Oral Alpha-4-Beta-7 Integrin Antagonist PN-943 Demonstrates Sustained Dose-Related Target Engagement Activity in a Multiple Ascending Dose Phase 1 Study

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[{"type":"text","content":"NEWARK, Calif., Aug. 1, 2019 /PRNewswire/ -- Protagonist Therapeutics, Inc. (Nasdaq:PTGX) today announced results from the completed Phase 1 normal healthy volunteer (NHV) study of PN-943, an oral, gut-restricted alpha-4-beta-7 integrin specific antagonist in development for the potential treatment of inflammatory bowel disease (IBD). Results of the first clinical study of PN-943 in a randomized, double-blind, placebo-controlled, dose escalation study in NHVs demonstrated that administration of PN-943 was safe and well tolerated. The pharmacokinetic and pharmacodynamic findings were consistent with the design of PN-943 as a gut-restricted alpha-4-beta-7 integrin antagonist. \n\"These dose-finding results from the multiple ascending dose (MAD) part of the Phase 1 study with two weeks of daily administration of PN-943 are consistent with the previously reported preclinical and Phase 1 single ascending dose (SAD) data with PN-943,\" commented Samuel Saks, M.D., Protagonist Chief Medical Officer. \"The MAD data show the additional benefit of sustained target engagement with repeated dosing compared to the SAD results. These observations provide additional confirmation of superior target engagement as compared with our first generation antagonist PTG-100. We are very encouraged by these findings and plan to initiate a Phase 2 ulcerative colitis study with PN-943 in early 2020.\"\n PN-943 has been designed as a second generation oral, gut-restricted, alpha-4-beta-7-integrin antagonist with superior potency in comparison to the previous candidate PTG-100 that has validated this novel approach based on our findings from the Phase 2 PROPEL trial in patients with ulcerative colitis (UC) with PTG-100. In the MAD part of the Phase 1 study, PN-943 was administered daily over 14 days. The new results from the MAD part of the study are briefly described below and a complete presentation of the Phase 1 study results is scheduled for the American College of Gastroenterology Conference on Oct. 28, 2019, in San Antonio. \nA summary of results of target engagement as measured by maximum blood receptor occupancy (%RO) and 24 hour area under the %RO curve (AUC0-24) on day 14 in alpha-4-beta-7 positive CD4 positive memory T cells is provided below (mean ± standard deviation). \nThe Phase 2 PROPEL trial of PTG-100 in patients with ulcerative colitis ha...

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