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

Details

Stereochemistry ACHIRAL
Molecular Formula C23H30N8O
Molecular Weight 434.5382
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RIBOCICLIB

SMILES

CN(C)C(=O)c1cc2c[nH]c(=Nc3ccc(cn3)N4CCNCC4)nc2n1C5CCCC5

InChI

InChIKey=RHXHGRAEPCAFML-UHFFFAOYSA-N
InChI=1S/C23H30N8O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28)

HIDE SMILES / InChI

Molecular Formula C23H30N8O
Molecular Weight 434.5382
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: Description was created based on several sources, including https://www.novartis.com/news/media-releases/novartis-cdk46-inhibitor-lee011-ribociclib-receives-fda-breakthrough-therapy https://www.ncbi.nlm.nih.gov/pubmed/26995305

Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. Ribociclib is in phase III clinical trials by Novartis for the treatment of postmenopausal women with advanced breast cancer. Phase II clinical trials are also in development for the treatment of liposarcoma, ovarian cancer, fallopian tube cancer, peritoneum cancer, endometrial cancer, and gastrointestinal cancer. Preregistration for Breast cancer (First-line therapy, Combination therapy, Late-stage disease) in the USA (PO) in November 2016.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: CHEMBL2366209
126.0 nM [IC50]
154.0 nM [IC50]
10.0 nM [IC50]
39.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
KISQALI

Approved Use

KISQALI is a kinase inhibitor indicated in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.

