Apilis is an oral phosphatidylinositol-3-kinase alpha (PI3K alpha) inhibitor, belonging to the kinase inhibitor class. By specifically inhibiting the activity of PI3K α, Apilis can block abnormal activation of the PI3K/Akt signaling pathway, thereby reducing excessive cell proliferation and abnormal tissue growth caused by PIK3CA gene mutations.

1、 Drug name and main ingredients

1. Common name: Alpelisib

2. Product Name: VIJOICE ®

3. Dosage form: Oral film coated tablets (50mg/125mg/200mg) and oral granules (50mg/pack)

4. Main ingredients: Each tablet/contains Apilis (active ingredient) and excipients (hydroxypropyl methylcellulose, magnesium stearate, microcrystalline cellulose, etc.).

2、 Indications

PIK3CA related overgrowth spectrum (PROS): Used to treat PROS patients aged 2 years and above with severe symptoms, requiring systematic treatment. This indication is based on accelerated approval and requires further validation of clinical benefits.

3、 Specifications and characteristics

1. Tablets:

50mg: light yellow circular tablet, engraved with "C7" and "NVR";

125mg: Dark yellow oval shaped tablet, engraved with "Y7" and "NVR";

200mg: Light yellow oval shaped tablets engraved with "CL7" and "NVR".

2. Granules:

50mg/pack, a mixture of white powder and granules.

4、 Usage and dosage

1. Adults: 250mg once daily, taken with meals;

2. Children (2 to<18 years old): The initial dose is 50mg once daily, and for those over 6 years old, it can be increased to 125mg after 24 weeks;

3. Usage: Swallow the whole tablet or prepare an oral suspension (tablet); Particles can be swallowed directly or mixed with soft food.

4. Missing server processing: can be replenished within 9 hours, skipped if exceeded; No need to take additional medication after vomiting.

5、 Dose adjustment

1. Adult dose reduction: first dose to 125mg, second dose to 50mg;

2. Reduce dosage for children: 125mg to 50mg;

3. Adjustment criteria: Adjust according to the grading of adverse reactions such as high blood sugar, rash, diarrhea, etc.

6、 Medication precautions

1. High blood glucose monitoring: regular monitoring of fasting blood glucose and HbA1c before and during treatment;

2. Skin reaction: Severe rash (such as SJS) requires permanent discontinuation of medication;

3. Infection risk: 17% of patients develop ≥ grade 3 infection;

4. Diet: Avoid grapefruit juice and take with meals.

7、 Medication for special populations

1. Pregnant women: prohibited (animal experiments show embryonic toxicity);

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within one week of discontinuation of medication;

3. Liver dysfunction: moderate to severe injuries require caution.

8、 Adverse reactions

1. Common (≥ 10%): Diarrhea (16%), Stomatitis (16%), Hyperglycemia (12%);

2. Serious reactions: pneumonia (14%), neutropenia (16%).

9、 Contraindications

It is contraindicated for those who are severely allergic to apremide or excipients.

10、 Drug interactions

1. Strong CYP3A4 inducers (such as rifampicin): avoid combination use;

2. BCRP inhibitors: may increase exposure to aprepitis.

11、 Storage method

Store at room temperature (20-25 ° C), away from light and moisture.

Note: If severe allergies, high blood sugar, or difficulty breathing occur, seek medical attention immediately. Regular monitoring of blood glucose and liver function is required during treatment.

Alpelisibinformation