Chemical compound From Wikipedia, the free encyclopedia
Alpelisib, sold under the brand name Piqray among others, is a medication used to treat certain types of breast cancer.[8] It is used together with fulvestrant.[8] It is taken by mouth.[8] It is marketed by Novartis.[8]
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| Trade names | Piqray, Vijoice |
| Other names | BYL719 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a619036 |
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| Routes of administration | By mouth |
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| ECHA InfoCard | 100.233.704 |
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| Formula | C19H22F3N5O2S |
| Molar mass | 441.47 g·mol−1 |
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Common side effects include high blood sugar, kidney problems, diarrhea, rash, low blood cells, liver problems, pancreatitis, vomiting, and hair loss.[8] It is an alpha-specific PI3K inhibitor.[8][9] It was approved for medical use in the United States in May 2019.[8][10]
Alpelisib is indicated in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen.[11]
In the European Union, alpelisib is indicated in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)‑positive, human epidermal growth factor receptor 2 (HER2)‑negative, locally advanced or metastatic breast cancer with a PIK3CA mutation after disease progression following endocrine therapy as monotherapy.[6]
In April 2022, the indication for alpelisib was expanded in the US to include the treatment of severe manifestations of PIK3CA-related overgrowth spectrum (PROS) in those who require systemic therapy.[5][12][13]
In May 2019, alpelisib was approved in the United States for use in combination with the endocrine therapy fulvestrant, to treat postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer following progression on or after an endocrine-based regimen.[8][4][10]
The U.S. Food and Drug Administration (FDA) also approved the companion diagnostic test, therascreen PIK3CA RGQ PCR Kit, to detect the PIK3CA mutation in a tissue and/or a liquid biopsy.[8]
The efficacy of alpelisib was studied in the SOLAR-1 trial (NCT02437318), a randomized trial of 572 postmenopausal women and men with HR-positive, HER2-negative, advanced or metastatic breast cancer whose cancer had progressed while on or after receiving an aromatase inhibitor.[8][14]
The FDA granted the application for alpelisib priority review designation and granted approval of Piqray to Novartis.[8] The FDA granted approval of the therascreen PIK3CA RGQ PCR Kit to Qiagen Manchester, Ltd.[8]
On 28 May 2020, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product alpelisib (Piqray), intended for the treatment of locally advanced or metastatic breast cancer with a PIK3CA mutation.[6] The applicant for this medicinal product is Novartis Europharm Limited.[6] Alpelisib was approved for medical use in the European Union in July 2020.[6]
Alpelisib was approved for medical use in the United States in May 2019,[8][10] in Australia in March 2020,[15] and in the European Union in July 2020.[6]
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