title: Trastuzumab emtansine: the first targeted chemotherapy for treatment of breast cancer.
abstract: Trastuzumab emtansine (T-DM1) is a novel antibody-drug conjugate, comprised of a potent cytotoxic drug connected via a stable linker to the anti-HER2 antibody, trastuzumab, thereby primarily targeting chemotherapy delivery to cells overexpressing the HER2 receptor. A Phase II randomized trial of T-DM1 in the front-line metastatic breast cancer setting revealed promising activity and improved safety compared with standard chemotherapy plus trastuzumab. Subsequently, a Phase III trial in patients with trastuzumab-pretreated metastatic breast cancer showed T-DM1 to be associated with prolonged progression-free and overall survival compared with lapatinib plus capecitabine. T-DM1 represents a major shift in the treatment of patients with breast cancer as it replaces traditional nontargeted chemotherapy with a 'smart' medication that directs the cytotoxic therapy to cancer cells by using a known biomarker.
authors.affiliation: Department of Medicine, Division of Hematology-Oncology, University of California at Los Angeles, CA, USA.
authors.forename: Parvin F
authors.initials: PF
authors.lastname: Peddi
authors.forename: Sara A
authors.initials: SA
authors.lastname: Hurvitz
mesh_terms: D000080044:Ado-Trastuzumab Emtansine; D061067:Antibodies, Monoclonal, Humanized / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D018931:Antineoplastic Agents, Hormonal / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D002986:Clinical Trials as Topic; D005260:Female; D006801:Humans; D008453:Maytansine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000378:metabolism; D000068878:Trastuzumab; D016896:Treatment Outcome
chemical_list: D000080044:Ado-Trastuzumab Emtansine; D061067:Antibodies, Monoclonal, Humanized; D018931:Antineoplastic Agents, Hormonal; D008453:Maytansine; D018719:Erb-b2 Receptor Tyrosine Kinases; D000068878:Trastuzumab; C508053:ERBB2 protein, human