• First Patient Dosed in Phase 1 Trial of Oral (CR845) KORSUVA™

First Patient Dosed in Phase 1 Trial of Oral (CR845) KORSUVA™

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

Study to evaluate Peptelligence®-Engineered Oral CR845 (CR845/difelikefalin) in Chronic Liver Disease Patients

BOONTON, NJ – March 1, 2018Enteris BioPharma, Inc., a biotechnology company developing innovative drug products built around its proprietary delivery technologies, congratulates Cara Therapeutics (Nasdaq: CARA) on the successful initiation of the Phase 1 clinical trial of its oral formulation of CR845/difelikefalin (KORSUVA™) in patients with chronic liver disease (CLD). The oral tablet formulation of KORSUVA was engineered using Enteris’ proprietary oral peptide and small molecule delivery technology, Peptelligence®.

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.

About Cara Therapeutics

Cara Therapeutics is a clinical-stage biopharmaceutical company focused on developing and commercializing new chemical entities designed to alleviate pain and pruritus by selectively targeting peripheral kappa opioid receptors (KORs). Cara is developing a novel and proprietary class of product candidates, led by CR845, a first-in-class KOR agonist that targets the body’s peripheral nervous system. In Phase 2 trials, CR845 has demonstrated statistically significant reductions in itch intensity and concomitant improvement in quality of life measures in patients with moderate-to-severe CKD-associated pruritus. Additionally, CR845 has also demonstrated initial signs of efficacy in patients with moderate-to-severe pain, without inducing many of the undesirable side effects typically associated with currently available opioid pain therapeutics.

About Enteris BioPharma

Enteris BioPharma, Inc. is a privately held, New Jersey-based biotechnology company offering innovative formulation solutions built around its proprietary drug delivery technologies. The Company’s proprietary oral delivery technology – Peptelligence® – has been the subject of numerous feasibility studies and active development programs, several of which are in late stage clinical development. Additionally, Enteris BioPharma is advancing an internal product pipeline of oral tablet reformulations of drug products that address significant treatment opportunities for which there is no oral delivery option. Enteris BioPharma’s most advanced internal product candidate, Ovarest® (oral leuprolide tablet), is an oral peptide being developed for the treatment of endometriosis. Tobrate® (oral tobramycin tablet) is also being developed by Enteris BioPharma for the treatment of uncomplicated urinary tract infection (uUTI). A third internal compound, octreotide, will be entering preclinical development in 2018. For more information on Enteris BioPharma and its proprietary oral peptide delivery technology, please visit https://www.EnterisBioPharma.com.

 For Enteris BioPharma:Enteris Media Relations:
Brian Zietsman, President & CFO
+1.973.453.3527
Jason Rando
Tiberend Strategic Advisors, Inc.
+1.212.375.2665
jrando@tiberend.com