Alpelisib in the Treatment of Breast Cancer: A Short Review on the Emerging Clinical Data

References

• SocietyACBreast cancer facts and figures 2019–2020. 910, 2020; Available from: https://www.cancer.org/content/dam/cancer-org/research/cancer-facts-and-statistics/breast-cancer-facts-and-figures/breast-cancer-facts-and-figures-2019-2020.pdf. Accessed 108, 2020.
   Google Scholar
• FinnRS, MartinM, RugoHS, et al. Palbociclib and letrozole in advanced breast cancer. N Engl J Med. 2016;375(20):1925. doi:10.1056/NEJMoa160730327959613
   PubMed Web of Science ®Google Scholar
• GoetzMP, ToiM, CamponeM, et al. MONARCH 3: abemaciclib as initial therapy for advanced breast cancer. J Clin Oncol. 2017;35(32):3638–3646. doi:10.1200/JCO.2017.75.615528968163
   PubMed Web of Science ®Google Scholar
• HortobagyiGN, StemmerSM, BurrisHA, et al. Ribociclib as first-line therapy for HR-positive, advanced breast cancer. N Engl J Med. 2016;375(18):1738–1748. doi:10.1056/NEJMoa160970927717303
   PubMed Web of Science ®Google Scholar
• NCCN Clinical Practice Guidelines in Oncology (NCCN guidelines). Breast cancer. Version 3.2020. Available from: https://www.nccn.org/professionals/physician_gls/pdf/breast.pdf. Accessed 41, 2020.
   Google Scholar
• RobertsonJFR, BondarenkoIM, TrishkinaE, et al. Fulvestrant 500 mg versus anastrozole 1 mg for hormone receptor-positive advanced breast cancer (FALCON): an international, randomised, double-blind, phase 3 trial. Lancet. 2016;388(10063):2997–3005. doi:10.1016/S0140-6736(16)32389-327908454
   PubMed Web of Science ®Google Scholar
• BaselgaJ, CamponeM, PiccartM, et al. Everolimus in postmenopausal hormone-receptor-positive advanced breast cancer. N Engl J Med. 2012;366(6):520–529. doi:10.1056/NEJMoa110965322149876
   PubMed Web of Science ®Google Scholar
• JonesRH, CasbardA, CarucciM, et al. Fulvestrant plus capivasertib versus placebo after relapse or progression on an aromatase inhibitor in metastatic, oestrogen receptor-positive breast cancer (FAKTION): a multicentre, randomised, controlled, phase 2 trial. Lancet Oncol. 2020;21(3):345–357. doi:10.1016/S1470-2045(19)30817-432035020
   PubMed Web of Science ®Google Scholar
• VerretB, CortesJ, BachelotT, AndreF, ArnedosM. Efficacy of PI3K inhibitors in advanced breast cancer. Ann Oncol. 2019;30(Suppl_10):x12–x20. doi:10.1093/annonc/mdz381
   Web of Science ®Google Scholar
• FritschC, HuangA, Chatenay-RivaudayC, et al. Characterization of the novel and specific PI3Kalpha inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther. 2014;13(5):1117–1129. doi:10.1158/1535-7163.MCT-13-086524608574
   PubMed Web of Science ®Google Scholar
• LoRussoPM. Inhibition of the PI3K/AKT/mTOR pathway in solid tumors. J Clin Oncol. 2016;34(31):3803–3815. doi:10.1200/JCO.2014.59.001827621407
   PubMed Web of Science ®Google Scholar
• Cancer Genome Atlas Network. Comprehensive molecular portraits of human breast tumours. Nature. 2012;490(7418):61–70.23000897
   PubMed Web of Science ®Google Scholar
• Stemke-HaleK, Gonzalez-AnguloAM, LluchA, et al. An integrative genomic and proteomic analysis of PIK3CA, PTEN, and AKT mutations in breast cancer. Cancer Res. 2008;68(15):6084–6091. doi:10.1158/0008-5472.CAN-07-685418676830
   PubMed Web of Science ®Google Scholar
• BaselgaJ, ImS-A, IwataH, et al. Buparlisib plus fulvestrant versus placebo plus fulvestrant in postmenopausal, hormone receptor-positive, HER2-negative, advanced breast cancer (BELLE-2): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet Oncol. 2017;18(7):904–916. doi:10.1016/S1470-2045(17)30376-528576675
   PubMed Web of Science ®Google Scholar
• Di LeoA, JohnstonS, LeeKS, et al. Buparlisib plus fulvestrant in postmenopausal women with hormone-receptor-positive, HER2-negative, advanced breast cancer progressing on or after mTOR inhibition (BELLE-3): a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet Oncol. 2018;19(1):87–100. doi:10.1016/S1470-2045(17)30688-529223745
   PubMed Web of Science ®Google Scholar
• VuylstekeP, Huizing M, Petrakova K, et al. Pictilisib PI3Kinase inhibitor (a phosphatidylinositol 3-kinase [PI3K] inhibitor) plus paclitaxel for the treatment of hormone receptor-positive, HER2-negative, locally recurrent, or metastatic breast cancer: interim analysis of the multicentre, placebo-controlled, phase II randomised PEGGY study. Ann Oncol. 2016;27(11):2059–2066.27573562
   PubMed Web of Science ®Google Scholar
• BaselgaJ, DentSF, CortésJ, et al. Phase III study of taselisib (GDC-0032) + fulvestrant (FULV) v FULV in patients (pts) with estrogen receptor (ER)-positive, PIK3CA -mutant (MUT), locally advanced or metastatic breast cancer (MBC): primary analysis from SANDPIPER. J Clin Oncol. 2018;36(18_suppl):LBA1006–LBA1006. doi:10.1200/JCO.2018.36.18_suppl.LBA1006
   Web of Science ®Google Scholar
• JuricD, RodonJ, TaberneroJ, et al. Phosphatidylinositol 3-kinase α–selective inhibition with alpelisib (BYL719) in PIK3CA -altered solid tumors: results from the first-in-human study. J Clin Oncol. 2018;36(13):1291–1299. doi:10.1200/JCO.2017.72.710729401002
   PubMed Web of Science ®Google Scholar
• FDA highlights of prescribing information: alpelisib. Version 5.2019. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212526s000lbl.pdf. Accessed 43, 2020.
