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Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles.
Li, Yuexian; Woo, Jiyeon; Chmielecki, Jessica; Xia, Cindy Q; Liao, Mingxiang; Chuang, Bei-Ching; Yang, Johnny J; Guan, Miao Y; Plesescu, Mihaela; Prakash, Shimoga R.
Afiliación
  • Li Y; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA. Electronic address: yuexianfrank.li@takeda.com.
  • Woo J; Boston University, 881 Commonwealth Avenue, Boston, MA 02215, USA.
  • Chmielecki J; Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
  • Xia CQ; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA.
  • Liao M; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA.
  • Chuang BC; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA.
  • Yang JJ; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA.
  • Guan MY; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA.
  • Plesescu M; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA.
  • Prakash SR; Department of Drug Metabolism and Pharmacokinetics, Takeda Pharmaceuticals International Co., 35 Landsdowne Street, Cambridge, MA 02139, USA.
Bioorg Med Chem Lett ; 26(2): 551-555, 2016 Jan 15.
Article en En | MEDLINE | ID: mdl-26642765
The design, synthesis, in vitro inhibitory potency, and pharmacokinetic (PK) profiles of Ko143 analogs are described. Compared to commonly used Ko143, the new breast cancer resistance protein (BCRP) inhibitor (compound A) showed the same potency and a significantly improved PK profile in rats (lower clearance [1.54L/h/kg] and higher bioavailability [123%]). Ko143 on the other hand suffers from poor bioavailability. Compared to Ko143, compound A would be a useful probe for delineating the role of BCRP during in vivo studies in animals.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dicetopiperazinas / Transportador de Casetes de Unión a ATP, Subfamilia G, Miembro 2 / Compuestos Heterocíclicos de 4 o más Anillos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Reino Unido
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dicetopiperazinas / Transportador de Casetes de Unión a ATP, Subfamilia G, Miembro 2 / Compuestos Heterocíclicos de 4 o más Anillos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Reino Unido