Clinical Trials

Date: 2018-02-15

Type of information: Completion of the trial

phase: 2

Announcement: treatment of the last patient

Company: Protalix BioTherapeutics (Israel)

Product: OPRX-106

Action mechanism:

• fusion protein. OPRX-106 is a plant cell-expressed recombinant human tumor necrosis factor receptor II fused to an IgG1 Fc domain (TNFRII-Fc), in development for oral administration. When administered orally and while passing through the digestive tract, the plant cells function as a natural delivery vehicle, having the unique attribute of a cellulose cell wall which makes them resistant to degradation compared to proteins produced via mammalian cell expression.

Disease: ulcerative colitis

Therapeutic area: Autoimmune diseases - Inflammatory diseases - Digestive diseases

Country: Israel

Trial details:

• The phase II clinical trial is a randomized, open label, 2-arm study of OPRX-106. Twenty-four patients were enrolled in the phase II study and were randomized to receive 2 mg or 8 mg of OPRX-106, administered orally, once daily, for 8 weeks, and 18 patients completed the trial. Key efficacy endpoints of the study, in addition to safety, include relevant disease parameters of the drug, including Mayo score and rectal bleeding. (NCT02768974)

Latest news:

• • On February 15, 2018, Protalix BioTherapeutics, announced the final dosing of the last patient in the Company’s phase II clinical trial evaluating OPRX-106, the Company’s oral antiTNF product candidate, in patients with ulcerative colitis . The company expects to report top-line results from this study by the end of March 2018.
• • On January 2, 2018, Protalix BioTherapeutics announced interim data from the first 14 patients that completed, to date, the phase II clinical trial of OPRX-106 in patients with ulcerative colitis. A total of 24 patients were enrolled and randomized to receive 2 mg or 8 mg of OPRX-106, administered orally, once daily, for 8 weeks. The first 14 patients have completed the study, and four patients are currently in treatment and follow-up. The trial evaluated key efficacy endpoints including clinical response and remission utilizing the Mayo score, as well as safety and pharmacokinetics.
• Data generated from the first 14 patients who completed the study demonstrates that 57% of the patients achieved clinical response and 36% achieved clinical remission at week 8.
• In the rectal bleeding analysis, a sub category of the Mayo score, 79% of those patients show an improvement. In addition, the majority of those patients show improvement in the study’s additional efficacy endpoints, with 86% of the patients achieved an improvement in calprotectin, a protein biomarker present in the feces indicating intestinal inflammation, and 64% have an improved Geboes score, a histopathological scoring for the assessment of disease activity in ulcerative colitis.
• Clinical response at week 8 is defined as a decrease in the Mayo score of at least 3 points and either a decrease in the sub-score for rectal bleeding of at least 1 point from baseline, or rectal bleeding sub-score of 0 or 1. Clinical remission at week 8 is defined as clinically symptom free, a Mayo score ? 2, with no individual sub-score exceeding 1 point after treatment.
• Treatment was well tolerated and the majority of adverse events have been mild to moderate and transient in nature, with headaches being the most common.   • On November 29, 2017, Protalix BioTherapeutics announced  the completion of enrollment in the Company’s phase II clinical trial evaluating OPRX-106, the Company’s oral antiTNF product candidate, in patients with ulcerative colitis (UC). OPRX-106 is the Company’s proprietary plant cell-expressed recombinant human tumor necrosis factor receptor II fused to an IgG1 Fc domain (TNFRII-Fc). When administered orally and while passing through the digestive tract, the plant cells function as a natural delivery capsule, having the unique attribute of a cellulose cell wall, which makes them resistant to degradation compared to proteins produced via mammalian cell expression systems. The Company expects to report top-line results from this study in the first quarter of 2018. “Despite a number of approved treatments for ulcerative colitis, there remains a large unmet medical need in this patient population,” said Mr. Moshe Manor, Protalix’s President and Chief Executive Officer. “We look forward to reporting initial results from our phase II study, which may provide proof of concept data not only for OPRX-106 in the treatment of UC, but also for our oral-delivery protein technology. If successful, OPRX-106 will be the first ever oral protein treatment, as currently there are no other oral recombinant protein treatments available.” The phase II clinical trial is a randomized, open label, 2-arm study of OPRX-106 in 19 patients with active mild to moderate ulcerative colitis. Patients have been randomized to receive 2 mg or 8 mg of OPRX-106 protein administered orally, once daily, for 8 weeks. Key efficacy endpoints of the study, in addition to safety, include relevant disease parameters of the drug, including Mayo score and rectal bleeding. • On November 30, 2016, Protalix BioTherapeutics announced that the first patient has been enrolled in its phase II clinical trial of OPRX-106 for the treatment of ulcerative colitis.  The phase II clinical trial is a randomized, open label, 2-arm study of OPRX-106 in 20 patients with active mild to moderate ulcerative colitis.  Patients will be randomized to receive 2 mg or 8 mg of OPRX-106 administered orally, once daily, for 8 weeks.  The primary endpoint of the study is safety, including monitoring for adverse events following daily administration of the drug.  Key efficacy endpoints include relevant disease parameters of the drug, including Mayo score and rectal bleeding. If successful, OPRX-106 will be the first ever oral enzyme treatment as currently there are no other oral enzyme treatments available.
• The Company completed a phase I clinical trial of OPRX-106 in 15 healthy volunteers, and the drug was found to be safe and well tolerated.  The results of the phase 1 clinical trial were announced in August 2015.  Immunomodulatory effect was observed, including activation of T Regulatory cells showing biological activity in the gut.  In addition, early efficacy signals of OPRX-106 have been demonstrated in preclinical studies using inflammatory bowel disease immune-mediated mouse models.  The results of the preclinical studies show that OPRX-106 attributes to a positive change in symptoms and in serum levels of anti-inflammatory markers.

Is general: Yes