Alpelisib is an oral PI3K α inhibitor, which is mainly used to treat HR+/HER2 advanced or metastatic breast cancer with PIK3CA mutation. This drug needs to be used in combination with Fluvistran and is suitable for patients who have progressed after endocrine therapy. The standard dose is 300mg per day taken with meals, with specific pharmacokinetic characteristics and precautions for drug interactions. At present, the drug has not been launched in China.

Overview of Drug 1

Aperix was developed by Novartis and approved by FDA in 2019 to target PIK3CA mutated breast cancer by inhibiting PI3K α pathway. As a small molecule inhibitor, its mechanism of action is clear and requires genetic testing to confirm mutations before use.

2 Indications and Usage

(1) Indications

It is applicable to adult patients with advanced breast cancer with HR+/HER2- and PIK3CA mutation. It shall meet the following requirements: the mutation is confirmed through FDA approval testing, and the disease progresses after endocrine therapy.

(2) Usage and dosage

Take 300mg (2 tablets 150mg) orally with meals daily, in combination with 500mg of Fluvistran (on days 1/15/29 and once a month). Swallow the entire tablet, and if missed, make up for it within 9 hours.

3 pharmacokinetics

The peak time is 2-4 hours, the protein binding rate is 89%, and the half-life is 8-9 hours. Mainly metabolized by CYP3A4, with 81% excreted through feces. Food can improve bioavailability and should be taken with meals at a fixed time.

4 Drug Interactions

Avoid using CYP3A4 strong inducers (such as rifampicin) in combination with BCRP inhibitors (such as cyclosporine), as the former reduces efficacy and the latter increases toxicity risk. Adverse reactions need to be monitored and alternative drugs considered.

5 Domestic listing situation

As of June 2026, Apilis has not been approved for listing in China and is not included in the scope of medical insurance reimbursement.