Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C13H10FN3.H3O4P |
Molecular Weight | 325.2322 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OP(O)(O)=O.[H][C@@]1(CCC2=CN=CN12)C3=CC=C(C=C3F)C#N
InChI
InChIKey=FMCPYRDGUZBOJZ-BTQNPOSSSA-N
InChI=1S/C13H10FN3.H3O4P/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13;1-5(2,3)4/h1,3,5,7-8,13H,2,4H2;(H3,1,2,3,4)/t13-;/m1./s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/26542280Curator's Comment: The description was created based on several sources, including
https://clinicaltrials.gov/ct2/show/NCT02697734 | https://clinicaltrials.gov/ct2/show/NCT02468193 | https://clinicaltrials.gov/ct2/show/NCT02372084 | https://www.ncbi.nlm.nih.gov/pubmed/25981165
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26542280
Curator's Comment: The description was created based on several sources, including
https://clinicaltrials.gov/ct2/show/NCT02697734 | https://clinicaltrials.gov/ct2/show/NCT02468193 | https://clinicaltrials.gov/ct2/show/NCT02372084 | https://www.ncbi.nlm.nih.gov/pubmed/25981165
Osilodrostat (INN, USAN) (developmental code name LCI-699) is an orally active, non-steroidal corticosteroid biosynthesis inhibitor which is under development by Novartis for the treatment of Cushing's syndrome and pituitary ACTH hypersecretion (a specific subtype of Cushing's syndrome). Osilodrostat specifically acts as a potent and selective inhibitor of aldosterone synthase (CYP11B2) and at higher dosages of 11β-hydroxylase (CYP11B1). Osilodrostat decreases plasma and urinary aldosterone levels and rapidly corrects hypokalemia, in patients with primary aldosteronism and hypertension. At doses ≥1 mg o.d. Osilodrostat markedly increases 11-deoxycortisol plasma levels and blunts ACTH-stimulated cortisol release in ≈20% of patients, consistent with the inhibition of CYP11B1. In patients with resistant hypertension, Osilodrostat produces a non-significant reduction in blood pressure, possibly due to the increase in 11-deoxycortisol levels and the stimulation of the hypothalamic-pituitary-adrenal feedback axis. Because of the lack of selectivity, poor antihypertensive effect, and short half-life, the development of Osilodrostat as antihypertensive was halted. As of 2017, Osilodrostat is in phase III and phase II clinical trials for the treatment of pituitary ACTH hypersecretion and Cushing's syndrome, respectively.
Originator
Sources: https://www.google.com/patents/WO2007024945
Curator's Comment: # Novartis A.-G.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2722 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24422519 |
0.2 nM [IC50] | ||
Target ID: CHEMBL1908 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24422519 |
2.9 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2340 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg 1 times / day multiple, oral dose: 5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2100 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg single, oral dose: 5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2170 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg single, oral dose: 5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
634 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg single, oral dose: 1.5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
999 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg 1 times / day multiple, oral dose: 1.5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
608 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg single, oral dose: 1.5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
6100 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg 1 times / day multiple, oral dose: 20 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
7200 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg single, oral dose: 20 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2130 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg 1 times / day multiple, oral dose: 5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
5490 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg single, oral dose: 20 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
4930 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg 1 times / day multiple, oral dose: 20 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
306 ng/mL |
30 mg 2 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OSILODROSTAT unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
7.91 ng/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
OSILODROSTAT unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
617 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg 1 times / day multiple, oral dose: 1.5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: UNKNOWN sex: FEMALE food status: FED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
11500 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg 1 times / day multiple, oral dose: 5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
12700 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg single, oral dose: 5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
15700 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg single, oral dose: 5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
2450 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg single, oral dose: 1.5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2690 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg 1 times / day multiple, oral dose: 1.5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
