Sancuso

Antiemesis via transdermal delivery

COMPANY: ProStrakan Inc.

PHARMACOLOGIC CLASS: Antiemetic (5-HT3 receptor blocker)

ACTIVE INGREDIENT: Granisetron 3.1mg/24hrs; transdermal delivery system (patch).

INDICATION: Prevention of nausea and vomiting in patients receiving moderately and/or highly emetogenic chemotherapy regimens of up to 5 consecutive days duration.

PHARMACOLOGY: Sancuso uses a transdermal patch system to deliver the antiemetic, granisetron, to the systemic circulation via passive diffusion. The absorption of drug from the patch is variable from patient to patient. A week after applying Sancuso daily in healthy subjects, there was a high intersubject variability in systemic exposure. Maximal concentration was reached at approximately 48 hours after patch application. Granisetron is a selective 5–hydroxytryptamine3 (5-HT3) receptor antagonist with little or no affinity for other serotonin receptors. Receptor sites for 5–hydroxytryptamine3 are located on vagal nerve terminals and in the chemoreceptor trigger zone in the brain. During emetogenic chemotherapy, mucosal enterochromaffin cells release serotonin, which stimulates 5-HT3 receptors, inducing vomiting. By blocking these 5-HT3 receptors, granisetron reduces emesis due to chemotherapy regimens.

CLINICAL TRIALS: A Phase 3 randomized, parallel group, double-blind, doubledummy study involving 641 patients was conducted to evaluate the effectiveness of Sancuso in the prevention of chemotherapy-induced nausea and vomiting. The efficacy of Sancuso was compared to that of oral granisetron 2mg once daily in the prevention of nausea and vomiting in patients receiving multiple- day chemotherapy. The primary endpoint was the proportion of patients with no vomiting and/or retching, no more than mild nausea, and no rescue medication from the first dose until 24 hours after the start of the last day’s chemotherapy dose. Sancuso was applied 24-to-48 hours before the first dose of chemotherapy, and was left on for 7 days. Oral granisetron was administered daily 1 hour before each dose of chemotherapy. The patch formulation was effective in 60.2% of patients and the oral administration of granisetron was effective in 64.8% of patients.

ADULTS: ≥18yrs: apply 1 patch to clean, dry, intact healthy skin on upper outer arm 24-to-48 hours before chemotherapy; remove at least 24 hours after chemotherapy is completed. May wear patch for up to 7 days. Do not cut patch.

CHILDREN: <18yrs: not recommended.

PRECAUTIONS: May mask progressive ilieus and/or gastric distention. Avoid direct sun or UV light (cover patch with clothing during use and for 10 days after removing patch). Pregnancy (Cat.B). Nursing mothers.

INTERACTIONS: Do not take with other granisetron products.

ADVERSE REACTIONS: Constipation; local irritation (remove patch if severe or if generalized skin reaction occurs), headache.

NOTE: Report suspected adverse events to Sancuso at (800) Sancuso or FDA at (800) FDA-1088.

HOW SUPPLIED: Patch—1 For more information call (800) Sancuso or visit www.Sancuso.com.