06-10-2016, 05:28 PM
KX02 (KX2-361), an oral dual src/pre-tubulin inhibitor with immune activation against brain tumors as a third mechanism of action, 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. This compound was discovered internally at Athenex. A Phase 1 clinical trial for KX02 commenced in early 2015 at three clinical sites in the United States.
In a well-established glioblastoma multiforme (GBM) brain tumor syngeneic mouse model, KX02 consistently cures the mice of their brain tumors after four weeks of therapy in 30-60% of treated animals. These pre-clinical studies showed that KX02 induced more necrosis in the GBM tumors compared to Temodar, and also resulted in more immune cell infiltration into the tumor tissues. Pharmacokinetic studies showed that KX02 is absorbed orally and has facile penetration into brain tissue from plasma, providing even higher drug levels in the brain than the plasma.
Athenex has received Orphan Drug designation for KX02 from the US FDA for the treatment of gliomas, which are the most common and aggressive form of brain cancer. Orphan drug status qualifies Athenex for seven years of exclusivity after formal marketing approval, as well as further development incentives.
XiangXue Pharmaceuticals in Guangzhou, China, is the collaborative development partner for KX02 in China. As a part of that partnership, XiangXue is preparing an IND application for the Chinese FDA.
In a well-established glioblastoma multiforme (GBM) brain tumor syngeneic mouse model, KX02 consistently cures the mice of their brain tumors after four weeks of therapy in 30-60% of treated animals. These pre-clinical studies showed that KX02 induced more necrosis in the GBM tumors compared to Temodar, and also resulted in more immune cell infiltration into the tumor tissues. Pharmacokinetic studies showed that KX02 is absorbed orally and has facile penetration into brain tissue from plasma, providing even higher drug levels in the brain than the plasma.
Athenex has received Orphan Drug designation for KX02 from the US FDA for the treatment of gliomas, which are the most common and aggressive form of brain cancer. Orphan drug status qualifies Athenex for seven years of exclusivity after formal marketing approval, as well as further development incentives.
XiangXue Pharmaceuticals in Guangzhou, China, is the collaborative development partner for KX02 in China. As a part of that partnership, XiangXue is preparing an IND application for the Chinese FDA.