LuciAlpe Alpelisib film coated tablets

Product Name

Generic Name: Alpelisib Tablets

Brand Names: Feiyiyue, Piqray, LuciAlpe

English Name: Alpelisib

Specification: 150 mg/tablet; 28 tablets/box

Description: Round, film-coated tablets for oral administration.

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

National Drug Approval Number: 03 L 1076/24

Pharmacological Actions

Mechanism of Action: Alpelisib is a phosphoinositide 3-kinase (PI3K) inhibitor that specifically inhibits the PI3Kα isoform. In cancer cells harboring *PIK3CA* gene mutations, the PI3Kα signaling pathway is hyperactivated, promoting tumor growth and resistance to endocrine therapy. By inhibiting this pathway, Alpelisib reverses resistance and acts synergistically with endocrine therapy, thereby inhibiting tumor cell proliferation.

Pharmacodynamics: In hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+/HER2-) advanced breast cancer harboring *PIK3CA* mutations, Alpelisib demonstrated significant anti-tumor activity when used in combination with fulvestrant.

Indications

In combination with fulvestrant, Alpelisib is indicated for the treatment of postmenopausal women and men with hormone receptor-positive, human epidermal growth factor receptor 2-negative (HR+/HER2-) locally advanced or metastatic breast cancer whose disease has progressed following an endocrine-based regimen, and whose tumor tissue is positive for *PIK3CA* mutations.

Dosage and Administration

Recommended Dosage: 300 mg orally once daily (consisting of one 200 mg tablet and two 50 mg tablets), taken with food.

Method of Administration: Swallow tablets whole; do not chew, crush, or split the tablets. Take the medication at approximately the same time each day.

Dosage Adjustment: To manage adverse reactions (e.g., severe rash, hyperglycemia), dosage adjustment strategies (such as a first dose reduction to 250 mg, followed by a second reduction to 200 mg) or temporary interruption of treatment are recommended based on the severity of the reaction.

Adverse Reactions

Common Adverse Reactions Include:

Hyperglycemia: Very common and potentially severe; requires close monitoring. Skin Reactions: Rash, alopecia, dry skin, nail disorders.

Gastrointestinal Reactions: Diarrhea, nausea, vomiting, decreased appetite, stomatitis.

Other: Fatigue, weight loss, lymphopenia, elevated liver enzymes (ALT/AST).

Contraindications

Contraindicated in patients with a history of severe hypersensitivity to alpelisib or to any of the excipients.

Precautions

1.  Severe Hyperglycemia: Severe hyperglycemia, including ketoacidosis, may occur. Fasting glucose and HbA1c levels should be measured prior to treatment, and blood glucose levels should be monitored periodically during treatment. Optimize antihyperglycemic regimens; suspend or permanently discontinue treatment if necessary.

2.  Severe Cutaneous Reactions: Including Stevens-Johnson syndrome and erythema multiforme. If a severe rash occurs, treatment should be interrupted and an evaluation performed.

3.  Diarrhea: Severe diarrhea may occur, potentially leading to dehydration and acute kidney injury. Patients are advised to report symptoms promptly and initiate anti-diarrheal treatment.

4.  Embryo-Fetal Toxicity: May cause harm to the fetus. Women of reproductive potential and men should use effective contraception during treatment and for a period of time following the last dose.

Drug Interactions

BCRP Inhibitors: Co-administration with certain drugs (e.g., [specific examples]) may increase alpelisib exposure; close monitoring for adverse reactions is required.

CYP3A4 Inducers: Co-administration with strong CYP3A4 inducers (e.g., rifampin, carbamazepine) should be avoided, as they may significantly decrease alpelisib plasma concentrations.

Storage

Store in the original sealed packaging at room temperature (20°C–25°C); protect from moisture.