Alpelisib (Piqray) is a kinase inhibitor, first approved in the United States in 2019. As a targeted therapy for specific types of advanced breast cancer, it exerts its effects by inhibiting the PI3Kα signaling pathway.

What Kind of Drug Is Alpelisib (Piqray)?

Indication Scope

Alpelisib in combination with fulvestrant is indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer.

These patients must have experienced disease progression during or after receiving endocrine therapy, and this status must be confirmed by an FDA-approved testing method.

Pharmacological Action

Alpelisib is a phosphatidylinositol-3-kinase (PI3K) inhibitor, primarily targeting PI3Kα.

Gain-of-function mutations in the PIK3CA gene lead to activation of PI3Kα and Akt signaling, cell transformation, and tumorigenesis in both in vitro and in vivo models.

In breast cancer cell lines, alpelisib inhibits the phosphorylation of PI3K downstream targets (including Akt) and exhibits activity in cell lines harboring PIK3CA mutations.

Patient Selection

Patients are selected based on the presence of one or more PIK3CA mutations in tumor tissue or plasma specimens.

If no mutation is detected in plasma specimens, tumor tissue should be tested.

Dosage Forms, Strengths and Characteristics of Alpelisib (Piqray)

Dosage Strengths

300 mg daily dose: 2 blister packs (56 tablets total), containing two 150 mg tablets per daily dose.

250 mg daily dose: 2 blister packs (56 tablets total), containing 14 tablets of 200 mg and 14 tablets of 50 mg.

200 mg daily dose: 1 blister pack (28 tablets total), containing 28 tablets of 200 mg.

Physical Characteristics

50 mg tablets: Light pink, un-scored, round film-coated tablets with curved edges and beveled sides. Imprinted with "L7" on one side and "NVR" on the other side.

150 mg tablets: Light red, un-scored, oval film-coated tablets with curved edges and beveled sides. Imprinted with "UL7" on one side and "NVR" on the other side.

200 mg tablets: Light red, un-scored, oval film-coated tablets with curved edges and beveled sides. Imprinted with "YL7" on one side and "NVR" on the other side.

Formulation Composition

Active ingredient: Alpelisib.

Inactive ingredients: Hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, and sodium starch glycolate.

Film coating contains: Hypromellose, iron oxide black, iron oxide red, polyethylene glycol 4000, talc, and titanium dioxide.

Storage Conditions for Alpelisib (Piqray)

Storage Conditions

Store at a suitable temperature of 20°C to 25°C (68°F to 77°F), with allowable short-term fluctuations between 15°C and 30°C (59°F to 86°F).

Special Precautions

The medication should be kept in its original packaging.

Store out of the reach of children.

Protect from direct sunlight and humid environments.