Summary: A humanized monoclonal antibody against the ERBB-2 RECEPTOR (HER2). As an ANTINEOPLASTIC AGENT, it is used to treat BREAST CANCER where HER2 is overexpressed.

Top Publications

  1. Sliwkowski M, Lofgren J, Lewis G, Hotaling T, Fendly B, Fox J. Nonclinical studies addressing the mechanism of action of trastuzumab (Herceptin). Semin Oncol. 1999;26:60-70 pubmed
    ..One of these antibodies, 4D5, has been fully humanized and is termed trastuzumab (Herceptin; Genentech, San Francisco, CA)...
  2. Goldenberg M. Trastuzumab, a recombinant DNA-derived humanized monoclonal antibody, a novel agent for the treatment of metastatic breast cancer. Clin Ther. 1999;21:309-18 pubmed
    ..b>Trastuzumab (Herceptin, Genentech, Inc...
  3. Hede K. Gastric cancer: trastuzumab trial results spur search for other targets. J Natl Cancer Inst. 2009;101:1306-7 pubmed publisher
  4. Roukos D. Targeting gastric cancer with trastuzumab: new clinical practice and innovative developments to overcome resistance. Ann Surg Oncol. 2010;17:14-7 pubmed publisher
  5. von Minckwitz G, Procter M, de Azambuja E, Zardavas D, Benyunes M, Viale G, et al. Adjuvant Pertuzumab and Trastuzumab in Early HER2-Positive Breast Cancer. N Engl J Med. 2017;377:122-131 pubmed publisher
    ..preoperative context and increases overall survival among patients with metastatic disease when it is added to trastuzumab and chemotherapy for the treatment of human epidermal growth factor receptor 2 (HER2)-positive breast cancer...
  6. Carvajal Hausdorf D, Schalper K, Bai Y, Black J, Santin A, Rimm D. Objective, domain-specific HER2 measurement in uterine and ovarian serous carcinomas and its clinical significance. Gynecol Oncol. 2017;145:154-158 pubmed publisher
    ..g. lapatinib or afatinib) alone or in combination with extracellular domain-directed drugs (e.g. trastuzumab, pertuzumab, T-DM1).
  7. Bellati F, Napoletano C, Ruscito I, Liberati M, Panici P, Nuti M. Cellular adaptive immune system plays a crucial role in trastuzumab clinical efficacy. J Clin Oncol. 2010;28:e369-70; author reply e371 pubmed publisher
  8. Carlson J, Nooruddin Z, Rusthoven C, Elias A, Borges V, Diamond J, et al. Trastuzumab emtansine and stereotactic radiosurgery: an unexpected increase in clinically significant brain edema. Neuro Oncol. 2014;16:1006-9 pubmed
    ..These patients were treated with stereotactic radiosurgery and trastuzumab emtansine, the newest FDA-approved agent for metastatic HER2+ breast cancer...
  9. Chakraborty A, Hatzis C, Digiovanna M. Co-targeting the HER and IGF/insulin receptor axis in breast cancer, with triple targeting with endocrine therapy for hormone-sensitive disease. Breast Cancer Res Treat. 2017;163:37-50 pubmed publisher

More Information


  1. Falchook G, Janku F, Tsao A, Bastida C, Stewart D, Kurzrock R. Non-small-cell lung cancer with HER2 exon 20 mutation: regression with dual HER2 inhibition and anti-VEGF combination treatment. J Thorac Oncol. 2013;8:e19-20 pubmed publisher
  2. Carlson R, Allred D, Anderson B, Burstein H, Carter W, Edge S, et al. Breast cancer. Clinical practice guidelines in oncology. J Natl Compr Canc Netw. 2009;7:122-92 pubmed
  3. Turcotte M, Allard D, Mittal D, Bareche Y, Buisseret L, José V, et al. CD73 Promotes Resistance to HER2/ErbB2 Antibody Therapy. Cancer Res. 2017;77:5652-5663 pubmed publisher
    ..this study, we investigated the role of CD73 on the activity of the anti-HER2/ErbB2 monoclonal antibody (mAb) trastuzumab. In a prospective, randomized phase III clinical trial evaluating the activity of trastuzumab, high levels of ..
