NEOCARZINOSTATIN COMPLEXES, A METHOD FOR PRODUCING THE SAME, AND AN ANTITUMOR AGENT CONTAINING SAID COMPLEXES AS AN ACTIVE COMPONENT

摘要

Novel neocarzinostatin complexes represented by the following formula (I): (SMA)n - (NCS) ........ (I) wherein n is an integer of 1-35, NCS represents neocarzinostatin residue, SMA represents a residue of a half esterified styrene-maleic acid copolymer having an average molecular weight of 1,000-10,000 in which the maleic acid portion consists of the following units. (1) maleic acid residue bound to NCS < IMG > (2) maleic acid residue which is free or bound to NCS by non-covalent bonding < IMG > provided that the total amount of the above described maleic acid residues (1) and (2) is from an average content of 0.1 per molecule to 60 mol % of SMA, and (3) half-esterified maleic acid residue < IMG > wherein R is a monohydric alcohol residue or a residue of monohydroxyalkyl ether of di or trihydric alcohol, are produced by reacting neocarzinostatin with a half esterified styrene-maleic anhydride copolymer having an average molecular weight of 1,000-10,000 and maleic anhydride residue of from an average content of 0.1 per molecule to 60 mole % of SMA. These neocarzinostatin complexes have a high affinity to tumor as well as an efficient recovery rate through the lymphatic systems, so that the anticancer agent having these complexes as the active component accumulates preferentially at tumor site and the lymphaties.