On April 16, 2015 Aeterna Zentaris Inc. (NASDAQ: AEZS, TSX: AEZ) (the "Company") reported that it has filed an application for a patent (European Patent Office priority application: EP15000132) on a novel method of manufacturing zoptarelin doxorubicin, its hybrid cytotoxic molecule that is the subject of a pivotal ZoptEC (Zoptarelin doxorubicin in Endometrial Cancer) Phase 3 clinical study in women with advanced, recurrent or metastatic endometrial cancer who have progressed and who have received one chemotherapeutic regimen with platinum and taxane (either as adjuvant or first-line treatment) (Press release, AEterna Zentaris, APR 16, 2015, View Source;q=653 [SID:1234506590]). The claimed manufacturing process is expected to result in a significant reduction in the cost of goods sold, providing a stronger competitive position for the Company.
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Zoptarelin doxorubicin is a complex molecule that combines a synthetic peptide carrier with doxorubicin, a well-known chemotherapy agent. The synthetic peptide carrier is a Luteinizing Hormone Releasing Hormone ("LHRH") agonist, a modified natural hormone with affinity for the LHRH receptor. The design of the compound allows for the specific binding and selective uptake of the cytotoxic conjugate by LHRH receptor-positive tumors. Potential benefits of this targeted approach include a better efficacy and a more favorable safety profile with lower incidence and severity of side effects as compared to doxorubicin alone.
Because zoptarelin doxorubicin is a complex molecule, it is expensive to synthesize. The patent application, which is entitled "Enzymatic process for the regioselective manufacturing of N-Fmoc-doxorubicin-14-O-dicarboxylic acid mono esters", may, if granted, make it difficult for generic manufacturers to produce the compound on a financially feasible basis after the Company’s composition of-matter patent on zoptarelin doxorubicin expires.
David A. Dodd, Chairman and Chief Executive Officer of the Company explained the significance of the patent application for the new synthesis process: "We believe that zoptarelin doxorubicin has the potential to become the first approved therapy in the U.S. for treating women within the targeted Phase 3 indication, as well as additional cancers that we might evaluate in the future. Our commitment is to ensure that patients and their physicians have such therapies that can potentially improve and extend the quality of lives. With the 2015 expiration date of the U.S. composition-of-matter patent on the horizon, we sought a means to maintain our advantage for this compound beyond the five-year period of exclusivity granted to new chemical entities, which we expect to apply to zoptarelin doxorubicin. The compound could be a very important oncology tool if our ZoptEC Phase 3 study achieves its endpoints. By reducing the complexity of production and cost of the compound, we will have greater flexibility in potentially ensuring that patients on a worldwide basis have access and can benefit from this therapy. We believe this patent, if granted, could provide that advantage by giving us a significant production and cost advantage in support of further development in additional indications. Finally, we are most proud that this manufacturing process was invented by our colleagues within the Company’s Frankfurt-based research and development staff."
The Company owns all rights to the new process. The Company intends to file a PCT patent application in January 2016, claiming priority of the filed EP patent application.
About Zoptarelin Doxorubicin
Zoptarelin doxorubicin represents a new targeting concept in oncology using a hybrid molecule composed of a synthetic peptide carrier and a well-known chemotherapy agent, doxorubicin. Zoptarelin doxorubicin is the first intravenous drug in advanced clinical development that directs the chemotherapy agent specifically to LHRH-receptor expressing tumors, resulting in a more targeted treatment with less damage to healthy tissue. The Company is currently conducting a ZoptEC (Zoptarelin doxorubicin in Endometrial Cancer) Phase 3 trial in women with advanced, recurrent or metastatic endometrial cancer, while zoptarelin doxorubicin is also in an investigator-initiated Phase 2 trial in prostate cancer. Aeterna Zentaris owns the worldwide rights to this compound except in China. On December 1, 2014, the Company entered into a Master Collaboration Agreement, a Technology Transfer and Technical Assistance Agreement and a License Agreement with Sinopharm A-Think Pharmaceuticals Co., Ltd for the development, manufacture and commercialization of zoptarelin doxorubicin in all human uses in the Peoples Republic of China, including Hong Kong and Macau. Sinopharm A-Think is a subsidiary of Sinopharm, the largest medical and healthcare group in China and on Fortune’s Global 500 list.
About Endometrial Cancer
Endometrial cancer is the most common gynecologic malignancy in developed countries and develops when abnormal cells amass to form a tumor in the lining of the uterus. It largely affects women over the age of 50 with a higher prevalence in Caucasians and a higher mortality rate among African Americans. According to the American Cancer Society, there will be more than 54,000 new cases of endometrial cancer in the U.S. alone in 2015, with about 20% of recurring disease.