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Review

Biological considerations and clinical applications of new HER2-targeted agents

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Pages 1497-1509 | Published online: 10 Jan 2014

References

  • Schlessinger J. Cell signaling by receptor tyrosine kinases. Cell103, 211–225 (2000).
  • Zhang X, Gureasko J, Shen K, Cole PA, Kuriyan J. An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor. Cell125, 1137–1149 (2006).
  • Miettinen PJ, Berger JE, Meneses J et al. Epithelial immaturity and multiorgan failure in mice lacking epidermal growth factor receptor. Nature376, 337–341 (1995).
  • Lee KF, Simon H, Chen H, Bates B, Hung MC, Hauser C. Requirement for neuregulin receptor erbB2 in neural and cardiac development. Nature378, 394–398 (1995).
  • Jones FE, Stern DF. Expression of dominant–negative ErbB2 in the mammary gland of transgenic mice reveals a role in lobuloaveolar development and lactation. Oncogene18, 3481–3490 (1999).
  • Harris AL, Nicholson S, Sainsbury R, Wright C, Farndon J. Epidermal growth factor receptor and other oncogenes as prognostic markers. Natl Cancer Inst. Monogr.11, 181–187 (1992).
  • Di Marco E, Pierce JH, Fleming TP et al. Autocrine interaction between TGF α and the EGF-receptor: quantitative requirements for induction of the malignant phenotype. Oncogene4, 831–838 (1989).
  • Menard S, Fortis S, Castiglioni F, Agresti R, Balsari A. HER2 as a prognostic factor in breast cancer. Oncology61(Suppl. 2), 67–72 (2001).
  • Slamon DJ, Clark GM, Wong SG, Levin WJ, Ulrich A, McGuire L. Human breast cancer: correlation of relapse and survival with amplification of the HER-2 neu oncogene. Science235, 177–182 (1987).
  • Press MF, Bernstein L, Thomas PA et al. HER-2/neu gene amplification characterized by fluorescence in situ hybridization: poor prognosis in node-negative breast carcinomas. J. Clin. Oncol.15, 2894–2904 (1997).
  • Wolff AC, Hammond EH, Schwartz JN et al. American Society of Clinical Oncology/College of American Pathologists guideline recommendations for human epidermal growth factor receptor 2 testing in breast cancer. J. Clin. Oncol.25, 118–145 (2007).
  • Slamon DJ, Leyland-Jones B, Shak S et al. Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. N. Engl. J. Med.344, 783–792 (2001).
  • Gomez HL, Doval DC, Chavez MA et al. Efficacy and safety of lapatinib as first-line therapy for ErbB2-amplified locally advanced or metastatic breast cancer. J. Clin. Oncol.26, 2999–3005 (2008).
  • Geyer CE, Forster J, Lindquist D et al. Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N. Engl. J. Med.355, 2733–2743 (2006).
  • Blackwell KL, Burstein HJ, Storniolo AM et al. Randomized study of lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer. J. Clin. Oncol.28, 1124–1130 (2010).
  • Konecny GE, Pegram MD, Venkatesan N et al. Activity of the dual kinase inhibitor lapatinib (GW572016) against HER2-overexpressing and trastuzumab-treated breast cancer cells. Cancer Res.66, 1630–1639 (2006).
  • 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 Res64, 3958–3965 (2004).
  • Mather B, Viswanathan K, Miller K, Long T. Michael addition reactions in macromolecular design for emerging technologies. Progress Polymer Sci.31, 487–531 (2006).
  • Yun C-H, Mengwasser KE, Toms AV et al. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc. Natl Acad. Sci. USA105, 2070–2075 (2008).
  • 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.15, 2552–2558 (2009).
  • Besse B, Eaton KD, Soria JV et al. Neratinib (HKI-272), an irreversible pan-ErbB receptor tyrosine kinase inhibitor: preliminary results of a Phase 2 trial in patients with advanced non-small cell lung cancer. Eur. J. Cancer6, 64 (2008).
