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Synonyms: BYL 719 | BYL-719 | NVP-BYL719 | Piqray®
alpelisib is an approved drug (FDA (2019), FDA (2020))
Compound class: Synthetic organic
Comment: Alpelisib is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor that exhibits antineoplastic activity. It is selective for the α isoform (PIK3CA). It was the first PIK3CA inhibitor to be approved for the treatment of breast cancer.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Furet P, Guagnano V, Fairhurst RA, Imbach-Weese P, Bruce I, Knapp M, Fritsch C, Blasco F, Blanz J, Aichholz R et al.. (2013)
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Bioorg Med Chem Lett, 23 (13): 3741-8. [PMID:23726034]
2. Lin S, Jin J, Liu Y, Tian H, Zhang Y, Fu R, Zhang J, Wang M, Du T, Ji M et al.. (2019)
Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis.
J Med Chem, 62 (19): 8873-8879. [PMID:31335136]
3. Markham A. (2019)
Alpelisib: First Global Approval.
Drugs, 79 (11): 1249-1253. [PMID:31256368]
4. Venot Q, Blanc T, Rabia SH, Berteloot L, Ladraa S, Duong JP, Blanc E, Johnson SC, Hoguin C, Boccara O et al.. (2018)
Targeted therapy in patients with PIK3CA-related overgrowth syndrome.
Nature, 558 (7711): 540-546. [PMID:29899452]