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Halaven eribulin

Yujin Park, Ji-Yeon Son, Byung-Mu Lee, Hyung Sik Kim, Sungpil Yoon
BACKGROUND/AIM: Eribulin mesylate, also called Halaven® (HAL), was recently developed as a microtubule-targeting drug and is used in the clinic for resistant or metastatic cancer. Previously, we showed that P-glycoprotein (P-gp)-overexpressing KBV20C oral cancer cells are highly resistant to HAL compared to sensitive KB cells. This qualitative study was designed to identify specific P-gp inhibitors that increase the sensitivity of highly resistant cancer cells to HAL. MATERIALS AND METHODS: In order to identify functional P-gp inhibitors, HAL-treated KBV20C cells were co-treated with P-gp inhibitors, verapamil, elacridar, cyclosporine A, mitotane, piperine, fumagillin, curcumin, indomethacin, probenecid, sulindac, tesmilifene, and C-4...
August 2017: Anticancer Research
Christy L Osgood, Meredith K Chuk, Marc R Theoret, Lan Huang, Kun He, Leah Her, Patricia Keegan, Richard Pazdur
On January 28, 2016, the FDA approved eribulin (Halaven; Eisai Inc.) for the treatment of patients with unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen. The approval was based on results from a single, randomized, open-label, active-controlled trial (Trial E7389-G000-309) enrolling 452 patients with advanced, locally recurrent or metastatic liposarcoma or leiomyosarcoma. Patients were randomized to eribulin 1.4 mg/m2 intravenously (i.v.) on days 1 and 8 or dacarbazine 850, 1,000, or 1,200 mg/m2 i...
November 1, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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...
2017: Current Topics in Medicinal Chemistry
Noriyuki Koyama, Shigeru Taniguchi, Kotaro Kodama, Osamu Tohyama, Hiroki Hasegawa, Taro Semba
No abstract text is available yet for this article.
2016: Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
Aline Hurtaud, Anne Donnadieu, Laurence Escalup, Paul H Cottu, Sandrine Baffert
BACKGROUND: There is no standard recommendation for metastatic breast cancer treatment (MBC) after two chemotherapy regimens. Eribulin (Halaven® ) has shown a significant improvement in overall survival (OS) in this setting. Its use may however be hampered by its cost, which is up to three times the cost of other standard drugs. We report the clinical outcomes and health care costs of a large series of consecutive MBC patients treated with Eribulin. METHODS: A monocentric retrospective study was conducted at Institut Curie over 1 year (August 2012 to August 2013)...
December 2016: Breast: Official Journal of the European Society of Mastology
Chris Fellner
Elbasvir/grazoprevir (Zepatier) for chronic hepatitis C virus; sumatriptin nasal powder (Onzetra Xsail) for migraine; eribulin mesylate (Halaven), now for liposarcoma; and extended-release amphetamine (Adzenys XR-ODT) for ADHD.
March 2016: P & T: a Peer-reviewed Journal for Formulary Management
T E Jones, G Tremblay, U Majethia, E Saunders, J G Gay Molina, R Gonzalez Balboa, Y Huesca
No abstract text is available yet for this article.
November 2015: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
Leslie Wilson, Manu Lopus, Herbert P Miller, Olga Azarenko, Stephen Riffle, Jennifer A Smith, Mary Ann Jordan
Eribulin mesylate (Halaven) is a microtubule-targeted anticancer drug used to treat patients with metastatic breast cancer who have previously received a taxane and an anthracycline. It binds at the plus ends of microtubules and has been shown to suppress plus end growth selectively. Because the class III β tubulin isotype is associated with resistance to microtubule targeting drugs, we sought to determine how βIII tubulin might mechanistically influence the effects of eribulin on microtubules. We found that while [(3)H]eribulin bound to bovine brain soluble tubulin depleted of βIII tubulin in a manner similar to that of unfractionated tubulin, it bound to plus ends of microtubules that were depleted of βIII-depleted tubulin with a maximal stoichiometry (20 ± 3 molecules per microtubule) higher than that of unfractionated microtubules (9 ± 2 molecules per microtubule)...
