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This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ACHIRAL
Molecular Formula C23H30N8O.ClH
Molecular Weight 470.998
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RIBOCICLIB HYDROCHLORIDE

SMILES

Cl.CN(C)C(=O)C1=CC2=C(N=C(NC3=NC=C(C=C3)N4CCNCC4)N=C2)N1C5CCCC5

InChI

InChIKey=JZRSIQPIKASMEV-UHFFFAOYSA-N
InChI=1S/C23H30N8O.ClH/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);1H

HIDE SMILES / InChI
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C23H30N8O
Molecular Weight 434.5373
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.

Originator

Approval Year

2017
411
Targets

Targets

Primary TargetPharmacologyConditionPotency
IMR-5
3
Target ID: CHEMBL2366209
Inhibitor
8504
 126.0 nM [IC50]
Inhibitor
8504
 154.0 nM [IC50]
Inhibitor
8504
 10.0 nM [IC50]
Inhibitor
8504
 39.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
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

2017
Primary
Phase III
665
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
625 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32706937/
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered: LETROZOLE
LETROZOLE
 RIBOCICLIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
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
LETROZOLE
 RIBOCICLIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
9810 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32706937/
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered: LETROZOLE
LETROZOLE
 RIBOCICLIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
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
LETROZOLE
 RIBOCICLIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
32.9 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/32706937/
600 mg single, oral
dose: 600 mg
route of administration: Oral
experiment type: SINGLE
co-administered: LETROZOLE
LETROZOLE
 RIBOCICLIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
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
LETROZOLE
 RIBOCICLIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
30%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/209092s004lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 2.0 years (range: 1.0–17.0)
Health Status: unhealthy
Age Group: 2.0 years (range: 1.0–17.0)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/31285369
https://pubmed.ncbi.nlm.nih.gov/29059492
unhealthy, 49 years (range: 31-66 years)
Health Status: unhealthy
Age Group: 49 years (range: 31-66 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31285369
https://pubmed.ncbi.nlm.nih.gov/29059492
Sources:
https://pubmed.ncbi.nlm.nih.gov/31285369
https://pubmed.ncbi.nlm.nih.gov/29059492
400 mg 1 times / day steady, oral
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
unhealthy, 57.0 years (range: 33–73 years)
Health Status: unhealthy
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
DLT: Febrile neutropenia...
Dose limiting toxicities:
Febrile neutropenia (grade 3, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
600 mg 1 times / day steady, oral
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
unhealthy, 57.0 years (range: 33–73 years)
Health Status: unhealthy
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
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:
https://pubmed.ncbi.nlm.nih.gov/29059492/
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
600 mg 1 times / day steady, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 2.0 years (range: 1.0–17.0)
Health Status: unhealthy
Age Group: 2.0 years (range: 1.0–17.0)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/29059492/
unhealthy, 57.0 years (range: 33–73 years)
Health Status: unhealthy
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
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:
https://pubmed.ncbi.nlm.nih.gov/29059492/
unhealthy, 57.0 years (range: 33–73 years)
Health Status: unhealthy
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
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:
https://pubmed.ncbi.nlm.nih.gov/29059492/
unhealthy, 57.0 years (range: 33–73 years)
Health Status: unhealthy
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
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:
https://pubmed.ncbi.nlm.nih.gov/29059492/
unhealthy, 57.0 years (range: 33–73 years)
Health Status: unhealthy
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
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:
https://pubmed.ncbi.nlm.nih.gov/29059492/
unhealthy, 57.0 years (range: 33–73 years)
Health Status: unhealthy
Age Group: 57.0 years (range: 33–73 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29059492/
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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:
https://pubmed.ncbi.nlm.nih.gov/28432176
unhealthy, 7.0 years (range: 1.0–20.0 years)
Health Status: unhealthy
Age Group: 7.0 years (range: 1.0–20.0 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/28432176
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
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
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209092s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946
substrate
1193
substrate
1388
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
Nav1.5
116

