Nippon Kayaku Kabushiki Kaisha

Manami Okazaki

Keiichirou Yamamoto

Keiichiro Yamamoto

Dai Kawamura

The purpose of the present invention is to provide a polymeric compound in which a camptothecin compound and an anti-cancer effect enhancer, particularly a PARP inhibitor, are bound to a single molecule, whereby it becomes possible to reduce the toxicity to normal cells and deliver and release the two components to an affected area with high efficiency to thereby improve the pharmacological efficacy of the two components. Provided is a polymeric compound represented by general formula (1). 

Polymeric compound having camptothecin compound and anti-cancer effect enhancer bound thereto, and use of same

[Problem]To provide a novel polymer derivative of a cytidine metabolic antagonist which allows release of a medicament irrespective of enzymes of the living body and is expected to have high therapeutic effects. [Solution] The polymer derivative of a cytidine metabolic antagonist in which a substituent represented by the general formula (I) or the general formula (II) [wherein Rand Reach independently represent a hydrogen atom or an optionally substituted (C1-C6)alkyl group, Rrepresents a hydrogen atom, an optionally substituted (C1-C40)alkyl group, an optionally substituted (C1-C40)aralkyl group, an optionally substituted aromatic group, an amino acid residue in which the carboxy group is protected, or an optionally substituted sugar residue, CX&#x2014;CY represents CH&#x2014;CH or C&#x2550;C (double bond), and A represents the residue of the cytidine metabolic antagonist except the amino group at the position 4] is bonded to the side-chain carboxy group of a block copolymer of a polyethylene-glycol structural moiety and a polymer having 10 or more carboxy groups.

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Tokyo, Japan

Manami Okazaki