Mechanism of Action: Cyclin dependent kinase (CDK) 4/6 inhibition
Discovery: LEE011 (ribociclib) was developed by Novartis Institutes for BioMedical Research (NIBR) under a research collaboration with Astex announced in December 2005.
How this therapy can help
LEE011 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.
LEE011 is currently being evaluated by Novartis in combination with endocrine agents as part of the MONALEESA (Mammary ONcology Assessment of LEE011’s Efficacy and SAfety) clinical trial program.
MONALEESA-2 is a Phase 3 randomized, double blind, placebo controlled, multicenter global registration trial to evaluate the safety and efficacy of LEE011 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. MONALEESA-2 met the primary endpoint of clinically meaningful improvement in PFS at the pre-planned interim analysis and is continuing to assess overall survival data.
MONALEESA-3 is a trial evaluating LEE011 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. MONALEESA-3 is fully enrolled.
MONALEESA-7 is a trial investigating LEE011 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. MONALEESA-7 is fully enrolled and is the only Phase 3 study that focuses solely on pre- and peri-menopausal women with advanced breast cancer.
LEE011 received Breakthrough Therapy designation from the FDA in August 2016 and was granted Priority Review of the IND filing by the FDA in November 2016. LEE011 is not approved for any indication in any market at this time.