.Pharmacolibrary.Drugs.L_AntineoplasticAndImmunomodulatingAgents.L01E_ProteinKinaseInhibitors.L01EM03_Alpelisib.Alpelisib .Pharmacolibrary.Drugs.L_AntineoplasticAndImmunomodulatingAgents.L01E_ProteinKinaseInhibitors.L01EM03_Alpelisib.Alpelisib| name: | Alpelisib |
| ATC code: | L01EM03 | route: | oral |
| n-compartments | 2 |
Alpelisib is an orally bioavailable selective inhibitor of phosphatidylinositol 3-kinase alpha (PI3Kα) isoform. It is primarily indicated and approved for the treatment of hormone receptor-positive, HER2-negative, PIK3CA-mutated advanced or metastatic breast cancer, used in combination with endocrine therapy. The drug is approved and in clinical use.
Pharmacokinetic parameters are reported in adult patients with advanced solid malignancies or metastatic breast cancer after administration of oral alpelisib 300 mg, the approved therapeutic dose.
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De Buck, SS, et al., & Goggin, TK (2014). Population pharmacokinetics and pharmacodynamics of BYL719, a phosphoinositide 3-kinase antagonist, in adult patients with advanced solid malignancies. British journal of clinical pharmacology 78(3) 543–555. DOI:10.1111/bcp.12378 PUBMED:https://pubmed.ncbi.nlm.nih.gov/24617631
Gajewska, M, et al., & Heimbach, T (2020). Physiologically Based Pharmacokinetic Modeling of Oral Absorption, pH, and Food Effect in Healthy Volunteers to Drive Alpelisib Formulation Selection. The AAPS journal 22(6) 134–None. DOI:10.1208/s12248-020-00511-7 PUBMED:https://pubmed.ncbi.nlm.nih.gov/33070288