Medical Information

The contraindications for Alpelisib mainly include severe allergic reactions, specific genetic states, and medication restrictions for special populations, which must be strictly followed to avoid life-threatening risks.

1. Taboo for severe hypersensitivity reactions

(1) It is contraindicated for patients who have experienced severe hypersensitivity reactions, including grade 3/4 reactions such as anaphylactic shock, angioedema, etc., to Apilis or any of its components.

(2) Patients who have experienced severe skin adverse reactions such as Stevens Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) in previous use should permanently discontinue use.

2. Genetic status taboo

(1) Non PIK3CA mutation patients are prohibited. This drug is only applicable to HR+/HER2- breast cancer patients with PIK3CA mutation confirmed by FDA approval testing.

3. Taboos for special populations

(1) Pregnant women are prohibited from using contraception, as animal studies have shown embryonic fetal toxicity. Women of childbearing age should take contraceptive measures during treatment and one week after discontinuation.

(2) Breastfeeding women are prohibited from using the medication. It is not yet clear whether the medication is secreted through breast milk, but breastfeeding should be stopped due to the potential risk of serious adverse reactions.

(3) Patients with uncontrolled or poorly controlled type 1/2 diabetes should not use it because it may cause life-threatening hyperglycemia complications.

4. Taboos related to comorbidities

(1) Patients with severe renal insufficiency should use it with caution, as there is no relevant research data to support its safety.

(2) Patients with active pneumonia or interstitial lung disease should not use it, as it may worsen respiratory symptoms and lead to respiratory failure..

5. The effects of other drugs on aprepitis

(1) Strong CYP3A4 inducer: When used in combination with strong CYP3A4 inducers, it can reduce the blood concentration of aprepitis and weaken its therapeutic effect. Avoid using strong inducers in combination and choose alternative drugs with no/weak induction potential.

(2) BCRP inhibitors: Combined use with BCRP inhibitors may significantly increase the blood concentration of aspirin and increase the risk of toxicity. During treatment, the use of BCRP inhibitors should be avoided, and if they cannot be replaced, adverse reaction monitoring should be strengthened.

6. The impact of Apilis on other drugs

(1) BCRP substrate: Apilis may inhibit BCRP transporters, and caution should be exercised when combined with BCRP substrates to prevent abnormal increases in substrate drug concentrations.

(2) Narrow therapeutic window drugs: When combining BCRP substrates with narrow therapeutic windows, it is recommended to adjust the dosage of the latter or choose alternative options to avoid serious adverse reactions.