Lucizbe Abemaciclib Tablets

Abemaciclib (Verzenio/Lucizbe) Detailed Product Information

Product Name: Abemaciclib Tablets

Other Chinese Names: Bomaxini

English Name: Abemaciclib Tablets

Brand Names: Verzenio / Lucizbe

Specification: 50 mg × 28 tablets/box

Manufacturer: Lucius Pharmaceutical (Laos) Co., Ltd.

Laos National Drug Approval Number: 03 L 1324/25

I. Indications

1. Early Breast Cancer

In combination with endocrine therapy (tamoxifen or an aromatase inhibitor), indicated as adjuvant therapy for patients with hormone receptor (HR)-positive, HER2-negative, node-positive early breast cancer at high risk of recurrence (e.g., ≥4 positive lymph nodes; or 1–3 positive lymph nodes with a tumor size ≥5 cm, histological Grade 3, or Ki-67 ≥20%).

Key Efficacy: The 4-year Invasive Disease-Free Survival (IDFS) rate reached 85.8%, representing a 6.4% improvement compared to the group receiving endocrine therapy alone.

2. Locally Advanced or Metastatic Breast Cancer

In combination with an aromatase inhibitor as initial endocrine-based therapy for postmenopausal patients;

In combination with fulvestrant for patients whose disease has progressed following prior endocrine therapy;

As monotherapy for patients with HR-positive, HER2-negative advanced breast cancer whose disease has progressed following endocrine therapy and chemotherapy.

II. Dosage and Administration

1. Standard Dosage

Combination Therapy: 150 mg orally, twice daily, taken with food (avoid grapefruit juice).

Monotherapy: 200 mg orally, once daily, taken with or without food.

2. Dosage Adjustment

Neutropenia: For Grade 3 (ANC 500–1000/mm³), suspend treatment; upon recovery, reduce the dose to 100 mg twice daily. For Grade 4 (ANC <500/mm³), discontinue treatment and monitor the patient. Diarrhea: Initiate loperamide at the first occurrence of loose stools; for Grade 2 diarrhea (4–6 bowel movements/day), suspend treatment until symptoms resolve; for Grade 3 diarrhea (≥7 bowel movements/day or requiring hospitalization), permanently discontinue the drug.

Hepatic Impairment: For patients with Child-Pugh Class C hepatic impairment, reduce the dosage to once daily (75 mg).

3. Special Populations

Elderly Patients: No dosage adjustment is required; however, patients aged ≥75 years require close monitoring for hematologic toxicity.

Hepatic and Renal Impairment: No dosage adjustment is required for mild to moderate impairment; use with caution in patients with severe renal impairment (eGFR <30 mL/min).

III. Adverse Reactions

1. Common Reactions (≥20%)

Hematologic System: Neutropenia (45.8%), anemia (83.8%), leukopenia (80.5%);

Gastrointestinal System: Diarrhea (86%), nausea (39%), vomiting (26%);

Other: Fatigue (40%), alopecia (27%), abnormal liver function (elevated ALT/AST).

2. Serious Risks

Infection: Pneumonia, urinary tract infection (5%); be alert for neutropenic sepsis;

Venous Thromboembolism: Deep vein thrombosis (5%), pulmonary embolism (2%);

Interstitial Lung Disease (ILD): Incidence <1%; requires permanent discontinuation of the drug.

IV. Contraindications and Precautions

1. Contraindications

Patients with hypersensitivity to abemaciclib or any of its excipients;

Pregnant or breastfeeding women (animal studies have demonstrated embryotoxicity).

2. Monitoring Requirements

Hematologic: Monitor complete blood counts prior to and weekly during treatment; once stable, re-evaluate every 2–4 weeks;

Liver Function: Monitor ALT/AST levels every 1–2 weeks for the first 6 weeks of treatment, and subsequently as clinically indicated;

Infection Screening: Screening for latent tuberculosis and vaccination against herpes zoster are recommended. V. Drug Interactions

1. CYP3A4 Inhibitors: With strong inhibitors (e.g., clarithromycin), the dosage must be reduced by 50% (to 100 mg twice daily); grapefruit juice should be avoided.

2. CYP3A4 Inducers: Strong inducers (e.g., rifampin) can reduce abemaciclib plasma concentrations by 95%; concomitant use should be avoided.

3. P-gp Substrates: May increase plasma concentrations of digoxin and dabigatran; monitoring is required.

VI. Pharmacological Mechanisms

Target: Selectively inhibits CDK4/6, blocks Rb protein phosphorylation, and inhibits the G1/S phase transition of the tumor cell cycle.

Metabolism: Primarily undergoes oxidative metabolism via CYP3A4; half-life is 29 hours, and bioavailability is 46%.

Excretion: 15% is excreted unchanged in feces, and 9% is excreted in urine.

VII. Dosage Forms and Storage

Tablet Specifications: 50 mg per tablet; 28 tablets per box.

Storage Conditions: Store at 20–25°C, protected from light and moisture.

Summary: As a CDK4/6 inhibitor, abemaciclib demonstrates significant efficacy in the treatment of HR+/HER2- breast cancer; however, strict monitoring for hematologic toxicity, diarrhea, and liver function abnormalities is required. Clinical use necessitates individualized dose adjustments, as well as careful attention to potential drug interactions and long-term safety management.