  • Chow L, Gupta S, Hershman DL et al. Safety and efficacy of neratinib (HKI-272) in combination with paclitaxel in ErbB2+ metastatic breast cancer. Cancer Res.69(Suppl.) (2009) (Abstract 5081).
  • Awada A Dirix L, Beck J et al. Safety and efficacy of neratinib (HKI-272) in combination with vinorelbine in ErbB2+ metastatic breast cancer. Cancer Res.69(Suppl.) (2009) (Abstract 5095).
  • 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.28, 1301–1307 (2010).
  • Remillard S, Rebhun LI, Howie GA, Kupchan SM. Antimitotic activity of the potent tumor inhibitor maytansine. Science189, 1002–1005 (1975).
  • Bhattacharyya B, Wolff J. Maytansine binding to the vinblastine sites of tubulin. FEBS Lett.75, 159–162 (1977).
  • Kupchan SM, Sneden AT, Branfman AR et al. Structural requirements for antileukemic activity among the naturally occurring and semisynthetic maytansinoids. J. Med. Chem.21, 31–37 (1978).
  • Blum RH, Wittenberg BK, Canellos GP et al. A therapeutic trial of maytansine. Cancer Clin. Trials1, 113–117 (1978).
  • Eagan RT, Ingle JN, Rubin J, Frytak S, Moertel CG. Early clinical study of an intermittent schedule for maytansine (NSC-153858): brief communication. J. Natl Cancer Inst.60, 93–96 (1978).
  • Chari RV, Martell BA, Gross JL et al. Immunoconjugates containing novel maytansinoids: promising anticancer drugs. Cancer Res.52, 127–131 (1992).
  • Beeram M, Burris HA, Modi S et al. A Phase I study of trastuzumab–DM1, a first-in-class HER2 antibody–drug conjugate (ADC), given every 3 weeks to patients with HER2+ metastatic breast cancer. J. Clin. Oncol.26, 15s (2008) (Abstract 1028).
  • Vogel CL, Burris HA, Limentani S et al. A Phase II study of trastuzumab–DM1 (T-DM1), a HER2 antibody–drug conjugate (ADC), in patients with HER2+ metastatic breast cancer (MBC): final results. J. Clin. Oncol.27, 15s(2009) (Abstract 1017).
  • Krop I, LoRusso P, Miller KD et al. A Phase II study of trastuzumab–DM1 (T-DM1), a novel HER2 antibody–drug conjugate, in HER2+ metastatic breast cancer patients previously treated with conventional chemotherapy, lapatinib, and trastuzumab. Cancer Res.69(Suppl. 3) (2009) (Abstract 710).
  • Burgess AW, Cho HS, Eigenbrot C et al. An open-and-shut case? Recent insights into the activation of EGF/ErbB receptors. Mol. Cell12, 541–552 (2003).
  • Graus -Porta D, Beerli RR, Daly JM, Hynes NE. ErbB-2, the preferred heterodimerization partner of all ErbB receptors, is a mediator of lateral signaling. EMBO J.16, 1647–1655 (1997).
  • Cho HS, Mason K, Ramyar KX et al. Structure of the extracellular region of HER2 alone and in complex with the herceptin Fab. Nature421, 756–760 (2003).
  • Agus DB, Akita RW, Fox WD et al. Targeting ligand-activated ErbB2 signaling inhibits breast and prostate tumor growth. Cancer Cell2, 127–137 (2002).
  • Friess T, Thier M, Scheuer W et al. Combination treatment with pertuzumab and tratuzumab against Calu-3 human NSCLC xenograft tumors is superior to monotherapy. Presented at: 17th Annual Meeting of the American Association for Cancer Research–National Cancer Institute–European Organisation for Research and Treatment of Cancer. Philadelphia, PA, USA, 14–18 November 2005.
  • Baselga J, Gelmon KA, Verma S et al. Phase II trial of pertuzumab and trastuzumab in patients with human epidermal growth factor receptor 2-positive metastatic breast cancer that progressed during prior trastuzumab therapy. J. Clin. Oncol.28, 1138–1144 (2010).
