Drug intelligence / Profile preview

ribociclib + nonsteroidal aromatase inhibitor ± luteinizing hormone-releasing hormone

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

Ribociclib + NSAI ± LHRH is a combination therapy used as adjuvant treatment for patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) early breast cancer at high risk of recurrence. Ribociclib is an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells. Nonsteroidal aromatase inhibitors (NSAI) such as letrozole or anastrozole inhibit the enzyme aromatase, reducing estrogen production and thus limiting the growth stimulus for HR+ breast cancer cells. In premenopausal women and men, a luteinizing hormone-releasing hormone (LHRH) agonist like goserelin is added to suppress ovarian/testicular function and further reduce estrogen levels. This regimen has demonstrated significant improvements in invasive disease-free survival and distant disease-free survival compared to NSAI alone in large phase III trials such as NATALEE[1][2][5][6].

Other names
ribociclib + NSAI ± LHRHribociclib plus nonsteroidal aromatase inhibitor with or without luteinizing hormone-releasing hormone agonist
02

Targets

CYP19A1 (Aromatase)GnRHR (Gonadotropin-releasing hormone receptor)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)

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