Cav1.2
58

CYP3A
227

CYP1A2
2153

CYP2E1
1060

CYP3A4/5
296

BCRP
910

OCT2
779

MATE1
415

BSEP
550
FMO3
77

BCRP
697

P-gp
2052

CYP1A2
1197

CYP2J2
71

CYP3A5
446

CYP2A6
626

CYP2B6
776

CYP2C8
810

CYP2C18
149

CYP2C19
1119

CYP2E1
729
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
MATE1
416
 yes [Ki 1.7 uM]
OCT2
782
 yes [Ki 1.9 uM]
CYP1A2
2333
 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
BCRP
985
 yes [Ki 24 uM]
CYP2E1
1146
 yes [Ki 24.5 uM]
CYP3A4/5
357
 yes [Ki 30 uM]
BSEP
554
 yes [Ki 4.7 uM]
CYP3A
317
 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
CYP1A2
1197
 minor
CYP2J2
71
 minor
CYP3A5
446
 minor
CYP2A6
626
 no
CYP2B6
776
 no
CYP2C18
149
 no
CYP2C19
1119
 no
CYP2C8
810
 no
CYP2C9
1193
 no
CYP2D6
1388
 no
CYP2E1
729
 no
BCRP
697
 weak
P-gp
2052
 weak
FMO3
77
 yes
CYP3A4
1946
 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

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Cav1.2
63
Nav1.5
119
hERG
2263
hERG
2263
LEQ803
3
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA003A9C
https://www.aablocks.com/goods/Goods/detail?id=AA003A9C
Aaron Chemicals
AR003B14
http://www.aaronchem.com/1211441-98-3
abcr GmbH
AB453201
http://www.abcr.com/shop/en/AB453201
Achemo Scientific Limited
AC-92785
http://www.achemo.com/search/?Keyword=1211441-98-3
Achemtek
0102-015188
http://www.achemtek.com/1211441-98-3
Acorn PharmaTech
ACN-040728
http://www.acornpharmatech.com/
Adooq BioScience
A13549
https://www.adooq.com/lee011.html
AK Scientific, Inc. (AKSCI)
2513AH
http://www.aksci.com/item_detail.php?cat=2513AH
AK Scientific, Inc. (AKSCI)
SYN1213
http://www.aksci.com/item_detail.php?cat=SYN1213
Alsachim
3243
http://www.alsachim.com/product-C4518-glo.bal-view.html
Ambinter
Amb22586452
http://www.ambinter.com/reference/22586452
Angel Pharmatech
AG-11323
http://www.angelpharmatech.com/1211441-98-3.html
Angene
AGN-PC-0WAMDE
http://www.angenechemical.com/productshow/AGN-PC-0WAMDE.html
ApexBio Technology
A8641
http://www.apexbt.com/lee011.html
Ark Pharm
AK174906
http://www.arkpharminc.com/products/1211441-98-3.html
AvaChem Scientific
6736
https://www.avachem.com/productSearch.asp?6736
Axon MedChem
2273
https://www.axonmedchem.com/product/2273
BioChemPartner
BCP08804
http://www.biochempartner.com/1211441-98-3-BCP08804
BioCrick
BCC3926
http://www.biocrick.com/LEE011-BCC3926.html
BioSynth
J-690066
https://www.biosynth.com/en/products/all-products/products/J-690079.html
BOC Sciences
1211441-98-3
https://www.bocsci.com/ribociclib-cas-1211441-98-3-item-462559.html
BOC Sciences
1328934-40-2
https://isotope.bocsci.com/product/ribociclib-d6-cas-1328934-40-2-351224.html
Boerchem
BC600363
http://www.boerchem.com/?product_43198.html
Chem Scene
CS-1750
http://www.chemscene.com/1211441-98-3.html
ChemieTek
CT-LEE011
http://www.chemietek.com/lee011-details.aspx
Chemspace
CSSB00015190620
https://chem-space.com/CSSB00015190620
ChemWise
AR60115
http://www.chemwisellc.com/product/ribociclib-lee011/
Clearsynth
CS-O-32732
https://www.clearsynth.com/en/CSO32732.html
Clearsynth
CS-T-30953
https://www.clearsynth.com/en/CST30953.html
DAOGE BIOPHARMA
DG21-13348
https://www.daogechem.com/product/1211441-98-3.html
DC Chemicals
DC7453
http://www.dcchemicals.com/product_show-Ribociclib_LEE011_.html
Debye Scientific
DA-35904
http://www.debyesci.com/cas_1211441-98-3.html
eNovation Chemicals
D372453
http://www.enovationchem.com/productDetails.asp?productID=D372453
eNovation Chemicals
Y0974892
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0974892
Excenen
EX-A304
http://www.excenen.com/searchresultlist.php?id=1211441-98-3
Finetech
FT-0700117
http://www.finetechnology-ind.com/prod/detail/pub/1211441-98-3.html
Hairui
HR142611
http://www.hairuichem.com/en/product/1211441-98-3.html
iChemical
EBD3317897
http://www.ichemical.com/products/1211441-98-3.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network
LN01328196
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01328196
Lancrix Chemicals
824360
http://www.lancrix.com/product/detail-14-1323.htm
Matrix Scientific
147253
https://www.matrixscientific.com/147253.html
MedChem Express
HY-15777
https://www.medchemexpress.com/LEE011.html
MuseChem
I000792
https://www.musechem.com/product/I000792.html
Parchem
47527
https://www.parchem.com/chemical-supplier-distributor/Ribociclib-------047527.aspx
Smolecule
S002107
http://www.smolecule.com/products/s002107
Smolecule
S541384
http://www.smolecule.com/products/s541384
Sun-shine Chemical
LEE011
http://www.sun-shinechem.com/1211441-98-3.html
Synblock Inc
SB18480
http://www.synblock.com/product/1211441-98-3.html
THE BioTek
bt-253544
https://www.thebiotek.com/product/inhibitors/bt-253544
THE BioTek
bt-280472
https://www.thebiotek.com/product/inhibitors/bt-280472
Tocris
7050
https://www.tocris.com/products/ribociclib_7050
TubePharm
Tube013
http://www.tubepharm.com/product/1211441-98-3,1256963-02-6-en.html
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