2730 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg single, oral dose: 1.5 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
50000 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg 1 times / day multiple, oral dose: 20 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
98000 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg single, oral dose: 20 mg/kg route of administration: Oral experiment type: SINGLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: MALE food status: FED |
|
13300 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
5 mg/kg 1 times / day multiple, oral dose: 5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
80400 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg single, oral dose: 20 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
51600 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
20 mg/kg 1 times / day multiple, oral dose: 20 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: ADULT sex: FEMALE food status: FED |
|
1680 ng × h/mL |
30 mg 2 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OSILODROSTAT unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
38.6 ng × h/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
OSILODROSTAT unknown | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
3010 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25981165/ |
1.5 mg/kg 1 times / day multiple, oral dose: 1.5 mg/kg route of administration: Oral experiment type: MULTIPLE co-administered: PASIREOTIDE |
OSILODROSTAT plasma | Rattus norvegicus population: HEALTHY age: UNKNOWN sex: FEMALE food status: FED |
Doses
Dose | Population | Adverse events |
---|---|---|
7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Disc. AE: Hypocortisolism... AEs leading to discontinuation/dose reduction: Hypocortisolism Sources: |
7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Disc. AE: Hypokalemia, Pituitary tumor NOS... Other AEs: Adrenal insufficiency, Fatigue... AEs leading to discontinuation/dose reduction: Hypokalemia (0.72%) Other AEs:Pituitary tumor NOS (5.8%) Adrenal insufficiency (43.1%) Sources: Fatigue (38.7%) Nausea (grade 1-2, 37.2%) Headache (30.7%) Edema (21.2%) Nasopharyngitis (19.7%) Vomiting (grade 1-2, 19%) Arthralgia (17.5%) Back pain (15.3%) Rash (15.3%) Diarrhea (grade 1-2, 14.6%) Blood corticotrophin increased (13.9%) Dizziness (13.9%) Abdominal pain (grade 1-2, 13.1%) Hypokalaemia (12.4%) Myalgia (12.4%) Decreased appetite (11.7%) Hormone level abnormal (11.7%) Hypotension (11.7%) Urinary tract infection (11.7%) Blood testosterone increased (10.9%) Pyrexia (10.9%) Anemia (10.2%) Cough (10.2%) Hypertension (10.2%) Influenza (10.2%) Adrenal insufficiency (43.1%) Fatigue (38.7%) Nausea (grade 1-2, 37.2%) Headache (30.7%) Edema (21.2%) Nasopharyngitis (19.7%) Vomiting (grade 1-2, 19%) Arthralgia (17.5%) Back pain (15.3%) Rash (15.3%) Diarrhea (grade 1-2, 14.6%) Blood corticotrophin increased (13.9%) Dizziness (13.9%) Abdominal pain (grade 1-2, 13.1%) Hypokalaemia (12.4%) Myalgia (12.4%) Decreased appetite (11.7%) Hormone level abnormal (11.7%) Hypotension (11.7%) Urinary tract infection (11.7%) Blood testosterone increased (10.9%) Pyrexia (10.9%) Anemia (10.2%) Cough (10.2%) Hypertension (10.2%) Influenza (10.2%) Hirsutism (9.5%) Acne (8.8%) Dyspepsia (8%) Insomnia (8%) Anxiety (7.3%) Depression (7.3%) Gastroenteritis (7.3%) Malaise (6.6%) Tachycardia (6.6%) Alopecia (5.8%) Transaminases increased (4.4%) QT interval prolonged (3.6%) Syncope (1.5%) Neutropenia (1.4%) Neutrophil count decreased (13.1%) ALT increased (grade 1, 4%) AST increased (grade 1, 4%) |
5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
DLT: Rash, Visual impairment... Other AEs: Nausea, Anaemia... Dose limiting toxicities: Rash (3%) Other AEs:Visual impairment (3%) Headache (3%) Paresis cranial nerve (3%) Pituitary tumour benign (3%) Hypocortisolism (3%) Nausea (11%) Sources: Anaemia (8%) Arthralgia (8%) Headache (8%) Asthenia (6%) Blood corticotrophin increased (6%) Constipation (6%) Depression (6%) Dizziness (6%) Fatigue (6%) Hirsutism (6%) Nasopharyngitis (6%) Cough (3%) Insomnia (3%) Urinary tract infection (3%) |
200 mg 1 times / day single, oral Highest studied dose Dose: 200 mg, 1 times / day Route: oral Route: single Dose: 200 mg, 1 times / day Sources: |
healthy n = 37 Health Status: healthy Sex: M Population Size: 37 Sources: |
Other AEs: Electrocardiogram QTc interval prolonged... Other AEs: Electrocardiogram QTc interval prolonged Sources: |
30 mg 2 times / day steady, oral (median) Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: steady Dose: 30 mg, 2 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 5 Sources: |
|
30 mg 2 times / day steady, oral Recommended Dose: 30 mg, 2 times / day Route: oral Route: steady Dose: 30 mg, 2 times / day Sources: |
unhealthy n = 5 Health Status: unhealthy Sex: M+F Population Size: 5 Sources: |
|
150 mg single, oral Studied dose Dose: 150 mg Route: oral Route: single Dose: 150 mg Sources: |
healthy n = 86 Health Status: healthy Sex: M+F Population Size: 86 Sources: |
Other AEs: QT interval prolonged... Other AEs: QT interval prolonged (3.6%) Sources: |
