Indication: Alpesib, or Alpelisib (INN), is approved for treating hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated advanced or metastatic breast cancer in both postmenopausal women and men.

Pharmacology: Alpesib selectively targets the alpha isoform of phosphatidylinositol-3-kinase (PI3Kα), suppressing the PI3K/AKT/mTOR signaling pathway, frequently altered in cancer cells with PIK3CA mutations. This action results in reduced tumor cell proliferation and increased apoptosis.

Dosage and Administration: The recommended dosage of Alpesib is 300 mg orally once daily, with food. Treatment should be maintained until disease progression or intolerable adverse effects occur.

Interactions: Alpesib may interact with medications metabolized by CYP3A4. Caution is advised with concurrent use of potent CYP3A4 inhibitors or inducers, and with drugs prolonging the QT interval or substrates of P-glycoprotein.

Side Effects: Common side effects of Alpesib include hyperglycemia, diarrhea, nausea, decreased appetite, rash, and fatigue. Serious adverse reactions may include severe hypersensitivity reactions, severe cutaneous adverse reactions (SCARs), and pneumonitis.

Precautions and Warnings:

• Patients should be monitored for hyperglycemia, with possible adjustments to antidiabetic therapy.
• Discontinue Alpesib if severe hypersensitivity reactions or SCARs occur.
• Regularly assess patients for respiratory symptoms indicative of pneumonitis, with treatment withholding or discontinuation as necessary.

Overdose Effect: Supportive care is recommended in cases of Alpesib overdose. No specific antidote exists; therefore, close monitoring for adverse reactions is crucial, with symptomatic treatment initiated as needed.