Anorexiant
PREGNANCY RECOMMENDATION: Contraindicated
BREASTFEEDING RECOMMENDATION: No Human Data—Potential Toxicity
PREGNANCY SUMMARY
No reports describing the use of lorcaserin in human pregnancy have been located. The animal reproduction data suggest moderate risk, but the absence of human pregnancy experience prevents a more complete assessment of embryo–fetal risk. However, the manufacturer classifies the drug as contraindicated in pregnancy because weight loss offers no potential benefit to a pregnant woman and may result in fetal harm (1).
FETAL RISK SUMMARY
Lorcaserin is an oral selective agonist of serotonin 2C receptors that are located in the hypothalamus. It 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, and type 2 diabetes). Lorcaserin is extensively metabolized to inactive metabolites. The drug is moderately (about 70%) bound to plasma proteins and has a plasma half-life of about 11 hours (1).
Reproduction studies have been conducted in rats and rabbits. In these species, plasma exposures during organogenesis that were 44 and 19 times, respectively, the human exposure (HE) revealed no evidence of teratogenicity or embryolethality. In a separate study, rats were given the drug from gestation through postnatal day 21 with doses resulting in exposures up to about 44 times the HE. The highest dose resulted in stillborns and lower pup viability, but all doses lowered pup body weight at birth, which persisted to adulthood. However, no developmental abnormalities or effects on reproductive performance in the offspring were observed at any dose (1).
Two-year carcinogenicity studies in mice were negative. In a similar study in rats, mammary adenocarcinoma and mammary fibroadenoma occurred in females. These findings may have been associated with drug-induced changes in prolactin homeostasis and their relevance to humans is unknown. In male rats, treatment-related neoplastic changes were noted in the subcutis (fibroadenoma, Schwannoma), the skin (squamous cell carcinoma), mammary gland, and the brain (astrocytoma). Lorcaserin was not mutagenic or genotoxic in multiple assays. No effects on fertility in male and female rats were observed (1).
It is not known if lorcaserin crosses the human placenta. The molecular weight (about 197 for the free base), moderate plasma protein binding, and the long plasma half-life suggest that the drug will cross to the embryo–fetus.
BREASTFEEDING SUMMARY
No reports describing the use of lorcaserin during human lactation have been located. The molecular weight (about 197 for the free base), moderate (about 70%) plasma protein binding, and the long (about 11 hours) plasma half-life suggest that the drug will be excreted into breast milk. The effect of the exposure on a nursing infant is unknown. The most common (>5%) adverse effects in nondiabetic patients were headache, dizziness, fatigue, nausea, dry mouth, and constipation (1). If a woman is receiving lorcaserin and chooses to nurse, her infant should be monitored for these adverse effects.
Reference
1.Product information. Belviq. Arena Pharmaceuticals GmbH, 2012.