  • Gianni L, Llado A, Bianchi G et al. Open-label, Phase II, multicenter, randomized study of the efficacy and safety of two dose levels of pertuzumab, a human epidermal growth factor receptor 2 dimerization inhibitor, in patients with human epidermal growth factor receptor 2-negative metastatic breast cancer. J. Clin. Oncol.28, 1131–1137 (2010).
  • Agus DB, Gordon MS, Taylor C et al. Phase I clinical study of pertuzumab, a novel HER dimerization inhibitor, in patients with advanced cancer. J. Clin. Oncol.23, 2534–2543 (2005).
  • Montemurro F, Donadio M, Clavarezza M et al. Outcome of patients with HER2-positive advanced breast cancer progressing during trastuzumab-based therapy. Oncologist11, 318–324 (2006).
  • Romond EH, Perez EA, Bryant J et al. Trastuzumab plus adjuvant chemotherapy for operable HER2-positive breast cancer. N. Engl. J. Med.353, 1673–1684 (2005).
  • Piccart-Gebhart MJ, Procter M, Leyland-Jones B et al. Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer. N. Engl. J. Med.353, 1659–1672 (2005).
  • Di Fiore PP, Pierce JH, Kraus MH, Segatto O, King CR, Aaronson SA. ErbB-2 is a potent oncogene when overexpressed in NIH/3T3 cells. Science237, 178–182 (1987).
  • Olayioye MA, Graus-Porta D, Beerli RR, Rohrer J, Gay B, Hynes NE. ErbB-1 and erbB-2 acquire distinct signaling properties dependent upon their dimerization partner. Mol. Cell Biol.18, 5042–5051 (1998).
  • Alimandi M, Romano A, Curia MC et al. Cooperative signaling of erbB3 and erbB2 in neoplastic transformation and human mammary carcinomas. Oncogene10, 1813–1821 (1995).
  • Kokai Y, Myers JN, Wada T et al. Synergistic interaction of p185c-neu and the EGF receptor leads to transformation of rodent fibroblasts. Cell58, 287–292 (1989).
  • Segatto O, King CR, Pierce JH, DiFiore PP, Aaronson SA. Different structural alterations upregulate in vitro tyrosine kinase activity and transforming potency of the erbB-2 gene. Mol. Cell Biol.8, 5570–5574 (1988).
  • Xia W, Liu L-H, Ho P, Spector NL. Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW72016. Oncogene23, 646–653 (2004).
  • Colomer R, Montero S, Lluch A et al. Circulating HER2 extracellular domain and resistance to chemotherapy in advanced breast cancer. Clin. Cancer Res.6, 2356–2362 (2000).
  • Molina MA, Saez R, Ramsey et al. NH(2)-terminal truncated HER-2 protein but not full-length receptor is associated with nodal metastasis in human breast cancer. Clin. Cancer Res.8, 347–353 (2002).
  • Lu Y, Zi X, Zhao Y, Mascarenhas D, Pollak M. Insulin-like growth factor-1 receptor signaling and resistance to trastuzumab. J. Natl Cancer Inst.93, 1852–1857 (2001).
  • Harris LN, You F, Schnitt SJ et al. Predictors of resistance to preoperative trastuzumab and vinorelbine for HER2-positive early breast cancer. Clin. Cancer Res.13, 1198–1207 (2007).
  • Nahta R, Yuan LXH, Zhang B, Kobayashi R, Esteva FJ. Insulin-like growth factor-1 receptor/human epidermal growth factor receptor 2 heterodimerization contributes to trastuzumab resistance of breast cancer cells. Cancer Res.65, 11118–11128 (2005).
  • Lai A, Sarcevic B, Prall OWJ, Sutherland RL. Insulin/insulin-like growth factor-I and estrogen cooperate to stimulate cyclin E-Cdk2 activation and cell cycle progression in MCF-7 breast cancer cells through differential regulation of cyclin E and p21WAF1/Cip. J. Biol. Chem.276, 25823–25833 (2001).
  • Le X-F, McWatters A, Wiener J, Wu J-Y, Mills GB, Bast RC Jr. Anti-HER2 antibody and heregulin suppress growth of HER2-overexpressing human breast cancer cells through different mechanisms. Clin. Cancer Res.6, 260–270 (2000).
