Advanced Cancer Therapeutics initiates Phase I trial of anti-cancer drug candidate PFK-158

4th June 2014 (Last Updated June 4th, 2014 18:30)

US-based Advanced Cancer Therapeutics (ACT) has initiated a Phase I dose escalation trial of PFK-158, an anti-cancer drug candidate, which inactivates a new cancer metabolism target never examined before in human clinical trials.

US-based Advanced Cancer Therapeutics (ACT) has initiated a Phase I dose escalation trial of PFK-158, an anti-cancer drug candidate, which inactivates a new cancer metabolism target never examined before in human clinical trials.

The US Food and Drug Administration (FDA) approved trial is designed to assess the safety, tolerability and anti-tumour activity of PFK-158 in cancer patients with solid tumours such as melanoma, lung, colon, breast and pancreatic cancer.

The small molecule therapeutic candidate PFK-158 is the first 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) inhibitor to undergo clinical trial testing in cancer patients.

PFKFB3 is activated by oncogenes and the low oxygen state in cancers, stimulates glucose metabolism and is required for the growth of cancer cells as tumours in mice.

"PFKFB3 is activated by oncogenes and the low oxygen state in cancers, stimulates glucose metabolism and is required for the growth of cancer cells as tumours in mice."

ACT has licensed PFK-158 from the James Graham Brown Cancer Center at the University of Louisville and it inhibits the substrate binding domain of PFKFB3 causing a marked reduction in the glucose uptake and growth of multiple cancer types in mice.

The company started recruiting patients for PFK-158 human clinical trials in May with the first clinical trial site located at the James Graham Brown Cancer Center.

Brown Cancer Center deputy director Jason Chesney said PFK-158 is not only a first-in-class cancer drug but also the first to target glucose metabolism by inhibiting PFKFB3.

"This unique mechanism of action has resulted in efficacy against a broad spectrum of human cancers caused by common mutations as well as synergy with targeted agents that are FDA approved for several cancer types," Chesney said.

"As a researcher, it is incredibly rewarding to witness your group's studies move into clinical trials and potentially save the lives of cancer patients."

ACT president and CEO Randall Riggs said: "This is a significant milestone for ACT and it supports our dedication to develop significant treatment advancements for cancer patients with first-in-class, potential breakthrough therapeutics like PFK-158."