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ETRASIMOD
A drug candidate for the treatment of immune-mediated and inflammatory diseases
Etrasimod is an investigational, once-daily, oral, selective, S1P receptor modulator designed for engagement of S1P receptors S1P1, S1P4, and S1P5. The purpose of this design is to partially and reversibly reduce lymphocyte levels at sites of inflammation while maintaining components of immune function.
Etrasimod is an investigational drug and is not currently approved for use by any health authority. This information is not intended to promote or recommend etrasimod for any use.
Proposed etrasimod MECHANISM OF ACTION:
S1P receptor modulation in IBD
Etrasimod clinical trials in GI DISEASES
PHASE 2ENROLLING
GLADIATOR UC is a Phase 2 52-week induction and maintenance study evaluating the safety and efficacy of once-daily, oral etrasimod in patients with moderately active ulcerative colitis (UC). Patients with a modified Mayo Score of 4-6 and endoscopic subscore ≥1 are eligible to participate in GLADIATOR UC (additional participation criteria apply).
- Patients that are ineligible for many UC trials due to lower disease activity may be eligible to participate in GLADIATOR UC
- Patients can remain on 5-aminosalicylic acid (5-ASA) and low-dose corticosteroids throughout the trial
- Patients are randomized 2:1 to etrasimod and placebo
- The treat-through design of the GLADIATOR UC trial does not re‑randomize patients at the transition from induction to maintenance
- Patients are eligible to enter an open-label extension and receive investigational drug for up to 5 years
ClinicalTrials.gov: NCT04607837, NCT03950232PHASE 2ENROLLING
VOYAGE is a Phase 2 dose-ranging clinical trial evaluating the safety and efficacy of once-daily, oral etrasimod in adult patients with eosinophilic esophagitis (EoE).
- Patients are randomized 3:3:2 to etrasimod 1 mg, etrasimod 2 mg, and placebo for a 24-week double-blind treatment period
- During the 28-week extended treatment period, patients in the etrasimod groups continue etrasimod, while patients in the placebo group are re‑randomized to one of the etrasimod dose groups
ClinicalTrials.gov: NCT04682639PHASE 2/3RECRUITING
CULTIVATE is a Phase 2/3 clinical trial program evaluating the efficacy and safety of once-daily, oral etrasimod in patients with moderately to severely active Crohn’s disease (CD).
- The CULTIVATE clinical trial program is designed as a Phase 2/3 program to facilitate an operationally seamless transition from the Phase 2 portion of the study to the Phase 3 portion
- The operationally seamless design helps ensure continuity for patients, investigators, and study staff, and maintains patient access to investigational study drug throughout the development process
ClinicalTrials.gov: NCT04173273 PHASE 3ENROLLMENT COMPLETE
ELEVATE UC is a Phase 3 program that includes ELEVATE 52, a 52-week induction and maintenance study, and ELEVATE 12, a 12‑week induction study. The ELEVATE UC program is evaluating the efficacy and safety of once-daily, oral etrasimod in patients with moderately to severely active UC.
- Patients can remain on 5-aminosalicylic acid (5-ASA) and low-dose corticosteroids throughout the trial
- Patients are randomized 2:1 to etrasimod and placebo
- The treat-through design of the ELEVATE 52 trial does not re‑randomize patients at the transition from induction to maintenance
- Patients are eligible to enter an open-label extension and receive the investigational drug for up to 5 years
ClinicalTrials.gov: NCT03945188, NCT03996369, NCT03950232 PHASE 2COMPLETE
OASIS was a Phase 2 12‑week randomized, placebo-controlled trial evaluating the safety and efficacy of two doses of
- Patients were randomized 1:1:1 to etrasimod 1 mg, etrasimod 2 mg, or placebo
- Patients who completed the 12‑week induction study were eligible to enter an open-label extension study of up to 40 weeks’ duration
ClinicalTrials.gov: NCT02447302, NCT02536404Etrasimod key references
Etrasimod, a novel sphingosine-1-phosphate (S1P) receptor modulator, lacks functional activity at S1P2 receptors
ASPET, 2017
Etrasimod (APD334), an oral, next-generation sphingosine-1-phosphate receptor modulator inhibits the development of colitis in lymphoid-null mice injected with colitogenic CD4+ T cells
ASPET, 2017Functional activity of etrasimod and a diverse panel of sphingosine-1-phosphate receptor (S1PR) modulators at S1P4 receptors
ASPET, 2017Preclinical safety assessment of etrasimod (APD334), an oral sphingosine-1-phosphate receptor (S1P) modulator with a favorable profile
AIBD, 2016The sphingosine-1-phosphate receptor (S1P) modulator etrasimod (APD334) demonstrates limited effects on heart rate in preclinical testing
AIBD, 2016Mass balance, metabolic disposition, and pharmacokinetics of [14C]etrasimod following oral administration to healthy male volunteers
AAPS PharmSci 360, 2019Safety, pharmacokinetics and pharmacodynamics of etrasimod (APD334), an oral, selective S1P receptor modulator, after single dose escalation in healthy volunteers
AIBD, 2016Etrasimod (APD334), a potent, selective, oral S1P receptor modulator with preclinical autoimmune disease-modifying activity exhibits favorable PK/PD properties in healthy volunteers
