There have been reports of noninfectious pneumonitis (including some with pulmonary hypertension as a secondary event), infections, and renal failure (including acute renal failure) in patients...
AI, aromatase inhibitor; CDK, cyclin-dependent kinase; ER, estrogen receptor; ERD, estrogen-receptor downregulator; G1, gap 1; G2, gap 2; M, mitosis; mTOR, mammalian target of rapamycin; P, phosphorylation; PI3K, phosphoinositide 3-kinase; Rb, retinoblastoma; S, synthesis; S6K1, p70 ribosomal S6 kinase 1; SERM, selective estrogen receptor modulator.
References: 1. Johnston SRD. Enhancing the efficacy of hormonal agents with selected targeted agents. Clin Breast Cancer. 2009;9(suppl 1):S28-S36. 2. Miller TW, Hennessy BT, González-Angulo AM, et al. Hyperactivation of phosphatidylinositol-3 kinase promotes escape from hormone dependence in estrogen receptor-positive human breast cancer. J Clin Invest. 2010;120(7):2406-2413. 3. Referenced with permission from the NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines®) for Breast Cancer V.2.2016. © National Comprehensive Cancer Network, Inc 2016. All rights reserved. Accessed May 18, 2016. To view the most recent and complete version of the guideline, go online to www.NCCN.org. NATIONAL COMPREHENSIVE CANCER NETWORK®, NCCN®, NCCN GUIDELINES®, and all other NCCN Content are trademarks owned by the National Comprehensive Cancer Network, Inc. 4. Osborne CK, Schiff R. Mechanisms of endocrine resistance in breast cancer. Annu Rev Med. 2011;62:233-247. 5. Ibrance [prescribing information]. New York, NY: Pfizer Inc; 2016. 6. Afinitor [prescribing information]. East Hanover, NJ: Novartis Pharmaceuticals Corp; 2016. 7. Johnston SRD. New strategies in estrogen receptor-positive breast cancer. Clin Cancer Res. 2010;16(7):1979-1987. 8. Yamamoto-Ibusuki M, Arnedos M, André F. Targeted therapies for ER+/HER2- metastatic breast cancer. BMC Med. 2015;13:137. 9. Laplante M, Sabatini DM. mTOR signaling at a glance. J Cell Sci. 2009;122:3589-3594. 10. Azab SS. Targeting the mTOR signaling pathways in breast cancer: more than the rapalogs. J Biochem Pharmacol Res. 2013;1(2):75-83. 11. Yuan R, Kay A, Berg WJ, Lebwohl D. Targeting tumorigenesis: development and use of mTOR inhibitors in cancer therapy. J Hematol Oncol. 2009;2:45. 12. Wullschleger S, Loewith R, Hall MN. TOR signaling in growth and metabolism. Cell. 2006;124:471-484. 13. Miller TW, Rexer BN, Garrett JT, Arteaga CL. Mutations in the phosphatidylinositol 3-kinase pathway: role in tumor progression and therapeutic implications in breast cancer. Breast Cancer Res. 2011;13(6):224. 14. Di Cosimo S, Baselga J. Management of breast cancer with targeted agents: importance of heterogeneity. Nat Rev Clin Oncol. 2010;7(3):139-147. 15. Ciruelos Gil EM. Targeting the PI3K/AKT/mTOR pathway in estrogen receptor-positive breast cancer. Cancer Treat Rev. 2014;40(7):862-871.
AFINITOR is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane after failure of treatment with letrozole or anastrozole.
Important Safety Information
AFINITOR is contraindicated in patients with hypersensitivity to everolimus, to other rapamycin derivatives, or to any of the excipients.
Angioedema With Concomitant Use of Angiotensin-Converting Enzyme (ACE) Inhibitors
Impaired Wound Healing
Laboratory Tests and Monitoring
Please see full Prescribing Information.