On June 2, 2022 A scientific team, led by the scientific founders of EtiraRx, reported that it has identified a small molecule, ERX-41, as a novel oral therapeutic agent that may have utility in treating multiple solid cancers, including triple negative breast cancer, glioblastoma, ovarian and pancreatic cancers (Press release, EtiraRx, JUN 2, 2022, View Source [SID1234616455]). EtiraRx, headquartered in Biolabs Pegasus Park, plans to initiate clinical trials as early as the first quarter of 2023.

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In the work, published in Nature Cancer, the researchers, led by Drs. Jung-Mo Ahn, Ganesh Raj and Ratna Vadlamudi, identified that ERX-41 dramatically enhances endoplasmic reticulum (ER) stress in cancer cells. Since aggressive cancer cells have higher basal levels of ER stress, the enhanced ER stress induced by ERX-41 is not compensated and causes cancer cell death. Normal cells have low basal of ER stress, can compensate for ERX-41 activity and do not undergo cell death after ERX-41 treatment. Using state-of-the-art molecular approaches, the team identified that the molecular target of ERX-41 is the protein encoded by the lysosomal acid lipase A (LIPA) gene and that pharmacologic inhibition of LIPA by ERX-41 enhances ER stress in cancer cells. The study set the foundation for clinical trials with patients with therapy-resistant cancers that are vulnerable to enhanced ER stress.

Said Dr. Raj, "These discoveries are exciting as they represent a novel approach to targeting the Achilles heel of many aggressive cancers- their vulnerability to enhanced ER stress. Our critical finding was that of a new therapeutic target (LIPA) and its undiscovered role in protein folding. By targeting LIPA with ERX-41, protein folding in the cancer cell was disrupted, causing ER stress and promoting cancer cell death. Our findings indicate the potential for an oral agent with a favorable therapeutic index to effectively treat patients with aggressive cancers, for whom options are limited."

EtiraRx is completing necessary preclinical studies and plans to initiate clinical trials with these compounds, which will take place the first quarter of 2023. Russell Hayward, CEO EtiraRx, said, "ERX-41 has the potential to be a first-in-class oral therapy that kills aggressive therapy-resistant cancers. We are committed to moving these drugs forward to clinical trials and make a difference in the lives of patients with lethal cancers."