Varubi™ (Rolapitant) — New Drug Approval

Varubi™ (rolapitant) — New Drug Approval

• On September 2, 2015, Tesaro announced the FDA approval of Varubi (rolapitant) in combination with other antiemetic agents in adults, for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

• Nausea and vomiting are common side effects experienced by cancer patients undergoing chemotherapy. Symptoms can persist for days after the chemotherapy drugs are administered.

— The delayed phase of nausea and vomiting occurs from 24 hours to 120 hours after the start of chemotherapy. It can result in serious health complications.

— Prolonged nausea and vomiting can lead to weight loss, dehydration, and malnutrition resulting in hospitalization.

• Varubi contains rolapitant, a substance P/neurokinin-1 (NK-1) receptor antagonist. Activation of NK-1 receptors plays a central role in nausea and vomiting induced by certain cancer chemotherapies, particularly in the delayed phase.

— Emend (aprepitant) is also an approved substance P/NK-1 receptor antagonist used for the prevention of chemotherapy induced nausea and vomiting. Currently, Emend is a brand-only product.

• The efficacy and safety of Varubi were established in three clinical trials involving 2,800 patients, comparing Varubi in combination with granisetron plus dexamethasone vs. placebo plus granisetron and dexamethasone.

— During the delayed phase of nausea and vomiting, patients treated with Varubi had a greater reduction in vomiting and use of rescue medication compared to the placebo group.

• Varubi is contraindicated in patients receiving thioridazine, a CYP2D6 substrate. A significant increase in plasma concentrations of thioridazine may result in QT prolongation and Torsades de Pointes.

• The warning and precaution of Varubi include interaction with CYP2D6 substrates with a narrow therapeutic index.

• In cisplatin-based highly emetogenic chemotherapy, the most common adverse reactions (≥ 5%) with Varubi use were neutropenia and hiccups.

• In moderately emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide, the most common adverse events (≥ 5%) with Varubi use were decreased appetite, neutropenia, and dizziness.

• The recommended oral dose of Varubi is 180 mg administered approximately 1 to 2 hours prior to the start of chemotherapy on day 1.

— Varubi should be given in combination with dexamethasone and a 5-HT3 receptor antagonist.

• Tesaro plans to launch Varubi in the fourth quarter of 2015. Varubi will be available as 90 mg tablets.

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