公开(公告)号：EP1922061B1

公开(公告)日：2008-12-17

申请号：EP06761981.7

申请日：2006-06-07

申请人： ZIOPHARM ONCOLOGY, INC.

发明人： ROESSLER, Berthold ,  RAAB, Gerhard ,  REISSMANN, Thomas

IPC分类号： A61K9/16 ,  A61K31/4439

CPC分类号： A61K9/1623 ,  A61K9/1652 ,  A61K31/4439 ,  Y02A50/465

摘要： The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable microtubule polymerization inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of Indibulin for oral administration comprising a granulate containing micronized Indibulin having a particle size of less than 20 mum for at least 99% of the volume of particles, at least one hydrophilic surfactant, and at least one capsulation excipient. The present invention also discloses a method of treating hyperproliferative disorders, malignancies and neoplasms with Indibulin.

摘要翻译： 本发明涉及用于口服给药难溶性且因此难以生物利用的微管蛋白抑制剂Indibulin的药物制剂及其制造方法。 具体而言，提供了用于口服给药的吲地布林药物制剂，其包含含有对于至少99体积％的颗粒具有小于20μm的粒度的微粉化吲地布林的颗粒，至少一种亲水性表面活性剂和一种 更多的包装赋形剂。

公开(公告)号：EP1922061B8

公开(公告)日：2010-09-08

申请号：EP06761981.7

申请日：2006-06-07

申请人： ZIOPHARM ONCOLOGY, INC.

发明人： ROESSLER, Berthold ,  RAAB, Gerhard ,  REISSMANN, Thomas

IPC分类号： A61K9/16 ,  A61K31/4439

CPC分类号： A61K9/1623 ,  A61K9/1652 ,  A61K31/4439 ,  Y02A50/465

摘要： The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable microtubule polymerization inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of Indibulin for oral administration comprising a granulate containing micronized Indibulin having a particle size of less than 20 mum for at least 99% of the volume of particles, at least one hydrophilic surfactant, and at least one capsulation excipient. The present invention also discloses a method of treating hyperproliferative disorders, malignancies and neoplasms with Indibulin.

公开(公告)号：EP1922061A2

公开(公告)日：2008-05-21

申请号：EP06761981.7

申请日：2006-06-07

申请人： ZIOPHARM ONCOLOGY, INC.

发明人： ROESSLER, Berthold ,  RAAB, Gerhard ,  REISSMANN, Thomas

IPC分类号： A61K9/16 ,  A61K31/4439

CPC分类号： A61K9/1623 ,  A61K9/1652 ,  A61K31/4439 ,  Y02A50/465

摘要： The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable microtubule polymerization inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of Indibulin for oral administration comprising a granulate containing micronized Indibulin having a particle size of less than 20 mum for at least 99% of the volume of particles, at least one hydrophilic surfactant, and at least one capsulation excipient. The present invention also discloses a method of treating hyperproliferative disorders, malignancies and neoplasms with Indibulin.

公开(公告)号：EP2091532A1

公开(公告)日：2009-08-26

申请号：EP07853153.0

申请日：2007-11-27

申请人： ZIOPHARM ONCOLOGY, INC.

发明人： WALLNER, Barbara P. ,  SCHWARTZ, Brian Eric ,  KOMARNITSKY, Philip B. ,  BACHER, Gerald ,  KUTSCHER, Bemhard ,  RAAB, Gerhard

IPC分类号： A61K31/404 ,  A61K31/4439 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61P35/04

CPC分类号： A61K31/4439 ,  A61K31/138 ,  A61K31/282 ,  A61K31/337 ,  A61K31/404 ,  A61K31/437 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/475 ,  A61K31/496 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61K31/565 ,  A61K31/566 ,  A61K31/569 ,  A61K31/573 ,  A61K31/704 ,  A61K31/7048 ,  A61K31/7068 ,  A61K33/24 ,  A61K38/08 ,  A61K45/06 ,  A61K2300/00

摘要： The invention provides combination therapy, wherein one or more other therapeutic agents are administered with indibulin or a pharmaceutically acceptable salt thereof and the combination is synergistic. Another aspect of the invention relates to the treatment of cancer with indibulin as a single agent. Another aspect of the invention relates to dosing regimen for administration of oral dosage forms of indibulin.