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Clinical data | |
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Trade names | Piqray, Vijoice |
Other names | BYL719 |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a619036 |
License data | |
Pregnancy category | |
Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
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CAS Number | |
PubChem CID | |
PubChem SID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.233.704 |
Chemical and physical data | |
Formula | C19H22F3N5O2S |
Molar mass | 441.47 g·mol−1 |
3D model ( JSmol) | |
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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]
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]
![]() | |
Clinical data | |
---|---|
Trade names | Piqray, Vijoice |
Other names | BYL719 |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a619036 |
License data | |
Pregnancy category | |
Routes of administration | By mouth |
ATC code | |
Legal status | |
Legal status | |
Identifiers | |
| |
CAS Number | |
PubChem CID | |
PubChem SID | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.233.704 |
Chemical and physical data | |
Formula | C19H22F3N5O2S |
Molar mass | 441.47 g·mol−1 |
3D model ( JSmol) | |
| |
|
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]
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]