• First Patient Dosed in Trial of Oral KORSUVA™

First Patient Dosed in Trial of Oral KORSUVA™

Enteris BioPharma’s “Feasibility-to-Licensing” Partner, Cara Therapeutics, Doses First Patient in Phase 2 Trial of Peptelligence®-Engineered Oral KORSUVA™

Study to evaluate Oral KORSUVA (CR845/difelikefalin) for the Treatment of Pruritus in Stage III-V Chronic Kidney Disease (CKD) Patients

BOONTON, N.J., July 19, 2018 /PRNewswire/Enteris BioPharma, Inc., a biotechnology company developing innovative drug products built around its proprietary oral peptide delivery technologies, congratulates Cara Therapeutics (Nasdaq: CARA) on the successful initiation of its Phase 2 clinical trial of Oral KORSUVA™ (CR845) in patients with pre-dialysis chronic kidney disease (CKD). The tablet formulation of Oral KORSUVA was engineered using Enteris’ proprietary oral peptide delivery technology, Peptelligence®.

The Oral KORSUVA Phase 2 initiation follows a successful Phase 1 trial in moderate-to-severe CKD Patients, which demonstrated that exposure levels with Oral KORSUVA tablets were approximately equivalent to the exposure level achieved with a 0.5 mcg/kg dose of intravenous (I.V.) CR845. Additionally, this Phase 2 initiation marks an important clinical advancement involving an oral formulation of Cara Therapeutics’ CR845. Oral KORSUVA 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 chronic liver disease patients.

The oral tablet formulation of CR845 was developed in accordance with a Manufacturing and Clinical Supply Agreement 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 phase 3/ commercial license to the Peptelligence™ technology for oral CR845 from Enteris at any time.

“We congratulate Cara Therapeutics on advancing Oral KORSUVA into Phase 2. This is clearly an important milestone for Cara and its pruritus programs, and also speaks volumes of the important ongoing relationship between Cara and Enteris,” said Joel Tune, chief executive officer and executive chairman of Enteris BioPharma. “Success in the clinic is the ultimate arbiter of any drug or technology. The advance of Oral KORSUVA into Phase 2 for CKD shortly followed the positive data from our own Phase 2a trial of Ovarest™ in endometriosis, collectively further demonstrating the ability of our Peptelligence platform to enable the oral delivery of peptide therapeutics across multiple drug compounds and multiple disease indications.”

“We remain pleased with our ongoing work with Enteris and are excited to advance our Oral KORSUVA program in pre-dialysis CKD patients into Phase 2,” stated Derek Chalmers, Ph.D., D.Sc., president and chief executive officer of Cara Therapeutics. “Throughout the remainder of this year, we plan to expand our clinical activities with Oral KORSUVA beyond CKD into additional patient populations, such as those with chronic hepatic and dermatologic conditions, in which treatment-resistant pruritus also remains a significant unmet medical need.”

The Phase 2, multicenter, randomized, double-blind, placebo-controlled 12-week trial is designed to evaluate the safety and efficacy of three dose levels (0.25 mg, 0.5 mg and 1 mg, once daily) of Oral KORSUVA versus placebo in approximately 240 stage III-V CKD patients with moderate-to-severe pruritus. The primary efficacy endpoint is the change from baseline in the weekly mean of the daily 24-hour Worst Itch Numeric Rating Scale (NRS) score at Week 12 of the treatment period. Secondary endpoints include change from baseline in itch-related quality of life scores at the end of Week 12, as assessed by the total Skindex-10 and 5-D itch scales, as well as the proportion of patients achieving an improvement from baseline ≥3 points with respect to the weekly mean of the daily 24-hour Worst Itch NRS score at week 12.

About Cara Therapeutics

Cara Therapeutics is a clinical-stage biopharmaceutical company focused on developing and commercializing new chemical entities designed to alleviate pruritus and pain by selectively targeting peripheral kappa opioid receptors (KORs). Cara is developing a novel and proprietary class of product candidates, led by KORSUVA™ (CR845/difelikefalin), a first-in-class KOR agonist that targets the body’s peripheral nervous system, as well as certain immune cells. In Phase 2 trials, KORSUVA injection has demonstrated statistically significant reductions in itch intensity and concomitant improvement in quality of life measures in hemodialysis patients with moderate-to-severe chronic kidney disease-associated pruritus (CKD-aP), and is currently being investigated in Phase 3 trials in hemodialysis patients with CKD-aP. Additionally, in a recently completed Phase 2/3 trial in post-operative patients, I.V. CR845/difelikefalin has demonstrated reduction in moderate-to-severe pain, while also reducing the incidence and intensity of nausea and vomiting throughout the post-operative period.

About Enteris BioPharma

Enteris BioPharma, Inc. is a privately held, New Jersey-based biotechnology company offering innovative formulation solutions utilizing its proprietary oral peptide drug delivery technology, Peptelligence®. The technology 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 initially for the treatment of endometriosis, with possible follow on indications, including uterine fibroid tumors, prostate cancer, in vitro fertilization, and central precocious puberty. 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, is currently in preclinical development. For more information on Enteris BioPharma and its proprietary oral 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