Patents

08415355
6
08685980
6
20100105653
3
20110152244
3
JP2012500785A
3
JP2013542257A
3

Sample Use Guides

In Vivo Use Guide
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
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 Mon Mar 31 23:42:16 GMT 2025
Edited
by admin
on Mon Mar 31 23:42:16 GMT 2025
Record UNII
63YF7YKW7E
Record Status Validated (UNII)
Record Version
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Name Type Language
RIBOCICLIB HYDROCHLORIDE
Common Name English
7H-PYRROLO(2,3-D)PYRIMIDINE-6-CARBOXAMIDE, 7-CYCLOPENTYL-N,N-DIMETHYL-2-((5-(1-PIPERAZINYL)-2-PYRIDINYL)AMINO)-, HYDROCHLORIDE (1:1)
Preferred Name English
Code System Code Type Description
DRUG BANK
DBSALT002059
Created by admin on Mon Mar 31 23:42:16 GMT 2025 , Edited by admin on Mon Mar 31 23:42:16 GMT 2025
PRIMARY
FDA UNII
63YF7YKW7E
Created by admin on Mon Mar 31 23:42:16 GMT 2025 , Edited by admin on Mon Mar 31 23:42:16 GMT 2025
PRIMARY
PUBCHEM
67242274
Created by admin on Mon Mar 31 23:42:16 GMT 2025 , Edited by admin on Mon Mar 31 23:42:16 GMT 2025
PRIMARY
CAS
1211443-80-9
Created by admin on Mon Mar 31 23:42:16 GMT 2025 , Edited by admin on Mon Mar 31 23:42:16 GMT 2025
PRIMARY
Related Record Type Details
Structure of RIBOCICLIB
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of RIBOCICLIB
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