Launch Date

1.48927676E12
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1168 ng/mL
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: LETROZOLE
RIBOCICLIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4714 ng × h/mL
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: LETROZOLE
RIBOCICLIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
30 h
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered: LETROZOLE
RIBOCICLIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
30%
RIBOCICLIB plasma
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
280 mg/m2 1 times / day steady, oral
Dose: 280 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 280 mg/m2, 1 times / day
Sources:
unhealthy, 2.0 years (range: 1.0–17.0)
n = 5
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 2.0 years (range: 1.0–17.0)
Sex: M+F
Population Size: 5
Sources:
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
900 mg 1 times / day multiple, oral
MTD
Dose: 900 mg, 1 times / day
Route: oral
Route: multiple
Dose: 900 mg, 1 times / day
Sources:
unhealthy, 49 years (range: 31-66 years)
n = 12
Health Status: unhealthy
Condition: grade IV glioma
Age Group: 49 years (range: 31-66 years)
Sex: M+F
Population Size: 12
Sources:
400 mg 1 times / day steady, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 57.0 years (range: 33–73 years)
n = 4
Health Status: unhealthy
Condition: Breast cancer|Esophagus cancer| Peritoneum cancer
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Population Size: 4
Sources:
DLT: Febrile neutropenia...
Dose limiting toxicities:
Febrile neutropenia (grade 3, 1 patient)
Sources:
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 57.0 years (range: 33–73 years)
n = 13
Health Status: unhealthy
Condition: Breast cancer|Esophagus cancer| Peritoneum cancer
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Population Size: 13
Sources:
DLT: Febrile neutropenia, QT interval prolonged...
Dose limiting toxicities:
Febrile neutropenia (grade 3, 1 patient)
QT interval prolonged (grade 3, 2 patients)
Neutropenia (grade 4, 1 patient)
Thrombocytopenia (grade 4, 1 patient)
Sources:
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
DLT: Thrombocytopenia...
Other AEs: Neutropenia, Leukopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 2 patients)
Other AEs:
Neutropenia (grade 3-4, 67%)
Leukopenia (grade 1-2, 25%)
Leukopenia (grade 3-4, 42%)
Anemia (grade 1-2, 50%)
Lymphopenia (grade 1-2, 17%)
Lymphopenia (grade 3-4, 33%)
Thrombocytopenia (grade 1-2, 8%)
Thrombocytopenia (grade 3-4, 42%)
Vomiting (grade 1-2, 42%)
Fatigue (grade 1-2, 33%)
Nausea (grade 1-2, 25%)
Electrocardiogram QTc interval prolonged (grade 1-2, 25%)
Decreased appetite (grade 1-2, 17%)
AST increased (grade 1-2, 25%)
Asthenia (grade 1-2, 8%)
Creatinine increased (grade 1-2, 8%)
Sources:
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Disc. AE: Neutropenia, Neutropenia...
Other AEs: Urinary tract infection, Urinary tract infection...
AEs leading to
discontinuation/dose reduction:
Neutropenia (grade 3, 50%)
Neutropenia (grade 4, 10%)
Vomiting (2%)
ALT increased (grade 1-2, 36%)
ALT increased (grade 3, 8%)
ALT increased (grade 4, 2%)
AST increased (grade 1-2, 37%)
AST increased (grade 3, 6%)
AST increased (grade 4, 1%)
QT interval prolonged (grade 2, 1 patient)
Hypokalemia (grade 3, 1 patient)
Other AEs:
Urinary tract infection (grade 1-2, 10%)
Urinary tract infection (grade 3, 1%)
Neutropenia (grade 1-2, 15%)
Leukopenia (grade 1-2, 12%)
Leukopenia (grade 3, 20%)
Leukopenia (grade 4, 1%)
Anemia (grade 1-2, 16%)
Anemia (grade 3, 1%)
Anemia (grade 4, <1%)
Lymphopenia (grade 1-2, 4%)
Lymphopenia (grade 3, 6%)
Lymphopenia (grade 4, 1%)
Decreased appetite (grade 1-2, 17%)
Decreased appetite (grade 3, 2%)
Headache (grade 1-2, 21%)
Headache (grade 3, <1%)
Insomnia (grade 1-2, 11%)
Insomnia (grade 3, <1%)
Dyspnea (grade 1-2, 11%)
Dyspnea (grade 3, 1%)
Back pain (grade 1-2, 18%)
Back pain (grade 3, 2%)
Nausea (grade 1-2, 50%)
Nausea (grade 3, 2%)
Diarrhea (grade 1-2, 34%)
Diarrhea (grade 3, 1%)
Vomiting (grade 1-2, 25%)
Vomiting (grade 3, 4%)
Constipation (grade 1-2, 24%)
Constipation (grade 3, 1%)
Stomatitis (grade 1-2, 11%)
Stomatitis (grade 3, <1%)
Abdominal pain (grade 1-2, 10%)
Abdominal pain (grade 3, 1%)
Alopecia (grade 1-2, 33%)
Rash (grade 1-2, 16%)
Rash (grade 3, 1%)
Pruritus (grade 1-2, 13%)
Pruritus (grade 3, 1%)
Fatigue (grade 1-2, 34%)
Fatigue (grade 3, 2%)
Fatigue (grade 4, <1%)
Pyrexia (grade 1-2, 12%)
Pyrexia (grade 3, <1%)
Edema peripheral (grade 1-2, 12%)
Blood bilirubin increased (grade 1-2, 8%)
Blood bilirubin increased (grade 3, 8%)
Blood bilirubin increased (grade 4, 2%)
Leukocyte count decreased (grade 1-2, 59%)
Leukocyte count decreased (grade 3, 31%)
Leukocyte count decreased (grade 4, 3%)
Neutrophil count decreased (grade 1-2, 33%)
Neutrophil count decreased (grade 3, 49%)
Neutrophil count decreased (grade 4, 11%)
Hemoglobin decreased (grade 1-2, 55%)
Hemoglobin decreased (grade 3, 2%)
Lymphocyte count decreased (grade 1-2, 37%)
Lymphocyte count decreased (grade 3, 12%)
Lymphocyte count decreased (grade 4, 2%)
Platelet count decreased (grade 1-2, 27%)
Platelet count decreased (grade 3, 1%)
Platelet count decreased (grade 4, <1%)
Creatinine increased (grade 1-2, 19%)
Creatinine increased (grade 3, 1%)
Phosphate decreased (grade 1-2, 7%)
Phosphate decreased (grade 3, 5%)
Phosphate decreased (grade 4, 1%)
Potassium decreased (grade 1-2, 9%)
Potassium decreased (grade 3, 1%)
Potassium decreased (grade 4, 1%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Fatigue grade 3, 1 patient
DLT
280 mg/m2 1 times / day steady, oral
Dose: 280 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 280 mg/m2, 1 times / day
Sources:
unhealthy, 2.0 years (range: 1.0–17.0)
n = 5
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 2.0 years (range: 1.0–17.0)
Sex: M+F
Population Size: 5
Sources:
Febrile neutropenia grade 3, 1 patient
DLT
400 mg 1 times / day steady, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
unhealthy, 57.0 years (range: 33–73 years)
n = 4
Health Status: unhealthy
Condition: Breast cancer|Esophagus cancer| Peritoneum cancer
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Population Size: 4
Sources:
Febrile neutropenia grade 3, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 57.0 years (range: 33–73 years)
n = 13
Health Status: unhealthy
Condition: Breast cancer|Esophagus cancer| Peritoneum cancer
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Population Size: 13
Sources:
QT interval prolonged grade 3, 2 patients
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 57.0 years (range: 33–73 years)
n = 13
Health Status: unhealthy
Condition: Breast cancer|Esophagus cancer| Peritoneum cancer
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Population Size: 13
Sources:
Neutropenia grade 4, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 57.0 years (range: 33–73 years)
n = 13
Health Status: unhealthy
Condition: Breast cancer|Esophagus cancer| Peritoneum cancer
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Population Size: 13
Sources:
Thrombocytopenia grade 4, 1 patient
DLT
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, 57.0 years (range: 33–73 years)
n = 13
Health Status: unhealthy
Condition: Breast cancer|Esophagus cancer| Peritoneum cancer
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Population Size: 13
Sources:
Decreased appetite grade 1-2, 17%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Lymphopenia grade 1-2, 17%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
