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ribociclib

Trade name: kisqali

Small moleculeapprovedBreakthrough Therapy FDA

Approved

Mar 13, 2017

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. — NCATS

Clinical trial activity

154 trials · 125 clinical orgs · 3 marketing orgs

Phase 1
68
Phase 2
103
Phase 3
25
Phase 4
5

Earliest trial started Dec 21, 2010 (NCT01237236)

Timeline

2010s

  1. Jan 1, 2010

    Novartis — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2013

    Novartis — Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 2013

    Novartis — Earliest Phase 3 Sponsor(trial)

  4. Mar 13, 2017

    Novartis — Earliest FDA Approval

  5. Mar 13, 2017

    Novartis — NDA Secondary Org

  6. Mar 13, 2017

    Novartis — NDA Organization

2020s

  1. May 1, 2023

    MSN Laboratories — Marketing Organization

  2. Jan 10, 2024

    Alembic — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • kisqali femara co-pack (copackaged)

    with letrozole

    Also known as letrozole and ribociclib

Approval history

  • approvedPriority reviewBreakthroughMar 13, 2017

Chemistry & pharmacology

Loading structure…

SMILES

CN(C)C(=O)c1cc2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n1C1CCCC1
Mol. weight
434.55 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

First in class

Sources

Also known as

  • kisqali
  • kisqali
  • kisqali
  • lee011
  • lee011
  • lee011
  • lee-011
  • lee-011
  • lee011-bba
  • lee011-bba
  • nvp-lee011
  • nvp-lee011
  • ribociclib
  • ribociclib
  • ribociclib
  • ribociclib
  • ribociclib
  • ribociclib
  • ribociclib
  • ribociclib succinate
  • ribociclib succinate
  • ribociclib succinate
  • ribociclib succinate

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07195227Phase 2Dec 1, 2025MedSIR
NCT07237256Phase 3Dec 1, 2025Borstkanker Onderzoek Groep, Canadian Cancer Trials Group, Curie Institute, German Breast Group Forschungs GmbH, Gruppo Italiano Mammella (GIM), Latin American Cooperative Oncology Group, Novartis, SOLTI Breast Cancer Research Group, Swiss Cancer Institute, UNICANCER
NCT07085767Phase 3Oct 31, 2025Novartis, Olema Pharmaceuticals, Inc.
NCT07174336Phase 3Oct 27, 2025Eli Lilly, Pfizer
NCT07164976Phase 1/Phase 2 (Phase 2)Oct 1, 2025Nagoya City University, Novartis
NCT07054190Phase 2Sep 9, 2025Roche
NCT06953882Phase 2Jul 9, 2025Breast Cancer Research Foundation, Novartis, Yale University
NCT06757634Phase 3Jun 30, 2025Celcuity
NCT06849947Phase 2Jun 30, 2025Sungkyunkwan University
NCT07002177Phase 1/Phase 2 (Phase 2)Jun 1, 2025Forward Pharmaceuticals Co., Ltd.
NCT06585969Phase 3May 1, 2025Danish Breast Cancer Cooperative Group
NCT06810492N/AApr 1, 2025Wuhan University
NCT06726148Phase 1/Phase 2 (Phase 2)Mar 26, 2025Novartis
NCT06760637Phase 3Jan 6, 2025Pfizer
NCT06959979Early Phase 1 (Phase 1)Nov 25, 2024Universita' Cattolica del Sacro Cuore
NCT06699472Phase 2Oct 31, 2024Fudan University
NCT06377852Phase 3Oct 29, 2024American Society of Clinical Oncology, Patient-Centered Outcomes Research Institute
NCT06656624Phase 2Aug 13, 2024Jiangnan University, Nanjing Medical University
NCT06380751Phase 3Aug 1, 2024AstraZeneca
NCT06569459Phase 2Jul 9, 2024Nanjing Medical University
Showing 20 of 154 trials
Page 1 / 8

Organizations

Research & Development (125)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
NovartisFor profit854252010
National Cancer Institute (NCI)Government9022015
Harvard UniversityAcademic/Hospital5422016
Array BioPharmaFor profit4412012
Nanjing Medical UniversityAcademic/Hospital4312023
PfizerFor profit4332022
SOLTI Breast Cancer Research GroupAcademic/Hospital4322017
UNICANCERAcademic/Hospital4332017
University of Texas at HoustonAcademic/Hospital4312015
Borstkanker Onderzoek GroepAcademic/Hospital3222017
Breast Cancer Research FoundationAcademic/Hospital3022021
RocheFor profit3322021
University of BarcelonaAcademic/Hospital3022017
University of MichiganAcademic/Hospital3322017
University of PennsylvaniaAcademic/Hospital3212015
AstraZenecaFor profit2222023
Barrow Neurological InstituteAcademic/Hospital2012016
Chinese Academy of Medical SciencesAcademic/Hospital2112023
Curie InstituteAcademic/Hospital2022022
Georgetown UniversityAcademic/Hospital2222017
125 organizations
Page 1 / 7

Marketing (5)

OrganizationOrg typeRelationshipDate
AlembicFor profitMKTGJan 10, 2024
MSN LaboratoriesFor profitMKTGMay 1, 2023
NovartisFor profitNDA2Mar 13, 2017
NovartisFor profitSYNMar 13, 2017
NovartisFor profitNDAMar 13, 2017