Details
Stereochemistry | ACHIRAL |
Molecular Formula | C23H30N8O.C4H6O4 |
Molecular Weight | 552.6253 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CCC(O)=O.CN(C)C(=O)C1=CC2=CN=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2N1C5CCCC5
InChI
InChIKey=NHANOMFABJQAAH-UHFFFAOYSA-N
InChI=1S/C23H30N8O.C4H6O4/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;5-3(6)1-2-4(7)8/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28);1-2H2,(H,5,6)(H,7,8)
DescriptionSources: https://newdrugapprovals.org/2015/10/19/ribociclib/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
Sources: https://newdrugapprovals.org/2015/10/19/ribociclib/
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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2366209 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24045179 |
126.0 nM [IC50] | ||
Target ID: CHEMBL614910 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24045179 |
154.0 nM [IC50] | ||
Target ID: CHEMBL331 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26995305 |
10.0 nM [IC50] | ||
Target ID: CHEMBL2508 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26995305 |
39.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | KISQALI Approved UseKISQALI 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 Date2017 |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1168 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27336726 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
4714 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27336726 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
30 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/27336726 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
30% |
RIBOCICLIB plasma | Homo sapiens |
Doses
Dose | Population | Adverse 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) Sources: QT interval prolonged (grade 3, 2 patients) Neutropenia (grade 4, 1 patient) Thrombocytopenia (grade 4, 1 patient) |
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%) Sources: 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%) |
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%) Other AEs: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) Urinary tract infection (grade 1-2, 10%) Sources: 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%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=66 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. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=63 Page: 63.0 |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
minor | |||
Page: - |
minor | |||
Page: - |
minor | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209092Orig1s000MultidisciplineR.pdf#page=33 Page: 33.0 |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02941926
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24045179
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)
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C2185
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1374639-75-4
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BG7HLX2919
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DBSALT002583
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100000170331
Created by
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ACTIVE MOIETY
SUBSTANCE RECORD