Dược Lực Học :
E7389, like its parent natural compound Halichondrin B, is classified as a tubulin depolymerizer, and it shows activity at least equal to the naturally occurring chemical. It acts to disrupt the polymerization of the microtubules necessary in mitosis.2 This general characteristic places E7389 in the group of drugs that includes Vinca alkaloids, dolastatins, cryptophycin, and so forth, but its tubulin interactions appear to be unique, and it was found to have greater activity against lung and breast tumors in animal studies than either the parent halichondrin B or paclitaxel.
Cơ Chế Tác Dụng :
E7389 is being studied in the treatment of cancer. It belongs to the family of drugs called antitubulin agents. It is the synthetic form of Halichondrin B (NSC 609395), a macrocyclic polyether initially isolated from the sponge Halichondria okadai.
E7389 can activate cellular apoptosis pathways under anchorage-independent and -dependent cell culture conditions. Prolonged mitotic blockage by E7389 can lead to apoptotic cell death of human cancer cells in vitro and can provide a mechanistic basis for the significant in vivo anticancer efficacy of E7389.
Chỉ Định :
Investigated for use/treatment in breast cancer, cancer/tumors (unspecified), head and neck cancer, lung cancer, prostate cancer, and sarcoma.