Pro-cytotoxic drug conjugates for anticancer therapy

A - Human Necessities – 61 – K

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Details

A61K 47/48 (2006.01) A61K 39/44 (2006.01) C07K 14/48 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2166798

Pro-cytotoxic drug conjugates for anticancer therapy comprising a homing agent first moiety, a spacer molecule second moiety covalently linked to the homing agent, and a third moiety covalently linked to the second moiety consisting of a pro-cytotoxic drug that is non-toxic extracellular but that, after internalization of the conjugate by proliferating tumor cells, is metabolized by one or more endogenous intracellular enzymes to a cytotoxic metabolic product, so that cell growth is arrested or the cells killed. Preferred pro-cytotoxic drugs are carboxyphosphamide or carboxysophosphamide.

Conjugués de médicaments pro-cytotoxiques destinés à la thérapie contre le cancer comprenant une première fraction d'agent de guidage, une deuxième fraction de molécule d'espacement liée par covalence à l'agent de guidage et une troisième fraction liée par covalence à la deuxième fraction, constituée d'un médicament pro-cytotoxique qui est extracellulairement non toxique mais qui, après l'adoption du conjugué par des cellules tumorales proliférantes, est métabolisé par une ou plusieurs enzymes intracellulaires endogènes sous forme d'un produit métabolique cytotoxique, de sorte que la croissance cellulaire est arrêtée ou que les cellules sont tuées. Les médicaments pro-cytotoxiques préférés sont le carboxyphosphamide ou le carboxyisophosphamide.

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