
discontinuation/dose reduction:
Blood creatinine increased (0.6%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (0.2%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134
healthy, adult
n = 6
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 6
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (16.7%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135
healthy, adult
n = 6
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 6
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (16.7%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140
Disc. AE: Diarrhea...
AEs leading to
discontinuation/dose reduction:
Diarrhea (2.6%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141
Disc. AE: Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (5.1%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142
Disc. AE: Vomiting...
AEs leading to
discontinuation/dose reduction:
Vomiting (2.6%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143
Disc. AE: Disturbance in attention...
AEs leading to
discontinuation/dose reduction:
Disturbance in attention (5.1%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144
Disc. AE: Dizziness...
AEs leading to
discontinuation/dose reduction:
Dizziness (5.1%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145
Disc. AE: Headache...
AEs leading to
discontinuation/dose reduction:
Headache (7.7%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146
Disc. AE: Anxiety...
AEs leading to
discontinuation/dose reduction:
Anxiety (7.7%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147
Disc. AE: Hot flush...
AEs leading to
discontinuation/dose reduction:
Hot flush (7.7%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 39.1 years
n = 41
Health Status: unhealthy
Condition: uncomplicated esophageal candidiasis
Age Group: mean age 39.1 years
Sex: M+F
Population Size: 41
Sources:
Disc. AE: Atrioventricular block...
AEs leading to
discontinuation/dose reduction:
Atrioventricular block (grade 2, 2.4%)
Sources:
533.3 mg 3 times / day multiple, oral (mean)
Highest studied dose
Dose: 533.3 mg, 3 times / day
Route: oral
Route: multiple
Dose: 533.3 mg, 3 times / day
Sources:
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources:
Other AEs: Rash...
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Disc. AE: Dizziness, Hypersensitivity...
Other AEs: Headache, Headache...
AEs leading to
discontinuation/dose reduction:
Dizziness (8.3%)
Hypersensitivity (8.3%)
Nausea (8.3%)
Other AEs:
Headache (grade 1, 8.3%)
Headache (grade 2, 8.3%)
Rash (grade 1, 8.3%)
Rash (grade 2, 8.3%)
Cough (grade 1, 16.7%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Disc. AE: Pancytopenia, Cardiac arrest...
AEs leading to
discontinuation/dose reduction:
Pancytopenia (0.4%)
Cardiac arrest (0.4%)
Cardio-respiratory arrest (0.4%)
Congestive cardiomyopathy (0.4%)
Supraventricular tachycardia (0.4%)
Optic neuropathy (0.4%)
Dysphagia (0.4%)
Small intestinal obstruction (0.4%)
Vomiting (0.4%)
Chills (0.4%)
Hepatitis acute (0.4%)
Aspergillosis (0.4%)
Bronchopneumonia (0.4%)
Bronchopulmonary aspergillosis (0.4%)
Endocarditis (0.4%)
Fungal infection (0.8%)
Infection (0.4%)
Pneumonia (0.4%)
Sepsis (0.4%)
Septic shock (0.8%)
Blood bilirubin increased (0.8%)
Blood sodium decreased (0.4%)
Transaminases increased (0.4%)
Myositis (0.4%)
Convulsion (0.8%)
Encephalopathy (0.4%)
Epilepsy (0.8%)
Confusional state (0.8%)
Renal failure (0.8%)
Renal failure acute (0.4%)
Acute respiratory failure (0.4%)
Dyspnoea (0.8%)
Respiratory distress (0.4%)
Respiratory failure (0.8%)
Dermatitis (0.4%)
Dermatitis allergic (0.4%)
Hypotension (0.4%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
Disc. AE: Acute respiratory failure, Chills...
AEs leading to
discontinuation/dose reduction:
Acute respiratory failure (0.4%)
Chills (0.4%)
Convulsion (0.8%)
Dyspnoea (0.8%)
Epilepsy (0.4%)
Hypotension (0.4%)
Respiratory failure (0.8%)
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
AEs

