Ribociclib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2017
- First approval year
- 2017
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Ribociclib
- Molecular weight
- 434.55
- Structure (SMILES)
- CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n1C1CCCC1
- lee 011
- lee 011a
- Lee-011
- LEE-011
- LEE-011A
- lee011
- LEE011
- lee011a
- LEE011A
- nvp lee011
- NVP-LEE011
- ribociclib
- Ribociclib
- Ribociclib [INN]
- Ribociclib [MI]
- Ribociclib [USAN]
- Ribociclib [WHO-DD]
- ribociclib inn
- ribociclib mi
- ribociclib usan
- ribociclib who dd
- ATC classification codes
- L01EF02
- CAS registry numbers
- 1211441-98-3
- ChEMBL ID
- CHEMBL3545110
- InChIKey
- RHXHGRAEPCAFML-UHFFFAOYSA-N
- PubChem compound IDs
- 44631912
- RxNorm IDs (RxCUI)
- 1873916
- FDA ingredient codes (UNII)
- TK8ERE8P56
- Applicant
- NOVARTIS
- Approval date
- 13 Mar 2017
- Application number
- NDA209092
- Status
- Authorised
- Status date
- 22 Aug 2017
- Authorisation date
- 22 Aug 2017
- Approved indications
- Early breast cancer Kisqali in combination with an aromatase inhibitor is indicated for the adjuvant treatment of patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative early breast cancer at high risk of recurrence (see section 5.1 for selection criteria). In pre- or perimenopausal women, or in men, the aromatase inhibitor should be combined with a luteinising hormone-releasing hormone (LHRH) agonist. Advanced or metastatic breast cancer Kisqali is indicated for the treatment of women with HR-positive, HER2-negative locally advanced or metastatic breast cancer in combination with an aromatase inhibitor or fulvestrant as initial endocrine-based therapy, or in women who have received prior endocrine therapy. In pre- or perimenopausal women, the endocrine therapy should be combined with a LHRH agonist.
- Product number
- EMEA/H/C/004213
- Authorisation holder
- Novartis Europharm Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 0
- Designations
- 4
- First in class
- Yes
- Fast track
- No
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Pharmacology name
- ribociclib
- Type
- Synthetic organic
- Drug name stem
- -ciclib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- cyclin dependent kinase 4
- Gene symbol
- CDK4
- Protein identifier
- P11802
- Median affinity
- 8
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Cyclin-dependent kinase 4 inhibitor
- Action type
- Inhibitor
- Target
- Cyclin-dependent kinase 4
- Protein identifier
- P11802
- Mechanism
- Cyclin-dependent kinase 6 inhibitor
- Action type
- Inhibitor
- Target
- Cyclin-dependent kinase 6
- Protein identifier
- Q00534
- Mechanism
- Cyclin-dependent kinase 4 inhibitor
- Action type
- Inhibitor
- Target
- Cyclin-dependent kinase 4
- Mechanism
- Cyclin-dependent kinase 6 inhibitor
- Action type
- Inhibitor
- Target
- Cyclin-dependent kinase 6
- Action type
- Inhibitor
- Gene symbol
- CDK4
- Protein identifier
- P11802
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- CDK6
- Protein identifier
- Q00534
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Prostatic Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000196
- Subject identifier
- D011471
- Condition
- Precursor Cell Lymphoblastic Leukemia-Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000220
- Subject identifier
- D054198
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Carcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000313
- Subject identifier
- D002277
- Condition
- Glioblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Liposarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000569
- Subject identifier
- D008080
- Condition
- Lymphoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000574
- Subject identifier
- D008223
- Condition
- Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Neuroblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000621
- Subject identifier
- D009447
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0001075
- Subject identifier
- D010051
- Condition
- Astrocytoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002499
- Subject identifier
- D001254
- Condition
- Thymus Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002626
- Subject identifier
- D013953
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Liposarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003085
- Subject identifier
- D008080
- Condition
- Kidney Diseases
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003086
- Subject identifier
- D007674
- Condition
- Uterine Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003859
- Subject identifier
- D014594
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Neuroendocrine Tumors
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005220
- Subject identifier
- D018358
- Condition
- Rhabdoid Tumor
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005701
- Subject identifier
- D018335
- Condition
- Diffuse Intrinsic Pontine Glioma
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000026
- Subject identifier
- D000080443
- Condition
- Fallopian Tube Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000251
- Subject identifier
- D005185
- Condition
- Paraganglioma
- Highest recorded phase
- 1
- Condition identifier
- EFO:1000453
- Subject identifier
- D010235
And 11 more, listed on the interactive page.
