Esperance Pharmaceuticals Presents Results From Phase 1 Study of EP-100 in Advanced, Refractory LHRH-Receptor Expressing Solid Tumors at ASCO

BATON ROUGE, La., June 4, 2012 /PRNewswire/ -- Esperance Pharmaceuticals presented its Phase 1 study of EP-100, a novel targeted membrane‐disrupting peptide (tMDP) in advanced solid tumors at the American Society for Clinical Oncology (ASCO) Annual Meeting in Chicago, Illinois. EP‐100 is designed to seek and destroy cancer cells that over‐express luteinizing hormone releasing hormone (LHRH) receptors on their surfaces. LHRH receptors are over‐expressed in a wide range of cancers. The Phase 1 study was designed to determine safety and maximum dose of EP-100, including a recommended dose for Phase 2 trials. Based on clinical experience of escalating doses in 38 patients in the Phase 1 study and on preclinical studies showing synergy of EP-100 with various chemotherapeutic agents, Esperance has begun enrollment of patients in a Phase 2 multi‐center trial for patients with advanced ovarian cancer randomized to EP‐100 in combination with paclitaxel versus paclitaxel alone.

"Results from the Phase 1 study suggest that LHRH expression is a viable target for therapy, and that EP-100 has potential as a targeted, well-tolerated therapeutic for tumor treatment in areas where many patients are running out of options," said lead investigator Ramesh K. Ramanathan, MD from the Virginia G. Piper Cancer Center/TGen, (Scottsdale, AZ). "I look forward to continuing progress with this exciting, new drug candidate in various later stage clinical trials."

"This Phase 1 study provided us with the information we needed to move forward with clinical trials in specific LHRH receptor expressing tumor types that are resistant to treatment," said Hector Alila, PhD, President and CEO of Esperance Pharmaceuticals. "Specifically, we believe there is a compelling rationale for the study of EP‐100 in ovarian cancer—which is known to over-express LHRH receptors. To this end we initiated a Phase 2 study in ovarian cancer in May and are hopeful EP‐100 may hold promise for this patient population with very few treatment options."

Study Results

Poster #3060 "A Phase 1 study of EP100, a Luteinizing Hormone Releasing Hormone (LHRH) Ligand Conjugated to a Synthetic Cytolytic Peptide in Patients with Advanced Refractory LHRH-Receptor (R)-Expressing Solid Tumors"

The Phase 1 study was designed to determine the maximum safe dosage for future Phase 2 trials of EP-100. The study screened 97 patients for LHRH-receptor (LHRH-R) expression, 53 were positive for expression and, subsequently, 37 patients for whom standard therapy had failed or for whom no standard therapy exists were enrolled and treated. Most patients had breast (n= 16, 42%) ovary (n=7,18%), colon (n=4, 11%) or uterine (n=3, 8%) cancer. Patients were treated in a 3 + 3 standard dose escalation schema. Doses were escalated 100% in the absence of a Grade 2 drug related toxicity. Therapy was generally well tolerated and a maximum tolerated dose was not reached at the highest dose of 40 mg/m2. One dose limiting toxicity of elevated liver enzymes was reported in a patient with liver metastasis and elevated transaminases at baseline; no other patients in this cohort or subsequent cohorts experienced increases in liver enzymes. The only other drug-related toxicity was an infusion-related skin reaction which dissipated upon cessation of infusion of EP-100. Best response observed was stable disease for >12 weeks in 5 patients. In 3 patients rapid, sustained decreases in luteinizing hormone/follicle stimulating hormone (LH/FSH) levels, indicative of EP-100 activity on gonadotrope cells in the anterior pituitary were noted. Antibody production against EP-100 was not observed in any patients.

Based on the Phase 1 results, a Phase 2 dose has been selected of 30-40 mg/m2 twice a week x 3 weeks and a randomized Phase 2 study of EP-100 in combination with weekly paclitaxel versus paclitaxel alone in patients with histologically confirmed epithelial ovarian carcinomas whose tumor express LHRH-R has been initiated. The study is currently enrolling patients.

About EP-100

EP-100, the lead candidate from Esperance's Cationic Lytic Peptide (CLYPTM) platform technology, is a targeted membrane-disrupting peptide (tMDP) designed to seek and destroy cancer cells that over-express luteinizing hormone releasing hormone (LHRH) receptors on their surfaces. LHRH receptors are over-expressed in a wide range of cancers including breast, prostate, endometrial, pancreatic, ovarian, blood, skin and testicular cancers.

About Esperance Pharmaceuticals

Esperance Pharmaceuticals, Inc. is a clinical stage company developing a new class of targeted anticancer drugs using its Cationic Lytic Peptide (CLYP™) platform technology. These drug candidates, called targeted membrane-disrupting peptides (tMDPs) and antibody drug conjugates (ADCs) selectively seek and destroy cancer cells, including cells known to be resistant to chemotherapeutic drugs, without harming normal cells. Targeting occurs through binding to specific receptors and antigens on the cell's surface. The Company was founded on patented technology discovered by scientists at the Pennington Biomedical Research Center, the Louisiana State (LSU) Ag Center and LSU main campus. Founding investors include the Louisiana Fund I, Themelios Ventures and Research Corporation Technologies. Additional investors include Sanofi, Advantage Capital Partners, Louisiana Technology Fund and private investors. More information can be found at www.esperancepharma.com.

SOURCE Esperance Pharmaceuticals