AEs

AESignificanceDosePopulation
Diarrhea 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.136
Vomiting 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.137
Blood creatinine increased 0.6%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.138
Headache 0.2%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139
healthy, adult
n = 490
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 490
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.139
Diarrhea 16.7%
Disc. AE
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134
healthy, adult
n = 6
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 6
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.134
Headache 16.7%
Disc. AE
40 mg 1 times / day multiple, oral
Studied dose
Dose: 40 mg, 1 times / day
Route: oral
Route: multiple
Dose: 40 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135
healthy, adult
n = 6
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 6
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.135
Diarrhea 2.6%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.140
Nausea 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.141
Vomiting 2.6%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.142
Disturbance in attention 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.143
Dizziness 5.1%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.144
Headache 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.145
Anxiety 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.146
Hot flush 7.7%
Disc. AE
600 mg 1 times / day multiple, oral
Studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147
healthy, adult
n = 39
Health Status: healthy
Age Group: adult
Sex: M+F
Population Size: 39
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.147
Atrioventricular block grade 2, 2.4%
Disc. AE
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
unhealthy, mean age 39.1 years
n = 41
Health Status: unhealthy
Condition: uncomplicated esophageal candidiasis
Age Group: mean age 39.1 years
Sex: M+F
Population Size: 41
Sources:
Rash 8.3%
533.3 mg 3 times / day multiple, oral (mean)
Highest studied dose
Dose: 533.3 mg, 3 times / day
Route: oral
Route: multiple
Dose: 533.3 mg, 3 times / day
Sources:
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources:
Dizziness 8.3%
Disc. AE
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Hypersensitivity 8.3%
Disc. AE
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Nausea 8.3%
Disc. AE
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Cough grade 1, 16.7%
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Headache grade 1, 8.3%
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Rash grade 1, 8.3%
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Headache grade 2, 8.3%
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Rash grade 2, 8.3%
400 mg 1 times / day multiple, oral (mean)
Studied dose
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
unhealthy, mean age 48.4 years
n = 12
Health Status: unhealthy
Condition: acute myeloid leukemia
Age Group: mean age 48.4 years
Sex: M+F
Population Size: 12
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31
Acute respiratory failure 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Aspergillosis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Blood sodium decreased 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Bronchopneumonia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Bronchopulmonary aspergillosis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Cardiac arrest 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Cardio-respiratory arrest 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Chills 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Congestive cardiomyopathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Dermatitis allergic 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Dermatitis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Dysphagia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Encephalopathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Endocarditis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Hepatitis acute 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Hypotension 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Infection 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Myositis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Optic neuropathy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Pancytopenia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Pneumonia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Renal failure acute 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Respiratory distress 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Sepsis 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Small intestinal obstruction 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Supraventricular tachycardia 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Transaminases increased 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Vomiting 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Blood bilirubin increased 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Confusional state 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Convulsion 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Dyspnoea 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Epilepsy 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Fungal infection 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Renal failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Respiratory failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Septic shock 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131
Acute respiratory failure 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
Chills 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
Epilepsy 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
Hypotension 0.4%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
Convulsion 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
Dyspnoea 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
Respiratory failure 0.8%
Disc. AE
200 mg 1 times / day multiple, oral
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
unhealthy, mean age 51.1 years
n = 257
Health Status: unhealthy
Condition: Invasive aspergillosis
Age Group: mean age 51.1 years
Sex: M+F
Population Size: 257
Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes [IC50 11.2 uM]
yes [IC50 25.7 uM]
yes [IC50 6.31 uM]
yes [IC50 92 uM]
yes [Ki 0.59 uM]
yes [Ki 0.622 uM]
yes [Ki 1.74 uM]
yes [Ki 2.86 uM]
yes [Ki 4.78 uM]
yes [Ki 4.82 uM]
yes [Ki 5.4 uM]
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
yes
yes
yes
yes (co-administration study)
Comment: Upon coadministration, ketoconazole increased the isavuconazole Cmax by 9% and isavuconazole AUC by 422% after multiple dose administration of ketoconazole (200 mg twice daily) for 24 days and a single dose of isavuconazonium equivalent to 200 mg of isavuconazole.
Page: 19.0
Tox targets
PubMed

