APELIDX Alpelisib Tablets

Generic Name: Alpelisib Tablets

Brand Names: Piqray, Vijoice, APELIDX

Specification: 50 mg × 28 tablets/box; 150 mg × 28 tablets/box

Manufacturer: Bigbear Pharmaceutical Laos

Drug Approval Number: 04 L 1331/25; 04 1331/25

[Composition]

Active Ingredient: Alpelisib

Chemical Name: (2S)-N1-[4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)pyridin-4-yl]thiazol-2-yl]pyrrolidine-1,2-dicarboxamide

[Indications]

1. Breast Cancer (Primary)

In combination with fulvestrant, for the treatment of:

Adult patients with hormone receptor-positive (HR+), HER2-negative (HER2-), and PIK3CA-mutated

Advanced or metastatic breast cancer

Whose disease has progressed following endocrine therapy

2. Other (Vijoice)

Treatment of PIK3CA-Related Overgrowth Spectrum (PROS) in patients aged ≥2 years who require systemic therapy.

[Dosage and Administration]

Breast Cancer (Adults)

Recommended dose: 300 mg (two 150 mg tablets) orally once daily, taken with food.

Administration: Swallow tablets whole; do not chew, crush, or split.

Missed dose: If ≤9 hours have passed since the scheduled time, take the missed dose; if >9 hours have passed, skip the missed dose and take the next dose at the regularly scheduled time the following day.

Vomiting: Do not take an additional dose on the same day; resume normal dosing the following day.

Duration of treatment: Continue until disease progression or until intolerable toxicity occurs.

Dose Adjustments (Adverse Reactions)

First dose reduction: 250 mg (one 200 mg tablet and one 50 mg tablet) orally once daily.

Second dose reduction: 200 mg orally once daily.

Still intolerable: Permanently discontinue treatment.

PROS (Adults/Children)

Adults: 250 mg orally once daily.

Children (≥2 years): Initial dose of 50 mg/day; for patients aged ≥6 years, the dose may be increased to 125 mg/day after 24 weeks of treatment.

[Adverse Reactions]

Common (≥10%)

Metabolic: Hyperglycemia (65%), weight loss (27%), hypocalcemia/hypokalemia/hypomagnesemia.

Dermatologic: Rash (52%), alopecia (20%), pruritus, dry skin.

Gastrointestinal: Diarrhea (58%), nausea (45%), vomiting, decreased appetite, stomatitis.

General: Fatigue (42%), headache (18%), peripheral edema (15%).

Serious (Requiring Discontinuation/Emergency Care)

Hyperglycemia: May lead to ketoacidosis; requires anti-hyperglycemic treatment.

Severe cutaneous reactions: Stevens-Johnson syndrome (SJS), Toxic Epidermal Necrolysis (TEN).

Pneumonia/Non-infectious pneumonitis: Dyspnea, cough, hypoxia.

Diarrhea with dehydration: Severe watery stools, electrolyte disturbances.

Hypersensitivity reactions: Facial swelling, dyspnea, hypotension.

[Contraindications]

Hypersensitivity to Alpelisib or to any of the excipients.

Severe hepatic impairment.

Pregnant or lactating women.

[Precautions]

1. **Hyperglycemia Monitoring**

Periodically monitor fasting/postprandial blood glucose and HbA1c levels prior to initiating treatment and throughout the course of therapy.

Patients with pre-existing diabetes require optimization of their glucose-lowering regimen.

If blood glucose exceeds 250 mg/dL, temporarily suspend the medication; resume at a reduced dose once glucose levels are controlled.

**2. Cutaneous Reactions**

Mild rash: Treat with antihistamines or topical corticosteroids.

Severe rash (characterized by blistering, exfoliation, or mucosal involvement): Permanently discontinue the medication.

**3. Pneumonitis**

Onset of cough, shortness of breath, or hypoxia: Immediately suspend the medication and conduct an evaluation.

Confirmed diagnosis of non-infectious pneumonitis: Permanently discontinue the medication.

**4. Diarrhea**

Treat early with anti-diarrheal agents (e.g., loperamide) and fluid replacement.

Grade 3–4 diarrhea: Temporarily suspend the medication; resume at a reduced dose once symptoms resolve.

**5. Embryo-Fetal Toxicity**

Contraindicated in pregnant women.

Women and men of reproductive potential: Practice strict contraception throughout the treatment period and for at least one week following discontinuation of the medication.

**6. Drug Interactions**

Concomitant use is prohibited: Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin).

Use with caution: CYP3A4 inhibitors (e.g., ketoconazole, erythromycin), BCRP substrates (e.g., rosuvastatin), and CYP2C9 substrates (e.g., warfarin).

**[Pharmacology and Toxicology]**

**Mechanism of Action:** Selectively inhibits PI3Kα (PIK3CA), thereby blocking the PI3K/AKT/mTOR signaling pathway and inhibiting tumor proliferation.

**Pharmacokinetics:** Peak plasma concentration is reached approximately 5 hours after oral administration; bioavailability increases when taken with food; protein binding is ≥97%; metabolized via CYP3A4; elimination half-life is 8–9 hours.

**[Storage]**

Store in a tightly sealed container at 20–25°C (excursions between 15–30°C are permitted) in a dry place.