October 27, 2015: Biochemistry
Kazato Inanaga, Takashi Fukuyama, Manabu Kubota, Yuki Komatsu, Hiroyuki Chiba, Akio Kayano, Katsuya Tagami
A novel and efficient method for the Cr(II)-mediated desulfonylation of α-sulfonyl ketone by a Cr-ligand-Mn system has been developed during the course of process research on Halaven (eribulin mesylate). This reaction is dramatically accelerated in the presence of an appropriate bipyridyl-type ligand. This system is applicable to reduction of α-sulfur-substituted ketones. In addition, a Cr-Cp2ZrCl2-Mn catalytic system is also applicable to desulfonylation of α-sulfonyl ketone.
June 19, 2015: Organic Letters
Hirofumi Mukai, Toshiaki Saeki, Ken Shimada, Yoichi Naito, Nobuaki Matsubara, Tadashi Nakanishi, Hiroshi Obaishi, Masayuki Namiki, Yasutsuna Sasaki
Eribulin mesylate (Halaven®) is a novel inhibitor of microtubule dynamics that has demonstrated a survival benefit in patients with locally recurrent or metastatic breast cancer who previously received at least two chemotherapeutic regimens including an anthracycline and a taxane. Although trastuzumab is indicated for patients with human epidermal growth factor receptor 2 positive (HER2+) breast cancer, a phase 1 study to evaluate tolerability/safety of eribulin mesylate with trastuzumab has not been conducted...
February 2015: Investigational New Drugs
J Menis, C Twelves
Although metastatic breast cancer remains essentially incurable, many patients previously treated with an anthracycline, taxane, and capecitabine are relatively fit and keen to receive further therapy. Several drugs are used in this setting, but with little evidence of clinically relevant benefit, and none have previously shown improved survival. Eribulin (Halaven®) is a nontaxane tubulin-binding agent with a novel mode of action, and was recently approved by the European Medicines Agency and US Food and Drug Agency as a single agent for patients with heavily pretreated metastatic breast cancer...
August 26, 2011: Breast Cancer: Targets and Therapy
Krystyna M Wozniak, Ying Wu, Mohamed H Farah, Bruce A Littlefield, Kenichi Nomoto, Barbara S Slusher
Eribulin mesylate (E7389, INN:eribulin mesilate Halaven(®)) is a non-taxane microtubule dynamics inhibitor currently in clinical use for advanced breast cancer. Other microtubule-targeting agents for breast cancer, including paclitaxel and ixabepilone, display a common treatment dose-limiting toxicity of peripheral neuropathy (PN). In an earlier study, we found eribulin mesylate had a lower propensity to induce PN in mice than either paclitaxel or ixabepilone. In the current study, we compared additional PN induced by paclitaxel versus eribulin mesylate when administered to mice with preexisting paclitaxel-induced PN...
October 2013: Neurotoxicity Research
Elias Pean, Sigrid Klaar, Eva Gil Berglund, Tomas Salmonson, Jeanett Borregaard, Kenneth F Hofland, Jens Ersbøll, Eric Abadie, Rosa Giuliani, Francesco Pignatti
The European Commission issued on March 17, 2011, a marketing authorization valid throughout the European Union (EU) for eribulin (Halaven; Eisai Limited). The decision was based on the favorable opinion of the Committee for Medicinal Products for Human Use recommending a marketing authorization for the treatment of patients with locally advanced or metastatic breast cancer who have progressed after at least 2 chemotherapeutic regimens for advanced disease. Eribulin mesylate is a structurally simplified synthetic analogue of halichondrin B, which is a natural product isolated from the marine sponge Halichondria okadai (ATC code L01XX41)...
