Fingolimod

The Basics

What is Fingolimod?

Used to prevent episodes of symptoms and slow the worsening of disability with relapsing-remitting forms of multiple sclerosis.

Brand names for Fingolimod

Gilenya

How Fingolimod is classified

Immunosuppressive Agents

Fingolimod During Pregnancy

Fingolimod pregnancy category

Category CNote that the FDA has deprecated the use of pregnancy categories, so for some medications, this information isn’t available. We still think it’s useful to list historical info, however, given what a common proxy this has been in the past.

What we know about taking Fingolimod while pregnant

There are no adequate and well-controlled studies in pregnant women. In oral studies conducted in rats and rabbits,, fingolimod demonstrated developmental toxicity, including teratogenicity (rats) and embryolethality, when given to, pregnant animals. In rats, the highest no-effect dose was less than the recommended human dose (RHD) of 0.5 mg/day on, a body surface area (mg/m2, ) basis. The most common fetal visceral malformations in rats included persistent truncus, arteriosus and ventricular septal defect. The receptor affected by fingolimod (sphingosine 1-phosphate receptor) is known, to be involved in vascular formation during embryogenesis. Because it takes approximately 2 months to eliminate, fingolimod from the body, potential risks to the fetus may persist after treatment ends [see Warnings and Precautions, (5.7, 5.8)]. GILENYA should be used during pregnancy only if the potential benefit justifies the potential risk to the, fetus. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to GILENYA during pregnancy. The FDA has reported some severe worsening of the disease in patients who stopped taking Fingolimod. Physicians are encouraged to enroll pregnant patients, or pregnant women may register themselves in the GILENYA pregnancy registry by calling 1-877-598-7237, sending an email to gpr@quintiles.com, or visiting www.gilenyapregnancyregistry.com. Risk Summary There are no adequate data on the developmental risk associated with the use of GILENYA in pregnant women. In oral studies conducted in rats and rabbits, fingolimod demonstrated developmental toxicity, including an increase in malformations (rats) and embryolethality, when given to pregnant animals. In rats, the highest no-effect dose was less than the recommended human dose of 0.5 mg/day on a body surface area (mg/m²) basis. The most common fetal visceral malformations in rats were persistent truncus arteriosus and ventricular septal defect. The receptor affected by fingolimod (sphingosine 1-phosphate receptor) is known to be involved in vascular formation during embryogenesis. In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%-4% and 15%-20%, respectively. The background risk of major birth defects and miscarriage for the indicated population is unknown. Clinical Considerations The possibility of severe increase in disability should be considered in women who discontinue or are considering discontinuation of GILENYA because of pregnancy or planned pregnancy. In many of the cases in which increase in disability was reported after stopping GILENYA, patients had stopped GILENYA because of pregnancy or planned pregnancy . For females planning to become pregnant, GILENYA should be stopped 2 months before conception [See Pregnancy] Data Animal Data When fingolimod was orally administered to pregnant rats during the period of organogenesis (0, 0.03, 0.1, and 0.3 mg/kg/day or 0, 1, 3, and 10 mg/kg/day), increased incidences of fetal malformations and embryo-fetal deaths were observed at all but the lowest dose tested (0.03 mg/kg/day), which is less than the recommended human dose (RHD) on a mg/m² basis. Oral administration to pregnant rabbits during organogenesis (0, 0.5, 1.5, and 5 mg/kg/day) resulted in increased incidences of embryo-fetal mortality and fetal growth retardation at the mid and high doses. The no-effect dose for these effects in rabbits (0.5 mg/kg/day) is approximately 20 times the RHD on a mg/m² basis. When fingolimod was orally administered to female rats during pregnancy and lactation (0, 0.05, 0.15, and 0.5 mg/kg/day), pup survival was decreased at all doses and a neurobehavioral (learning) deficit was seen in offspring at the high dose. The low-effect dose of 0.05 mg/kg/day is similar to the RHD on a mg/m² basis

Taking Fingolimod While Breastfeeding

What are recommendations for lactation if you're taking Fingolimod?

Although fingolimod and its active metabolite are highly bound in maternal plasma and unlikely to reach the breastmilk in large amounts, it is potentially toxic to the breastfed infant. Because there is no published experience with fingolimod during breastfeeding, expert opinion generally recommends that it should be avoided during breastfeeding, especially while nursing a newborn or preterm infant.[1][2][3][4][5] However, the manufacturer’s labeling does not recommend against its use in breastfeeding.

Maternal / infant drug levels

Although fingolimod and its active metabolite are highly bound in maternal plasma and unlikely to reach the breastmilk in large amounts, it is potentially toxic to the breastfed infant. Because there is no published experience with fingolimod during breastfeeding, expert opinion generally recommends that it should be avoided during breastfeeding, especially while nursing a newborn or preterm infant.[1][2][3][4][5] However, the manufacturer’s labeling does not recommend against its use in breastfeeding.

Possible effects of Fingolimod on milk supply

Relevant published information was not found as of the revision date.

Possible alternatives to Fingolimod

(Multiple Sclerosis) Glatiramer, Immune Globulin, Interferon Beta.