Iqbal N. Human epidermal growth factor receptor 2 (HER2) in cancers: overexpression and therapeutic implications. Mol Biol Int. 2014;2014:852748.
Tai W, Mahato R, Cheng K. The role of HER2 in cancer therapy and targeted drug delivery. J Control Release. 2010;146(3):264–75.
Wang T, Xu Y, Sheng S, et al. HER2 somatic mutations are associated with poor survival in HER2-negative breast cancers. Cancer Sci. 2017;108(4):671–7.
Schroeder RL, Stevens CL, Sridhar J. Small molecule tyrosine kinase inhibitors of ErbB2/HER2/Neu in the treatment of aggressive breast cancer. Molecules. 2014;19(9):15196–212.
Puma Biotechnology Inc. Nerlynx (neratinib): US prescribing information. 2017. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf. Accessed 19 July 2017.
Rabindran SK, Discafani CM, Rosfjord EC, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res. 2004;64(11):3958–65.
FDA. FDA approves neratinib for extended adjuvant treatment of early stage HER2-positive breast cancer [media release]. 17 Jul 2017. https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm567259.htm.
Canonici A, Gijsen M, Mullooly M, et al. Neratinib overcomes trastuzumab resistance in HER2 amplified breast cancer. Oncotarget. 2013;4(10):1592–605.
Menderes G, Bonazzoli E, Bellone S, et al. Efficacy of neratinib in the treatment of HER2/neu-amplified epithelial ovarian carcinoma in vitro and in vivo. Med Oncol. 2017;34(5):91.
Schwab CL, English DP, Black J, et al. Neratinib shows efficacy in the treatment of HER2 amplified carcinosarcoma in vitro and in vivo. Gynecol Oncol. 2015;139(1):112–7.
Lopez S, Cocco E, Black J, et al. Dual HER2/PIK3CA targeting overcomes single-agent acquired resistance in HER2-amplified uterine serous carcinoma cell lines in vitro and in vivo. Mol Cancer Ther. 2015;14(11):2519–26.
Shimamura T, Ji H, Minami Y, et al. Non-small-cell lung cancer and Ba/F3 transformed cells harboring the ERBB2 G776insV_G/C mutation are sensitive to the dual-specific epidermal growth factor receptor and ERBB2 inhibitor HKI-272. Cancer Res. 2006;66(13):6487–91.
Schwartz L, Croessmann S, Avogadri-Connors F, et al. Neratinib/fulvestrant but not fulvestrant alone maintain complete responses after treatment with trastuzumab/paclitaxel of mice bearing ER+/HER2+ xenografts [abstract no. 4818]. Cancer Res. 2017;77(13 Suppl.).
Montemurro F, Di Cosimo S, Arpino G. Human epidermal growth factor receptor 2 (HER2)-positive and hormone receptor-positive breast cancer: new insights into molecular interactions and clinical implications. Ann Oncol. 2013;24(11):2715–24.
Zhao XQ, Xie JD, Chen XG, et al. Neratinib reverses ATP-binding cassette B1-mediated chemotherapeutic drug resistance in vitro, in vivo, and ex vivo. Mol Pharmacol. 2012;82(1):47–58.
Breslin S, Lowry MC, O’Driscoll L. Neratinib resistance and cross-resistance to other HER2-targeted drugs due to increased activity of metabolism enzyme cytochrome P4503A4. Br J Cancer. 2017;116(5):620–5.
Hug B, Abbas R, Leister C, et al. A single-dose, crossover, placebo- and moxifloxacin-controlled study to assess the effects of neratinib (HKI-272) on cardiac repolarization in healthy adult subjects. Clin Cancer Res. 2010;16(15):4016–23.
Wang J, Li-Chan XX, Atherton J, et al. Characterization of HKI-272 covalent binding to human serum albumin. Drug Metab Dispos. 2010;38(7):1083–93.
Abbas R, Hug BA, Leister C, et al. Pharmacokinetics of oral neratinib during co-administration of ketoconazole in healthy subjects. Br J Clin Pharmacol. 2011;71(4):522–7.
Keyvanjah K, DiPrimeo D, Li A, et al. Pharmacokinetics of neratinib during coadministration with lansoprazole in healthy subjects. Br J Clin Pharmacol. 2017;83(3):554–61.
Chan A, Delaloge S, Holmes FA, et al. Neratinib after trastuzumab-based adjuvant therapy in patients with HER2-positive breast cancer (ExteNET): a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial. Lancet Oncol. 2016;17(3):367–77.
Chan A, Delaloge S, Holmes FA, et al. Neratinib after trastuzumab-based adjuvant therapy in early-stage HER2+ breast cancer: 3-year analysis from a phase 3 randomized, placebo-controlled, double-blind trial (ExteNET) [abstract no. S5-02]. Cancer Res. 2016;76(4 Suppl 1).
Park JW, Liu MC, Yee D, et al. Adaptive randomization of neratinib in early breast cancer. N Engl J Med. 2016;375(1):11–22.
Burstein HJ, Sun Y, Dirix LY, et al. Neratinib, an irreversible ErbB receptor tyrosine kinase inhibitor, in patients with advanced ErbB2-positive breast cancer. J Clin Oncol. 2010;28(8):1301–7.
Martin M, Bonneterre J, Geyer CE Jr, et al. A phase two randomised trial of neratinib monotherapy versus lapatinib plus capecitabine combination therapy in patients with HER2+ advanced breast cancer. Eur J Cancer. 2013;49(18):3763–72.