AIBD, 2016Safety, tolerability and lymphocyte-lowering properties of etrasimod (APD334), an oral, potent, next-generation, selective S1P receptor modulator, after dose escalation in healthy volunteers
ECCO, 2017Early and durable symptom control in patients with moderately-to-severely active ulcerative colitis treated with etrasimod (APD334) in the randomized, double-blind, placebo-controlled, phase 2 OASIS trial and open-label extension
ACG, 2020Early and durable symptom control in patients with moderately-to-severely active ulcerative colitis treated with etrasimod (APD334) in the randomised, double-blind, placebo-controlled, phase 2 OASIS trial and open-label extension
UEG, 2020Histologic remission and mucosal healing in a randomized, placebo-controlled, phase 2 study of etrasimod in patients with moderately to severely active ulcerative colitis
DDW, 2019Histological remission and mucosal healing in a randomised, placebo-controlled, phase 2 study of etrasimod in patients with moderately to severely active ulcerative colitis
ECCO, 2019 (J Crohns Colitis, 2019)Effect of etrasimod on circulating lymphocyte subsets: data from a randomized phase 1 study in healthy Japanese and Caucasian men
Am J Gastroenterol, 2020Effect of etrasimod on circulating lymphocyte subsets: data from a randomized phase 1 study in healthy Japanese and Caucasian men
DDW, 2021DOP078: Pharmacology and safety of etrasimod (APD334), an oral, potent, next-generation , selective S1P receptor modulator
ECCO, 2017DOP077: Immunomodulatory effects of etrasimod (APD334), an oral, potent, next-generation , selective S1P receptor modulator
ECCO, 2017Safety and immune modulatory properties of etrasimod (APD334), a next-generation oral, selective sphingosine 1-phosphate receptor modulator, in healthy volunteers
ECCO, 2018Pharmacokinetics and circulating total lymphocyte count pharmacodynamic response from single and multiple oral doses of etrasimod in Japanese and Caucasian healthy male subjects
J Crohns Colitis, 2020Pharmacokinetics and circulating total lymphocyte count pharmacodynamic response from single and multiple oral doses of etrasimod in Japanese and Caucasian healthy male subjects
ECCO, 2020Faecal calprotectin and C-reactive protein levels are correlated with long term clinical and endoscopic outcomes: analysis of the OASIS open label extension trial of etrasimod for ulcerative colitis
ECCO, 2020Fecal calprotectin and C-reactive protein levels are correlated with long term clinical and endoscopic outcomes: analysis of the OASIS open label extension trial of etrasimod for ulcerative colitis
DDW, 2020Correlation of fecal calprotectin and C-reactive protein concentrations with clinical outcomes and endoscopic disease activity in patients with ulcerative colitis receiving induction therapy with etrasimod
Gastroenterology, 2019Correlation of fecal calprotectin and C-reactive protein concentrations with clinical outcomes and endoscopic disease activity in patients with ulcerative colitis receiving induction therapy with etrasimod
DDW, 2019Pharmacokinetics, safety, and tolerability of etrasimod (APD334) in subjects with mild, moderate, or severe hepatic impairment: a single-dose, open-label, parallel-group study
J Crohns Colitis, 2021Pharmacokinetics, safety, and tolerability of etrasimod (APD334) in participants with mild, moderate, or severe hepatic impairment: a single-dose, open-label, parallel-group study
ECCO, 2021Pharmacokinetics, safety, and tolerability of etrasimod (APD334) in subjects with mild, moderate, or severe hepatic impairment: a single-dose, open-label, parallel-group study
UEG, 2021Steady-state trough concentrations and their relationship to selected demographic and clinical response measures in etrasimod-treated patients with moderately-to-severely active ulcerative colitis
WCOG, 2019Steady-state trough concentrations and their relationship to selected demographic and clinical response measures in etrasimod-treated patients with moderately-to-severely active ulcerative colitis
NASPGHAN, 2019Receptor profile and efficacy of etrasimod (APD334), an oral, next-generation sphingosine-1-phosphate receptor modulator in development for ulcerative colitis
UEG, 2016Long-term efficacy and safety of etrasimod for ulcerative colitis: results from the open-label extension of the OASIS study
UEG, 2019Long-term safety and efficacy of etrasimod for ulcerative colitis: results from the open-label extension of the OASIS study
J Crohns Colitis, 2021Efficacy and safety of etrasimod in a phase 2 randomized trial of patients with ulcerative colitis
Gastroenterology, 2020The selective sphingosine 1-phosphate receptor modulator etrasimod regulates lymphocyte trafficking and alleviates experimental colitis
J Pharmacol Exp Ther, 2019Sphingosine-1-phosphate lyase inhibition alters the S1P gradient and ameliorates Crohn’s-like ileitis by suppressing thymocyte maturation
Inflamm Bowel Dis, 2020Etrasimod improves quality of life in adults with moderate-to-severe ulcerative colitis: results from the phase 2 OASIS trial and open-label extension
UEG, 2021
