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Novel brain cancer drug proceeds to the Phase II clinical trial - drugdiscovery.com


Novel brain cancer drug proceeds to the Phase II clinical trial - drugdiscovery.com
The major obstacle for the treatment of malignant brain diseases is the protective blood-brain barrier (BBB), which restricts drug delivery into the central nervous system. To circumvent this issue, a new strategy has been developed called G-Technology which uses pegylated liposomes with glutathione attached to the end of the PEG chains (2B3-101). By the aid of the externally bound glutathione molecules, the liposomes become the substrate of the endogenous glutathione transporter expressed highly on the BBB. The liposomes are loaded with the conventional anticancer agent doxorubicin, the delivery of which into the brain tissue is significantly facilitated upon systemic administration.

In relation to the similar but glutathione-free liposomal formulation of doxorubicin (marketed as Doxil/Caelyx), the drug retention in brain was almost three times higher after repeated administration of 2B3-101 at the same dose suggesting that this chemotherapeutic drug encapsulated in liposomes can improve the treatment of brain cancer. Glutathione pegylated liposomal doxorubicin is in phase I/IIa clinical trials both as single agent and in combination with trastuzumab in patients with solid tumors, brain metastases, or recurrent malignant glioma.

By Ferenc Zsila M.D., Ph.D.

Tags: blood-brain barrier, brain tumor, brain cancer, drug delivery, doxorubicin, G-Technology, liposome - August 21, 2013


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