Literature DB >> 31256368

Alpelisib: First Global Approval.

Anthony Markham1.   

Abstract

Alpelisib (Piqray™)-an orally available phosphatidylinositol 3-kinase (PI3K) inhibitor with specific activity against PI3K alpha (PI3Kα)-is being developed by Novartis for the treatment of breast cancer. Alpelisib has demonstrated efficacy in combination with fulvestrant as treatment for hormone receptor (HR)-positive, human epidermal growth factor receptor-2 (HER2)-negative breast cancer in patients with a PIK3CA mutation and was recently approved for this indication in the USA. This article summarizes the milestones in the development of alpelisib leading to this first approval.

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Year:  2019        PMID： 31256368     DOI： 10.1007/s40265-019-01161-6

Source DB:  PubMed          Journal:  Drugs        ISSN： 0012-6667            Impact factor:   9.546


  59 in total

Review 1.  New and Emerging Targeted Therapies for Vascular Malformations.

Authors:  An Van Damme; Emmanuel Seront; Valérie Dekeuleneer; Laurence M Boon; Miikka Vikkula
Journal:  Am J Clin Dermatol       Date:  2020-10       Impact factor: 7.403

2.  Overexpression of ABCB1 and ABCG2 contributes to reduced efficacy of the PI3K/mTOR inhibitor samotolisib (LY3023414) in cancer cell lines.

Authors:  Chung-Pu Wu; Cheng-Yu Hung; Sabrina Lusvarghi; Yang-Hui Huang; Pin-Jung Tseng; Tai-Ho Hung; Jau-Song Yu; Suresh V Ambudkar
Journal:  Biochem Pharmacol       Date:  2020-07-04       Impact factor: 5.858

Review 3.  Regulation of breast cancer metastasis signaling by miRNAs.

Authors:  Belinda J Petri; Carolyn M Klinge
Journal:  Cancer Metastasis Rev       Date:  2020-09       Impact factor: 9.264

Review 4.  Targeting the PI3K pathway and DNA damage response as a therapeutic strategy in ovarian cancer.

Authors:  Tzu-Ting Huang; Erika J Lampert; Cynthia Coots; Jung-Min Lee
Journal:  Cancer Treat Rev       Date:  2020-04-10       Impact factor: 12.111

Review 5.  Alterations and molecular targeting of the GSK-3 regulator, PI3K, in head and neck cancer.

Authors:  Michelle J Lee; Nan Jin; Jennifer R Grandis; Daniel E Johnson
Journal:  Biochim Biophys Acta Mol Cell Res       Date:  2020-02-19       Impact factor: 4.739

Review 6.  PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects.

Authors:  Rosalin Mishra; Hima Patel; Samar Alanazi; Mary Kate Kilroy; Joan T Garrett
Journal:  Int J Mol Sci       Date:  2021-03-27       Impact factor: 5.923

7.  Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.

Authors:  Ashish Thakur; Gregory J Tawa; Mark J Henderson; Carina Danchik; Suiyang Liu; Pranav Shah; Amy Q Wang; Garrett Dunn; Md Kabir; Elias C Padilha; Xin Xu; Anton Simeonov; Surender Kharbanda; Richard Stone; Gurmit Grewal
Journal:  J Med Chem       Date:  2020-04-08       Impact factor: 7.446

Review 8.  PIK3CA gene aberrancy and role in targeted therapy of solid malignancies.

Authors:  Owen Willis; Khalil Choucair; Abdurahman Alloghbi; Laura Stanbery; Rex Mowat; F Charles Brunicardi; Lance Dworkin; John Nemunaitis
Journal:  Cancer Gene Ther       Date:  2020-01-28       Impact factor: 5.987

Review 9.  Molecular events in the pathogenesis of vulvar squamous cell carcinoma.

Authors:  Deyin Xing; Oluwole Fadare
Journal:  Semin Diagn Pathol       Date:  2020-09-25       Impact factor: 3.464

Review 10.  Overlapping Molecular Pathways Leading to Autism Spectrum Disorders, Fragile X Syndrome, and Targeted Treatments.

Authors:  Maria Jimena Salcedo-Arellano; Ana Maria Cabal-Herrera; Ruchi Harendra Punatar; Courtney Jessica Clark; Christopher Allen Romney; Randi J Hagerman
Journal:  Neurotherapeutics       Date:  2020-11-19       Impact factor: 7.620
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