Esperance Pharmaceuticals Initiates Clinical Studies For EP-100, In Patients With Cancer

Esperance Pharmaceuticals has begun enrollment and dosing of patients in a phase 1 study of EP-100 in patients with advanced solid tumors. EP-100, the candidate from Esperance’s Cationic Lytic Peptide (CLYP) platform technology, is a targeted membrane-disrupting peptide (tMDP) designed to seek and destroy cancer cells that over-express luteinising hormone releasing hormone (LHRH) receptors on their surfaces.

The phase 1 study is a multi-center, open-label, dose escalating study designed to evaluate the safety, pharmacodynamic and pharmacokinetic properties of EP-100. The study will enroll adult patients up to a total of 36 patients that are either refractory to the standard of care or for which no standard of care exists.

EP-100 will be administered intravenously for three out of four weeks. Once the maximum tolerated dose (MTD) has been established, additional subjects with specific diagnoses of either breast, ovarian, endometrial, pancreatic or prostate cancer will be enrolled and dosed at the MTD.

Results from preclinical studies of EP-100 have shown that the drug regresses established tumors in breast, prostate, ovarian and endometrial cancer xenografts in mice.

In in-vivo studies, the efficacy of EP-100 in comparison to saline or untargeted membrane-disrupting peptide or cisplatinum was studied in an ovarian cancer xenograft model (OVCAR-3). EP-100 regressed established OVCAR-3 xenografts following weekly injections at doses as low as 0.2mg/kg bodyweight (p<0.03 vs baseline).

In comparison, tumor growth was observed across the saline control, untargeted membrane-disrupting peptide and cisplatinum arms. In addition, in the EP-100 arm tumor volumes, weights and CA125 were reduced. LHRH receptor levels were also reduced and PET imaging revealed that EP-100 treated tumors became necrotic, lacking viable tumor cells after treatment. EP-100 was well tolerated in all treated groups.