Drug intelligence / Profile preview

ribociclib + nonsteroidal aromatase inhibitor

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

Overview

Ribociclib + nonsteroidal aromatase inhibitor (NSAI) is a combination therapy used for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Ribociclib is a small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which are key regulators of the cell cycle; by inhibiting these kinases, ribociclib blocks the transition from the G1 to S phase, thereby suppressing tumor cell proliferation. The nonsteroidal aromatase inhibitor component (typically letrozole or anastrozole) works by inhibiting the enzyme aromatase, which converts androgens into estrogens, thereby reducing circulating estrogen levels and depriving hormone-sensitive tumor cells of growth signals. This combination is being evaluated in clinical trials, such as HERO-KC23, as a first-line treatment compared to chemotherapy in patients with rapid disease progression.

Brand names
FemaraArimidex
Other names
ribociclib + NSAIribociclib + letrozoleribociclib + anastrozole
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)ABCB1 (P-glycoprotein)CDK4 (Cyclin-dependent kinase 4)SLCO1B3 (Organic anion transporting polypeptide 1B3)CYP19A1 (Aromatase)CDK9 (Cyclin-dependent kinase 9)OCT2 (Organic cation transporter 2)OCT1 (Organic cation transporter 1)ABCG2 (Breast cancer resistance protein)CYP3A4 (Cytochrome P450 3A4)CDK6 (Cyclin-dependent kinase 6)

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