Mar. 5, 2007 — Arrowhead Research Corp.(ARWR) says its majority-owned subsidiary Insert Therapeutics has signed a definitive agreement with R&D Biopharmaceuticals to acquire an exclusive, world-wide license to multiple second generation epothilone anticancer drugs. Insert will apply its proprietary Cyclosert transport system to select second generation epothilones now in development at R&D.
Epothilones, despite their promise as potent anti-cancer drugs, have encountered clinical difficulties due to their toxic side effects in patients. Cyclosert is the first nanoparticle drug transport platform to be designed de novo and synthesized specifically to overcome limitations in existing technologies used for the systemic transport of therapeutics to targeted sites within the body.
Based on small cyclic repeating molecules of glucose called cyclodextrins, its application to these second generation epothilone drugs are expected to promote their ability to inhibit the growth of human cancer cells while remaining non-toxic and non-immunogenic at therapeutic doses. In particular, the system is designed to keep the drugs non-toxic until they actually reach the targeted tumor cells where active drug is released in a controlled fashion.
“This is a significant step for both Insert Therapeutics and cancer care delivery in general,” said Edward Jacobs, Chief Executive Officer and President of Insert Therapeutics. “We hope this collaboration will allow a broader range of cancer patients to realize a potentially greater therapeutic effect from potent cancer drugs that may otherwise have been too toxic for them to receive.”
“We are excited about this strategic partnership with R&D-Biopharmaceuticals,” said R. Bruce Stewart, Chairman of Arrowhead. “We expect to continue to enhance the overall effectiveness of cancer treatment with other therapeutic candidates in the future.” “The combination of the Cyclosert technology has already demonstrated impressive effectiveness with other cytotoxics”, Wolfgang Richter, Managing Director of R&D-Biopharmaceuticals added.
“The collaboration with Insert Therapeutics is expected to fully leverage the potential of the new second generation epothilones.”
Epothilones are naturally occurring microtubule depolymerisation inhibitors, which stop the growth of human cancer cells in vitro at nano or even subnanomolar concentrations. Their attractive preclinical profile has made epothilones important lead structures in the search for improved cytotoxic anticancer drugs. R&D will use its proprietary know-how to synthesize novel and proprietary epothilone derivates, whose pharmaceutical profile will be evaluated in the relevant testing systems. Promising candidates showing the best profile will be considered for full preclinical development.
First generation epothilones are in clinical development by numerous pharmaceutical companies. Among the aims of second generation epothilone development is to optimize them for biological selectivity, stability, and water solubility. All of these properties have been shown to be effectively enhanced in other cytotoxic agents by use of the Cyclosert transport system. The combination of a second generation epothilone with Cyclosert should be highly competitive in this crowded field.