Antineoplastic conjugates of transferrin, albumin and polyethylene glycol

Method for the treatment of a cancer disease, wherein said cancer disease comprises bladder, lung, mamma, melanoma or prostrate carcinomas, comprising the step of treating an organism having said cancer disease with a conjugate of a cytostatic compound and transferrin or albumin or a polyethylene glycol, wherein:

• (a) said cytostatic compound is coupled via a spacer comprising a group which is derived from a maleinimido group, to thiolated transferrin or thiolated albumin or to polyethylene glycol having at least one HS or H2N group;
• or
• (b) 2 to 30 equivalents of said cytostatic compound are each coupled via a spacer comprising a group which is derived from a maleinimido group, to thiolated albumin, wherein the thiolated albumin is conjugated via a group which is derived from a bismaleinimido compound to transferrin or a monoclonal antibody which is directed to a tumor associated antigen;
• wherein said thiolated transferrin or said thiolated albumin has 1 to 30 HS groups on the average, and said polyethylene glycol has a mass of about between 5,000 and 200,000 Da, and
• wherein said group which is derived from a bismaleinimido compound is formed through conjugating said thiolated albumin, which is coupled to 2 to 30 equivalents of said cytostatic compounds, with a bismaleinimide compound of tie formula XI:
• wherein Z=—CO—NH—(CH2)n—NH—CO—, —CO—O—(CH2)n—O—CO—, —CH═N—(CH2)n—N═CH—, —CH═N—NH—(CH2)n—NH—N═CH— or —CH═N—NH—CO—(CH2)n—CO—NH—N═CH— and n=2-12, and wherein R is an aliphatic carbon chain having 1-6 carbon atoms or a substituted or unsubstituted benzyl group or a substituted or unsubstituted phenylene group.