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KISQALI® (ribociclib) mechanism of action

Indications:1

 

  • KISQALI is indicated for the treatment of women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (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 luteinising hormone-releasing hormone (LHRH) agonist

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

To learn more about the safety profile of KISQALI, visit our portal page here.

For full safety profile information, please refer to the KISQALI Summary of Product Characteristics.

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

KISQALI selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4/6) in eligible patients with HR+/HER2– aBC, 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– aBC

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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

aBC, advanced breast cancer; CDK4, cyclin-dependent kinase 4; CDK6, cyclin-dependent kinase 6; E2F, E2 transcription factor; ER, oestrogen receptor; HER2−, human epidermal growth factor receptor 2-negative; HR+, hormone receptor-positive; IC50, half-maximal inhibitory concentration; pRb, retinoblastoma protein.

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 | March 2025 | 442145

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.