Halaven® (eribulin) Demonstrates Anti-proliferative Activity in Selected Soft Tissue Sarcoma Cell Lines, New Data Show - Seite 2

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Notes to Editors  

Halaven^® (eribulin)  

Eribulin is the first in the halichondrin class of microtubule dynamics inhibitors with a novel mechanism of action. Structurally eribulin is a simplified and synthetically produced version of halichondrin B, a natural product isolated from the marine sponge Halichondria okadai. Eribulin is believed to work by inhibiting the growth phase of microtubule dynamics which prevents cell division. Eribulin also induces vascular remodelling, suppresses migration and invasion of cancer cells, and reverses the epithelial-to-mesenchymal transition in many cancer cell lines.

Eribulin is currently indicated for the treatment of women with locally advanced or metastatic breast cancer who have progressed after at least one chemotherapeutic regimen for advanced disease. Prior therapy should have included an anthracycline and a taxane in either the adjuvant or metastatic setting, unless patients were not suitable for these treatments.^[6]

About Soft Tissue Sarcomas 

Soft tissue sarcoma is a collective term for a diverse group of malignant tumours. Soft tissue sarcomas are cancers which originate from mesenchymal (connective tissue) cell types - adipocytes and smooth muscle cells.

Unlike other cancers such as non-small cell lung cancer (NSCLC), soft tissue sarcomas are mostly diagnosed with localised disease, and many are amenable to complete surgical removal, yet relapse rates can be as high as 50 percent.^[7] Outcomes for patients with advanced disease are poor, with median survival around one year or less. Due to the rarity of these tumours, evidence for prognostic factors is weak and not well understood.^[8]

Eribulin in soft tissue sarcoma model - study details^[1]

• Anti-proliferation activity of eribulin was examined in 6 human STS cell lines at several doses.
• To analyse the effect of eribulin on morphological change in a test tube, 3 human STS cell lines were treated with eribulin at 1, 3, and 10 nmol/L for 7 days. Gene expression change was analysed.
• For tumour blood perfusion (the process of delivery of nutrients to arterial blood to a capillary bed in the tissue) analysis in SK-LMS-1 xenografts, eribulin was administered at doses of 0.38, 0.75, and 1.5 mg/kg and tumour blood perfusion was calculated 5 days after the administration.
• Eribulin showed anti-proliferation activity in vitro and in vivo against all 6 cell lines in a dose dependent manner. Eribulin showed significant antitumor activity against 4 xenografts (Ewing's sarcoma, leiomyosarcoma, liposarcoma and fibrosarcoma) in a dose dependent manner. Eribulin treatment for 7 days induced apparent morphological change in 3 cell lines. In addition, eribulin significantly enhanced tumour blood perfusion compared to vehicle control 5 days after the administration in leiomyosarcoma xenografts at all doses. Eribulin might cause differentiation of STS cells and remodelling of tumour vasculature to enhance tumour blood perfusion.
• Eribulin showed mitotic effect and non-mitotic effect, which may decrease tumour metastatic potency in STS, as well in breast cancer.

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