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https://www.readbyqxmd.com/read/28133215/-long-term-survival-of-a-patient-with-stage-iv-breast-cancer-and-an-intrathoracic-space-occupying-metastatic-lesion
#1
Toshimori Koh, Tomohito Sakai, Shunji Kato, Shoji Hirajima, Minoru Nishio, Koji Soga, Atsushi Oguro, Noboru Nakagawa
A 50-year old woman noticed left axillary lymph node swelling and presented at our hospital. CNB showed adenocarcinoma( pap-tub, ER+, PgR+, HER2 3+). CT revealed a right lung metastatic nodule and swollen lymph nodes above the left collarbone and left axilla. However, no breast tumor was found at that time. We diagnosed occult breast cancer, TxN3bM1 (lung), Stage IV . FEC(100), paclitaxel, letrozole, anastrozole, exemestane plus trastuzumab, tegafur/uracil plus trastuzumab, and lapatinib plus capecitabine were sequentially administered...
November 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/28131055/lc-ms-ms-method-for-the-simultaneous-determination-of-lys-mcc-dm1-mcc-dm1-and-dm1-as-potential-intracellular-catabolites-of-the-antibody-drug-conjugate-trastuzumab-emtansine-t-dm1
#2
Yazhong Liu, Fang Zhou, Hua Sang, Hui Ye, Qianying Chen, Lan Yao, Ping Ni, Guangji Wang, Jingwei Zhang
Lysine-MCC-DM1, MCC-DM1 and DM1 are potential catabolites of trastuzumab emtansine (T-DM1). A convenient liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated to detect these catabolites simultaneously in in vitro investigations for the first time. Protein precipitation was utilized to prepare the samples. Chromatographic separation was achieved on a Phenomenex Kinetex C18 column (100×2.1mm, 2.6μm) with mobile-phase gradient elution. The calibration curves of each analyte ranging from 1 to 100nM showed good linearity (r(2)>0...
January 12, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28119394/use-and-outcomes-of-targeted-therapies-in-early-and-metastatic-her2-positive-breast-cancer-in-australia-protocol-detailing-observations-in-a-whole-of-population-cohort
#3
Benjamin Daniels, Sarah J Lord, Belinda E Kiely, Nehmat Houssami, Philip Haywood, Christine Y Lu, Robyn L Ward, Sallie-Anne Pearson
BACKGROUND: The management of human epidermal growth factor receptor 2 (HER2)-positive breast cancer (BC) has changed dramatically with the introduction and widespread use of HER2-targeted therapies. However, there is relatively limited real-world information on patterns of use, effectiveness and safety in whole of population cohorts. The research programme detailed in this protocol will generate evidence on the prescribing patterns, safety monitoring and outcomes of patients with BC treated with HER2-targeted therapies in Australia...
January 24, 2017: BMJ Open
https://www.readbyqxmd.com/read/28110417/splenic-enlargement-and-bone-marrow-hyperplasia-in-patients-receiving-trastuzumab-emtansine-for-metastatic-breast-cancer
#4
Michael Kosmin, Andreas Makris, Noorulhuda Jawad, David Woolf, David Miles, Anwar R Padhani
BACKGROUND: An association between trastuzumab-emtansine (T-DM1) and splenic enlargement is reported in preclinical data, and has been noted anecdotally in patients receiving T-DM1 at our institution. Use of whole-body MRI examinations (WB-MRI) allows for detailed bone marrow assessment and semi-automated splenic volume calculations. OBJECTIVE: To retrospectively evaluate changes in splenic volume versus evidence of bone marrow hyperplasia and/or changes in portal venous pressure in patients receiving T-DM1 for metastatic breast cancer...
January 21, 2017: Targeted Oncology
https://www.readbyqxmd.com/read/28108597/bispecific-antibodies-and-antibody-drug-conjugates-adcs-bridging-her2-and-prolactin-receptor-improve-efficacy-of-her2-adcs
#5
Julian Andreev, Nithya Thambi, Andres E Perez Bay, Frank J Delfino, Joel H Martin, Marcus P Kelly, Jessica R Kirshner, Ashique Rafique, Arthur Kunz, Thomas Nittoli, Douglas MacDonald, Christopher Daly, William Olson, Gavin Thurston
The properties of cell surface proteins targeted by Antibody-drug conjugates (ADCs) have not been fully exploited; of particular importance are the rate of internalization and the route of intracellular trafficking. In this study we compared the trafficking of HER2, which is the target of the clinically approved ADC ado-trastuzumab emtansine (T-DM1), with that of prolactin receptor (PRLR), another potential target in breast cancer. In contrast to HER2, we found that PRLR is rapidly and constitutively internalized, and traffics efficiently to lysosomes, where it is degraded...
