Data shared at the 13th
Phase III program with OTEZLA (apremilast) in ulcerative colitis expected to begin in 2018
In the study, a total of 170 patients were randomized to placebo,
apremilast 40 mg BID or apremilast 30 mg BID. The primary endpoint of
the study was Total
"The achievement of clinical remission, which requires endoscopic
improvement of the mucosa, is a meaningful goal in the treatment of
ulcerative colitis," said presenting author
Clinical remission as measured by Partial
Additional secondary endpoints examined in the trial, including endoscopic remission (Mayo Endoscopic Score ≤1), TMS clinical response, serum biomarkers and mucosal healing (combined endoscopic and histologic remission), showed clinically meaningful improvements for apremilast 30 mg BID versus placebo.
"The strength of these data advances our plans to initiate a phase III
program for OTEZLA® (apremilast) 30 mg in ulcerative
Treatment-emergent adverse events reported in at least 5 percent of patients treated with apremilast included headache (23 percent with apremilast 30 mg BID, 26 percent with apremilast 40 mg BID and 7 percent with placebo); viral upper respiratory tract infection (9 percent, 4 percent and 2 percent, respectively); nausea (5 percent, 11 percent and 9 percent); abdominal pain (5 percent, 2 percent and 2 percent); back pain (0 percent, 6 percent and 2 percent); and asthenia (5 percent, 2 percent and 3 percent).
Apremilast is not approved for the treatment of ulcerative colitis in
any country. In
About Ulcerative Colitis
Ulcerative colitis is a chronic, relapsing condition triggered by an abnormal, prolonged immune response that creates long-lasting inflammation and ulcers (sores) in the mucosa (lining) of the large intestine (colon). Symptoms usually develop over time, rather than suddenly. The disease can be debilitating and can sometimes lead to life-threatening complications. Ulcerative colitis is the most common form of inflammatory bowel disease worldwide. About one in every 198 people in Europe and one in every 402 people in North America have ulcerative colitis. In 2004, 2.1 million prescriptions were written to treat ulcerative colitis, and 716,000 ambulatory care visits were related to the disease. In 2010, there were 107,000 hospitalizations due to ulcerative colitis.
OTEZLA® (apremilast) 30 mg tablets is an oral small-molecule inhibitor of phosphodiesterase 4 (PDE4) specific for cyclic adenosine monophosphate (cAMP). PDE4 inhibition results in increased intracellular cAMP levels, which is thought to indirectly modulate the production of inflammatory mediators. The specific mechanism(s) by which OTEZLA exerts its therapeutic action in patients is not well defined.
OTEZLA® (apremilast) is indicated for the treatment of patients with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.
OTEZLA is indicated for the treatment of adult patients with active psoriatic arthritis.
IMPORTANT SAFETY INFORMATION
OTEZLA® (apremilast) is contraindicated in patients with a known hypersensitivity to apremilast or to any of the excipients in the formulation
Warnings and Precautions
Diarrhea, Nausea and Vomiting: Cases of severe diarrhea, nausea, and vomiting were associated with the use of OTEZLA. Most events occurred within the first few weeks of treatment. In some cases, patients were hospitalized. Patients 65 years of age or older and patients taking medications that can lead to volume depletion or hypotension may be at a higher risk of complications from severe diarrhea, nausea, or vomiting. Monitor patients who are more susceptible to complications of diarrhea or vomiting; advise patients to contact their healthcare provider. Consider OTEZLA dose reduction or suspension if patients develop severe diarrhea, nausea, or vomiting
Depression: Carefully weigh the risks and benefits of treatment with OTEZLA for patients with a history of depression and/or suicidal thoughts/behavior, or in patients who develop such symptoms while on OTEZLA. Patients, caregivers, and families should be advised of the need to be alert for the emergence or worsening of depression, suicidal thoughts or other mood changes, and they should contact their healthcare provider if such changes occur
Psoriasis: Treatment with OTEZLA is associated with an increase in depression. During clinical trials, 1.3% (12/920) of patients reported depression compared to 0.4% (2/506) on placebo; Depression was reported as serious in 0.1% (1/1308) of patients exposed to OTEZLA, compared to none in placebo-treated patients (0/506). Suicidal behavior was observed in 0.1% (1/1308) of patients on OTEZLA, compared to 0.2% (1/506) on placebo. One patient treated with OTEZLA attempted suicide; one patient on placebo committed suicide
Psoriatic Arthritis: Treatment with OTEZLA is associated with an increase in depression. During clinical trials, 1.0% (10/998) reported depression or depressed mood compared to 0.8% (4/495) treated with placebo. Suicidal ideation and behavior was observed in 0.2% (3/1441) of patients on OTEZLA, compared to none in placebo treated patients. Depression was reported as serious in 0.2% (3/1441) of patients exposed to OTEZLA, compared to none in placebo treated patients (0/495). Two patients who received placebo committed suicide compared to none on OTEZLA
Weight Decrease: Monitor body weight regularly; evaluate unexplained or clinically significant weight loss, and consider discontinuation of OTEZLA
Psoriasis: Body weight loss of 5-10% occurred in 12% (96/784) of patients treated with OTEZLA and in 5% (19/382) of patients treated with placebo. Body weight loss of ≥10% occurred in 2% (16/784) of patients treated with OTEZLA compared to 1% (3/382) of patients treated with placebo
Psoriatic Arthritis: Body weight loss of 5-10% was reported in 10% of patients taking OTEZLA and in 3.3% of patients taking placebo.
Drug Interactions: Apremilast exposure was decreased when OTEZLA was
co-administered with rifampin, a strong
Psoriasis: Adverse reactions reported in ≥5% of patients were (OTEZLA%, placebo%): diarrhea (17, 6), nausea (17, 7), upper respiratory tract infection (9, 6), tension headache (8, 4), and headache (6, 4)
Psoriatic Arthritis: Adverse reactions reported in at least 2% of patients taking OTEZLA, that occurred at a frequency at least 1% higher than that observed in patients taking placebo, for up to 16 weeks (after the initial 5-day titration), were (OTEZLA%, placebo%): diarrhea (7.7, 1.6); nausea (8.9, 3.1); headache (5.9, 2.2); upper respiratory tract infection (3.9, 1.8); vomiting (3.2, 0.4); nasopharyngitis (2.6, 1.6); upper abdominal pain (2.0, 0.2)
Use in Specific Populations
Pregnancy and Nursing Mothers: OTEZLA is Pregnancy Category C; it has not been studied in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether apremilast or its metabolites are present in human milk. Caution should be exercised when OTEZLA is administered to a nursing woman
Renal Impairment: OTEZLA dosage should be reduced in patients with severe renal impairment (creatinine clearance less than 30 mL/min); for details, see Dosage and Administration, Section 2, in the Full Prescribing Information
Please click here for Full Prescribing Information.
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Patrick E. Flanigan III, 908-673-9969
Corporate Vice President, Investor Relations
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