  4. Spreckelmeyer S, Ramogida C, Rousseau J, Arane K, Bratanovic I, Colpo N, et al. p-NO2-Bn-H4neunpa and H4neunpa-Trastuzumab: Bifunctional Chelator for Radiometalpharmaceuticals and 111In Immuno-Single Photon Emission Computed Tomography Imaging. Bioconjug Chem. 2017;28:2145-2159 pubmed publisher
    ..bifunctional chelator p-SCN-Bn-H4neunpa and its immunoconjugate H4neunpa-trastuzumab for 111In radiolabeling are synthesized...
  5. Ross J. Saving lives with accurate HER2 testing. Am J Clin Pathol. 2010;134:183-4 pubmed publisher
  6. Lee H, Jeong N, Lee Y, Seo Y, Kim C, Lee J, et al. Radiation recall dermatitis and pneumonitis induced by trastuzumab (Herceptin®). Int J Dermatol. 2014;53:e159-60 pubmed
  7. Dokmanovic M, King K, Mohan N, Endo Y, Wu W. Cardiotoxicity of ErbB2-targeted therapies and its impact on drug development, a spotlight on trastuzumab. Expert Opin Drug Metab Toxicol. 2017;13:755-766 pubmed publisher
    b>Trastuzumab, a therapeutic monoclonal antibody directed against ErbB2, is often noted as a successful example of targeted therapy...
  8. Costa C, Molina M, Baro T, Aguilar A, De Las Heras P, Fuste P, et al. Could the truncated variant of ERBB2 be present in the squamous carcinomas of the cervix?. Virchows Arch. 2008;453:535-6 pubmed publisher
    ..In some cases, gene amplification correlates with protein overexpression and predicts response to trastuzumab. We analyzed the expression of ERBB2 in a group of 40 patients diagnosed with infiltrating squamous cervical ..
  9. Doss S, Robertson J, Adam J. Lapatinib or trastuzumab in combination with an aromatase inhibitor for first-line treatment of metastatic hormone-receptor-positive breast cancer that overexpresses HER2. Lancet Oncol. 2012;13:766-7 pubmed
  10. Jaeger B, Neugebauer J, Andergassen U, Melcher C, Schochter F, Mouarrawy D, et al. The HER2 phenotype of circulating tumor cells in HER2-positive early breast cancer: A translational research project of a prospective randomized phase III trial. PLoS ONE. 2017;12:e0173593 pubmed publisher
    ..Future follow-up evaluation will assess whether this discrepancy may contribute to trastuzumab resistance.
  11. Inadomi K, Kusaba H, Matsushita Y, Tanaka R, Mitsugi K, Arimizu K, et al. Efficacy and Safety Analysis of Oxaliplatin-based Chemotherapy for Advanced Gastric Cancer. Anticancer Res. 2017;37:2663-2671 pubmed
    ..Subsequent oxaliplatin-based therapy after cisplatin exhibited modest efficacy, especially in cases with cisplatin intolerance. ..
  12. McGuire A, Kalinina O, Holian E, Curran C, Malone C, McLaughlin R, et al. Differential impact of hormone receptor status on survival and recurrence for HER2 receptor-positive breast cancers treated with Trastuzumab. Breast Cancer Res Treat. 2017;164:221-229 pubmed publisher
    ..Yet the impact of hormone receptor status on outcome after Trastuzumab has received little attention...
  13. Eisenstein M. Medicine: Eyes on the target. Nature. 2015;527:S110-2 pubmed publisher
  14. Kashiwagi S, Asano Y, Goto W, Takada K, Takahashi K, Hatano T, et al. Using TILs to Predict Therapeutic Effect of Chemotherapy (Pertuzumab, Trastuzumab, Docetaxel) on HER2-positive Breast Cancer. Anticancer Res. 2017;37:5623-5630 pubmed
    ..We evaluated that chemotherapy with a TPD regimen (trastuzumab, pertuzumab, docetaxel) against HER2-positive breast cancer, using TILs as indicators.