Freedman RA, Gelman RS, Wefel JS, et al. Translational Breast Cancer Research Consortium (TBCRC) 022: a phase II trial of neratinib for patients with human epidermal growth factor receptor 2-positive breast cancer and brain metastases. J Clin Oncol. 2016;34(9):945–52.
Awada A, Colomer R, Inoue K, et al. Neratinib plus paclitaxel vs trastuzumab plus paclitaxel in previously untreated metastatic ERBB2-positive breast cancer: the NEfERT-T randomized clinical trial. JAMA Oncol. 2016;2(12):1557–64.
Chow LW, Xu B, Gupta S, et al. Combination neratinib (HKI-272) and paclitaxel therapy in patients with HER2-positive metastatic breast cancer. Br J Cancer. 2013;108(10):1985–93.
Saura C, Garcia-Saenz JA, Xu B, et al. Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2-positive breast cancer. J Clin Oncol. 2014;32(32):3626–33.
Awada A, Dirix L, Manso Sanchez L, et al. Safety and efficacy of neratinib (HKI-272) plus vinorelbine in the treatment of patients with ErbB2-positive metastatic breast cancer pretreated with anti-HER2 therapy. Ann Oncol. 2013;24(1):109–16.
Gajria D, Modi S, Saura C, et al. A phase I/II study of neratinib plus temsirolimus in HER2+ metastatic breast cancer reveals ongoing HER2 pathway dependence in many patients despite several lines of HER2 targeted therapy [abstract no. P5-19-04]. Cancer Res. 2015;75(9 Suppl.).
Freedman RA, Gelman RS, Melisko ME, et al. TBCRC 022: phase II trial of neratinib + capecitabine for patients (pts) with human epidermal growth factor receptor 2 (HER2+) breast cancer brain metastases (BCBM) [abstract]. In: ASCO Annual Meeting; 2017.
Abraham J, Puhalla SL, Sikov W, et al. NSABP FB-10: phase Ib dose-escalation trial evaluating trastuzumab emtansine (T-DMI) with neratinib (N) in women with metastatic HER2+ breast cancer (MBC) [abstract no. CT013]. Cancer Res. 2017;77(13 Suppl).
Jankowitz RC, Abraham J, Tan AR, et al. Safety and efficacy of neratinib in combination with weekly paclitaxel and trastuzumab in women with metastatic HER2positive breast cancer: an NSABP Foundation Research Program phase I study. Cancer Chemother Pharmacol. 2013;72(6):1205–12.
Ma CX, Bose R, Gao F, et al. Neratinib efficacy and circulating tumor DNA detection of HER2 mutations in HER2 non-amplified metastatic breast cancer. Clin Cancer Res. 2017. doi:10.1158/1078-0432.CCR-17-0900.
Hyman D, Piha-Paul S, Saura C, et al. Neratinib + fulvestrant in ERBB2-mutant, HER2-non-amplified, estrogen receptor (Ex positive, metastatic breast cancer (MBC): preliminary analysis from the phase II SUMMIT trial [abstract no. PD2-08]. Cancer Res. 2017;77(4 Suppl).
Sequist LV, Besse B, Lynch TJ, et al. Neratinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor: results of a phase II trial in patients with advanced non-small-cell lung cancer. J Clin Oncol. 2010;28(18):3076–83.
Gandhi L, Besse B, Mazieres J, et al. Neratinib ± temsirolimus in HER2-mutant lung cancers: an international, randomized phase II study [abstract no. MA04.02]. J Thorac Oncol. 2017;12(1 Suppl.):S358–9.
Jacobs SA, Lee JJ, George Jr TJ, et al. NSABP FC-7: a phase Ib study evaluating neratinib (N) and cetuximab (Cmab) in patients (pts) with quadruple wild-type (quad wt) (KRAS/NRAS/BRAF/PI3KCA wt) metastatic colorectal cancer (mCRC) resistant to Cmab [abstract no. C46]. Mol Cancer Ther. 2015;14(12 Suppl 2).
Wong KK, Fracasso PM, Bukowski RM, et al. A phase I study with neratinib (HKI-272), an irreversible pan ErbB receptor tyrosine kinase inhibitor, in patients with solid tumors. Clin Cancer Res. 2009;15(7):2552–8.
Ito Y, Suenaga M, Hatake K, et al. Safety, efficacy and pharmacokinetics of neratinib (HKI-272) in Japanese patients with advanced solid tumors: a phase 1 dose-escalation study. Jpn J Clin Oncol. 2012;42(4):278–86.
Gandhi L, Bahleda R, Tolaney SM, et al. Phase I study of neratinib in combination with temsirolimus in patients with human epidermal growth factor receptor 2-dependent and other solid tumors. J Clin Oncol. 2014;32(2):68–75.
Hyman D, Piha-Paul S, Rodon J, et al. Neratinib in HER2 or HER3 mutant solid tumors: SUMMIT, a global, multi-histology, open-label, phase 2 “basket” study [abstract no. CT001 and slide presentation]. Cancer Res. 2017;77(13 Suppl).
Ibrahim E, Tripathy D, Wilkinson M, et al. Effects of adding budesonide or colestipol to loperamide prophylaxis on neratinib-associated diarrhea in patients (pts) with HER2+ early-stage breast cancer (eBC): the CONTROL trial [abstract no. CT128 plus Poster]. Cancer Res. 2017;77(13 Suppl.).