UCERIS

AbsorptionDistal Ulcerative Colitis Patients Based on population pharmacokinetic analysis from sparse PK samples from phase 3 studies,the estimated AUC 0-12 following administration of UCERIS rectal foam 2 mg twice a day was 4.31 ng*hr/mL with a CV of 64% in the target patient population.

DistributionThe volume of distribution (V SS ) of budesonide varies between 2.2 and 3.9 L/kg in healthy subjects and in patients. Plasma protein binding is estimated to be 85 to 90% in the concentration range...

The safety and efficacy of UCERIS rectal foam were evaluated in 2 replicate, randomized, double-blind, placebo-controlled, multi-center trials (Studies 1 and 2). Participants in the trials were adult patients with active mild-to-moderate distal ulcerative colitis with disease extending at least 5 cm but no further than 40 cm from the anal verge (confirmed by endoscopy). To be eligible, patients had to have a Modified Mayo Disease Activity Index (MMDAI) score between 5 and 10, inclusive, a rectal bleeding subscore of 2 or 3, and an endoscopy subscore of 2 or 3. The MMDAI score ranges from 0 to ...

Serious and important adverse reactions include:

• Hypercorticism and adrenal axis suppression [see Warnings and Precautions ( 5.1 )]
• Symptoms of steroid withdrawal in those patients transferring from systemic glucocorticosteroid therapy [see Warnings and Precautions ( 5.2 )]
• Increased susceptibility to infection [see Warnings and Precautions ( 5.3 )]
• Other glucocorticosteroid effects [see Warnings and Precautions ( 5.4 )] Most common adverse reactions (≥ 2%) are decreased blood cortisol, ...

UCERIS rectal foam is contraindicated in patients with a history of a known hypersensitivity to budesonide or any of the ingredients of UCERIS rectal foam. Reactions have included anaphylaxis [see Adverse Reactions ( 6.2 )] . Known hypersensitivity to budesonide or any of the ingredients in UCERIS rectal foam. ( 4 )

• Hypercorticism and adrenal suppression: Follow general warnings concerning glucocorticosteroids. ( 5.1 )
• Impaired Adrenal Function in Patients Transferred from Other Glucocorticoids: Taper slowly from glucocorticosteroids with high systemic effects; monitor for withdrawal symptoms and unmasking of allergies (rhinitis, eczema). ( 5.2 )
• Increased Risk of Infection, including serious and fatal chicken pox and measles: Monitor patients with active or quiescent tuberculosis infection, untreated...

7 DRUG INTERACTIONS CYP3A4 Inhibitors (e.g., ketoconazole, grapefruit juice): May cause increased systemic corticosteroid effects; avoid concomitant use. ( 7.1 ) 7.1 CYP3A4 Inhibitors The active ingredient of UCERIS rectal foam, budesonide, is metabolized by CYP3A4. Inhibitors of CYP3A4 activity (such as ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, cyclosporine and g...