  15. Reeder Hayes K, Meyer A, Hinton S, Meng K, Carey L, Dusetzina S. Comparative Toxicity and Effectiveness of Trastuzumab-Based Chemotherapy Regimens in Older Women With Early-Stage Breast Cancer. J Clin Oncol. 2017;35:3298-3305 pubmed publisher
    Purpose The combination of chemotherapy and trastuzumab is the standard of care for adjuvant treatment of human epidermal growth factor receptor 2-positive breast cancer...
  16. Pivot X, Spano J, Espie M, Cottu P, Jouannaud C, Pottier V, et al. Patients' preference of trastuzumab administration (subcutaneous versus intravenous) in HER2-positive metastatic breast cancer: Results of the randomised MetaspHer study. Eur J Cancer. 2017;82:230-236 pubmed publisher
    HannaH (NCT00950300) and PrefHer (NCT01401166) studies validated the subcutaneous (H-s.c.) formulation of trastuzumab as effective and safe as intravenous (H-i.v.) and highly preferred by patients in early breast cancer...
  17. Morimura O, Minami T, Kijima T, Koyama S, Otsuka T, Kinehara Y, et al. Trastuzumab emtansine suppresses the growth of HER2-positive small-cell lung cancer in preclinical models. Biochem Biophys Res Commun. 2017;488:596-602 pubmed publisher
    ..HER2-upregulated cisplatin- or etoposide-resistant SCLC cells were sensitive to trastuzumab-mediated ADCC...
  18. Torres S, Maralani P, Verma S. Activity of T-DM1 in HER-2 positive central nervous system breast cancer metastases. BMJ Case Rep. 2014;2014: pubmed publisher
    ..with whole brain irradiation (WBI), followed by capecitabine and lapatinib (December 2011-March 2013) and trastuzumab and lapatinib (May 2013-August 2013). Then, the brain MRI showed progression...
  19. Grover S, Leong D, Chakrabarty A, Joerg L, Kotasek D, Cheong K, et al. Left and right ventricular effects of anthracycline and trastuzumab chemotherapy: a prospective study using novel cardiac imaging and biochemical markers. Int J Cardiol. 2013;168:5465-7 pubmed publisher
  20. Weiler D, Diebold J, Strobel K, Aebi S, Gautschi O. Rapid response to trastuzumab emtansine in a patient with HER2-driven lung cancer. J Thorac Oncol. 2015;10:e16-7 pubmed publisher
  21. Fan X, Brezski R, Fa M, Deng H, Oberholtzer A, Gonzalez A, et al. A single proteolytic cleavage within the lower hinge of trastuzumab reduces immune effector function and in vivo efficacy. Breast Cancer Res. 2012;14:R116 pubmed publisher
    ..b>Trastuzumab is a humanized IgG1 therapeutic monoclonal antibody for the treatment of HER2-overexpressing breast cancers, ..
  22. Okita R, Shimizu K, Nojima Y, Yukawa T, Maeda A, Saisho S, et al. Lapatinib enhances trastuzumab-mediated antibody-dependent cellular cytotoxicity via upregulation of HER2 in malignant mesothelioma cells. Oncol Rep. 2015;34:2864-70 pubmed
    ..It was reported that the tyrosine kinase inhibitor (TKI) lapatinib enhanced trastuzumab-mediated antibody-dependent cellular cytotoxicity (ADCC) in HER2-positive breast cancer, suggesting that this ..
  23. Li H, Morokoshi Y, Nagatsu K, Kamada T, Hasegawa S. Locoregional therapy with ?-emitting trastuzumab against peritoneal metastasis of human epidermal growth factor receptor 2-positive gastric cancer in mice. Cancer Sci. 2017;108:1648-1656 pubmed publisher
    ..We have found, however, that locoregionally administered trastuzumab armed with astatine-211 (211 At-trastuzumab) is effective against human epidermal growth factor ..