   Google Scholar
• JuricD, JankuF, RodónJ, et al. Alpelisib plus fulvestrant in PIK3CA -altered and PIK3CA -wild-type estrogen receptor–positive advanced breast cancer. JAMA Oncol. 2019;5(2):e184475. doi:10.1001/jamaoncol.2018.447530543347
   PubMed Web of Science ®Google Scholar
• AndreF, CiruelosE, RubovszkyG, et al. Alpelisib for PIK3CA -mutated, hormone receptor–positive advanced breast cancer. N Engl J Med. 2019;380(20):1929–1940. doi:10.1056/NEJMoa181390431091374
   PubMed Web of Science ®Google Scholar
• BrandãoM, CaparicaR, EigerD, et al. Biomarkers of response and resistance to PI3K inhibitors in estrogen receptor-positive breast cancer patients and combination therapies involving PI3K inhibitors. Ann Oncol. 2019;30(Suppl_10):x27–x42. doi:10.1093/annonc/mdz280
   PubMed Web of Science ®Google Scholar
• RazaviP, DicklerMN, ShahPD, et al. Alterations in PTEN and ESR1 promote clinical resistance to alpelisib plus aromatase inhibitors. Nat Cancer. 2020;1(4):382–393. doi:10.1038/s43018-020-0047-132864625
   PubMedGoogle Scholar
• VasanN, Razavi P, Johnson JL, et al. Double PIK3CA mutations in cis increase oncogenicity and sensitivity to PI3Kα inhibitors. Science. 2019;366(6466):714–723.31699932
   PubMed Web of Science ®Google Scholar
• Martínez-SáezO, ChicN, PascualT, et al. Frequency and spectrum of PIK3CA somatic mutations in breast cancer. Breast Cancer Res. 2020;22(1):45. doi:10.1186/s13058-020-01284-932404150
   PubMed Web of Science ®Google Scholar
• RugoHS, Lerebours F, Ciruelos E, et al. Alpelisib (ALP) + fulvestrant (FUL) in patients (pts) with PIK3CA-mutated (mut) hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2–) advanced breast cancer (ABC) previously treated with cyclin-dependent kinase 4/6 inhibitor (CDKi) + aromatase inhibitor (AI): bYLieve study results. J Clin Oncol. 2020;38(15_suppl):1006.31880950
   PubMed Web of Science ®Google Scholar
• HankerAB, PfefferleAD, BalkoJM, et al. Mutant PIK3CA accelerates HER2-driven transgenic mammary tumors and induces resistance to combinations of anti-HER2 therapies. Proc Natl Acad Sci U S A. 2013;110(35):14372–14377. doi:10.1073/pnas.130320411023940356
   PubMed Web of Science ®Google Scholar
• JainS, ShahAN, Santa-MariaCA, et al. Phase I study of alpelisib (BYL-719) and trastuzumab emtansine (T-DM1) in HER2-positive metastatic breast cancer (MBC) after trastuzumab and taxane therapy. Breast Cancer Res Treat. 2018;171(2):371–381. doi:10.1007/s10549-018-4792-029850984
   PubMed Web of Science ®Google Scholar
• CostaRLB, HanHS, GradisharWJ. Targeting the PI3K/AKT/mTOR pathway in triple negative breast cancer: a review. Breast Cancer Res Treat. 2018;169(3):397–406. doi:10.1007/s10549-018-4697-y29417298
   PubMed Web of Science ®Google Scholar