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BioLineRx白血病新药临床前研究数据积极

  1. BioLineRx
  2. BL-8040
  3. CXCR4
  4. 白血病

来源:生物谷 2014-02-17 08:52

2014年2月17日讯 /生物谷BIOON/ --以色列生物医药公司BioLineRx公司最近在Molecular Cancer Therapeutics杂志上披露了其治疗慢性白血病的新药BL-8040的临床前研究数据。在动物学实验和小鼠实验中,BL-8040单独使用和与imatinib联合使用都表现出良好效果。以imatinib为代表的酪氨酸激酶抑制剂是常见的白血病药物,但是很多白血病患者表现出对酪氨酸激酶抑制剂抗性,使得医疗上急切希望有新的白血病药物出现。当BL-8040与低剂量imatinib联合使用时表现出协同作用,对小鼠肿瘤生长抑制率达到95%。BL-8040是一种CXCR4拮抗剂,CXCR4是一种趋化因子受体,高表达时能够导致癌症的发生。BL-8040通过阻断这种受体来促进细胞程序性死亡,从而达到治疗白血病的目的。

BioLineRx公司希望于今年第二季度开始对BL-8040的临床一期研究。(生物谷Bioon.com)

详细英文报道:

Israel's BioLineRx ($BLRX) has unveiled positive preclinical data for its experimental treatment for chronic myeloid leukemia, a progressive blood and bone marrow cancer.

The results, published in Molecular Cancer Therapeutics, found that BioLineRx's investigational therapy BL-8040 was effective on its own and in combination with imatinib at inhibiting human chronic myeloid leukemia cells in culture and on human tumors that were engrafted in mice. According to the findings, BL-8040 treatment induced programmed cell death of tumor cells in vitro and had a synergistic effect with imatinib at low doses.

When combined with low-dose imatinib in mice engrafted with chronic myeloid leukemia tumors, BL-8040 significantly inhibited tumor growth, achieving a 95% suppression. The drug also reversed the protective effect of the bone marrow stroma on leukemia cells, which induced programmed cell death.

Chronic myeloid leukemia is characterized by production of too many white blood cells, which is caused by a constantly producing active oncogenic tyrosine kinase. Tyrosine kinase inhibitors like imatinib mesylate (Gleevec) have revolutionized the treatment of chronic myeloid leukemia and are the go-to drugs for many patients. But some patients have dormant leukemic stem cells that are resistant to tyrosine kinase inhibitors, making them susceptible to leukemia resistance and recurrence and underscoring the need for new drugs to target these stem cells. In these patients, their bone marrow microenvironments protect dormant leukemic stem cells from therapy-induced cell death.

BL-8040 acts as an antagonist for CXCR4, a chemokine receptor directly involved in tumor progression, growth of new blood vessels in the tumor, metastasis and cell survival. CXCR4 is overexpressed in more than 70% of human cancers and is often associated with disease severity.

BioLineRx currently is studying the investigational drug in Phase II clinical trials for acute myeloid leukemia and hopes to begin Phase I trials for BL-8040 for stem cell mobilization in the second quarter of this year.

 

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