Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C13H10FN3 |
Molecular Weight | 227.237 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
FC1=C(C=CC(=C1)C#N)[C@H]2CCC3=CN=CN23
InChI
InChIKey=USUZGMWDZDXMDG-CYBMUJFWSA-N
InChI=1S/C13H10FN3/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13/h1,3,5,7-8,13H,2,4H2/t13-/m1/s1
Molecular Formula | C13H10FN3 |
Molecular Weight | 227.237 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 |
---|---|---|---|---|
7.91 ng/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
OSILODROSTAT plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
306 ng/mL |
30 mg 2 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OSILODROSTAT plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
38.6 ng × h/mL |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
OSILODROSTAT plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
1680 ng × h/mL |
30 mg 2 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OSILODROSTAT plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
63.6% |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
OSILODROSTAT plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
|
63.6% |
30 mg 2 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
OSILODROSTAT plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Disc. AE: Hypocortisolism... AEs leading to discontinuation/dose reduction: Hypocortisolism Sources: |
7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F 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 Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F 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 Health Status: healthy Sex: M Sources: |
Other AEs: Electrocardiogram QTc interval prolonged... Other AEs: Electrocardiogram QTc interval prolonged Sources: |
30 mg 2 times / day steady, oral Highest studied dose Dose: 30 mg, 2 times / day Route: oral Route: steady Dose: 30 mg, 2 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F 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 Health Status: unhealthy Sex: M+F Sources: |
|
150 mg single, oral Studied dose Dose: 150 mg Route: oral Route: single Dose: 150 mg Sources: |
healthy Health Status: healthy Sex: M+F Sources: |
Other AEs: QT interval prolonged... Other AEs: QT interval prolonged (3.6%) Sources: |
20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F 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 Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hypokalemia | 0.72% Disc. AE |
7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Neutropenia | 1.4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Syncope | 1.5% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Anemia | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Anemia | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Cough | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Cough | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hypertension | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hypertension | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Influenza | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Influenza | 10.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Blood testosterone increased | 10.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Blood testosterone increased | 10.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Pyrexia | 10.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Pyrexia | 10.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Decreased appetite | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Decreased appetite | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hormone level abnormal | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hormone level abnormal | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hypotension | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hypotension | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Urinary tract infection | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Urinary tract infection | 11.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hypokalaemia | 12.4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hypokalaemia | 12.4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Myalgia | 12.4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Myalgia | 12.4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Neutrophil count decreased | 13.1% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Blood corticotrophin increased | 13.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Blood corticotrophin increased | 13.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Dizziness | 13.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Dizziness | 13.9% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Back pain | 15.3% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Back pain | 15.3% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Rash | 15.3% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Rash | 15.3% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Arthralgia | 17.5% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Arthralgia | 17.5% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Nasopharyngitis | 19.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Nasopharyngitis | 19.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Edema | 21.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Edema | 21.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
QT interval prolonged | 3.6% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Headache | 30.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Headache | 30.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Fatigue | 38.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Fatigue | 38.7% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Transaminases increased | 4.4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Adrenal insufficiency | 43.1% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Adrenal insufficiency | 43.1% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Alopecia | 5.8% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Pituitary tumor NOS | 5.8% Disc. AE |
7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Malaise | 6.6% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Tachycardia | 6.6% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Anxiety | 7.3% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Depression | 7.3% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Gastroenteritis | 7.3% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Dyspepsia | 8% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Insomnia | 8% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Acne | 8.8% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Hirsutism | 9.5% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
ALT increased | grade 1, 4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
AST increased | grade 1, 4% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Abdominal pain | grade 1-2, 13.1% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Abdominal pain | grade 1-2, 13.1% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 14.6% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Diarrhea | grade 1-2, 14.6% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Vomiting | grade 1-2, 19% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Vomiting | grade 1-2, 19% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Nausea | grade 1-2, 37.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Nausea | grade 1-2, 37.2% | 7 mg 2 times / day steady, oral Recommended Dose: 7 mg, 2 times / day Route: oral Route: steady Dose: 7 mg, 2 times / day Sources: |
unhealthy, 19-70 years Health Status: unhealthy Age Group: 19-70 years Sex: M+F Sources: |
Nausea | 11% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Cough | 3% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Insomnia | 3% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Urinary tract infection | 3% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Headache | 3% DLT |
5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Hypocortisolism | 3% DLT |
5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Paresis cranial nerve | 3% DLT |
5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Pituitary tumour benign | 3% DLT |
5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Rash | 3% DLT |
5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Visual impairment | 3% DLT |
5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Asthenia | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Blood corticotrophin increased | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Constipation | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Depression | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Dizziness | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Fatigue | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Hirsutism | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Nasopharyngitis | 6% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Anaemia | 8% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Arthralgia | 8% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F Sources: |
Headache | 8% | 5 mg 2 times / day steady, oral Recommended Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: |
unhealthy, 20-69 years Health Status: unhealthy Age Group: 20-69 years Sex: M+F 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 Health Status: healthy Sex: M Sources: |
|
QT interval prolonged | 3.6% | 150 mg single, oral Studied dose Dose: 150 mg Route: oral Route: single Dose: 150 mg Sources: |
healthy Health Status: healthy Sex: M+F Sources: |
Pituitary-dependent Cushing's syndrome | grade 3-5, 15.8% | 20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Hypertension | grade 3-5, 21.1% | 20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Adrenal insufficiency | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Anaemia | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Depression | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Headache | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Sources: |
Lipase increased | grade 3-5, 5.3% | 20 mg 1 times / day steady, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: steady Dose: 20 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F 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 |
PubMed
Title | Date | PubMed |
---|---|---|
Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review. | 2015 |
|
Medical therapy for Cushing's disease: adrenal steroidogenesis inhibitors and glucocorticoid receptor blockers. | 2015 Apr |
|
Therapy of endocrine disease: steroidogenesis enzyme inhibitors in Cushing's syndrome. | 2015 Jun |
|
Medical treatment of Cushing disease: new targets, new hope. | 2015 Mar |
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.
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:34:17 GMT 2025
by
admin
on
Mon Mar 31 21:34:17 GMT 2025
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Record UNII |
5YL4IQ1078
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C471
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EU-Orphan Drug |
EU/3/14/1345
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FDA ORPHAN DRUG |
405113
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DTXSID40156570
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44139752
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DB11837
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1304733-26-3
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CD-130
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C131535
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2286252
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m12237
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5YL4IQ1078
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928134-65-0
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5YL4IQ1078
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Osilodrostat
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100000176720
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PRIMARY |
Related Record | Type | Details | ||
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METABOLIC ENZYME -> INHIBITOR |
WEAK INHIBITION
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METABOLIC ENZYME -> INHIBITOR |
WEAK INHIBITION
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> INHIBITOR |
TIME-DEPENDENT INHIBITION
Ki
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> INHIBITOR |
osilodrostat inhibited the activity of human CYP11B1 dose-dependently with IC50 values of 2.5 ± 0.1 nM (n = 4).
IC50
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METABOLIC ENZYME -> SUBSTRATE | |||
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METABOLIC ENZYME -> INHIBITOR |
MODERATE INHIBITION
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METABOLIC ENZYME -> INHIBITOR |
WEAK INHIBITION
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EXCRETED UNCHANGED |
AMOUNT EXCRETED
URINE
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SALT/SOLVATE -> PARENT |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
URINE
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METABOLITE -> PARENT |
MAJOR
PLASMA
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METABOLITE -> PARENT |
URINE
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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Tmax | PHARMACOKINETIC |
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blood-to-plasma ratio | PHARMACOKINETIC |
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