It is intended to provide water-soluble derivative of camptothecins which are excellent in therapeutic effect and suitable for chemotherapy for cancer. Namely, a water-soluble high-molecular weight derivative of camptothencins being excellent in sustained-release which is obtained by ester-bonding a carboxylic acid group of a polyethylene glycol-polycarboxylic acid polymer to a phenolic hydroxyl group of phenolic camptothencins.