Nippon Kayaku Kabushiki Kaisha

Takeshi Onda

Akira Masuda

Keiichirou Yamamoto

Masayuki Kitagawa

Keizou Ishikawa

Kazutoshi Takashio

Ken Yamakawa

Hiroko Mashiba

Chisato Tomiyama

Yasushi Yoneta

Yuichi Akatsu

Ayaka Mochizuki

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

[Problems] To provide a novel taxane derivative which can release the medicinal substance in a bioenzyme-independent manner, is expected to have an effective therapeutic efficacy, and has a water-solubility. [Means for Solving Problems] Disclosed is a polymer conjugate of a taxane, which comprises a polymer having a polyethylene glycol moiety and two or more succinic acid monoamide moieties and a taxane, wherein a carboxylate group in the polymer and an alcoholic hydroxyl group in the taxane are bound to each other via an ester bonding.

Polymer conjugate of taxane

A derivative of a cytidine metabolic antagonist which can exert a high therapeutic effect at a low dose. A polymeric derivative of a cytidine metabolic antagonist which comprises a polymeric compound having a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a cytidine metabolic antagonist, which has such a structure that the carboxyl group in the side chain of the polymeric compound and an amino group in the cytidine metabolic antagonist are bound together to form an amide bond.

Polymeric derivative of cytidine metabolic antagonist

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Kita-ku, Japan

Takeshi Onda