Topical MEK Inhibitor Under Study in Cutaneous Squamous Cell Carcinoma
Posted: Friday, May 7, 2021
Preclinical research presented at the 2021 Society for Investigative Dermatology Virtual Meeting (Abstract 487) suggests the topical MEK inhibitor NFX-179 is safe and effective in the chemoprevention of cutaneous squamous cell carcinoma. Kenneth Y. Tsai, MD, PhD, of Moffitt Cancer Center, and colleagues reported that NFX-179 reduced cutaneous squamous cell carcinoma cells by suppressing the ERK pathway in the skin.
“We are thrilled with the compelling evidence these data provide, that topical application of NFX-179 has the potential to be a safe, effective strategy for prevention of cutaneous squamous cell carcinoma in high-risk individuals, and we feel very optimistic about moving into clinical trials,” Dr. Tsai said in a press release. “These data also validate a rational design approach for the precision targeting of diseases of the skin, particularly for cancer prevention.”
The researchers used a UV-induced model of cutaneous squamous cell carcinoma and topically applied NFX-179 gel. Results showed a 60% decrease in new cutaneous squamous cell carcinomas when the gel was used at doses of 0.1% for more than 28 days. When the dosage increased to 0.5%, there was a 92% reduction in cutaneous squamous cell carcinoma. There were no reported systemic or skin toxicities.
To study the local effectiveness of the NFX-179 gel, the team applied 0.5% of NFX-179 to half of the back of five mice. A vehicle gel without the NFX-179 was applied to the other half of the back for comparison purposes. They observed the gel caused a “near-complete suppression” of cutaneous squamous cell carcinoma—but solely in the drug-treated area. Further molecular analysis showed NFX-179 appears to work in a dose-dependent manner and inhibited ERK signaling to prevent formation of cutaneous squamous cell carcinoma.
Disclosures: The researchers provided no disclosure information.