  24. Moasser M. Two dimensions in targeting HER2. J Clin Oncol. 2014;32:2074-7 pubmed publisher
  25. Broughton M, Westgaard A, Paus E, Øijordsbakken M, Henanger K, Naume B, et al. Specific antibodies and sensitive immunoassays for the human epidermal growth factor receptors (HER2, HER3, and HER4). Tumour Biol. 2017;39:1010428317707436 pubmed publisher
    The use of trastuzumab in patients with breast cancer that overexpresses human epidermal growth factor receptor 2 has significantly improved treatment outcomes...
  26. Yang Y, Guo R, Tian X, Zhang Z, Zhang P, Li C, et al. Synergistic anti-tumor activity of Nimotuzumab in combination with Trastuzumab in HER2-positive breast cancer. Biochem Biophys Res Commun. 2017;489:523-527 pubmed publisher
    ..Here, we investigated the anti-tumor activity of the combination of an HER2 inhibitor, trastuzumab with an EGFR-inhibitor, nimotuzumab in HER2-overexpressing breast cancer...
  27. Vicier C, Dieci M, Arnedos M, Delaloge S, Viens P, Andre F. Clinical development of mTOR inhibitors in breast cancer. Breast Cancer Res. 2014;16:203 pubmed publisher
    ..Preclinical studies have suggested that the mTOR pathway may play a role in the resistance to hormone therapy, trastuzumab and chemotherapy for breast cancer...
  28. Lavaud P, Andre F. Strategies to overcome trastuzumab resistance in HER2-overexpressing breast cancers: focus on new data from clinical trials. BMC Med. 2014;12:132 pubmed publisher
    ..b>Trastuzumab, an anti-HER2 monoclonal antibody, improves outcome in women with early and metastatic breast cancer...
  29. Beck A, Goetsch L, Dumontet C, Corvaia N. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16:315-337 pubmed publisher
    ..After half a century of research, the approvals of brentuximab vedotin (in 2011) and trastuzumab emtansine (in 2013) have paved the way for ongoing clinical trials that are evaluating more than 60 further ADC ..
  30. Kikuchi T, Shimizu H, Akiyama Y, Taniguchi S. In situ delivery and production system of trastuzumab scFv with Bifidobacterium. Biochem Biophys Res Commun. 2017;493:306-312 pubmed publisher
    A monoclonal antibody targeting human epidermal growth factor receptor-2 (HER2), trastuzumab has become a standard treatment for HER2-positive breast cancer...
  31. Nishio K, Sakai K, Togashi Y. [PI3K and mTOR pathway and molecular targeted agents]. Nihon Rinsho. 2015;73:1315-22 pubmed
    ..PIK3CA mutations are the predictive markers for anti-EGFR antibodies, trastuzumab, and lapatinib...
  32. Menderes G, Bonazzoli E, Bellone S, Altwerger G, Black J, Dugan K, et al. Superior in vitro and in vivo activity of trastuzumab-emtansine (T-DM1) in comparison to trastuzumab, pertuzumab and their combination in epithelial ovarian carcinoma with high HER2/neu expression. Gynecol Oncol. 2017;147:145-152 pubmed publisher
    ..The objective of this study was to compare the anti-tumor activity of HER2/neu-targeting monoclonal antibodies, trastuzumab (T), pertuzumab (P), combination of trastuzumab and pertuzumab (T+P) and trastuzumab-emtansine (T-DM1) in EOC ..
  33. Nishimura R, Toh U, Tanaka M, Saimura M, Okumura Y, Saito T, et al. Role of HER2-Related Biomarkers (HER2, p95HER2, HER3, PTEN, and PIK3CA) in the Efficacy of Lapatinib plus Capecitabine in HER2-Positive Advanced Breast Cancer Refractory to Trastuzumab. Oncology. 2017;93:51-61 pubmed publisher
    ..using lapatinib plus capecitabine (LC) and to evaluate the influence of the estrogen receptor (ER) status in trastuzumab-refractory HER2-positive advanced breast cancer. Eighty patients were enrolled in this study...
