Item 8.01 Other Events.
We are providing the following information to
summarize
and update certain aspects of our publicly disclosed description of our clinical programs.
Etrasimod
Etrasimod, an orally available modulator of the S1P receptor, is our internally discovered investigational drug candidate intended for the potential treatment of a number of autoimmune diseases. S1P receptor modulators have been demonstrated to be involved in several biological responses, including lymphocyte trafficking from lymph nodes to the peripheral blood. By isolating lymphocytes in lymph nodes, fewer immune cells are available in the circulating blood to effect tissue damage. Drugs in this class have been associated with certain side effects, including cardiovascular effects, respiratory effects, infection, macular edema and elevations in liver enzymes. We have optimized etrasimod as a potent and selective small molecule S1P receptor modulator that reduces the severity of disease in preclinical autoimmune-disease models.
We are currently developing etrasimod for ulcerative colitis. In July 2015, we initiated patient dosing in a 12-week, randomized, double-blind and placebo-controlled Phase 2 clinical trial of etrasimod for ulcerative colitis. We are working diligently to obtain data from this trial by the end of 2017. To achieve our goal of obtaining data from this trial by the end of 2017 and lower costs, we are assessing potential changes to the trial protocol that we believe would improve data readout and enhance overall efficiency of the trial, while maintaining study conduct, data integrity, patient safety and the overall study objectives.
In addition, to further enhance the overall profile of our etrasimod program, we intend to explore development in additional indications, including
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Dermatological Extra-Intestinal Manifestations (EIM) in Inflammatory Bowel Disease (IBD)
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Pyoderma Gangrenosum (PG)
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Primary Biliary Cirrhosis (PBC)
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We are designing exploratory Phase II clinical trials for each of these additional indications. We intend to initiate these Phase II trials during 2017.
Ralinepag
Ralinepag, an oral
, selective
IP receptor
agonist
targeting the prostacyclin pathway
, is our
internally discovered investigational drug candidate intended for the treatment of pulmonary
arterial hypertension, or PAH.
In September 2014, ralinepag was
granted
orphan drug status for the treatment of PAH by the FDA.
In January 2015, we initiated patient dosing in a 22-week, randomized, double-blind and placebo-controlled Phase 2 clinical trial of ralinepag. We completed enrollment in the trial in December 2016 and expect to obtain data from this trial by the end of the third quarter of 2017.
APD371
APD371, an orally available, peripherally restricted, highly selective, full agonist of the cannabinoid-2 (CB2) receptor, is an internally discovered investigational drug candidate we are exploring for the treatment of pain.
In October 2015, we initiated a Phase 1 multiple-ascending dose trial of APD371. In the first half of 2016, we completed this trial with favorable results. In the first quarter of 2017, we intend to commence a Phase 2 clinical trial of APD371 for pain associated with Crohn’s disease and expect to obtain data from this trial by the end of 2017.
Temanogrel
Temanogrel, an orally available inverse agonist of the serotonin 2A receptor, is an internally discovered investigational drug candidate intended for the treatment of thrombotic diseases. We believe temanogrel has the potential to inhibit serotonin-
mediated
platelet aggregation and vasoconstriction. We believe temanogrel’s dual mechanism may be therapeutically
useful
for the treatment or prevention of thrombotic diseases.
We previously completed a Phase 1a clinical evaluation of temanogrel, and provided Ildong Pharmaceuticals Co., Ltd., the development and
commercialization
rights to temanogrel in South Korea (while we retained all other rights worldwide). Ildong is not currently advancing temanogrel in clinical trials for South Korea. We are continuing to evaluate options for this program.