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Antitumor efficacy and biodistribution of liposomal sepantronium bromide (YM155), a novel small-molecule survivin suppressant.
Kawano, Hiroki; Shakushiro, Kohsuke; Nakata, Mari; Kita, Aya; Maeda, Atsushi; Watanabe, Shunsuke; Sako, Kazuhiro; Oku, Naoto.
Afiliación
  • Kawano H; Pharmaceutical Research and Technology Labs., Technology, Astellas Pharma Inc., Yaizu-shi, Japan; Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Japan. Electronic address: hiroki.kawano@astellas.com.
  • Shakushiro K; Pharmaceutical Research and Technology Labs., Technology, Astellas Pharma Inc., Yaizu-shi, Japan; Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Japan.
  • Nakata M; Drug Discovery Research, Astellas Pharma Inc., Tsukuba-shi, Japan.
  • Kita A; Drug Discovery Research, Astellas Pharma Inc., Tsukuba-shi, Japan.
  • Maeda A; Pharmaceutical Research and Technology Labs., Technology, Astellas Pharma Inc., Yaizu-shi, Japan.
  • Watanabe S; Pharmaceutical Research and Technology Labs., Technology, Astellas Pharma Inc., Yaizu-shi, Japan.
  • Sako K; Pharmaceutical Research and Technology Labs., Technology, Astellas Pharma Inc., Yaizu-shi, Japan.
  • Oku N; Department of Medical Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Japan.
Eur J Pharm Biopharm ; 88(1): 283-9, 2014 Sep.
Article en En | MEDLINE | ID: mdl-24993306
Sepantronium bromide (YM155) exhibits time-dependent antitumor activity, although the plasma half-life of YM155 after a bolus intravenous (i.v.) administration is very short. Therefore, greater antitumor efficacy is obtained by continuous infusion than by bolus i.v. administration. In the present study, we attempted to liposomalize YM155 to obtain a longer circulation time than that achieved by bolus i.v. administration and yet retain sufficient antitumor activity. Encapsulation of YM155 in polyethylene glycol-coated liposomes extended the half-life of the drug, and high tumor accumulation of the drug was observed. Bolus i.v. administration of liposomal YM155 by a weekly administration regimen showed antitumor activity comparable to that obtained by the continuous infusion without severe toxicity in a murine xenograft model. Therefore, this liposomal formulation can be a new dosage form of YM155 that achieves sufficient efficacy and safety and is a more convenient administration regimen for users. It should be noted that liposomal YM155 showed unexpectedly high accumulation in the kidneys. This is a specific finding for liposomal YM155, offering important information for the consideration of the potential toxicity of liposomal YM155.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Represoras / Naftoquinonas / Proteínas Inhibidoras de la Apoptosis / Imidazoles / Antineoplásicos Tipo de estudio: Prognostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Eur J Pharm Biopharm Asunto de la revista: FARMACIA / FARMACOLOGIA Año: 2014 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Represoras / Naftoquinonas / Proteínas Inhibidoras de la Apoptosis / Imidazoles / Antineoplásicos Tipo de estudio: Prognostic_studies Límite: Animals / Humans / Male Idioma: En Revista: Eur J Pharm Biopharm Asunto de la revista: FARMACIA / FARMACOLOGIA Año: 2014 Tipo del documento: Article Pais de publicación: Países Bajos