Chemistry:Alpelisib
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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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Formula | C19H22F3N5O2S |
Molar mass | 441.47 g·mol−1 |
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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]
Medical uses
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]
Research
Dietary supplementation with the PI3Ki alpelisib from middle age extends the median (by an average of 10%) and maximal lifespan of mice, an effect that was more pronounced in females.[14][15] While long-term PI3Ki treatment was well tolerated and led to greater strength and balance, negative impacts on common human aging markers, including reductions in bone mass and mild hyperglycemia, were also evident.[15] These results suggest that while pharmacological suppression of insulin receptor (IR)/insulin-like growth factor receptor (IGFR) targets could represent a promising approach to delaying some aspects of aging, caution should be taken in translation to humans.[15]
History
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][16]
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]
Society and culture
Legal status
Alpelisib was approved for medical use in the United States in May 2019,[8][10] in Australia in March 2020,[17] and in the European Union in July 2020.[6]
References
- ↑ 1.0 1.1 "Piqray Australian prescription medicine decision summary". 27 March 2020. https://www.tga.gov.au/apm-summary/piqray.
- ↑ "Updates to the Prescribing Medicines in Pregnancy database". 12 May 2022. https://www.tga.gov.au/resources/resource/guidance/updates-prescribing-medicines-pregnancy-database.
- ↑ "Summary Basis of Decision (SBD) for Piqray". 23 October 2014. https://hpr-rps.hres.ca/reg-content/summary-basis-decision-detailTwo.php?linkID=SBD00493&lang=en.
- ↑ 4.0 4.1 "Piqray- alpelisib tablet Piqray- alpelisib kit". 12 June 2020. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b20b4e18-7a4b-4500-a08f-06c6dab0ee5b.
- ↑ 5.0 5.1 "Vijoice- alpelisib tablet Vijoice- alpelisib kit". 7 April 2022. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=638069a4-aee0-46c9-9e21-54ad449c163c.
- ↑ 6.0 6.1 6.2 6.3 6.4 6.5 "Piqray EPAR". 26 May 2020. https://www.ema.europa.eu/en/medicines/human/EPAR/piqray. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
- ↑ "Piqray Product information". https://ec.europa.eu/health/documents/community-register/html/h1455.htm.
- ↑ 8.00 8.01 8.02 8.03 8.04 8.05 8.06 8.07 8.08 8.09 8.10 8.11 8.12 "FDA approves first PI3K inhibitor for breast cancer". U.S. Food and Drug Administration (FDA) (Press release). 24 May 2019. Archived from the original on 25 November 2019. Retrieved 29 May 2019.
This article incorporates text from this source, which is in the public domain.
- ↑ "PIK3CA-Mutated, Hormone Receptor-Positive Advanced Breast Cancer". The New England Journal of Medicine 380 (20): 1929–1940. May 2019. doi:10.1056/NEJMoa1813904. PMID 31091374.
- ↑ 10.0 10.1 10.2 "Drug Approval Package: Piqray". U.S. Food and Drug Administration (FDA). 18 June 2019. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212526Orig1s000TOC.cfm.
- ↑ "Piqray (alpelisib) tablets HR+/HER2- Advanced Breast Cancer Treatment". https://www.hcp.novartis.com/products/piqray/metastatic-breast-cancer/.
- ↑ "FDA approves alpelisib for PIK3CA-related overgrowth spectrum". 6 April 2022. https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-alpelisib-pik3ca-related-overgrowth-spectrum.
This article incorporates text from this source, which is in the public domain.
- ↑ "FDA approves Novartis Vijoice (alpelisib) as first and only treatment for select patients with PIK3CA-Related Overgrowth Spectrum (PROS)". Novartis (Press release). 6 April 2022. Archived from the original on 6 April 2022. Retrieved 9 April 2022.
- ↑ Garth E. (February 2023). Researchers identify drug that may increase longevity. Longevity.Technology
- ↑ 15.0 15.1 15.2 Hedges, C. P., Shetty, B., Broome, S. C., MacRae, C., Koutsifeli, P., Buckels, E. J., ... & Merry, T. L. (2023). Dietary supplementation of clinically utilized PI3K p110α inhibitor extends the lifespan of male and female mice. Nature Aging, 3, 162–172. https://doi.org/10.1038/s43587-022-00349-y
- ↑ "Drug Trials Snapshots: Piqray". 14 June 2019. https://www.fda.gov/drugs/drug-trials-snapshots-piqray.
This article incorporates text from this source, which is in the public domain.
- ↑ "AusPAR: Alpelisib". 3 September 2020. https://www.tga.gov.au/auspar/auspar-alpelisib.
External links
- "Alpelisib". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name/alpelisib.
- Clinical trial number NCT02437318 for "Study Assessing the Efficacy and Safety of Alpelisib Plus Fulvestrant in Men and Postmenopausal Women With Advanced Breast Cancer Which Progressed on or After Aromatase Inhibitor Treatment. (SOLAR-1)" at ClinicalTrials.gov
![]() | Original source: https://en.wikipedia.org/wiki/Alpelisib.
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