Kinex Pharmaceuticals, a specialty pharmaceutical company focused on the development and commercialization of next generation therapies for cancer and immunomodulatory diseases, announced that the first patient has been dosed with KX2-361 at Roswell Park Cancer Institute.
KX2-361 (KX02), a dual src/pre-tubulin inhibitor, is a small molecule drug that has shown potent inhibitory activity against a broad panel of brain tumor cell lines, including those that are resistant to Temozolomide (T98G), the most widely used chemotherapy for the treatment of malignant glioma. In a well-established brain tumor mouse model, KX2-361 consistently clears brain tumors after 4 weeks of therapy, in 30-60% of treated animals. These studies showed that KX2-361 induced significant necrosis compared to Temodar, and the treated animals also generated an immune response to the glioblastoma tumor cells. Pharmacokinetic studies have demonstrated that KX2-361 is absorbed orally and has approximately 75% penetration into brain tissue from plasma.
Dr David Hangauer, chief scientific officer of Kinex said “I am very pleased to see KX02 advance into the first clinical study. This compound was internally discovered and developed at Kinex through our proprietary Mimetica Technology Platform. The pre-clinical efficacy data that we have obtained during development is especially exciting because of the potential for this compound to engage the immune system and to effect cures as consistently demonstrated in the animal model of glioblastoma”.
Kinex Pharmaceuticals has also received orphan drug designation for KX2-361 for the treatment of gliomas, which are the most common and aggressive form of brain cancer. Orphan drug status qualifies Kinex for seven years of exclusivity after formal marketing approval, as well as further development incentives. A Phase 1 clinical trial for KX2-361 has commenced at Roswell Park Cancer Institute and the Cleveland Clinic. A third site has been identified and will initiate during the fourth quarter of 2014. Dosing of the first patient has taken place at Roswell Park Cancer Institute where enrollment is expected to be robust based on the unique mechanism of action of this drug as well as the pre-clinical data that has been generated.
“KX02 has an exciting pre-clinical profile and I am looking forward to obtaining clinical data for KX02”, said Dr Rudolf Kwan, chief medical officer at Kinex Pharmaceuticals. “The phase 1 study will determine the maximum tolerated dose in subjects with all types of primary malignancies and with brain metastasis and we will further evaluate the activity of KX02 in an expansion cohort of glioma patients”.
Kinex Pharmaceuticals has licensed the rights to KX2-361 for the Greater China territory to XiangXue Pharmaceuticals (Guangzhou, China). YongHui Wang, chairman and CEO of XiangXue Pharmaceuticals, said, “Kinex is a great collaboration partner, and I am delighted to see that KX02 has entered the clinic. XiangXue is excited with the pre-clinical profile of KX02. We are completing additional pre-clinical studies that are required for an IND to be filed with the CFDA in China. A phase 1 study in Chinese patients with brain tumors is expected to initiate soon after the IND is allowed in China.”