BACKGROUND: Eribulin mesilate (eribulin), a first-in-class halichondrin B-based microtubule dynamics inhibitor, has been shown to promote vascular remodeling and reversal of epithelial-mesenchymal transition (EMT) apart from its antimitotic activity in breast cancer models. MATERIALS AND METHODS: Anti-proliferative activity of eribulin was examined in vitro and in vivo in several human soft tissue sarcoma (STS) cell lines. To assess tumor blood perfusion and phenotypic changes, eribulin was investigated in a leiomyosarcoma xenograft and in vitro in liposarcoma and leiomyosarcoma cell lines. RESULTS: Eribulin showed anti-proliferative activity in vitro against all six cell lines investigated, with 50% inhibitory concentration values of around 1 nmol/l, as well as significant antitumor activity against four xenografts in vivo. In addition, eribulin significantly enhanced tumor blood perfusion in xenografts and induced morphological changes and up-regulation of differentiation marker genes. CONCLUSION: In pre-clinical models, eribulin showed anti-proliferative activity against a variety of histopathological subtypes of STS. Eribulin might also cause tumor vasculature remodeling to enhance tumor blood perfusion and induce tumor cell differentiation. Copyright
BACKGROUND:Eribulin mesilate (eribulin), a first-in-class halichondrin B-based microtubule dynamics inhibitor, has been shown to promote vascular remodeling and reversal of epithelial-mesenchymal transition (EMT) apart from its antimitotic activity in breast cancer models. MATERIALS AND METHODS: Anti-proliferative activity of eribulin was examined in vitro and in vivo in several humansoft tissue sarcoma (STS) cell lines. To assess tumor blood perfusion and phenotypic changes, eribulin was investigated in a leiomyosarcoma xenograft and in vitro in liposarcoma and leiomyosarcoma cell lines. RESULTS:Eribulin showed anti-proliferative activity in vitro against all six cell lines investigated, with 50% inhibitory concentration values of around 1 nmol/l, as well as significant antitumor activity against four xenografts in vivo. In addition, eribulin significantly enhanced tumor blood perfusion in xenografts and induced morphological changes and up-regulation of differentiation marker genes. CONCLUSION: In pre-clinical models, eribulin showed anti-proliferative activity against a variety of histopathological subtypes of STS. Eribulin might also cause tumor vasculature remodeling to enhance tumor blood perfusion and induce tumor cell differentiation. Copyright
Authors: Andrew J Robles; Raushan T Kurmasheva; Abhik Bandyopadhyay; Doris A Phelps; Stephen W Erickson; Zhao Lai; Dias Kurmashev; Yidong Chen; Malcom A Smith; Peter J Houghton Journal: Clin Cancer Res Date: 2020-03-17 Impact factor: 12.531
Authors: Eric S Schafer; Rachel E Rau; Stacey Berg; Xiaowei Liu; Charles G Minard; David D'Adamo; Rachael Scott; Larisa Reyderman; Gresel Martinez; Sandhya Devarajan; Joel M Reid; Elizabeth Fox; Brenda J Weigel; Susan M Blaney Journal: Pediatr Blood Cancer Date: 2018-05-02 Impact factor: 3.167
Authors: Panagiotis Koliou; Vasilios Karavasilis; Maria Theochari; Seth M Pollack; Robin L Jones; Khin Thway Journal: Cancer Manag Res Date: 2018-02-01 Impact factor: 3.989
Authors: Michiko Sugawara; Krista Condon; Earvin Liang; Christopher DesJardins; Edgar Schuck; Kazutomi Kusano; W George Lai Journal: Cancer Chemother Pharmacol Date: 2017-06-29 Impact factor: 3.333