Enteris BioPharma's "Feasibility-to-Licensing" Partner, Cara Therapeutics, Doses First Patient in Phase 1 Trial of Oral KORSUVA™

BOONTON, N.J., March 1, 2018

The Oral KORSUVA Phase 1 initiation marks the fourth clinical program involving an oral formulation of Cara Therapeutics' CR845. Oral CR845 is also the subject of a Phase 2 program in chronic pain, a Phase 1 program in hemodialysis chronic kidney disease and a Phase 1 program in non-hemodialysis chronic kidney disease patients.

The oral tablet formulation of CR845 was developed in accordance with a Manufacturing and Clinical Supply Agreement between Cara Therapeutics and Enteris whereby Enteris utilized its Peptelligence technology to enable the active ingredient, which was initially formulated for I.V. or injection administration, to be delivered orally. Under the terms of the "Feasibility-to-Licensing" program, Enteris will continue to manufacture the oral tablet formulation of CR845 for current and potential future studies through Phase 2 that Cara Therapeutics elects to pursue. Cara Therapeutics has the opportunity to negotiate a license to the Peptelligence™ technology for oral CR845 from Enteris at any time.

"We congratulate Cara Therapeutics on the initiation of its fourth clinical program involving oral CR845; this time for the treatment of pruritus associated with chronic liver disease," said Joel Tune, chief executive officer and executive chairman of Enteris BioPharma. "Extending Oral CR845 into the treatment of pruritus related to liver disease further illustrates Peptelligence as a technology-of-choice for enabling the transition of peptide therapeutics from injection to oral delivery.  In multiple mid to late-stage clinical studies, including our internally developed assets, Peptelligence facilitated peptides have been shown to be safe and well tolerated and have demonstrated clinically meaningful efficacy and enhanced bioavailability."

"We believe that Oral KORSUVA has the potential to bring significant relief to patients suffering from CLD-associated pruritus," stated Derek Chalmers, Ph.D., D.Sc., president and chief executive officer of Cara Therapeutics. "We are pleased to continue our work with Enteris and initiate this new Phase 1 study with the potential to advance oral CR845 into a Phase 2 clinical trial for an important indication."

The Phase 1 trial is designed to examine the pharmacokinetics and safety of twice-daily tablet strengths of oral KORSUVA (1mg tablet) in up to 60 patients with CLD, and up to 12 matched healthy control subjects dosed over an eight-day treatment period in patients with mild, moderate or severe CLD based on their Child-Pugh classification (i.e., Class A, B and C). In addition, PK and safety tolerability will be assessed with KORSUVA up to 5.0mg tablet strength in mild and moderate CLD patients.

The U.S. Food and Drug Administration has conditionally accepted KORSUVA as the trade name of difelikefalin injection. CR845/difelikefalin is an investigational drug product and its safety and efficacy have not been fully evaluated by any regulatory authority.