Premium Nahrungsergänzungsmittel | artgerecht

Abemaciclib: Uses, Dosage and Side Effects

Abemaciclib is a targeted cancer medication used to treat hormone receptor-positive, HER2-negative breast cancer in adults. It works by blocking enzymes that drive tumour cell growth.

Regular tips about health Regular tips about health

Things worth knowing about "Abemaciclib"

Abemaciclib is a targeted cancer medication used to treat hormone receptor-positive, HER2-negative breast cancer in adults. It works by blocking enzymes that drive tumour cell growth.

What is Abemaciclib?

Abemaciclib is a targeted cancer therapy belonging to the class of drugs known as CDK4/6 inhibitors (cyclin-dependent kinase inhibitors). It is marketed under the brand name Verzenios and is approved for use in adults with hormone receptor-positive (HR+), HER2-negative (HER2-) advanced or metastatic breast cancer. Depending on the clinical situation, abemaciclib can be used in combination with endocrine therapy or as a monotherapy.

Indications

Abemaciclib is indicated in the following clinical settings:

In combination with an aromatase inhibitor (e.g., letrozole or anastrozole) as first-line therapy for HR+, HER2- advanced breast cancer in postmenopausal women and in men.
In combination with fulvestrant for HR+, HER2- advanced breast cancer in women who have previously received endocrine therapy.
As monotherapy for HR+, HER2- advanced breast cancer in women following prior hormone therapy and chemotherapy.
As adjuvant therapy (after surgery) in combination with endocrine therapy in high-risk patients with early-stage HR+, HER2- breast cancer.

Mechanism of Action

Abemaciclib selectively inhibits the enzymes cyclin-dependent kinase 4 and 6 (CDK4 and CDK6). These kinases play a central role in regulating the cell cycle, specifically the transition from the G1 phase to the S phase (DNA synthesis phase). By inhibiting CDK4/6, abemaciclib keeps the retinoblastoma protein (Rb) in its hypophosphorylated state, which blocks the activity of the transcription factor E2F, thereby slowing or halting tumour cell proliferation. In addition, abemaciclib promotes tumour cell senescence (a state of permanent growth arrest) and can induce programmed cell death (apoptosis).

Dosage and Administration

Abemaciclib is taken orally as a film-coated tablet. The recommended dose depends on the indication:

Combination therapy: 150 mg twice daily (every 12 hours), taken continuously without treatment breaks.
Monotherapy: 200 mg twice daily (every 12 hours), taken continuously.

The tablets may be taken with or without food. Dose reductions may be required in cases of certain side effects or when co-administered with strong CYP3A4 inhibitors. Treatment should be continued until disease progression or unacceptable toxicity.

Side Effects

Like all cancer medications, abemaciclib can cause side effects. The most common include:

Diarrhoea: Very common, especially at the start of therapy; early treatment with loperamide is recommended.
Neutropenia: Reduction in white blood cell count, increasing the risk of infection.
Anaemia and thrombocytopenia (low platelet count).
Nausea and vomiting.
Fatigue and tiredness.
Elevated liver enzymes (ALT, AST) in the blood; regular liver function monitoring is required.
Interstitial lung disease / pneumonitis: Rare but serious; patients should watch for shortness of breath or new cough.
Impaired kidney function (elevated serum creatinine).

Drug Interactions

Abemaciclib is primarily metabolised by the liver enzyme CYP3A4. Interactions are therefore possible with drugs or foods that inhibit or induce this enzyme:

Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, grapefruit juice): may increase abemaciclib blood levels; dose adjustment is required.
Strong CYP3A4 inducers (e.g., rifampicin, carbamazepine, St John's Wort): may reduce the efficacy of abemaciclib; these should be avoided if possible.

Contraindications and Precautions

Hypersensitivity to the active substance or any of the excipients.
Pregnancy and breastfeeding: Abemaciclib may harm the unborn child. Women of childbearing potential must use effective contraception during treatment.
Regular monitoring of blood counts as well as liver and kidney function tests is necessary throughout therapy.

References

European Medicines Agency (EMA): Verzenios (abemaciclib) - Product Information and European Public Assessment Report (EPAR). Available at: https://www.ema.europa.eu/en/medicines/human/EPAR/verzenios
Sledge GW Jr et al. - MONARCH 2: Abemaciclib in Combination With Fulvestrant in Women With HR+/HER2- Advanced Breast Cancer Who Had Progressed While Receiving Endocrine Therapy. Journal of Clinical Oncology, 2017. PMID: 28580882.
Johnston SRD et al. - Abemaciclib Combined with Endocrine Therapy for the Adjuvant Treatment of HR+, HER2-, Node-Positive, High-Risk, Early Breast Cancer (monarchE). Journal of Clinical Oncology, 2020. PMID: 32928971.

Building Blocks for a Healthy Life

As an integrated manufacturer, we develop & produce evidence-based, patented, and non-patented formulations. We work exclusively with plant and natural extracts according to the strictest purity & quality standards.
The combination of science & modern technology with the laws of nature creates solutions consistently tailored to humans – for the highest good: health.