PALM BEACH GARDENS, Fla.--(BUSINESS WIRE)--Tyrogenex, a leader in the development of novel kinase inhibitors to target angiogenesis, today announced that the University of Wisconsin presented a new trial concept of investigational agent X-82, as a “Trials in Progress” poster at the 51st Annual Meeting of the American Society of Clinical Oncology (ASCO) in Chicago. The study titled, “Pharmacodynamic study using FLT PET/CT in advanced solid malignancies treated with a sequential combination of X-82 and docetaxel,” focuses on the optimization of a VEGFR/PDGFR TKI in combination with docetaxel.
The study is designed to take advantage of the pharmacokinetic profile of X-82 by combining it with docetaxel during the VEGF withdrawal flare to maximize the therapeutic index of chemotherapy. The University of Wisconsin is conducting the Phase I/II study with X-82 and docetaxel to determine the safety and efficacy using an optimized dosing scheme. Once the pharmacodynamics portion of the study has been completed, enrollment will be expanded with up to an additional 60 patients.
“We are excited to be involved in the first clinical trial to evaluate X-82 in combination with docetaxel,” said Justine Bruce, M.D., Associate Professor, Hematology/Oncology, University of Wisconsin. “Prior combination trials using VEGFR TKI and chemotherapy utilized a concurrent and non-sequential approach. The negative results from these prior combination trials could be attributed to an antagonist effect from the suboptimal scheduling of chemotherapy and VEGFR TKI agents.”
Dr. Bruce presented the poster during ASCO’s Developmental Therapeutics – Clinical Pharmacology and Experimental Therapeutics poster session.
“Data indicate that X-82 may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. We know that certain chemotherapies, such as docetaxel, kill tumor cells by stopping them from dividing or by stopping them from spreading. We believe the addition of X-82 to docetaxel will further decrease tumor cell growth,” said Michael D. Webb, Tyrogenex President and CEO. “Additionally, we expect to demonstrate that administering X-82 and docetaxel one at a time instead of concurrently in patients with solid tumors may demonstrate lower toxicity and higher tolerability and efficacy.”
Tyrogenex is developing X-82 as a targeted therapeutic for ophthalmological diseases and solid tumors. Preliminary data from a Phase 1 single agent study show that X-82 is well tolerated and did not exhibit any dose-limiting toxicity during the study.
In oncology, VEGFR tyrosine kinase inhibitors, such as X-82, typically have demonstrated benefit in a variety of cancers though dosage, and use of this class in combination with other therapies, has been limited by side effects. Phase 1 data show that X-82 could have a significantly lower toxicity profile, which may make it an ideal candidate for combination therapy.
For ophthalmology, the company has initiated a Phase 2 study known as “APEX,” for wet AMD in Previously treated Eylea patients with X-82. The study is designed to evaluate the safety and efficacy of X-82 in the prevention of vision loss due to wet AMD. A Phase 1 study showed X-82 was able to maintain or improve vision in all subjects who received the drug for the six-month study duration, and most subjects did not require any rescue injections during that time. There were no dose-limiting toxicities encountered during the study.