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Kisqali (LEE011)

Novartis · FDA-approved active Small molecule Quality 66/100

Kisqali works by blocking a protein called cyclin-dependent kinase 4, which helps cancer cells grow and divide.

Kisqali (LEE011) by Novartis is a marketed CDK4 inhibitor for the adjuvant treatment of early breast cancer, positioned in a competitive landscape alongside palbociclib and abemaciclib. Its key strength lies in its mechanism of action, which effectively blocks cyclin-dependent kinase 4, aiding in the inhibition of cancer cell growth and division. The primary risk to Kisqali is the upcoming patent expiry in 2028, which could lead to increased competition from generics.

At a glance

Generic nameLEE011
Also known asribociclib, Kisqali, Ribociclib, ribociclib
SponsorNovartis
Drug classKinase Inhibitor
TargetCyclin-dependent kinase 4
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved
First approval2017
Annual revenue3600

Mechanism of action

Ribociclib is an inhibitor of cyclin-dependent kinase (CDK) and 6. These kinases are activated upon binding to D-cyclins and play crucial role in signaling pathways which lead to cell cycle progression and cellular proliferation. The cyclin D-CDK4/6 complex regulates cell cycle progression through phosphorylation of the retinoblastoma protein (pRb). In vitro, ribociclib decreased pRb phosphorylation leading to arrest in the G1 phase of the cell cycle and reduced cell proliferation in breast cancer cell lines. In vivo, treatment with single agent ribociclib in rat xenograft model with human tumor cells led to decreased tumor volumes, which correlated with inhibition of pRb phosphorylation. In studies using patient-derived estrogen receptor positive breast cancer xenograft models, combination of ribociclib and antiestrogen (e.g., letrozole) resulted in increased tumor growth inhibition compared to each drug alone. Additionally, the combination of ribociclib and

Approved indications

Common side effects

Drug interactions

Key clinical trials

Patents

PatentExpiryType

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity
SEC EDGARRevenue + earnings

Competitive intelligence

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