KISQALI® (ribociclib) mechanism of action

Indications:1

 

Advanced breast cancer (aBC)
KISQALI is indicated for the treatment of women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative aBC in combination with an aromatase inhibitor (AI) or fulvestrant as initial endocrine-based therapy, or in women who have received prior endocrine therapy (ET)

  • In pre/perimenopausal women, the ET should be combined with a a luteinising hormone-releasing hormone (LHRH) agonist

Early breast cancer (eBC)
KISQALI, in combination with an AI, is indicated for the adjuvant treatment of patients with HR+/HER2− eBC at high risk of recurrence (see section 5.1 of the SmPC for selection criteria)

  • In pre/perimenopausal women, or in men, the AI should be combined with an LHRH agonist

KISQALI is not recommended to be used in combination with tamoxifen.

For more information on the safety profile of KISQALI in aBC click here, and eBC click here.

Please consult your local Summary of Product Characteristics for the full KISQALI safety and tolerability profile.

Droplet icon with the text 'CDK4/6i'.

KISQALI selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4/6) in patients with HR+/HER2– breast cancer, thus potentially inhibiting tumour growth1

Information on this page is based on pre-clinical research. They should not be extrapolated to clinical response.

The role of CDK4/6 in HR+/HER2– breast cancer

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Mechanism of action of KISQALI

KISQALI is a selective inhibitor of CDK4 and CDK61,2

KISQALI works by binding to the cyclin-CDK4/6 complex to inhibit the function of CDK4 and arrest the cell cycle, reducing the proliferation of cancer cells.1,2

Kisqali mechanism of action diagram showing how KISQALI works by binding to the cyclin-CDK4/6 complex to inhibit the function of CDK4.¹ ²

Adapted from Sammons SL, et al. 2017.3

In biochemical assays, KISQALI results in 50% inhibition (IC50) values of 0.01 (4.3 ng/ml) and 0.039 μM (16.9 ng/ml) for CDK4 and CDK6, respectively.1

Learn about the safety profile of KISQALI in aBC

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Learn about the safety profile of KISQALI in eBC

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aBC, advanced breast cancer; Al, aromatase inhibitor; CDK4, cyclin-dependent kinase 4; CDK6, cyclin-dependent kinase 6; E2F, E2 transcription factor; eBC, early breast cancer; ER, oestrogen receptor; ET, endocrine therapy; HER2−, human epidermal growth factor receptor 2-negative; HR+, hormone receptor-positive; IC50, half-maximal inhibitory concentration; LHRH, luteinising hormone-releasing hormone; pRb, retinoblastoma protein; SmPC, summary of product characteristics.

References

  1. KISQALI® (ribociclib) Summary of Product Characteristics. 

  2. Kim S, et al. Oncotarget 2018;9(81):35226–35240 and supplementary data.

  3. Sammons SL, et al. Curr Cancer Drug Targets 2017;17(7):637–649.

UK | November 2025 | FA-11551667

Adverse events should be reported. Reporting forms and information can be found at www.mhra.gov.uk/yellowcard. Adverse events should also be reported to Novartis online through the pharmacovigilance intake (PVI) tool at www.novartis.com/report, or alternatively email [email protected] or call 01276 698370.