January 20, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28091366/trastuzumab-emtansine-and-cost-based-decision-making
#6
EDITORIAL
The Lancet
No abstract text is available yet for this article.
7, 2017: Lancet
https://www.readbyqxmd.com/read/28062707/optimization-of-a-pegylated-glucuronide-monomethylauristatin-e-linker-for-antibody-drug-conjugates
#7
Patrick J Burke, Joseph Z Hamilton, Scott C Jeffrey, Joshua H Hunter, Svetlana O Doronina, Nicole M Okeley, Jamie B Miyamoto, Martha E Anderson, Ivan J Stone, Michelle L Ulrich, Jessica K Simmons, Erica E McKinney, Peter D Senter, Robert P Lyon
The emergence of antibody-drug conjugates (ADC), such as brentuximab vedotin and ado-trastuzumab emtansine, has led to increased efforts to identify new payloads and develop improved drug-linker technologies. Most antibody payloads impart significant hydrophobicity to the ADC, resulting in accelerated plasma clearance and suboptimal in vivo activity, particularly for conjugates with high drug-to-antibody ratios (DAR). We recently reported on the incorporation of a discrete PEG24 polymer as a side chain in a β-glucuronidase-cleavable monomethylauristatin E (MMAE) linker to provide homogeneous DAR 8 conjugates with decreased plasma clearance and increased antitumor activity in xenograft models relative to a non-PEGylated control...
January 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28056739/from-natural-products-to-designer-drugs-development-and-molecular-mechanisms-of-action-of-novel-anti-microtubule-breast-cancer-therapeutics
#8
Tejashree Mahaddalkar, Manu Lopus
Microtubule-targeted drugs (MTDs) have been on the forefront of breast cancer chemotherapy. Classic MTDs, such as paclitaxel and their semisynthetic derivatives, have achieved considerable success in the clinical management of breast neoplasms. In order to improve the specificity and to reduce undesirable, dose-limiting toxicities of these drugs, a plethora of novel compounds are being synthesized and investigated in laboratories worldwide. Due to their crucial roles during cell division, and to the fact that the suppression of their innate 'dynamic instability' can arrest cell cycle progression, microtubules formed an attractive target for cancer chemotherapy...
4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056202/trastuzumab-emtansine-with-or-without-pertuzumab-versus-trastuzumab-plus-taxane-for-human-epidermal-growth-factor-receptor-2-positive-advanced-breast-cancer-primary-results-from-the-phase-iii-marianne-study
#9
Edith A Perez, Carlos Barrios, Wolfgang Eiermann, Masakazu Toi, Young-Hyuck Im, Pierfranco Conte, Miguel Martin, Tadeusz Pienkowski, Xavier Pivot, Howard Burris, Jennifer A Petersen, Sven Stanzel, Alexander Strasak, Monika Patre, Paul Ellis
Purpose Trastuzumab and pertuzumab are human epidermal growth factor receptor 2 (HER2) -targeted monoclonal antibodies, and trastuzumab emtansine (T-DM1) is an antibody-drug conjugate that combines the properties of trastuzumab with the cytotoxic activity of DM1. T-DM1 demonstrated encouraging efficacy and safety in a phase II study of patients with previously untreated HER2-positive metastatic breast cancer. Combination T-DM1 and pertuzumab showed synergistic activity in cell culture models and had an acceptable safety profile in a phase Ib and II study...
January 10, 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28018954/regression-of-metastatic-radiation-chemotherapy-resistant-uterine-serous-carcinoma-overexpressing-her2-neu-with-trastuzumab-emtansine-tdm-1
#10
Alessandro D Santin, Stefania Bellone, Natalia Buza, Peter E Schwartz
BACKGROUND: The management of uterine-serous-carcinoma (USC) no longer amenable to treatment with surgery, radiation and/or chemotherapy remains dismal. Alternative therapeutic options are desperately needed. CASE: We describe the case of a heavily pretreated 74-year-old patient with a recurrent USC overexpressing HER2/neu at 3 + level by IHC treated with the anti-HER2/neu antibody-drug-conjugate (ADC) trastuzumab-emtansine (TDM-1-Kadcyla-Genentech/Roche). She experienced a remarkable clinical response to TDM-1 with a complete resolution of a large metastatic, radiation/chemotherapy resistant tumor deposit in her abdominal wall muscle confirmed by multiple CAT scans and a prolonged systemic control of her disease...