September 1, 2012: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Sarah L Scarpace
BACKGROUND: Eribulin mesylate is a halichondrin B analogue that acts as a nontaxane microtubule dynamics inhibitor. Eribulin was approved in the United States in 2010 for the treatment of metastatic breast cancer for patients who have received at least 2 metastatic breast cancer chemotherapeutic regimens, including an anthracycline and a taxane. Eribulin is administered as a single agent at 1.4 mg/m(2) IV for 2 to 5 minutes on days 1 and 8 of a 21-day cycle. OBJECTIVES: The goals of this article are to review eribulin's medication profile, including pharmacology, pharmacokinetic properties, efficacy, and tolerability...
July 2012: Clinical Therapeutics
Jessica N Preston, Meghana V Trivedi
OBJECTIVE: To review the chemistry, pharmacology, pharmacokinetics, safety, and efficacy of eribulin (Halaven). DATA SOURCES: A literature search (up to December 2011) using the terms eribulin, Halaven, ER-086526, and E7389 was performed with PubMed, Google Scholar, selected Ovid bibliography searches, and the abstract search tool from the American Society of Clinical Oncology Annual Meetings and the San Antonio Breast Cancer Symposia. Additional references from the bibliographies of these articles were also assessed...
June 2012: Annals of Pharmacotherapy
Murray J Towle, Kenichi Nomoto, Makoto Asano, Yoshito Kishi, Melvin J Yu, Bruce A Littlefield
BACKGROUND: Eribulin is a pharmaceutically and structurally optimized analog of the marine sponge natural product halichondrin B. Its salt form, eribulin mesylate (Halaven®) is clinically used in the United States, the European Union, and Japan for the treatment of heavily pretreated patients with metastatic breast cancer, who previously received an anthracycline and a taxane. Early preclinical studies of this new inhibitor of microtubule dynamics showed high antitumor potency towards several human cancer types in vitro and in vivo...
May 2012: Anticancer Research
Martha Donoghue, Steven J Lemery, Weishi Yuan, Kun He, Rajeshwari Sridhara, Stacy Shord, Hong Zhao, Anshu Marathe, Lori Kotch, Josephine Jee, Ying Wang, Liang Zhou, William M Adams, Vaishali Jarral, Anne Pilaro, Richard Lostritto, Joseph E Gootenberg, Patricia Keegan, Richard Pazdur
This work describes the considerations that led to the approval by the U.S. Food and Drug Administration (FDA), on November 15, 2010, of eribulin mesylate (Halaven; Eisai, Inc.) for the treatment of patients with refractory metastatic breast cancer. The FDA review focused primarily on the results of a single randomized, open-label, multicenter trial of 762 patients with refractory locally advanced or metastatic breast cancer. The patients were randomized to receive eribulin or any single-agent treatment of the physician's choice, selected prior to randomization...
March 15, 2012: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
Candida Nastrucci, Alfredo Cesario, Patrizia Russo
Discovery, isolation, biochemical/pharmacological characterization, pre-clinical and clinical trials of drugs derived from the marine environment are continuously developing and increasing. One of the most promising area is cancer therapy. Currently, there are two drugs approved by the Food and Drug Administration (FDA) and European Agency for the Evaluation of Medicinal Products (EMA) in cancer treatment, namely Cytarabine (Cytosar-U1®) and Eribulin (E7389 or Halaven®). Trabectedin (ET-743 or Yondelis1®), approved by EMA, is completing key Phase III studies in the U...
May 1, 2012: Recent Patents on Anti-cancer Drug Discovery
Noriyuki Koyama, Takeshi Tokunaga, Wakana Ogasawara, Miyuki Murakami, Yuji Yamashita
No abstract text is available yet for this article.
November 2011: Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica
Toru Mukohara, Shunji Nagai, Hirofumi Mukai, Masayuki Namiki, Hironobu Minami
Eribulin mesylate (Halaven™, E7389) is a synthetic analog of the marine natural product halichondrin B that acts via a mechanism distinct from conventional tubulin-targeted agents. This Phase I study ( identifier: NCT00326950) was the first to investigate eribulin mesylate in Japanese patients. The study determined the recommended dose, MTD, DLTs, safety, pharmacokinetics, and antitumor activity of eribulin administered on Days 1 and 8 of a 21-day cycle in Japanese patients with advanced solid tumors...
October 2012: Investigational New Drugs
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