Must-read for patients: Overview of basic information in the Chinese instructions for Apelvis

1. Generic name: Alpelisib, Alpelisib

Product name:PIQRAY

Other names: Abolib, Aikli

2. Who can take Apelvis? Indications?

Alpelisib may be used in combination with fulvestrant for the treatment of patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer (BC), primarily in postmenopausal women and men, detected during or after an endocrine-based regimen or by an FDA-approved test.

3. What are the side effects of Apelvis?

The most common side effects of Apelix include diarrhea, rash, nausea, fatigue, loss of appetite, stomatitis (inflammation of the oral mucosa), vomiting, weight loss, and hair loss; after its launch, adverse events such as uveitis, colitis, hyperglycemic hyperosmolar nonketotic syndrome (HHNKS), angioedema, and drug reactions with eosinophilia and systemic symptoms (DRESS) have also occurred.

4. How should you take Apelvis?

1. Before treatment: Doctors will select patients to receive Apelvistreatment HR-positive, HER2-negative advanced or metastatic breast cancer based on whether one or more PIK3CA mutations are present in tumor tissue or plasma samples.

2. Recommended dosage: Apelvis is available in the form of oral tablets, as indicated in the prescription guide. The recommended dose is 300 mg (two 150 mg film-coated tablets) once daily, taken with food, and treatment continues until disease progression or unacceptable toxicity occurs. When administered with fulvestrant, the dose of fulvestrant is 500 mg on days 1, 15, and 29, and monthly thereafter, subject to adjustment based on its prescribing information.

3. Medication management: Apelvis tablets usually need to be swallowed whole. The tablets should not be chewed, crushed or split before swallowing. Tablets should not be taken if they are broken, cracked, or incomplete. If you miss a dose of Apelvis, take it after your usual doseTake with food within 9 hours. After more than 9 hours, skip the day's dose; however, if the patient vomits after taking the dose, the patient is advised not to take additional doses that day; in both cases, it is recommended to resume the dosing schedule at the normal time the next day.

4. Patients with dysphagia: If the patient cannot swallow the tablets whole, they can be dissolved in water. Place the tablets in a drinking glass with 60-120mL (2-4 ounces) of water. Wait 5 minutes, then crush the tablets, stir the mixture with a spoon, and drink immediately. Then add another 2 to 3 tablespoons of water to the glass and stir with the same spoon to rinse out any remaining particles in the glass. Drink all of this mixture to ensure the patient has taken all the medication, repeating if necessary.

5. How to store Apelvis?

Apelixis is available as 50 mg, 150 mg and 200 mg film-coated tablets and can be stored at 20°C to 25°C (68°F to 77°F), with an allowed excursion between 15°C and 30°C (59°F to 86°F).

6. How does Apelis work?

Apelix is a phosphatidylinositol-3-kinase (PI3K) inhibitor, which mainly has inhibitory activity against PI3Kα. In in vitro and in vivo models, gain-of-function mutations in the gene encoding the PI3K catalytic alpha subunit (PIK3CA) lead to activation of PI3Kα and Akt signaling, cellular transformation, and tumorigenesis.

In breast cancer cells, inhibition of PI3K by apelvis treatment can induce an increase in estrogen receptor (ER) transcription. In a xenograft model derived from an ER-positive, PIK3CA-mutated cancer breast cancer cell line, the combination of apelvis and fulvestrant showed increased anti-tumor activity compared to treatment alone.

7. What will happen if you overdose on Apelvis?

Experience with apelvis overdose in clinical trials is limited. In clinical studies, apelix was administered at doses up to 450 mg once daily. In the cases of accidental overdoses of apellis reported in clinical studies, adverse reactions associated with overdose were consistent with the known safety profile of apelix and included hyperglycemia, nausea, fatigue, and rash. If necessary, initiate general symptomatic and supportive measures in all cases of overdose. There is no known antidote for apelix.

8. Who cannot take Apelvis?

Apelix is contraindicated in patients with severe hypersensitivity to it or any of its components.