February 2017: Gynecologic Oncology Reports
https://www.readbyqxmd.com/read/27999336/debouganin-diabody-fusion-protein-overcomes-drug-resistance-to-adcs-comprised-of-anti-microtubule-agents
#11
Shilpa Chooniedass, Rachelle L Dillon, Arjune Premsukh, Peter J Hudson, Gregory P Adams, Glen C MacDonald, Jeannick Cizeau
Antibody drug conjugates (ADC), comprised of highly potent small molecule payloads chemically conjugated to a full-length antibody, represent a growing class of therapeutic agents. The targeting of cytotoxic payloads via the specificity and selectivity of the antibody has led to substantial clinical benefits. However, ADC potency can be altered by mechanisms of resistance such as overexpression of efflux pumps or anti-apoptotic proteins. DeBouganin is a de-immunized variant of bouganin, a ribosome-inactivating protein (RIP) that blocks protein synthesis, thereby leading to apoptosis...
December 17, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27995530/a-phase-i-pharmacokinetic-study-of-trastuzumab-emtansine-t-dm1-in-patients-with-human-epidermal-growth-factor-receptor-2-positive-metastatic-breast-cancer-and-normal-or-reduced-hepatic-function
#12
Chunze Li, Priya Agarwal, Ekaterina Gibiansky, Jin Yan Jin, Susan Dent, Anthony Gonçalves, Ihsan Nijem, Alexander Strasak, Marie-Laurence Harle-Yge, Nataliya Chernyukhin, Pat LoRusso, Sandhya Girish
OBJECTIVE: The aim of this study was to evaluate the pharmacokinetics (PK) of trastuzumab emtansine (T-DM1) and relevant analytes in patients with human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer and hepatic impairment. METHODS: Patients were enrolled in three independent parallel cohorts based on hepatic function per Child-Pugh criteria: normal hepatic function, mild hepatic impairment, and moderate hepatic impairment. Patients received T-DM1 3...
December 19, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27872093/a-novel-platinum-ii-based-bifunctional-adc-linker-benchmarked-using-89zr-desferal-and-auristatin-f-conjugated-trastuzumab
#13
Niels J Sijbrandi, Eugen Merkul, Joey A Muns, Dennis C J Waalboer, Kevin Adamzek, Marije Bolijn, Veronica Montserrat, Govert W Somsen, Rob Haselberg, Paul J G M Steverink, Hendrik-Jan Houthoff, Guus A M S van Dongen
Greater control is desirable in the stochastic conjugation technology used to synthesize antibody-drug conjugates (ADC). We have shown recently that a fluorescent dye can be stably conjugated to a mAb using a bifunctional platinum(II) linker. Here, we describe the general applicability of this novel linker technology for the preparation of stable and efficacious ADCs. The ethylenediamine platinum(II) moiety, herein called Lx, was coordinated to Desferal (DFO) or auristatin F (AF) to provide storable "semifinal" products, which were directly conjugated to unmodified mAbs...
January 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/27866859/trastuzumab-emtansine-for-her2-positive-breast-cancer
#14
Priya Venkatesan
No abstract text is available yet for this article.
December 2016: Lancet Oncology
https://www.readbyqxmd.com/read/27843957/whether-her2-positive-non-breast-cancers-are-candidates-for-treatment-with-ado-trastuzumab-emtansine
#15
REVIEW
Azadeh Moghaddas, Ali Borhani
The National Comprehensive Cancer Network (NCCN) has recommended Ado-trastuzumab emtansine (T-DM1) as a preferred agent for patients with human epidermal growth factor receptor-2 (HER2)-positive metastatic breast cancer and prior trastuzumab therapy. Overexpression of HER2 was reported in other cancer types such as bladder, gastric and urogenital carcinosarcomas similar to what is discovered in breast cancer. Some preclinical studies demonstrated the potential anti-tumor effects of T-DM1 in HER2-positive non-breast cancers...
October 2016: Journal of Research in Pharmacy Practice
https://www.readbyqxmd.com/read/27781258/-research-status-quo-and-progression-in-targeted-therapy-for-advanced-gastric-cancer
#16
Rui Feng, Xiaotian Zhang, Sheng Yang
With the deeper research of the proliferation, invasion and metastasis mechanisms of the gastric cancer, targeted therapy has become a hot spot in this field. The exploration of targeted agents for gastric cancer is mainly concentrated upon the drugs that target human epidermal growth factor receptor (HER) family, the vascular endothelial growth factor (VEGF), the phosphatidylinositol 3-kinase-protein kinase/mammalian target of rapamycin (PI3K/mTOR) and the NF-κB signaling pathways. The targeted drugs relevant to HER family include the Cetuximab, Nimotuzumab, Matuzumab, Panitumumab and Erlotinib which are aimed at HER-1, the Trastuzumab, Pertuzumab and T-DM1 (trastuzumab emtansine) which are aimed at HER-2, and the Lapatinib and Afatinib which are the multi-target agents of HER...
