Auritec Pharmaceuticals, LLC

Long-acting Injectable Tacrolimus for Chronic Immunosuppression - Project Summary the Broad, Long-term Goal of This Direct to Phase Ii Sbir Is to Improve Immunosuppression Outcomes in Organ Transplant Recipients by Developing a Long-acting Injectable Calcineurin Inhibitor (cni). for More Than Two Decades, Tacrolimus Is a Valuable Pharmacological Tool in the Prophylaxis of Organ Transplant Rejection. It Is Commercially Available as Twice and Once-daily Oral Pills. Oral Formulations Undergo First-pass Metabolism and Suffer From Low and Variable Bioavailability Which in Turn Leads to High Intra- and Inter- Patient Pharmacokinetic (PK) Variability. Tacrolimus Has a Narrow Therapeutic Index, Hence Sub-therapeutic Blood Levels (<5 NG/ML) Results in Organ Rejection Whereas Supra-therapeutic Levels (>15 NG/ML) Are Toxic. Daily Dosing Has Been Associated With Medication Non-adherence. the Medical Costs Transplant Recipients With Poor Adherence Are ~$30,000 Higher Than Patients With High Adherence at 3 Years Post-transplant. Thus, the Three Reported Unmet Needs Are Higher Medication Adherence, Better Outcomes of Graft Survival, and Linear PK Profile. Auritec Pharmaceuticals Has Developed a Subcutaneous Injectable Formulation of Tacrolimus That Provides Consistent Therapeutic Blood Levels of the Drug for 30 Days After a Single Administration. the Product Is Based on Auritec’s Innovative Plexis Technology That Has Shown Clinical Proof of Concept in Two Phase 1 Trials. the Plexis Technology Is Differentiated From Other Long-acting Injectable Technologies in Terms of Its High Drug Loading, Scalable Manufacturing Process, and More Linear Release Kinetics. the Product Has Demonstrated Safe and Sustained Release of Tacrolimus in a First-in-human Safety/pk Study Using the “exploratory Ind” Approach. PK Modeling Shows That a Monthly Dosing Schedule Can Be Readily Achieved in Transplant Recipients to Maintain Tacrolimus Blood Levels in the Safe and Efficacious Range (5-15 NG/ML). the Benefits of Our Product Include 1) Complete Medication Adherence for 1 Month After One Administration; 2) Fewer Episodes of Graft Rejections; 3) Simpler Dosing Schedule, and; 4) a Smooth PK Profile Without Sub- or Supra-therapeutic Levels. the Populations Anticipated to Benefit From the Product Are: Patients Who Have Demonstrated Tolerability to Tacrolimus But Find It Challenging to Adhere to a Daily Fixed Schedule (such as Younger Patients) And/or Rapid Metabolizers of Tacrolimus. the End Result Will Be a Cost-effective Maintenance Therapy for Maintenance Therapy. the Specific Aims of This Direct to Phase Ii Sbir Are to Perform Activities in Pursuit of a “traditional Phase 1 Ind” Allowance. the Proposed Work Includes - Manufacturing in Accordance With Current Good Manufacturing Practices (CGMP); Animal Testing in Compliance With Good Laboratory Practices (GLP); Analytical Method Development; Chemistry, Manufacturing and Controls (CMC) Testing; and Finally, Ind Submission to the Fda. These Efforts Will Result in an Ind Approval and Allow for the First-in-human Testing of Safety, PK, and Preliminary Efficacy in Transplant Recipients. Successful Completion of This Work Will Further De-risk the Product by Bringing It Closer to Clinical Testing and Making It Attractive to Investors.