Alpelisib

Indications

Cancer

Alpelisib is used together with fulvestrant to treat postmenopausal women and men who have advanced or metastatic breast cancer that is hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative and PIK3CA-mutated. The mutation must be detected by an FDA-approved test, and the cancer must have progressed on or after an endocrine-based regimen.

⚠️ Always consult a registered physician before taking any medicine.

Pharmacology

Alpelisib is an inhibitor of phosphatidylinositol-3-kinase (PI3K), and it works mainly against PI3Kα. Gain-of-function mutations in the gene that codes for the catalytic α-subunit of PI3K (PIK3CA) activate PI3Kα and Akt-signaling. This leads to cellular transformation and the formation of tumors in both in vitro and in vivo models.

Breast cancer cell lines gave similar findings. Alpelisib blocked the phosphorylation of PI3K downstream targets, including Akt, and it showed activity in cell lines carrying a PIK3CA mutation. Xenograft models, including breast cancer models, showed the same pattern: Alpelisib inhibited the PI3K/Akt signaling pathway and reduced tumor growth.

PI3K inhibition by Alpelisib has been shown to raise estrogen receptor (ER) transcription in breast cancer cells. When Alpelisib was combined with fulvestrant, antitumor activity was greater than with either treatment alone. This was seen in xenograft models derived from ER-positive, PIK3CA mutated breast cancer cell lines.

Pregnancy & Breastfeeding

Pregnancy: Animal data and the way Alpelisib works suggest it can cause fetal harm when a pregnant woman takes it. Lactation: There is no data on whether Alpelisib passes into human milk, or on its effects on milk production or on the breastfed child. Because the breastfed child could have serious adverse reactions, women who are breastfeeding are advised not to breastfeed during treatment and for 1 week after the last dose. Infertility: Findings from animal studies suggest Alpelisib may impair fertility in males and females of reproductive potential.

⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.

Dosage Reference

⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.

Adults: The recommended dose of Alpelisib is 300 mg (two 150 mg film coated tablets) taken by mouth once daily with food. Treatment continues until the disease progresses or unacceptable toxicity occurs. Patients should take their dose at about the same time each day. Swallow the tablets whole, and don't chew, crush or split them. A tablet that is broken, cracked or otherwise not intact should not be taken. If a dose is missed, it can be taken with food within 9 hours after the usual time. After more than 9 hours, skip the dose for that day and take it at the usual time the next day. If the patient vomits after taking the dose, advise them not to take an additional dose that day, and to go back to the usual schedule the next day at the usual time. When fulvestrant is given with Alpelisib, the recommended dose of fulvestrant is 500 mg on Days 1, 15 and 29, and once monthly after that.

Side Effects & Interactions

Side Effects

No side-effect data recorded yet.

Key Interactions

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