VELSIPITY (etrasimod arginine)

Etrasimod mean (SD) steady-state maximum plasma concentration (C max ) was 113 (27.5) ng/mL and area under the time concentration curve at the dosing interval (AUC tau ) was 2162 (488) ng*h/mL at the recommended dosage. Etrasimod C max and AUC are approximately dose proportional from 0.7 mg to 2 mg (0.35 times up to the recommended dosage). Etrasimod steady state is reached within 7 days with an accumulation of approximately 2- to 3-fold compared to the first dose.

AbsorptionThe median (range) ...

The efficacy of VELSIPITY was evaluated in 2 randomized, double-blind, placebo-controlled clinical studies [UC-1 (NCT03945188) and UC-2 (NCT03996369)] in adult subjects with moderately to severely active ulcerative colitis who had an inadequate response, loss of response, or intolerance to one or more of the following treatment options: oral aminosalicylates, corticosteroids, thiopurines, Janus kinase (JAK) inhibitors, or biologic therapies (e.g., TNF blocker, anti-integrin, anti-IL12/23). UC-1 was a 52-week study and UC-2 was a 12-week study. In both studies, subjects were randomized to VELSI...

The following serious adverse reactions are described elsewhere in the labeling:

• Infections [see Warnings and Precautions (5.1) ]
• Bradyarrhythmia and Atrioventricular Conduction Delays [see Warnings and Precautions (5.2) ]
• Liver Injury [see Warnings and Precautions (5.3) ]
• Macular Edema [see Warnings and Precautions (5.4) ]
• Increased Blood Pressure [see Warnings and Precautions (5.5) ]
• Fetal Risk [see Warnings and Precautions (5.6) ]
• Cutaneous Malignancies [see Warnings and Precaut...

VELSIPITY is contraindicated in patients who:

• In the last 6 months, have experienced a myocardial infarction, unstable angina pectoris, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization, or Class III or IV heart failure [see Warnings and Precautions (5.2) ] .
• Have a history or presence of Mobitz type II second-degree or third-degree AV block, sick s...

• 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. ( 5.1 )
• Bradyarrhythmia and Atrioventricular Conduction Delays : May result in a transient decrease in heart rate and AV conduction delays. Obtain a...

7 DRUG INTERACTIONS Etrasimod is primarily metabolized by CYP2C8, CYP2C9, and CYP3A4. Table 3 includes drugs with clinically important drug interactions when administered concomitantly with VELSIPITY and instructions for preventing or managing them. Consult the labeling of concomitantly used drugs to obtain further information. The effect of concomitant use of VELSIPITY with a combination of separ...