PubMed

TitleDatePubMed
Drug evaluation: BAL-8557--a novel broad-spectrum triazole antifungal.
2006 Aug
Multiple-dose pharmacokinetics and safety of the new antifungal triazole BAL4815 after intravenous infusion and oral administration of its prodrug, BAL8557, in healthy volunteers.
2006 Jan
Single-ascending-dose pharmacokinetics and safety of the novel broad-spectrum antifungal triazole BAL4815 after intravenous infusions (50, 100, and 200 milligrams) and oral administrations (100, 200, and 400 milligrams) of its prodrug, BAL8557, in healthy volunteers.
2006 Jan
Investigational antimicrobial drugs for bloodstream infections.
2008 Aug
New and investigational triazole agents for the treatment of invasive fungal infections.
2008 Dec
Isavuconazole: a new and promising antifungal triazole for the treatment of invasive fungal infections.
2008 Dec
New and emerging treatments for fungal infections.
2008 Jan
Cryptococcus gattii: An Emerging Cause of Fungal Disease in North America.
2009
In vitro activities of isavuconazole against opportunistic filamentous and dimorphic fungi.
2009 Feb
Efficacy of isavuconazole, voriconazole and fluconazole in temporarily neutropenic murine models of disseminated Candida tropicalis and Candida krusei.
2009 Jan
Antifungal susceptibilities among different serotypes of Cryptococcus gattii and Cryptococcus neoformans.
2009 Jan
In vitro activity of isavuconazole against Trichosporon, Rhodotorula, Geotrichum, Saccharomyces and Pichia species.
2009 Jul
In vitro antifungal activity of isavuconazole against 345 mucorales isolates collected at study centers in eight countries.
2009 Jun
New triazoles and echinocandins: mode of action, in vitro activity and mechanisms of resistance.
2009 Oct
Comparison of adverse events between oral and intravenous formulations of antimicrobial agents: a systematic review of the evidence from randomized trials.
2009 Oct
New generation azole antifungals in clinical investigation.
2009 Sep
Clinical safety and tolerability issues in use of triazole derivatives in management of fungal infections.
2010
In vitro activities of eight antifungal drugs against 55 clinical isolates of Fonsecaea spp.
2010 Apr
[Recent advances in the study of new antifungal lead compounds].
2010 Aug
Rhinocladiella aquaspersa, proven agent of verrucous skin infection and a novel type of chromoblastomycosis.
2010 Aug
In vitro antifungal susceptibilities and amplified fragment length polymorphism genotyping of a worldwide collection of 350 clinical, veterinary, and environmental Cryptococcus gattii isolates.
2010 Dec
Novel triazole antifungal drugs: focus on isavuconazole, ravuconazole and albaconazole.
2010 Feb
Isavuconazole: a comprehensive review of spectrum of activity of a new triazole.
2010 Nov
Antifungal susceptibility, serotyping, and genotyping of clinical Cryptococcus neoformans isolates collected during 18 years in a single institution in Madrid, Spain.
2010 Nov
In vitro activity of isavuconazole against 140 reference fungal strains and 165 clinically isolated yeasts from Japan.
2010 Oct
Microsatellite typing and susceptibilities of serial Cryptococcus neoformans isolates from Cuban patients with recurrent cryptococcal meningitis.
2010 Oct 4
Opportunistic fungi: a view to the future.
2010 Sep
In vitro antifungal activities of isavuconazole and comparators against rare yeast pathogens.
2010 Sep
Chromatographic and electrophoretic techniques used in the analysis of triazole antifungal agents-a review.
2010 Sep 15
In vitro activity of isavuconazole against 208 Aspergillus flavus isolates in comparison with 7 other antifungal agents: assessment according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
2011 Dec
Isavuconazole activity against Aspergillus lentulus, Neosartorya udagawae, and Cryptococcus gattii, emerging fungal pathogens with reduced azole susceptibility.
2013 Sep
Isavuconazole: Pharmacology, Pharmacodynamics, and Current Clinical Experience with a New Triazole Antifungal Agent.
2015 Nov
Isavuconazole: A New Broad-Spectrum Triazole Antifungal Agent.
2015 Nov 15
Patents

Sample Use Guides

Loading Dose: 372 mg isavuconazonium sulfate (equivalent to 200 mg of isavuconazole) every 8 hours for 6 doses (48 hours) via oral (2 capsules) or intravenous administration (1 reconstituted vial) Maintenance Dose: 372 mg isavuconazonium sulfate (equivalent to 200 mg of isavuconazole) once daily via oral (2 capsules) or intravenous administration (1 reconstituted vial) starting 12 to 24 hours after the last loading dose.
Route of Administration: Other
Isavuconazole exhibited MIC50 values of 1–4 ug/ mL and MIC90 values of 4–16 ug/mL, against Mucorales isolates. MIC90 against Aspergillus fumigatus was 0.5–2 ug/ml, MIC90 against Aspergillus terreus was 0.5–4 ug/ml, MIC90 against Aspergillus flavus was 1–16 ug/ml, MIC90 against Aspergillus niger was 2–4 ug/ml.
Name Type Language
ISAVUCONAZOLE
INN   MI   WHO-DD  
INN  
Official Name English
ISAVUCONAZOLE [WHO-DD]
Common Name English
4-(2-((2R,3R)-3-(2,5-DIFLUOROPHENYL)-3-HYDROXY-4-(1H-1,2,4-TRIAZOL-1-YL)BUTAN-2-YL)-1,3-THIAZOL-4-YL)BENZONITRILE
Systematic Name English
BAL-4815
Code English
ISAVUCONAZOLE [MI]
Common Name English
ISAVUCONAZOLE [INN]
Common Name English
Classification Tree Code System Code
WHO-ATC J02AC05
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
NCI_THESAURUS C514
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
NDF-RT N0000175487
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
Code System Code Type Description
WIKIPEDIA
ISAVUCONAZOLE
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
EPA CompTox
241479-67-4
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
NCI_THESAURUS
C64543
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
ChEMBL
CHEMBL409153
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
NDF-RT
N0000187061
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY Organic Cation Transporter 2 Inhibitors [MoA]
CAS
241479-67-4
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
INN
8783
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
EVMPD
SUB128138
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
DRUG BANK
DB11633
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
NDF-RT
N0000185503
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
RXCUI
1720882
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY RxNorm
MERCK INDEX
M6419
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY Merck Index
NDF-RT
N0000182141
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
FDA UNII
60UTO373KE
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY
PUBCHEM
6918485
Created by admin on Sat Jun 26 14:25:22 UTC 2021 , Edited by admin on Sat Jun 26 14:25:22 UTC 2021
PRIMARY