Lorcaserin is an investigational product for smoking cessation. The efficacy and safety of lorcaserin for smoking cessation have not been established.
"We are pleased that this proof-of-concept trial provides what we believe is the first clinical evidence that a selective serotonin 2C agonist may have a treatment effect for smoking cessation," said
The 12-week, randomized, double-blind, placebo-controlled trial assessed the efficacy and safety of lorcaserin as a potential aid to smoking cessation. In the trial, 603 active smokers were randomized to receive lorcaserin 10 mg once daily (QD), 10 mg twice daily (BID) or placebo in a 1:1:1 ratio. Patients at baseline were dependent on nicotine and averaged 18 cigarettes per day. Patients were dosed for two weeks before attempting to quit around Day 15 of the trial and received smoking cessation counseling during the trial.
"Smoking is recognized as one of the greatest global public health challenges, but unfortunately millions of people around the world continue to smoke and find it hard to quit," said
The primary objective of the trial was assessment of smoking cessation efficacy. The carbon monoxide confirmed continuous abstinence rate (CAR), defined as no reported smoking or other nicotine use and an end-expiratory exhaled carbon monoxide measurement of less than or equal to ten parts per million, measured during the last four weeks of the trial (Weeks 9-12), was the basis for determining efficacy. The primary endpoint was achieved by 5.6%, 8.7%, and 15.3% of patients in the placebo, QD and BID groups, respectively (p-value = 0.003 and odds ratio = 3.02 for BID vs. placebo; the result for QD vs. placebo was not statistically significant).
Secondary objectives for the trial included assessment of body weight change and of safety and tolerability. At Week 12 in the MITT population, there was a statistically significant difference in weight between lorcaserin BID and placebo (-0.98 kg and -0.01 kg, respectively, p-value = 0.0004).
The overall adverse event profile appears similar to the profile in previous trials of lorcaserin, with the most common adverse events being headache, nausea, constipation, dizziness and dry mouth.
According to the
About Lorcaserin for Smoking Cessation
Internally discovered at Arena, lorcaserin is believed to selectively activate serotonin 2C receptors in the brain. Preclinical data suggest that serotonin 2C receptors may modulate the mesolimbic dopaminergic reward system. The exact mechanism of action of lorcaserin is not known.
About BELVIQ® (lorcaserin HCl) CIV for Chronic Weight Management
Lorcaserin is marketed in
BELVIQ is believed to decrease food consumption and promote satiety by selectively activating serotonin 2C receptors in the brain. The exact mechanism of action of BELVIQ is not known.
IMPORTANT SAFETY INFORMATION
- BELVIQ should not be taken during pregnancy or by women who are planning to become pregnant.
Warnings and Precautions
- BELVIQ is a serotonergic drug. The development of potentially life-threatening serotonin syndrome or Neuroleptic Malignant Syndrome (NMS)-like reactions have been reported during use of serotonergic drugs, including, but not limited to, selective serotonin-norepinephrine reuptake inhibitors, and selective serotonin reuptake inhibitors, tricyclic antidepressants, bupropion, triptans, dietary supplements such as St. John's Wort and tryptophan, drugs that impair metabolism of serotonin (including monoamine oxidase inhibitors), dextromethorphan, lithium, tramadol, antipsychotics or other dopamine antagonists, particularly when used in combination. Patients should be monitored for the emergence of serotonin syndrome symptoms or NMS-like reactions, including agitation, hallucinations, coma, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, diarrhea, and muscle rigidity. Treatment with BELVIQ and any concomitant serotonergic or antidopaminergic agents should be discontinued immediately if the above events occur, and supportive symptomatic treatment should be initiated.
- Patients should not take BELVIQ in combination with drugs that have been associated with valvular heart disease (e.g., cabergoline). In clinical trials, 2.4% of patients taking BELVIQ and 2.0% of patients taking placebo developed valvular regurgitation: none of these patients was symptomatic. BELVIQ should be used with caution in patients with congestive heart failure (CHF). Patients who develop signs and symptoms of valvular heart disease, including dyspnea, dependent edema, CHF, or a new cardiac murmur, should be evaluated and discontinuation of BELVIQ should be considered.
- Impairment in attention, memory, somnolence, confusion, and fatigue, have been reported in patients taking BELVIQ. Patients should not drive a car or operate heavy machinery until they know how BELVIQ affects them.
- The recommended dose of 10 mg twice daily should not be exceeded, as higher doses may cause euphoria, hallucination, and dissociation. Monitor patients for the development or worsening of depression, suicidal thoughts or behaviors, and/or any changes in mood. Discontinue BELVIQ in patients who develop suicidal thoughts or behaviors.
- Weight loss may increase the risk of hypoglycemia in patients with type 2 diabetes mellitus who are being treated with antidiabetic medications, so measurement of blood sugar levels before and during treatment with BELVIQ is recommended. Decreases in doses of antidiabetic medications or changes in medication regimen should be considered.
- Men who experience priapism should immediately discontinue BELVIQ and seek emergency medical attention. BELVIQ should be used with caution with erectile dysfunction medications. BELVIQ should be used with caution in men who have conditions that might predispose them to priapism (e.g., sickle cell anemia, multiple myeloma, or leukemia), or in men with anatomical deformation of the penis (e.g., angulation, cavernosal fibrosis, or Peyronie's disease).
- Because BELVIQ may cause a slow heartbeat, it should be used with caution in patients with a history of bradycardia or heart block greater than first degree.
- Consider monitoring for CBC changes, prolactin excess, and pulmonary hypertension.
Most Common Adverse Reactions
- In patients without diabetes: headache (17%), dizziness (9%), fatigue (7%), nausea (8%), dry mouth (5%), and constipation (6%).
- In patients with diabetes: hypoglycemia (29%), headache (15%), back pain (12%), cough (8%), and fatigue (7%).
- BELVIQ should not be taken by women who are nursing.
BELVIQ is a federally controlled substance (CIV) because it may be abused or lead to drug dependence.
Arena is embracing the challenge of improving health by seeking to bring innovative medicines targeting G protein-coupled receptors to patients. Arena's internally discovered drug, BELVIQ® (lorcaserin HCl), is approved in
Certain statements in this press release are forward-looking statements that involve a number of risks and uncertainties. Such forward-looking statements include statements about the advancement, therapeutic indication, use, safety, efficacy, mechanism of action, and potential of BELVIQ or lorcaserin, including as a potential aid for smoking cessation; significance of the top-line results from the Phase 2 trial investigating lorcaserin for smoking cessation, including in advancing knowledge about lorcaserin and its potential development; future presentation of the trial results; a selective serotonin 2C agonist's treatment effect for smoking cessation; evaluation of the full data set and determining next steps regarding further development of lorcaserin for smoking cessation; rights, obligations and activities under the marketing and supply agreement among Arena and
Type Press Release
Date Released November 03, 2014