20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Other AEs: Headache, Adrenal insufficiency... Other AEs: Headache (grade 3-5, 5.3%) Sources: Adrenal insufficiency (grade 3-5, 5.3%) Hypertension (grade 3-5, 21.1%) Anaemia (grade 3-5, 5.3%) Depression (grade 3-5, 5.3%) Lipase increased (grade 3-5, 5.3%) Pituitary-dependent Cushing's syndrome (grade 3-5, 15.8%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hypocortisolism | Disc. AE | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hypokalemia | 0.72% Disc. AE |
7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Neutropenia | 1.4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Syncope | 1.5% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Anemia | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Anemia | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Cough | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Cough | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hypertension | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hypertension | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Influenza | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Influenza | 10.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Blood testosterone increased | 10.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Blood testosterone increased | 10.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Pyrexia | 10.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Pyrexia | 10.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Decreased appetite | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Decreased appetite | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hormone level abnormal | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hormone level abnormal | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hypotension | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hypotension | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Urinary tract infection | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Urinary tract infection | 11.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hypokalaemia | 12.4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hypokalaemia | 12.4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Myalgia | 12.4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Myalgia | 12.4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Neutrophil count decreased | 13.1% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Blood corticotrophin increased | 13.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Blood corticotrophin increased | 13.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Dizziness | 13.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Dizziness | 13.9% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Back pain | 15.3% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Back pain | 15.3% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Rash | 15.3% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Rash | 15.3% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Arthralgia | 17.5% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Arthralgia | 17.5% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Nasopharyngitis | 19.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Nasopharyngitis | 19.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Edema | 21.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Edema | 21.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
QT interval prolonged | 3.6% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Headache | 30.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Headache | 30.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Fatigue | 38.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Fatigue | 38.7% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Transaminases increased | 4.4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Adrenal insufficiency | 43.1% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Adrenal insufficiency | 43.1% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Alopecia | 5.8% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Pituitary tumor NOS | 5.8% Disc. AE |
7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Malaise | 6.6% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Tachycardia | 6.6% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Anxiety | 7.3% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Depression | 7.3% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Gastroenteritis | 7.3% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Dyspepsia | 8% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Insomnia | 8% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Acne | 8.8% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Hirsutism | 9.5% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
ALT increased | grade 1, 4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
AST increased | grade 1, 4% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Abdominal pain | grade 1-2, 13.1% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Abdominal pain | grade 1-2, 13.1% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Diarrhea | grade 1-2, 14.6% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Diarrhea | grade 1-2, 14.6% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Vomiting | grade 1-2, 19% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Vomiting | grade 1-2, 19% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Nausea | grade 1-2, 37.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Nausea | grade 1-2, 37.2% | 7 mg 2 times / day steady, oral (typical) Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years n = 137 Health Status: unhealthy Condition: Cushing's disease Age Group: 19-70 years Sex: M+F Population Size: 137 Sources: |
