Evomax

Overview

International: Goofice

Indications

Chronic Constipation

Contraindications

Patients with medical history of hypersensitivity to the ingredients of Elobixibat. • Patients with a documented intestinal obstruction associated with a tumor or hernia or with the suspicion of such conditions. (Intestinal obstruction may be aggravated.)

Adverse Effects

Adverse reactions, including laboratory abnormalities, were reported in 292/631 patients (46.3%) from clinical studies conducted until the approval. Major adverse reactions include abdominal pain in 120 patients (19.0%) and diarrhoea in 99 patients (15.7%).

Special Warnings & Precautions

Elobixibat may cause abdominal pain or diarrhoea; dose reduction, drug withdrawal or discontinuation should be considered depending on the patient’s symptoms and the need for continuing treatment with Elobixibat should be carefully evaluated on a regular basis to avoid continuing aimless administration.

Mechanism of Action

Elobixibat inhibits bile acid reabsorption via ileal bile acid transporter (IBAT) expressed on the epithelial cells of the terminal ileum and thereby increases the amount of bile acid passing into the large intestinal lumen. Bile acid promotes the secretion of water and electrolytes into the large intestinal lumen. Bile acid promotes the secretion of water and electrolytes into the large intestinal lumen and enhances the colonic motility. Therefore, Elobixibat induces the therapeutic effect on constipation.

Pharmacokinetics

Absorption: A single oral dose of Elobixibat Tablets 5 mg, 10 mg or 15 mg was administered to patients with chronic constipation before breakfast and the pharmacokinetic parameters were noted in 5 mg tablets Cmax (pg/mL) 186.8±87.1, AUC0-∞ (pg•h/mL) 837.8±572.9, Tmax (h) 1.8±1.6, t1/2 (h) 3.3±3.1 Distribution: In vitro human plasma protein binding rate of elobixibat was in excess of 99% with human blood to plasma concentration ratio less than 5%. Metabolism: Unchanged and monohydroxy forms of elobixibat were found in feces pooled over 24 to 48 hours post-dose, while the percentages of radioactivity were 96.06% and 3.16%, respectively, indicating that the majority was unchanged form. Excretion: When a single oral dose of Elobixibat Tablets 5 mg was administered to patients with chronic constipation under fasting conditions, the cumulative urine drug excretion rate up to 144 hours post-dose was approximately 0.01% of the amount of dose, indicating that drug excretion into urine was almost absent.

Drug Use in Pregnancy

Elobixibat should be used in pregnant women and women who may possibly be pregnant only if the expected therapeutic benefits outweigh the possible risks associated with treatment.