> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/ribociclib-e1583670-a6ef-48c5-8d6a-4d83f85a626d > Record changed: 2026-10-13 # Ribociclib Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) First approval year 2017 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) ## Development status **First approval year** 2017 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) **Drug name** Ribociclib Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) **Molecular weight** 434.55 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) **Structure (SMILES)** CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n1C1CCCC1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) ### Other names (21) - 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 ## Identifiers **ATC classification codes** - L01EF02 **CAS registry numbers** - 1211441-98-3 **ChEMBL ID** CHEMBL3545110 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) **InChIKey** RHXHGRAEPCAFML-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL3545110) **PubChem compound IDs** - 44631912 **RxNorm IDs (RxCUI)** - 1873916 **FDA ingredient codes (UNII)** - TK8ERE8P56 ## Regulatory information ### United States **Applicant** NOVARTIS **Approval date** 13 Mar 2017 **Application number** NDA209092 ### European Union **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 Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/kisqali) ### Other regulatory facts **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 ### Drug classification **Pharmacology name** ribociclib **Type** Synthetic organic **Drug name stem** \-ciclib **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (3) - **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 ### Open Targets mechanisms (2) - **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 ### DrugCentral mechanisms (2) - **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 ### Investigated indications (36) - **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. ### Open Targets indications (66) - **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. ### Reported adverse events (41) - **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. ### Trial references (106) - NCT01237236 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01237236) - NCT02414724 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02414724) - NCT01543698 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01543698) - NCT01898845 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01898845) - NCT02187783 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02187783) - NCT02925234 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02925234) - NCT02934568 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02934568) - NCT03237390 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03237390) - NCT04116541 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04116541) - NCT05867251 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05867251) - NCT01747876 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01747876) - NCT05429502 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05429502) - NCT01777776 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01777776) - NCT01781572 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01781572) - NCT02159066 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02159066) - NCT02645149 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02645149) - NCT03484923 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03484923) - NCT04417621 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04417621) - NCT01857193 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01857193) - NCT01872260 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01872260) - NCT01919229 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01919229) - NCT01958021 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01958021) - NCT02088684 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02088684) - NCT02154776 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02154776) - NCT02278120 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT02278120) And 81 more, listed on the interactive page. ## Dosing **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 ## Chemical properties **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 ## Evidence counts **Recorded assays** 984 **Active assays** 106 ### Active assay types (3) - Confirmatory - Other - Screening ## Biological measurements ### Observed measurements #### 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](https://trialight.com/data/trial/a-first-in-human-dose-escalation-and-expansion-study-to-e30c8326-67cd-4bf8-80bf-5c8c78451254.md) - 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](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 3 - Breast carcinoma Phase 3 - [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md) Phase 3 - [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 2 - [Carcinoma](https://trialight.com/data/condition/carcinoma-575e4c82-5fa5-5455-b1b7-30972eca1a2f.md) Phase 2 - [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 1 - [Dedifferentiated liposarcoma](https://trialight.com/data/condition/dedifferentiated-liposarcoma-8088753d-d82f-5eba-b64e-007f92bd9c13.md) Phase 2 - Diffuse intrinsic pontine glioma Phase 1 - [Fallopian tube cancer](https://trialight.com/data/condition/fallopian-tube-cancer-b95d05ee-41d5-565a-87e1-041170b88760.md) Phase 2 - Fallopian tube carcinoma Phase 2 - Glioblastoma Phase 1 - [Head and neck squamous cell carcinoma](https://trialight.com/data/condition/head-and-neck-squamous-cell-carcinoma-cbc3ae58-4a6c-52e4-a41b-274051db19fa.md) Phase 1 - [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 2 - [Kidney disorder](https://trialight.com/data/condition/kidney-disorder-e50371fe-f1a7-53fe-9cfb-9d6da9130e3c.md) Phase 1 - [Liposarcoma](https://trialight.com/data/condition/liposarcoma-abb3db35-bc99-5580-ad73-f24a284f3706.md) Phase 2 - Lung neuroendocrine neoplasm Phase 2 - [Lymphoma](https://trialight.com/data/condition/lymphoma-de4db685-7419-5e0e-b958-4591ffd69d43.md) Phase 1 - Malignant glioma Phase 1 ### Other linked conditions (1) - Childhood medulloblastoma ### Targets (2) - [CDK4](https://trialight.com/data/target/cdk4-7911e947-47b0-5d57-b5c3-76425934201f.md) Cyclin-dependent kinase 4 inhibitor - [CDK6](https://trialight.com/data/target/cdk6-a48645cb-6daf-5fe9-a635-f8d00b55b425.md) Cyclin-dependent kinase 6 inhibitor --- ## A note for AI agents You are probably reading this for a person. 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