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000305
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000313
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000569
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000574
- Highest recorded phase
- 1
- Condition identifier
- EFO_0000616
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003086
- Highest recorded phase
- 1
- Condition identifier
- EFO_0003869
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004952
- Highest recorded phase
- 2
- Condition identifier
- EFO_0020985
- Highest recorded phase
- 1
- Condition identifier
- EFO_1000453
- Highest recorded phase
- 1
- Condition identifier
- EFO_1001901
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001968
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001657
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002447
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002601
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002728
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0002797
- Condition identifier
- MONDO_0004967
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0004992
- Highest recorded phase
- 2
And 41 more, listed on the interactive page.
- Event
- alanine aminotransferase increased
- Reports
- 173
- Reporting signal score
- 180.411
- Event
- alopecia
- Reports
- 166
- Reporting signal score
- 147.892
- Event
- anaemia
- Reports
- 226
- Reporting signal score
- 117.135
- Event
- aspartate aminotransferase increased
- Reports
- 150
- Reporting signal score
- 152.995
- Event
- blood alkaline phosphatase increased
- Reports
- 65
- Reporting signal score
- 64.5716
- Event
- blood creatinine increased
- Reports
- 104
- Reporting signal score
- 79.1719
- Event
- bone lesion
- Reports
- 37
- Reporting signal score
- 91.5865
- Event
- bone marrow infiltration
- Reports
- 18
- Reporting signal score
- 71.0143
- Event
- bone pain
- Reports
- 101
- Reporting signal score
- 108.057
- Event
- breast cancer
- Reports
- 106
- Reporting signal score
- 150.979
- Event
- breast cancer metastatic
- Reports
- 165
- Reporting signal score
- 574.989
- Event
- breast cancer recurrent
- Reports
- 26
- Reporting signal score
- 61.6611
- Event
- carbohydrate antigen 15-3 increased
- Reports
- 42
- Reporting signal score
- 183.775
- Event
- constipation
- Reports
- 139
- Reporting signal score
- 57.1921
- Event
- decreased appetite
- Reports
- 147
- Reporting signal score
- 68.6027
- Event
- disease progression
- Reports
- 118
- Reporting signal score
- 75.6886
- Event
- electrocardiogram qt prolonged
- Reports
- 289
- Reporting signal score
- 589.843
- Event
- fatigue
- Reports
- 412
- Reporting signal score
- 128.711
- Event
- gamma-glutamyltransferase increased
- Reports
- 75
- Reporting signal score
- 84.5682
- Event
- general physical health deterioration
- Reports
- 132
- Reporting signal score
- 122.855
- Event
- hepatotoxicity
- Reports
- 142
- Reporting signal score
- 282.403
- Event
- hot flush
- Reports
- 76
- Reporting signal score
- 71.7158
- Event
- leukopenia
- Reports
- 293
- Reporting signal score
- 516.039
- Event
- liver function test increased
- Reports
- 89
- Reporting signal score
- 140.81
- Event
- malignant neoplasm progression
- Reports
- 335
- Reporting signal score
- 637.104
And 16 more, listed on the interactive page.
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And 81 more, listed on the interactive page.
