Abemaciclib

Abemaciclib, manufactured by Lucius Pharmaceuticals, offers a highly cost-effective treatment option for patients with HR+/HER2- breast cancer due to its potent CDK4/6 inhibitory activity and favorable safety profile. It effectively prolongs patients' survival and improves their quality of life.

The following is a detailed introduction to the drug Abemaciclib, including key information such as its ingredients, target population, and dosage and administration.

Active Ingredient:

The active ingredient of Abemaciclib is Abemaciclib itself, an oral kinase inhibitor with the chemical name: 2-Pyrimidinamine, N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-.

Target Population:

Abemaciclib is indicated for adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer, including:

Patients with early-stage high-risk breast cancer;

Patients with late-stage or metastatic breast cancer;

Patients whose disease has progressed following prior endocrine therapy and chemotherapy.

Dosage and Administration:

Recommended Dosage:

In combination with endocrine therapy (e.g., tamoxifen or aromatase inhibitors): The recommended dose is 150 mg orally, twice daily.

As monotherapy: The recommended dose is 200 mg orally, twice daily.

Dose adjustments should be made based on individual safety and tolerability.Recommended Article: Dosage and Administration of Abemaciclib

Special Populations:

Pregnant women: Abemaciclib should be avoided as it may cause fetal harm.

Lactating women: Breastfeeding should be discontinued during treatment.

Patients with hepatic or renal impairment: Dose adjustments or avoidance of use may be necessary based on individual conditions.

Overdosage:

There is no specific antidote for Abemaciclib overdosage.In case of overdosage, general supportive care should be administered, and the patient's vital signs and adverse reactions should be closely monitored.

Storage:

Abemaciclib should be stored at 20°C to 25°C (68°F to 77°F), with a permitted excursion range of 15°C to 30°C (59°F to 86°F).

Pharmacokinetics:

Absorption: Abemaciclib is rapidly absorbed following oral administration, with a bioavailability of approximately 45%.

Exposure: The plasma exposure (AUC) and Cmax increase approximately proportionally with dose escalation.

Metabolism: Primarily metabolized in the liver; metabolites M2, M18, and M20 exhibit comparable activity to the parent drug.

Elimination: The elimination half-life is approximately 18.3 hours.

FDA，2025.02