  • Nicholson RI, Hutcheson IR, Knowlden JM et al. Nonendocrine pathways and endocrine resistance; observations with antiestrogens and signal transduction inhibitors in combination. Clin. Cancer Res.10, 346s–354s (2004).
  • Tang CK, Perez C, Grunt T, Waibel C, Cho C, Lupu R. Involvement of heregulin-β2 in the acquisition of the hormone-independent phenotype of breast cancer cells. Cancer Res.56, 3350–3358 (1996).
  • Knowlden JM, Hutcheson IR, Jones HE et al. Elevated levels of epidermal growth factor receptor/cerB2 heterodimers mediate an autocrine growth regulatory pathway in tamoxifen-resistant MCF-7 cells. Endocrinology144, 1032–1044 (2003).
  • Nicholson RI, Staka C, Boyns F, Hutcheson IR, Gee JM. Growth factor-driven mechanisms associated with resistance to estrogen deprivation in breast cancer: new opportunities for therapy. Endocr. Relat. Cancer11, 623–641 (2004).
  • Massarweh S, Osborne CK, Jiang S et al. Mechanisms of tumor regression and resistance to estrogen deprivation and fulvestrant in a model of estrogen receptor-positive, HER-2/neu-positive breast cancer. Cancer Res.66, 8266–8273 (2006).
  • Mackey JR, Kaufman B, Clemens M et al. Trastuzumab plus anastrozole versus anastrozole alone for the treatment of postmenopausal women with human epidermal growth factor receptor 2-positive, hormone receptor-positive metastatic breast cancer: results from the randomized Phase III TAnDEM study. J. Clin. Oncol.27, 5529–5537 (2009).
  • Johnston S, Pippen J Jr, Pivot X et al. Lapatinib combined with letrozole versus letrozole and placebo as first-line therapy for postmenopausal hormone receptor-positive metastatic breast cancer. J. Clin. Oncol.27, 5538–5546 (2009).
  • Fisher B, Costantino JP, Wickerham DL et al. Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study. J. Natl Cancer Inst.90, 1371–1388 (1998).
  • Vogel GV, Costantino JP, Wickerham DL et al. Effects of tamoxifen vs. raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP study of tamoxifen and raloxifene (STAR) P-2 trial. JAMA295, 2727–2741 (2006).
  • Cuzick J, Forbes J, Edwards R et al. First results from the International Breast Cancer Intervention Study (IBIS-1): a randomised prevention trial. Lancet360, 817–824 (2002).
  • Yen L, You XL, Al Moustafa AE et al. Heregulin selectively upregulates vascular endothelial growth factor secretion in cancer cells and stimulates angiogenesis. Oncogene19, 3460–3469 (2000).
  • Konecny GE, Meng YG, Untch M et al. Association between HER-2/neu and vascular endothelial growth factor expression predicts clinical outcome in primary breast cancer patients. Clin. Cancer Res.10, 1706–1716 (2004).
  • Pegram M, Chan D, Dichmann R et al. Phase II combined biological therapy targeting the HER2 proto-oncogene and the vascular endothelial growth factor using trastuzumab (T) and bevacizumab (B) as first line treatment of HER2-amplified breast cancer. Proceedings of: 29th Annual San Antonio Breast Cancer Symposium. San Antonio, TX, USA, 14–17 December 2006 (Abstract 301).
  • Marks PA, Richon VM, Rifkind RA. Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells. J. Natl Cancer Inst.92, 1210–1216 (2000).
  • Xu W, Mimnaugh E, Rosser MFN et al. Sensitivity of mature ErbB2 to geldanamycin is conferred by its kinase domain and is mediated by the chaperone protein Hsp90. J. Biol. Chem.276, 3702–3708 (2001).
  • Chandarlapaty S, Scaltriti M, Angelini P et al. Inhibitors of HSP90 block p95–HER2 signaling in trastuzumab-resistant tumors and suppress their growth. Oncogene29, 325–334 (2010).

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