AST increased grade 1-2, 25%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Electrocardiogram QTc interval prolonged grade 1-2, 25%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Leukopenia grade 1-2, 25%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Nausea grade 1-2, 25%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Fatigue grade 1-2, 33%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Vomiting grade 1-2, 42%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Anemia grade 1-2, 50%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Asthenia grade 1-2, 8%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Creatinine increased grade 1-2, 8%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Thrombocytopenia grade 1-2, 8%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Lymphopenia grade 3-4, 33%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Leukopenia grade 3-4, 42%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Thrombocytopenia grade 3-4, 42%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Neutropenia grade 3-4, 67%
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Thrombocytopenia grade 4, 2 patients
DLT
470 mg/m2 1 times / day steady, oral
MTD
Dose: 470 mg/m2, 1 times / day
Route: oral
Route: steady
Dose: 470 mg/m2, 1 times / day
Sources:
unhealthy, 7.0 years (range: 1.0–20.0 years)
n = 12
Health Status: unhealthy
Condition: Malignant Rhabdoid Tumors | Neuroblastoma
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Population Size: 12
Sources:
Vomiting 2%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Abdominal pain grade 1-2, 10%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Urinary tract infection grade 1-2, 10%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Dyspnea grade 1-2, 11%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Insomnia grade 1-2, 11%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Stomatitis grade 1-2, 11%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Edema peripheral grade 1-2, 12%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Leukopenia grade 1-2, 12%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Pyrexia grade 1-2, 12%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Pruritus grade 1-2, 13%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Neutropenia grade 1-2, 15%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Anemia grade 1-2, 16%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Rash grade 1-2, 16%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Decreased appetite grade 1-2, 17%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Back pain grade 1-2, 18%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Creatinine increased grade 1-2, 19%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Headache grade 1-2, 21%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Constipation grade 1-2, 24%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Vomiting grade 1-2, 25%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Platelet count decreased grade 1-2, 27%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Alopecia grade 1-2, 33%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Neutrophil count decreased grade 1-2, 33%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Diarrhea grade 1-2, 34%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Fatigue grade 1-2, 34%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
ALT increased grade 1-2, 36%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Lymphocyte count decreased grade 1-2, 37%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
AST increased grade 1-2, 37%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Lymphopenia grade 1-2, 4%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Nausea grade 1-2, 50%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Hemoglobin decreased grade 1-2, 55%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Leukocyte count decreased grade 1-2, 59%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Phosphate decreased grade 1-2, 7%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Blood bilirubin increased grade 1-2, 8%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Potassium decreased grade 1-2, 9%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
QT interval prolonged grade 2, 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Hypokalemia grade 3, 1 patient
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Abdominal pain grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Anemia grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Constipation grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Creatinine increased grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Diarrhea grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Dyspnea grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Platelet count decreased grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Potassium decreased grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Pruritus grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Rash grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Urinary tract infection grade 3, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Lymphocyte count decreased grade 3, 12%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Back pain grade 3, 2%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Decreased appetite grade 3, 2%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Fatigue grade 3, 2%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Hemoglobin decreased grade 3, 2%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Nausea grade 3, 2%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Leukopenia grade 3, 20%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Leukocyte count decreased grade 3, 31%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Vomiting grade 3, 4%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Neutrophil count decreased grade 3, 49%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Phosphate decreased grade 3, 5%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Neutropenia grade 3, 50%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Lymphopenia grade 3, 6%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
AST increased grade 3, 6%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Blood bilirubin increased grade 3, 8%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
ALT increased grade 3, 8%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Headache grade 3, <1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Insomnia grade 3, <1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Pyrexia grade 3, <1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Stomatitis grade 3, <1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Leukopenia grade 4, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Lymphopenia grade 4, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Phosphate decreased grade 4, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Potassium decreased grade 4, 1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
AST increased grade 4, 1%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Neutropenia grade 4, 10%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Neutrophil count decreased grade 4, 11%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Blood bilirubin increased grade 4, 2%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Lymphocyte count decreased grade 4, 2%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
ALT increased grade 4, 2%
Disc. AE
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Leukocyte count decreased grade 4, 3%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Anemia grade 4, <1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Fatigue grade 4, <1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Platelet count decreased grade 4, <1%
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Co-administed with::
letrozole
Sources:
unhealthy, adult
n = 334
Health Status: unhealthy
Condition: postmenopausal
Age Group: adult
Sex: F
Population Size: 334
Sources:
Overview

