ALIALPELISIB Alpelisib Tablets

I. Basic Information

Generic Name: Alpelisib Tablets

Brand Names: Piqray, Vijoice, ALIALPELISIB

English Name: Alpelisib

Specification: 50 mg/tablet; 28 tablets/box

Manufacturer: Lao United Pharmaceutical Group Co., Ltd.

Approval Number (Lao National Drug Administration): 07 L 1376/25

Storage Conditions: Store at 20°C to 25°C; excursions between 15°C and 30°C are permitted. Keep the medication in its original packaging, protected from moisture and light, and out of the reach of children.

Mechanism of Action: Alpelisib is a selective phosphoinositide 3-kinase (PI3K) inhibitor, primarily targeting the PI3Kα isoform. PI3Kα is frequently mutated in various cancers, leading to the hyperactivation of the PI3K/AKT/mTOR signaling pathway; by selectively inhibiting mutant PI3Kα, Alpelisib blocks downstream signaling, thereby inhibiting tumor cell growth and proliferation.

II. Indications

Piqray (Breast Cancer Treatment): Indicated in combination with fulvestrant for the treatment of postmenopausal women and men with advanced or metastatic breast cancer that is hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and *PIK3CA*-mutated.

Vijoice (PROS Treatment): Indicated for the treatment of adults and pediatric patients 2 years of age and older with PIK3CA-Related Overgrowth Spectrum (PROS) who require systemic therapy.

III. Dosage and Administration

Piqray (Breast Cancer Treatment): The recommended dosage is 300 mg (two 150 mg film-coated tablets) taken orally once daily, with food. When used in combination with fulvestrant, the recommended dosage of fulvestrant is 500 mg administered on Days 1, 15, and 29, and once monthly thereafter. Treatment should be continued until disease progression or unacceptable toxicity occurs.

Vijoice (PROS Treatment): The recommended dosage for adults is 250 mg taken orally once daily. For children aged 2 years and older, the initial dose is 50 mg orally, once daily. For children under 6 years of age, the maintenance dose is 50 mg orally, once daily; for children aged 6 years and older, the dose may be increased to 125 mg orally, once daily, after 24 weeks of treatment, with a maximum dose of 125 mg/day. When the patient reaches 18 years of age, a gradual increase in dosage up to 250 mg/day may be considered.

IV. Adverse Reactions

Common Adverse Reactions: Include hyperglycemia, rash, gastrointestinal symptoms (such as diarrhea, nausea, vomiting, decreased appetite), fatigue, asthenia, stomatitis, mucositis, weight loss, alopecia, etc.

Serious Adverse Reactions: May include severe allergic reactions, severe cutaneous reactions, pneumonia, dehydration secondary to diarrhea, etc.

V. Precautions

Hyperglycemia: Blood glucose levels should be monitored regularly during treatment; anti-hyperglycemic therapy should be initiated or optimized as necessary.

Severe Cutaneous Reactions: Patients should seek immediate medical attention if a severe rash develops; treatment may need to be interrupted or discontinued.

Diarrhea: May lead to dehydration; patients require close monitoring and timely management.

Embryo-Fetal Toxicity: May cause harm to the fetus; women of reproductive potential should use effective contraception during treatment.

Drug Interactions: Caution is advised when co-administering with strong inducers or inhibitors of CYP3A4.

VI. Contraindications

Contraindicated in patients with severe hypersensitivity to alpelisib or to any of the excipients. Use with caution in patients with severe hepatic impairment.

VII. Use in Specific Populations

Hepatic Impairment: A reduced dosage is recommended for patients with moderate or severe hepatic impairment.

Renal Impairment: No dosage adjustment is required for patients with mild to moderate renal impairment; data are limited for patients with severe renal impairment.

Pediatric Patients: Vijoice may be used in children aged 2 years and older, in accordance with the recommended dosage regimen.

Geriatric Patients: No specific dosage adjustment is required; however, elderly patients may be more susceptible to adverse reactions.

Pregnant Women: May cause fetal harm; contraindicated.

Lactating Women: It is recommended to either discontinue breastfeeding or discontinue the medication.