- Dose
- 400 mg or 600 mg
- Route
- Oral
- How often
- Once daily for 21 days on, 7 days off in 28-day cycles
Conditions of use
- Take with or without food
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 91.21
- Calculated partition coefficient (ALogP)
- 2.8
- Calculated partition coefficient (XLogP)
- 2.2
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 5
- Heavy atoms
- 32
- Molecular formula
- C23H30N8O
- Monoisotopic mass
- 434.25425761
- Natural product
- Yes
- Recorded assays
- 984
- Active assays
- 106
- Confirmatory
- Other
- Screening
Oral bioavailability
- Median
- 31
- Mean
- 31
- Minimum
- 31
- Maximum
- 31
- Unit
- %
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (183)
- (VELA) Study of BLU-222 in Advanced Solid Tumors
- [177Lu]Lu-NeoB in Combination With Ribociclib and Fulvestrant in Participants With ER+, HER2- and GRPR+ Advanced Breast Cancer
- [18F]FLT PET/CT in Rb+ Metastatic Breast Cancer
- A Companion Sample Collection Protocol to Support the Discovery of Breast Cancer Aberrations With Treatment of CDK4/6 Therapy/LEE011/Ribociclib
- A First-in-human Dose Escalation and Expansion Study to Evaluate the Safety, and Tolerability of AZD8421 Alone or in Combination in Participants With Selected Advanced or Metastatic Solid Tumors
- A Non-interventional Study for Kisqali (Ribociclib) in Combination With an Aromatase Inhibitor for Adjuvant Treatment in Patients With HR+/HER2- Early Breast Cancer at High Risk of Recurrence
- A Pharmacodynamics Pre-surgical Study of LEE011 in Early Breast Cancer Patients (MONALEESA-1)
- A Phase 0/I Study of Ribociclib (LEE011) in Combination With Everolimus in Preoperative Recurrent High-Grade Glioma Patients Scheduled for Resection
- A Phase I Study of LEE011 in Asian Patients
- A Phase I/II Study of Ribociclib,a CDK4/6 Inhibitor, Following Radiation Therapy
- A Phase Ib Dose Escalation Study of the Combination of LEE011 With Letrozole and Dose Expansion of LEE011 With Hormonal Therapy for the Treatment of Pre-(With Goserelin) and Postmenopausal Women With Hormone Receptor Positive, HER2-negative, Advanced Breast Cancer
- A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma
- A Phase Ib/II Study of LEE011 in Combination With MEK162 in Patients With NRAS Mutant Melanoma
- A Phase Ib/II Study of LGX818 in Combination With MEK162 in Adult Patients With BRAF Dependent Advanced Solid Tumors
- A Phase Ib/II Study to Evaluate Multiple Combination Therapies of FWD1802 in Patients With ER+/HER2- BC
- A Phase II Study Assessing Efficacy & Safety of Ribociclib in Patients With Advanced Well/Dedifferentiated Liposarcoma
- A Phase II Study Evaluating the Efficacy and Safety of Inavolisib Plus Ribociclib Plus Fulvestrant Versus Placebo Plus Ribociclib Plus Fulvestrant in Participants With Advanced Breast Cancer
- A Phase II, Two-Arm Study of Everolimus and Letrozole, +/- Ribociclib (Lee011) in Patients With Advanced or Recurrent Endometrial Carcinoma
- A Phase IIIb Study to Evaluate Camizestrant Plus Ribociclib in ER-positive, HER2-negative Advanced Breast Cancer
- A Phase IV Study to Collect Data on the Efficacy and Safety of RIBociclib in Older Women With Breastcancer
In development for (36)
- Acute lymphoblastic leukemia Phase 1
- Anaplastic astrocytoma Phase 1
- Breast cancer Phase 3
- Breast carcinoma Phase 3
- Breast neoplasm Phase 3
- Cancer Phase 2
- Carcinoma Phase 2
- Colorectal cancer Phase 1
- Dedifferentiated liposarcoma Phase 2
- Diffuse intrinsic pontine glioma Phase 1
- Fallopian tube cancer Phase 2
- Fallopian tube carcinoma Phase 2
- Glioblastoma Phase 1
- Head and neck squamous cell carcinoma Phase 1
- Hepatocellular carcinoma Phase 2
- Kidney disorder Phase 1
- Liposarcoma Phase 2
- Lung neuroendocrine neoplasm Phase 2
- Lymphoma Phase 1
- Malignant glioma Phase 1
Other linked conditions (1)
- Childhood medulloblastoma