October 25, 2016: Zhonghua Wei Chang Wai Ke za Zhi, Chinese Journal of Gastrointestinal Surgery
https://www.readbyqxmd.com/read/27768588/heregulin-expressing-her2-positive-breast-and-gastric-cancer-exhibited-heterogeneous-susceptibility-to-the-anti-her2-agents-lapatinib-trastuzumab-and-t-dm1
#17
Yoshikane Nonagase, Kimio Yonesaka, Hisato Kawakami, Satomi Watanabe, Koji Haratani, Takayuki Takahama, Naoki Takegawa, Hiroto Ueda, Junko Tanizaki, Hidetoshi Hayashi, Takeshi Yoshida, Masayuki Takeda, Yasutaka Chiba, Takao Tamura, Kazuhiko Nakagawa, Junji Tsurutani
BACKGROUND: Overexpression of heregulin, a HER3 ligand, is one mechanism that confers resistance to the anti-HER2 agents trastuzumab and lapatinib. We investigated the impact of heregulin expression on the efficacy of HER2-targeted therapeutic agents, including trastuzumab, trastuzumab emtansine (T-DM1) and lapatinib, in vitro and in vivo and evaluated the heregulin messenger RNA (mRNA) levels in specimens from patients with HER2-positive breast or gastric cancer. RESULTS: Cell proliferation and apoptosis assays demonstrated that heregulin conferred robust resistance to lapatinib and trastuzumab via HER3-Akt pathway activation followed by survivin overexpression; however, heregulin conferred minimal or no resistance to T-DM1 and paclitaxel...
October 19, 2016: Oncotarget
https://www.readbyqxmd.com/read/27723970/glutathione-sensitive-hyaluronic-acid-ss-mertansine-prodrug-with-a-high-drug-content-facile-synthesis-and-targeted-breast-tumor-therapy
#18
Ping Zhong, Jian Zhang, Chao Deng, Ru Cheng, Fenghua Meng, Zhiyuan Zhong
Low tolerability and tumor selectivity restricts many potent anticancer drugs including mertansine from wide clinical use. Here, glutathione-activatable hyaluronic acid-SS-mertansine prodrug (HA-SS-DM1) was designed and developed to achieve enhanced tolerability and targeted therapy of CD44+ human breast tumor xenografts. DM1 was readily conjugated to HA using 2-(2-pyridyldithio)-ethylamine as a linker. Notably, HA-SS-DM1 with a high DM1 content of 20 wt % had a mean size of ∼170 nm at concentrations above 0...
November 14, 2016: Biomacromolecules
https://www.readbyqxmd.com/read/27699747/-new-hope-for-her2-positive-metastatic-breast-cancer-treatment-trastuzumab-emtansine-t-dm1-from-the-perspective-of-nursing-care
#19
Hsiao-Hsuan Kuo, Wei-Wu Chen
Human epidermal growth factor receptor (HER2)-positive breast cancer is associated with a more aggressive disease and poor prognosis. The development of trastuzumab, a HER2-targeted agent, has changed the paradigm of HER2-positive breast cancer treatment and improved survival rates dramatically. However, metastatic HER2-positive breast cancer patients eventually develop resistance to this treatment regimen eventually. A new anti-HER2 antibody-drug conjugate, Trastuzumab emtansine (T-DM1), has been shown to improve treatment efficacy...
October 2016: Hu Li za Zhi the Journal of Nursing
https://www.readbyqxmd.com/read/27698471/anti-tubulin-drugs-conjugated-to-anti-erbb-antibodies-selectively-radiosensitize
#20
Stephen R Adams, Howard C Yang, Elamprakash N Savariar, Joe Aguilera, Jessica L Crisp, Karra A Jones, Michael A Whitney, Scott M Lippman, Ezra E W Cohen, Roger Y Tsien, Sunil J Advani
Tumour resistance to radiotherapy remains a barrier to improving cancer patient outcomes. To overcome radioresistance, certain drugs have been found to sensitize cells to ionizing radiation (IR). In theory, more potent radiosensitizing drugs should increase tumour kill and improve patient outcomes. In practice, clinical utility of potent radiosensitizing drugs is curtailed by off-target side effects. Here we report potent anti-tubulin drugs conjugated to anti-ErbB antibodies selectively radiosensitize to tumours based on surface receptor expression...
October 4, 2016: Nature Communications
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