Overview

Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes [Ki 1.7 uM]
yes [Ki 1.9 uM]
yes [Ki 13 uM]
no (co-administration study)
Comment: The effect of multiple doses of 400 mg ribociclib on caffeine was minimal, with Cmax decreased by 10% and AUC increased slightly by 20%. Only weak inhibitory effects on CYP1A2 substrates are predicted using PBPK modeling at 600 mg ribociclib once daily dose and there is no need for dose adjustment
Page: 66.0
yes [Ki 24 uM]
yes [Ki 24.5 uM]
yes [Ki 30 uM]
yes [Ki 4.7 uM]
yes
yes (co-administration study)
Comment: Coadministration of midazolam (CYP3A4 substrate) with multiple doses of 400 mg ribociclib increased the midazolam exposure by 3.8-fold.
Page: 63.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
minor
minor
minor
no
no
no
no
no
no
no
no
weak
weak
yes
yes
yes (co-administration study)
Comment: In a dedicated drug-interaction trial, concomitant ritonavir (a strong CYP3A4 inhibitor) increased a single dose ribociclib's Cmax by 1.7-fold and the AUC by 3.2-fold
Page: 33.0
Tox targets
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
The landscape of somatic copy-number alteration across human cancers.
2010 Feb 18
A synthetic lethal interaction between K-Ras oncogenes and Cdk4 unveils a therapeutic strategy for non-small cell lung carcinoma.
2010 Jul 13
Liver X receptors as regulators of macrophage inflammatory and metabolic pathways.
2011 Aug
Therapeutic response to CDK4/6 inhibition in breast cancer defined by ex vivo analyses of human tumors.
2012 Jul 15
Therapeutic targeting of the cyclin D3:CDK4/6 complex in T cell leukemia.
2012 Oct 16
The requirement for cyclin D function in tumor maintenance.
2012 Oct 16
A CDK4/6 inhibitor enhances cytotoxicity of paclitaxel in lung adenocarcinoma cells harboring mutant KRAS as well as wild-type KRAS.
2013 Jul
Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma.
2013 Nov 15
Patents

