Clinical Pipeline

DiscoveryPhase 1Phase 2Phase 3Marketed

Kisqali® (ribociclib)

CDK4/6 inhibitor (Oncology)

.....

Partner: novartis-med

Mechanism of Action:  Cyclin dependent kinase (CDK) 4/6 inhibition

Indication: Oncology

Discovery: Kisqali® (ribociclib, formerly known as LEE011) was developed by Novartis Institutes for BioMedical Research (NIBR) under a research collaboration with Astex announced in December 2005.

Learn about the Kisqali drug discovery program:

How this therapy can help

Kisqali® is a selective CDK inhibitor, a new class of drugs that help slow the progression of cancer by inhibiting two proteins called CDK 4 and 6 (CDK4/6). These proteins, when over-activated in a cell, can enable cancer cells to grow and divide too quickly. Kisqali® is the only CDK4/6 inhibitor, in combination with endocrine therapy, to show superior overall survival compared to endocrine therapy alone in advanced breast cancer.

Marketed product

Kisqali® received US marketing approval by the FDA in March 2017 and by the EMA in August 2017 as a first-line drug treatment for postmenopausal women with HR+/HER2- advanced breast cancer in combination with an aromatase inhibitor. For full prescribing and safety information please see here.

Kisqali® received US marketing approval in July 2018 and European marketing approval in December 2018 as a first-line drug treatment in combination with an aromatase inhibitor for the treatment of pre-, peri- or postmenopausal women with HR+/HER2- advanced or metastatic breast cancer and also for use in combination with fulvestrant as both first-line and second-line therapy in postmenopausal women.

Kisqali® has now been approved for use in more than 75 countries including the US and EU member states.

Clinical studies

Kisqali® continues to be evaluated by Novartis in combination with a number of other endocrine agents as part of the ongoing MONALEESA (Mammary ONcology Assessment of LEE011’s Efficacy and SAfety) clinical trial program.

The MONALEESA-2 Phase 3 randomized, double blind, placebo controlled, multicenter global registration trial to evaluate the safety and efficacy of Kisqali® in combination with letrozole compared to letrozole alone in postmenopausal women with HR+/HER2- advanced breast cancer who received no prior therapy for their advanced breast cancer met its primary endpoint at the pre-planned interim analysis due to superior efficacy compared to letrozole alone. Overall Survival follow-up is ongoing for this trial.

MONALEESA-3 evaluated Kisqali® in combination with fulvestrant compared to fulvestrant alone in men and post-menopausal women with HR+/HER2- advanced breast cancer who have received no or a maximum of one prior endocrine therapy. The results of the trial have shown that Kisqali® in combination with fulvestrant show superior overall survival in postmenopausal women advanced breast cancer. Overall Survival follow-up is ongoing for this trial.

MONALEESA-7 evaluated Kisqali® in combination with endocrine therapy and goserelin compared to endocrine therapy and goserelin alone in pre-menopausal women with HR+/HER2- advanced breast cancer who have not previously received endocrine therapy. The results read out in July 2019 showed that Kisqali® in combination with endocrine therapy and goserelin shows statistically superior overall survival in advanced breast cancer.

The NATALEE study is a Phase III clinical trial of Kisqali® with endocrine therapy in the adjuvant treatment of HR+/HER2- early breast cancer being conducted in collaboration with Translational Research In Oncology (TRIO).