Ribociclib is a cyclin-dependent kinase inhibitor used to treat HR+, HER2- breast cancer. These proteins, when over-activated, can enable cancer cells to grow and divide too quickly.
- Mechanism
- Curator reviewed · 3 references
Ribociclib is a selective inhibitor of cyclin-dependent kinases (CDK) 4 and 6. These kinases are activated upon binding to D-cyclins and are downstream of signaling pathways which lead to cell cycle progression and cellular proliferation. The cyclin D-CDK4/6 complex regulates cell cycle progression through phosphorylation of the retinoblastoma protein (pRb). Ribociclib has been shown in vitro to decrease pRb phosphorylation, resulting in arrest in the G1 phase of the cell cycle and reduced proliferation in breast cancer-derived models. The inhibition of pRb phosphorylation is correlated with a decrease in the volume of tumor cells.
- Primary indication
- Ribociclib is indicated in combination with an aromatase inhibitor (e.g. letrozole) for the adjuvant treatment of adults with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative stage II and III early breast cancer...Curator reviewed · 7 structured indications
- Formula / weight
- C23H30N8O · 434.548 g/mol (avg)
- First approval
- Canada, 2018 · United States, 2017 · European Union, 2020
- Code names
- LEE-011 · LEE-011A
- Brand names
Resolves to
RHXHGRAEPCAFML-UHFFFAOYSA-NSMILESCN(C)C(=O)C1=CC2=CN=C(NC3=CC=C(C=N3)N3CCNCC3)N=C2N1C1CCCC1What you can answer from here — as of September 23, 2026
Which drugs share a target with Ribociclib, and which of those have an active Phase 3 trial?
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