Nippon Kayaku Kabushiki Kaisha

Ken Yamakawa

Tsuyoshi Fukuda

Masaharu Nakamura

Akira Masuda

Takuya Kato

Keiichirou Yamamoto

Takeshi Onda

Ayaka Mochizuki

Chisato Tomiyama

Yasushi Yoneta

Yuichi Akatsu

According to the present invention, there is a demand for novel platinum(IV) complex which has sufficient water-solubility, stability, antitumor activity, and the like that are required as a medicine, and may be used clinically. Thus, provided is a platinum(IV) complex represented by the following General Formula (I) [wherein Xand Xeach represent a halogen atom or are bonded together to form a dicarboxylate selected from the group consisting of oxalate, malonate, succinate, and o-phthalate; and Y represents a halogen atom. 

Platinum (IV) complex

A DDS preparation of a platinum complex, which exhibits a superior antitumor effect required as a medicine and reduced side effects, that is, a clinically usable DDS preparation of a platinum complex, which is conjugated to a polymer carrier that is different from conventional carriers, is desired. Provided is a polymer conjugate of a platinum(II) complex, the polymer conjugate including: a block copolymer having a polyethylene glycol structural moiety and a polyaspartic acid moiety or a polyglutamic acid moiety; a sulfoxide derivative introduced into a side-chain carboxyl group of the block copolymer; and a platinum(II) complex coordinate-bonded to a sulfoxide group of the sulfoxide derivative.

Polymer conjugate of sulfoxide derivative-coordinated platinum(II) complex

A physiologically active substance-conjugated block copolymer having enhanced efficacy and/or safety is provided by enhancing the property of penetrating into a target diseased tissue and/or enhancing excretability, compared to known physiologically active substance-conjugated block copolymer, and suppressing sensitization of the physiologically active substance to normal tissues other than a target diseased tissue. Disclosed is a block copolymer including a polyethylene glycol segment connected with a polyamino acid derivative segment conjugated with a physiologically active substance, in which the molecular weight of the block copolymer is from 2 kilodaltons to 15 kilodaltons, and the light scattering intensity of a 1 mg/mL aqueous solution of the physiologically active substance-conjugated block copolymer as measured with a laser light scattering photometer is at least twice or more the light scattering intensity of toluene.

Block copolymer conjugate of physiologically active substance

Growing community of inventors

Tokyo, Japan

Ken Yamakawa