  34. Rainone P, Riva B, Belloli S, Sudati F, Ripamonti M, Verderio P, et al. Development of 99mTc-radiolabeled nanosilica for targeted detection of HER2-positive breast cancer. Int J Nanomedicine. 2017;12:3447-3461 pubmed publisher
    ..We have developed a 99mTc-radiolabeled nanosilica system, functionalized with a trastuzumab half-chain, able to act as drug carrier and SPECT radiotracer for the identification of HER2-positive breast ..
  35. Gschwantler Kaulich D, Tan Y, Fuchs E, Hudelist G, Köstler W, Reiner A, et al. PTEN expression as a predictor for the response to trastuzumab-based therapy in Her-2 overexpressing metastatic breast cancer. PLoS ONE. 2017;12:e0172911 pubmed publisher
    Even though trastuzumab is an effective therapy in early stage Her-2+ breast cancer, 40-50% of advanced Her-2+ breast cancer patients develop trastuzumab resistance...
  36. Guglin M, Munster P, Fink A, Krischer J. Lisinopril or Coreg CR in reducing cardiotoxicity in women with breast cancer receiving trastuzumab: A rationale and design of a randomized clinical trial. Am Heart J. 2017;188:87-92 pubmed publisher
    b>Trastuzumab (TZB) is an established therapy for HER2-positive breast cancer...
  37. Mendelsohn J, Baselga J. The EGF receptor family as targets for cancer therapy. Oncogene. 2000;19:6550-65 pubmed
    ..Clinical activity with these antibodies has been documented: trastuzumab, a humanized anti-ErbB2 MAb, is active and was recently approved in combination with paclitaxel for the therapy ..
  38. Golay J, Bologna L, André P, Buchegger F, Mach J, Boumsell L, et al. Possible misinterpretation of the mode of action of therapeutic antibodies in vitro: homotypic adhesion and flow cytometry result in artefactual direct cell death. Blood. 2010;116:3372-3; author reply 3373-4 pubmed publisher
  39. Barinoff J, Schmidt M, Schneeweiss A, Schoenegg W, Thill M, Keitel S, et al. Primary metastatic breast cancer in the era of targeted therapy - Prognostic impact and the role of breast tumour surgery. Eur J Cancer. 2017;83:116-124 pubmed publisher
    ..One study investigated trastuzumab therapy for human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer in addition to ..
  40. Gall V, Philips A, Qiao N, Clise Dwyer K, Perakis A, Zhang M, et al. Trastuzumab Increases HER2 Uptake and Cross-Presentation by Dendritic Cells. Cancer Res. 2017;77:5374-5383 pubmed publisher HER2+ breast cancer patients in the adjuvant setting suggest synergy between the vaccines and trastuzumab, the mAb targeting the HER2 protein...
  41. Moore K, Thomas G, Duffy S, Warwick J, Gabe R, Chou P, et al. Therapeutic targeting of integrin ?v?6 in breast cancer. J Natl Cancer Inst. 2014;106: pubmed publisher
    ..97, 95% CI = 1.16 to 3.35, P = .01). Monotherapy with 264RAD or trastuzumab slowed growth of MCF-7/HER2-18 and BT-474 xenografts similarly (P < ...
  42. Burris H, Kurkjian C, Hart L, Pant S, Murphy P, Jones S, et al. TAK-228 (formerly MLN0128), an investigational dual TORC1/2 inhibitor plus paclitaxel, with/without trastuzumab, in patients with advanced solid malignancies. Cancer Chemother Pharmacol. 2017;80:261-273 pubmed publisher
    ..profile, and antitumor activity of investigational oral TORC1/2 inhibitor TAK-228 plus paclitaxel, with/without trastuzumab, in patients with advanced solid malignancies...
  43. Dimasi N, Fleming R, Zhong H, Bezabeh B, Kinneer K, Christie R, et al. Efficient Preparation of Site-Specific Antibody-Drug Conjugates Using Cysteine Insertion. Mol Pharm. 2017;14:1501-1516 pubmed publisher
    ..A selected cysteine-inserted ADC demonstrated potent dose-dependent anti-tumor activity in a xenograph tumor mouse model of human breast adenocarcinoma expressing the oncofetal antigen 5T4. ..