Sample Use Guides

Ribociclib oral (3 weeks on/1 week off) in combination with oral once daily letrozole: 600 mg ribociclib QD + 2.5 mg letrozole QD
Route of Administration: Oral
Ribociclib significantly reduced proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis at nanomolar concentrations (mean IC50 of 307 nM in sensitive lines)
Substance Class Chemical
Created
by admin
on Sat Jun 26 04:11:44 UTC 2021
Edited
by admin
on Sat Jun 26 04:11:44 UTC 2021
Record UNII
TK8ERE8P56
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RIBOCICLIB
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
LEE011
Code English
RIBOCICLIB [INN]
Common Name English
LEE-011A
Code English
RIBOCICLIB [USAN]
Common Name English
RIBOCICLIB [MI]
Common Name English
7H-PYRROLO(2,3-D)PYRIMIDINE-6-CARBOXAMIDE, 7-CYCLOPENTYL-N,N-DIMETHYL-2-((5-(1-PIPERAZINYL)-2-PYRIDINYL)AMINO)-
Systematic Name English
RIBOCICLIB [WHO-DD]
Common Name English
LEE011A
Code English
LEE-011
Code English
Classification Tree Code System Code
NDF-RT N0000175605
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
WHO-ATC L01XE42
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
NCI_THESAURUS C2185
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
Code System Code Type Description
NCI_THESAURUS
C95701
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
MERCK INDEX
M12002
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
FDA UNII
TK8ERE8P56
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
INN
9968
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
EVMPD
SUB180246
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
ChEMBL
CHEMBL3545110
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
WIKIPEDIA
Ribociclib
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
DRUG BANK
DB11730
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
PUBCHEM
44631912
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
LACTMED
Ribociclib
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
DRUG CENTRAL
5218
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
CAS
1211441-98-3
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
RXCUI
1873916
Created by admin on Sat Jun 26 04:11:44 UTC 2021 , Edited by admin on Sat Jun 26 04:11:44 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
EXCRETED UNCHANGED
FECAL
METABOLIC ENZYME -> SUBSTRATE
Coadministration of a strong CYP3A4 inducer (rifampin) decreased the plasma AUC of ribociclib by 89%. The concomitant use of strong CYP3A4 inducers with ribociclib should be avoided.: In a dedicated drug-interaction trial, concomitant ritonavir (a strong CYP3A4 inhibitor) increased a single dose ribociclib’s Cmax by 1.7-fold and the AUC by 3.2-fold.
EXCRETED UNCHANGED
URINE
TRANSPORTER -> INHIBITOR
Ki
TRANSPORTER -> INHIBITOR
Ki
METABOLIC ENZYME -> INHIBITOR
A time-dependent inhibitor (TDI) of CYP3A4/5 (Ki,u: 4.44 ?M; kinact: 0.02 min-1 ). In vivo, ribociclib is a CYP3A perpetrator . Ribociclib dosed at 400 mg QD increased the coadministrated midazolam (a sensitive CYP3A4 substrate) AUC by 3.8-fold. Ribociclib given at the recommended dose of 600 mg QD is predicted to increase the midazolam AUC by 5.2-fold.
TIME-DEPENDENT INHIBITION
Ki
BINDER->LIGAND
BINDING
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
IC50
METABOLIC ENZYME -> INHIBITOR
Ki
TARGET -> INHIBITOR
IC50
Related Record Type Details
METABOLITE ACTIVE -> PARENT
Related Record Type Details
ACTIVE MOIETY