Alpesib Tablet contains Alpelisib, an oral targeted anticancer agent used in combination therapy for specific types of advanced breast cancer. It is designed for precision treatment in patients whose tumors harbor a PIK3CA mutation, offering a personalized therapeutic approach after progression on endocrine-based regimens. Alpesib represents a significant advancement in the management of hormone receptor–positive breast cancer.

রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Therapeutic Class

Cytotoxic Chemotherapy

Indications

Alpesib is indicated in combination with fulvestrant for the treatment of:

• Postmenopausal women and men with hormone receptor (HR)-positive,

• HER2-negative,

• PIK3CA-mutated advanced or metastatic breast cancer,

as detected by an FDA-approved test, following progression on or after an endocrine-based therapy.

Pharmacology

Alpelisib is a selective inhibitor of phosphatidylinositol-3-kinase alpha (PI3Kα). Gain-of-function mutations in the PIK3CA gene lead to abnormal activation of the PI3K/AKT signaling pathway, promoting tumor cell growth, survival, and proliferation.

Alpelisib inhibits phosphorylation of downstream signaling targets such as Akt, particularly in breast cancer cells harboring PIK3CA mutations. In vivo studies have shown that Alpelisib suppresses PI3K/AKT signaling and reduces tumor growth in xenograft models. Additionally, PI3K inhibition increases estrogen receptor (ER) transcription, enhancing the antitumor efficacy when combined with fulvestrant. This combination has demonstrated superior antitumor activity compared to either agent alone.

Dosage & Administration

• Recommended dose: 300 mg once daily (two 150 mg film-coated tablets) taken orally with food

• Continue treatment until disease progression or unacceptable toxicity

• Tablets should be swallowed whole; do not chew, crush, or split

• Do not take tablets that are broken or damaged

• If a dose is missed, it may be taken with food within 9 hours; otherwise skip the dose

• If vomiting occurs after dosing, do not take an additional dose that day

• Recommended fulvestrant dose when used in combination:

  • 500 mg on Days 1, 15, and 29, then once monthly thereafter

Drug Interactions

• Effect of other drugs on Alpesib: Not fully established

• Effect of Alpesib on other drugs: Not fully established
  Caution is advised when co-administering with other therapies, and clinical monitoring is recommended.

Contraindications

Alpelisib is contraindicated in patients with known severe hypersensitivity to Alpelisib or any of its components.

Side Effects

Reported adverse reactions include:

• Lung problems, including pneumonitis

Patients should be monitored closely for respiratory symptoms and other treatment-related adverse effects.

রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Pregnancy & Lactation

• Alpelisib may cause fetal harm based on animal studies and its mechanism of action

• Pregnant women should be advised of potential risks

• Breastfeeding is not recommended during treatment and for 1 week after the final dose

• Alpelisib may impair fertility in both males and females of reproductive potential

Precautions & Warnings

• Permanently discontinue Alpesib in cases of severe hypersensitivity reactions

• Severe cutaneous reactions such as Stevens-Johnson Syndrome and Erythema Multiforme have been reported

• Monitor fasting plasma glucose (FPG) and HbA1c before and during treatment due to the risk of hyperglycemia

• Permanently discontinue in confirmed cases of pneumonitis

• Initiate antidiarrheal therapy promptly if diarrhea occurs

• Effective contraception is required during treatment due to the risk of fetal harm

Use in Special Populations

• No clinically significant pharmacokinetic differences based on age, sex, race, body weight, or mild to moderate renal impairment

• No dose adjustment required for mild to severe hepatic impairment

• Effect in severe renal impairment is unknown

• Safety and efficacy in pediatric patients have not been established

• No overall differences in effectiveness observed in patients aged 65 years and older

Storage Conditions

Store below 30°C in a cool, dry place.
Protect from light.
Keep out of the reach of children.