Lorcaserin Hydrochloride

Lorcaserin hydrochloride Basic Information

 

Product Name: Lorcaserin hydrochloride

CAS: 846589-98-8

MF: C11H15Cl2N

MW: 232.15

EINECS: 1592732-453-0

Solubility: Soluble in DMSO > 10 mM

Form: Powder

Stability: Hygroscopic

Lorcaserin hydrochloride is a serotonin 2C receptor agonist indicated for the treatment of chronic weight management in adults with a body mass index (BMI) of 30 or greater (obese) as an addition to a reduced-calorie diet and exercise. It is also approved for use by adults with a BMI of 27 or greater (overweight) and who have at least one weight-related condition such as high blood pressure (hypertension), type 2 diabetes, or high cholesterol (dyslipidemia).

Lorcaserin is an orally active, potent and selective 5-hydroxytryptamine receptor (5-HT2C) agonist (human/rat Ki = 15 /29 nM) with 18- and 104-fold higher potency than 5-HT2A and 5-HT2B by cellular inositol phosphate accumulation assay (EC50 = 9, 168, 943 nM, respectively) and good selectivity over 5-HT1A/3/4C/5A/6/7 and a panel of 67 other GPCRs and ion channels. Chronic daily treatment to rats (4.5-18 mg/kg p.o. b.i.d.) maintained on a high fat diet causes reductions in food intake and body weight gain.

Lorcaserin hydrochloride is indicated as an adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adult patients with an initial body mass index (BMI) of:

30 kg/m² or greater (obese), or 27 kg/m² or greater (overweight) in the presence of at least one weight related comorbid condition (e.g., hypertension, dyslipidemia, type 2 diabetes)

The recommended dose of BELVIQ is 10 mg administered orally twice daily. Do not exceed recommended dose.

BELVIQ can be taken with or without food.

Response to therapy should be evaluated by week 12. If a patient has not lost at least 5% of baseline body weight, discontinue BELVIQ, as it is unlikely that the patient will achieve and sustain clinically meaningful weight loss with continued treatment [see Clinical Studies].

BMI is calculated by dividing weight (in kg) by height (in meters) squared.

BMI = weight (kg)/height (m)^2

For example, if you weigh 160 pounds and are 5 foot 6 inches, or 66 inches tall, your personal formula is this: 160 divided by 66 squared (which is 4,356) times 703 equals 25.8

• Serotonin Syndrome or NMS-like Reactions
• Valvular Heart Disease
• Cognitive Impairment
• Psychiatric Disorders
• Hypoglycemia
• Heart Rate Decreases
• Hematological Changes
• Prolactin Elevation

Lorcaserin used in combination with diet and exercise, results in modest weight loss of about 12.9 lb (5.8 kg) compared with 5.6 lb (2.5 kg) with placebo.3 On average, about 47% of patients will lose at least 5% of their body weight (about 11.1 lb [5 kg]) compared with 23% of patients receiving placebo (number needed to treat [NNT] = 4). About 22% of patients will lose at least 10% of their body weight vs. 9% of patients receiving placebo (NNT = 7). This weight loss is maintained, on average, for two years. Weight loss occurs early, and those who do not lose 5% of their body weight in the first three months are unlikely to achieve 5% loss by 52 weeks. Weight loss also occurs in patients with type 2 diabetes who are not taking insulin, although not to the same extent.4 Stopping lorcaserin after one year results in an average weight gain that is within 2.2 lb (1 kg) of baseline. There is no research on the effect of lorcaserin on mortality, incidence of diabetes, or other patient-oriented outcomes.

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