Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H17F2N5OS |
| Molecular Weight | 437.465 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](C1=NC(=CS1)C2=CC=C(C=C2)C#N)[C@](O)(CN3C=NC=N3)C4=C(F)C=CC(F)=C4
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
DescriptionCurator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24187505
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
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207500Orig1207501Orig1s000PharmR.pdf
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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3390825 |
|||
Target ID: CHEMBL3390824 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Curative | CRESEMBA Approved UseCresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis. Launch Date1.42560002E12 |
|||
| Curative | CRESEMBA Approved UseCresemba is an azole antifungal indicated for use in the treatment of invasive aspergillosis and invasive mucormycosis. Launch Date1.42560002E12 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Dose | Population | Adverse 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%) Other AEs:Hypersensitivity (8.3%) Nausea (8.3%) Headache (grade 1, 8.3%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.31Headache (grade 2, 8.3%) Rash (grade 1, 8.3%) Rash (grade 2, 8.3%) Cough (grade 1, 16.7%) |
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%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.131Cardiac 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%) |
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%) Sources: Page: nda/2015/207500Orig1207501Orig1s000MedR.pdf - p.149Chills (0.4%) Convulsion (0.8%) Dyspnoea (0.8%) Epilepsy (0.4%) Hypotension (0.4%) Respiratory failure (0.8%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| 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 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical 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
| Target | Modality | Activity | Metabolite | Clinical 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
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| Cryptococcus gattii: An Emerging Cause of Fungal Disease in North America. | 2009 |
|
| Efficacy of isavuconazole, voriconazole and fluconazole in temporarily neutropenic murine models of disseminated Candida tropicalis and Candida krusei. | 2009 Jan |
|
| 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 activity of isavuconazole against 140 reference fungal strains and 165 clinically isolated yeasts from Japan. | 2010 Oct |
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 | ||
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Systematic Name | English | ||
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Code | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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WHO-ATC |
J02AC05
Created by
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NCI_THESAURUS |
C514
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NDF-RT |
N0000175487
Created by
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| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
ISAVUCONAZOLE
Created by
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PRIMARY | |||
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DTXSID2058251
Created by
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PRIMARY | |||
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C64543
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PRIMARY | |||
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CHEMBL409153
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PRIMARY | |||
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N0000187061
Created by
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PRIMARY | Organic Cation Transporter 2 Inhibitors [MoA] | ||
|
241479-67-4
Created by
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PRIMARY | |||
|
8783
Created by
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PRIMARY | |||
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SUB128138
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PRIMARY | |||
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DB11633
Created by
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PRIMARY | |||
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N0000185503
Created by
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PRIMARY | P-Glycoprotein Inhibitors [MoA] | ||
|
1720882
Created by
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PRIMARY | RxNorm | ||
|
85979
Created by
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PRIMARY | |||
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M6419
Created by
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PRIMARY | Merck Index | ||
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N0000182141
Created by
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PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
|
60UTO373KE
Created by
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PRIMARY | |||
|
6918485
Created by
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PRIMARY |
ACTIVE MOIETY
