Etrasimod

DAE Class; Rx

Common Brand Names; Velsipity

• Sphingosine 1-Phosphate Receptor Modulators, Gastrointestinal

Sphingosine 1-phosphate (S1P) receptor 1 modulator; binds with high affinity to S1P receptors 1, 4, and 5

Blocks capacity of lymphocytes to egress from lymphoid organs, reducing number of lymphocytes in peripheral blood to decrease inflammation

Mechanism by which etrasimod exerts therapeutic effects in ulcerative colitis is unknown, but may involve reduction of lymphocyte migration into the intestines

Indicated for adults with moderately-to-severely active ulcerative colitis (UC)

In previous 6 months, experienced myocardial infarction, unstable angina pectoris, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or Class III or IV heart failure

History or presence of Mobitz type II second-degree or third-degree atrioventricular (AV) block, sick sinus syndrome, or sinoatrial block, unless patient has a functioning pacemaker

1-10%

Headache (6-9%)

Elevated liver tests (5-6%)

Dizziness (5%)

Arthralgia (4%)

Nausea (3-4%)

Hypertension (3%)

Urinary tract infection (3%)

Hypercholesterolemia (3%)

Urinary tract infection (3%)

Bradycardia (3%)

Herpes viral infection (2%)

Decrease in visual acuity (2.6%)

Cautions

Hypertension reported; monitor blood pressure during treatment and manage appropriately

Based on animal studies, may cause fetal harm when administered to pregnant females

Reductions in absolute forced expiratory volume over 1 second (FEV1) were observed; perform spirometric evaluation of respiratory function during therapy if clinically indicated

Pregnancy

Based on findings from animal studies, fetal harm may occur when administered to pregnant females

Lactation

• There are no data on presence of etrasimod in human milk, effects on the breastfed infants, or effects of the drug on milk production
• When orally administered to female rats during pregnancy and lactation, etrasimod was detected in the plasma of offspring, suggesting excretion of etrasimod in milk

Ulcerative Colitis

Indicated for adults with moderately-to-severely active ulcerative colitis (UC)

2 mg PO qDay

Dosage Modifications

Renal impairment

• Minimally excreted in urine; no dosage adjustment necessary

Hepatic impairment

• Mild or moderate (Child-Pugh A and B): No dosage adjustment necessary
• Severe (Child-Pugh C): Not recommended

Etrasimod