Etragut

Etragut is a sphingosine 1-phosphate receptor modulator indicated for the treatment of moderately to severely active ulcerative colitis in adults.

Dosage & Administration

The recommended dosage of Etrasimod is 2 mg orally once daily. Swallow the tablet whole, with or without food. If a dose is missed, take the missed dose at the next scheduled time; do not double the next dose.

Most common adverse reactions (incidence ≥5%) are: headache, elevated liver tests, and dizziness.

Infections
: May increase the risk of infections. Obtain a complete blood count (CBC) before initiation of treatment. Monitor for infection during treatment and for 5 weeks after discontinuation. Consider interruption of treatment if a serious infection develops. Avoid use of live attenuated vaccines during and for up to 5 weeks after treatment.
Bradyarrhythmia and Atrioventricular Conduction Delays
: May result in a transient decrease in heart rate and AV conduction delays. Obtain an
electrocardiogram (ECG) to assess for preexisting cardiac conduction abnormalities before starting treatment. Consider cardiology consultation for conduction abnormalities or concomitant use with other drugs that decrease heart rate.
Liver Injury
: Elevations of aminotransferases may occur. Obtain transaminase and bilirubin levels before initiating Etragut. Discontinue if significant liver injury is confirmed.
Macular Edema
: May increase the risk of macular edema. Obtain a baseline evaluation of the fundus, including the macula, near the start of treatment with Etragut. Periodically conduct an evaluation of the fundus, including the macula, while on therapy and any time there is a change in vision. Consider discontinuing Etragut if macular edema develops.
Increased Blood Pressure
: Monitor blood pressure during treatment.
Fetal Risk
: May cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception during treatment and for one week after stopping Etragut.
Cutaneous Malignancies
: Obtain a skin examination prior to or shortly after the start of treatment and periodically during treatment, especially if risk factors. Promptly evaluate suspicious skin lesions.
Posterior Reversible Encephalopathy Syndrome (PRES)
: If symptoms develop, obtain a physical and neurological exam, and consider MRI.
Respiratory Effects
: May cause a decline in pulmonary function. Assess pulmonary function (e.g., spirometry) if clinically indicated.
Unintended Additive Immune System Effects from Prior Treatment with Immunosuppressive or Immune-Modulating Drugs
: Consider the half-life and mode of action of prior therapies.
Immune System Effects After Stopping Etragut
: If using concomitant immunosuppressants, monitor patients for infectious complications for up to 5 weeks after the last dose of Etragut

Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1, 4, and 5 (S1P
1,4,5
). Etrasimod has minimal activity on S1P
3
(25-fold lower than C
max
at the recommended dose) and no activity on S1P
2
. Etrasimod partially and reversibly blocks the capacity of lymphocytes to egress from lymphoid organs, reducing the number of lymphocytes in peripheral blood. The mechanism by which etrasimod exerts therapeutic effects in UC is unknown but may involve the reduction of lymphocyte migration into the intestines.