Nausea | 11% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Cough | 3% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Insomnia | 3% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Urinary tract infection | 3% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Headache | 3% DLT |
5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Hypocortisolism | 3% DLT |
5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Paresis cranial nerve | 3% DLT |
5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Pituitary tumour benign | 3% DLT |
5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Rash | 3% DLT |
5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Visual impairment | 3% DLT |
5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Asthenia | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Blood corticotrophin increased | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Constipation | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Depression | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Dizziness | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Fatigue | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Hirsutism | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Nasopharyngitis | 6% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Anaemia | 8% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Arthralgia | 8% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Headache | 8% | 5 mg 2 times / day steady, oral (median) Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years n = 36 Health Status: unhealthy Condition: Cushing's disease Age Group: 20-69 years Sex: M+F Population Size: 36 Sources: |
Electrocardiogram QTc interval prolonged | 200 mg 1 times / day single, oral Highest studied dose Dose: 200 mg, 1 times / day Route: oral Route: single Dose: 200 mg, 1 times / day Sources: |
healthy n = 37 Health Status: healthy Sex: M Population Size: 37 Sources: |
|
QT interval prolonged | 3.6% | 150 mg single, oral Studied dose Dose: 150 mg Route: oral Route: single Dose: 150 mg Sources: |
healthy n = 86 Health Status: healthy Sex: M+F Population Size: 86 Sources: |
Pituitary-dependent Cushing's syndrome | grade 3-5, 15.8% | 20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Hypertension | grade 3-5, 21.1% | 20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Adrenal insufficiency | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Anaemia | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Depression | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Headache | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Lipase increased | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral (median) Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy n = 19 Health Status: unhealthy Condition: Cushing's disease Sex: M+F Population Size: 19 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
yes [Km 30.4 uM] | unlikely Comment: Due to the available high Km,u values (~30 μM) for CYP3A4, CYP2B6 and CYP2D6, these enzymes are not likely saturated at clinically relevant doses since Cmax is about 0.88 μM following multiple dose administration of 30 mg osilodrostat twice daily Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212801Orig1s000ClinPharmR.pdf#page=9 Page: 9.0 |
|||
yes [Km 36.1 uM] | unlikely Comment: Due to the available high Km,u values (~30 μM) for CYP3A4, CYP2B6 and CYP2D6, these enzymes are not likely saturated at clinically relevant doses since Cmax is about 0.88 μM following multiple dose administration of 30 mg osilodrostat twice daily Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212801Orig1s000ClinPharmR.pdf#page=9 Page: 9.0 |
|||
yes [Km 36.1 uM] | unlikely Comment: Due to the available high Km,u values (~30 μM) for CYP3A4, CYP2B6 and CYP2D6, these enzymes are not likely saturated at clinically relevant doses since Cmax is about 0.88 μM following multiple dose administration of 30 mg osilodrostat twice daily Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212801Orig1s000ClinPharmR.pdf#page=9 Page: 9.0 |
|||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/212801Orig1s000PharmR.pdf#page=31 Page: 31.0 |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02697734
1, 5, 10, or 20 mg/day for 48-weeks
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24900631
For in vitro measurement of aldosterone activity, human adrenocortical carcinoma NCI-H295R cells are seeded in NBS 96-well plates at a density of 25,000 cells/well in 100 μl of a growth medium containing DMEM/F12 supplemented with 10% FCS, 2.5% Nuserum, 1 μg ITS/ml, and 1x antibiotic/antimycotic. The medium is changed after culturing for 3 days at 37 C under an atmosphere of 5% CO2/95% air. On the following day, cells are rinsed with 100 μl of DMEM/F12 and incubated with 100 μl of treatment medium containing 1 µM Ang II and a compound 7n (Osilodrostat) at different concentrations in quadruplicate wells at 37C for 24 hr. At the end of incubation, 50 μl of medium is withdrawn from each well for measurement of aldosterone production by an RIA using mouse anti-aldosterone monoclonal antibodies.
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