LOUISVILLE, Ky. ―Advanced Cancer Therapeutics (ACT), a privately held company dedicated to bringing new anti-cancer therapies to market, announced today that the University of Texas MD Anderson Cancer Center in Houston and the University of Texas Health Science Center at San Antonio have been added as human clinical trial sites for PFK-158, a first-in-man/first-in-class inhibitor of PFKFB3, an enzyme that controls glycolysis and that is overexpressed in most hematological and solid tumors. The two new clinical trial sites are expected to begin enrolling patients Jan. 1, 2015.
PFK-158 was discovered and developed by ACT and was based on the initial drug discovered at the University of Louisville’s James Graham Brown Cancer Center, a part of KentuckyOne Health. The cancer center began recruiting patients for clinical trials in May 2014. Within weeks of opening the first clinical trial site, ACT was able to open the second clinical trial site, Georgetown University Medical Center in Washington, also in May 2014.
“We were pleased to partner with MD Anderson and UT Health Science Center at San Antonio to expand the number of clinical trial sites for PFK-158,” said ACT President and CEO Randall B. Riggs. “PFK-158 is a first-in-man, novel anti-cancer drug that prevents tumor cells from using glucose as a fuel source for tumor survival, growth and metastasis and is currently in a Phase 1 clinical study in the United States.”
In November 2014, PFK-158 was chosen by Informa and Kantar Health as one of the “2014 Top 10 Most Interesting Oncology Projects to Watch.”
PFK-158 is a small molecule that inactivates a novel cancer metabolism target never before examined in human clinical trials. Last spring, the U.S. Food and Drug Administration (FDA) approved a Phase 1 dose escalation study that is evaluating the safety, tolerability and anti-tumor activity of PFK-158 in cancer patients with solid tumors such as prostate, lung, ovarian, melanoma, breast and pancreatic cancer.
PFK-158 is the first 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) inhibitor to undergo clinical trial testing in cancer patients. The target, PFKFB3, is activated by oncogenes and the low oxygen state in cancers, stimulates glucose metabolism and is required for the growth of cancer cells.
PFK-158, which has been licensed by ACT from the James Graham Brown Cancer Center, inhibits the substrate binding domain of PFKFB3 causing a marked reduction in the glucose uptake and growth in multiple preclinical cancer models.