  44. Kalsi R, Feigenberg S, Kwok Y, Tkaczuk K, Mehta M, Chumsri S. Brain metastasis and response to ado-trastuzumab emtansine: a case report and literature review. Clin Breast Cancer. 2015;15:e163-6 pubmed publisher
  45. Tran W, Gangeh M, Sannachi L, Chin L, Watkins E, Bruni S, et al. Predicting breast cancer response to neoadjuvant chemotherapy using pretreatment diffuse optical spectroscopic texture analysis. Br J Cancer. 2017;116:1329-1339 pubmed publisher
    ..0/81.0% and an accuracy of 79.5%. This study demonstrated that the pretreatment DOS texture features can predict breast cancer response to NAC and potentially guide treatments. ..
  46. Ríos Luci C, García Alonso S, Díaz Rodríguez E, Nadal Serrano M, Arribas J, Ocaña A, et al. Resistance to the Antibody-Drug Conjugate T-DM1 Is Based in a Reduction in Lysosomal Proteolytic Activity. Cancer Res. 2017;77:4639-4651 pubmed publisher
    b>Trastuzumab-emtansine (T-DM1) is an antibody-drug conjugate (ADC) that was approved recently to treat HER2+ breast cancers...
  47. Goulet D, Zwolak A, Chiu M, Nath A, Atkins W. Diffusion of Soluble Aggregates of THIOMABs and Bispecific Antibodies in Serum. Biochemistry. 2017;56:2251-2260 pubmed publisher
    ..The results indicate that small aggregates of several IgG platforms are not likely to aggregate with serum components, but nanometer-scale aggregates larger than trimers can interact with the serum in an Ab-dependent manner...
  48. Lambert J, Morris C. Antibody-Drug Conjugates (ADCs) for Personalized Treatment of Solid Tumors: A Review. Adv Ther. 2017;34:1015-1035 pubmed publisher
    ..vedotin in 2011 for treating Hodgkin lymphoma and anaplastic large cell lymphoma, and approval of ado-trastuzumab emtansine in 2013 for treating HER2-positive breast cancer...
  49. Hao S, Tian W, Gao B, Jiang Y, Zhang X, Zhang S, et al. Does dual HER-2 blockade treatment increase the risk of severe toxicities of special interests in breast cancer patients: A meta-analysis of randomized controlled trials. Oncotarget. 2017;8:19923-19933 pubmed publisher
    ..EMBASE, Cochrane library) to identify relevant studies that comparing anti-HER2 monotherapy (lapatinib or trastuzumab or pertuzumab) with dual HER-2 blockade treatment (pertuzumab plus trastuzumab or trastuzumab plus lapatinib) ..
  50. Iorfida M, Dellapasqua S, Bagnardi V, Cardillo A, Rotmensz N, Mastropasqua M, et al. HER2-negative (1+) breast cancer with unfavorable prognostic features: to FISH or not to FISH?. Ann Oncol. 2012;23:1371-2 pubmed publisher
  51. Gligorov J, Ataseven B, Verrill M, De Laurentiis M, Jung K, Azim H, et al. Safety and tolerability of subcutaneous trastuzumab for the adjuvant treatment of human epidermal growth factor receptor 2-positive early breast cancer: SafeHer phase III study's primary analysis of 2573 patients. Eur J Cancer. 2017;82:237-246 pubmed publisher
    To assess the safety and tolerability of adjuvant subcutaneous trastuzumab (Herceptin® SC, H SC), delivered from an H SC Vial via hand-held syringe (Cohort A) or single-use injection device (Cohort B), with or without ..
  52. Wright J. Nanotechnology: Deliver on a promise. Nature. 2014;509:S58-9 pubmed publisher
  53. Kulkarni S, Bill A, Godse N, Khan N, Kass J, Steehler K, et al. TMEM16A/ANO1 suppression improves response to antibody-mediated targeted therapy of EGFR and HER2/ERBB2. Genes Chromosomes Cancer. 2017;56:460-471 pubmed publisher
    ..Cells resistant to trastuzumab, a monoclonal antibody targeting HER2, showed an increase in TMEM16A expression and heightened sensitivity to ..