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FDA Approval for Two Antiemetics

doi: 10.1097/01.COT.0000471994.26363.60
FDA Updates
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Varubi (Rolapitant)

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The U.S. Food and Drug Administration has approved the use of Varubi (rolapitant) in combination with other antiemetic agents for adults to prevent delayed-phase chemotherapy-induced nausea and vomiting. Varubi is a selective and competitive antagonist of human substance P/neurokinin 1 (NK-1) receptors with a plasma half-life of approximately seven days.

Activation of NK-1 receptors is known to play a central role in nausea and vomiting induced by certain cancer chemotherapies, particularly in the delayed phase.

This approach “Chemotherapy-induced nausea and vomiting remains a major issue that can disrupt patients' lives and sometimes their therapy,” Amy Egan, MD, MPH, Deputy Director of the Office of Drug Evaluation III in the FDA's Center for Drug Evaluation and Research, said in a news release. “This approval provides cancer patients with another treatment option for the prevention of the delayed phase of nausea and vomiting caused by chemotherapy.”

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Varubi, marketed by Tesaro Inc., is approved for the treatment of nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, both emetogenic and highly emetogenic. The drug is a 180 milligram oral tablet that should be administered approximately one to two hours prior to chemotherapy administration in combination with a 5-HT3 receptor antagonist and dexamethasone.

Varubi's safety and efficacy were evaluated in three randomized, double-blind, controlled clinical trials that, combined, included 2,800 patients receiving highly or moderately emetogenic chemotherapy drugs. Patients received Varubi in combination with granisetron and dexamethasone or they received a combination of granisetron, dexamethasone, and placebo. Patients treated with Varubi combination had greater reduction in vomiting and need for rescue medication for nausea and vomiting during the delayed phase compared with the patients receiving the placebo combination.

Varubi inhibits the CYP2D6 enzyme, which is responsible for metabolizing certain drugs. Varubi is contraindicated with the use of thioridazine, a drug metabolized by the CYP2D6 enzyme, because use of the two drugs together may increase the amount of thioridazine in the blood and cause an abnormal heart rhythm that can be serious.

The most common side effects in patients treated with Varubi are neutropenia, hiccups, decreased appetite, and dizziness.

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Emend (Aprepitant): New Indication

The agency also approved the use of Emend (aprepitant) capsules for use in combination with other antiemetic agents for the prevention of acute and delayed chemotherapy-induced nausea and vomiting in patients as young as 12, as well as for patients younger than 12 who weigh at least 30 kg (about approximately 66 pounds).

Emend, a substance P/neurokinin 1 (NK1) receptor antagonist, marketed by Merck, is approved for chemotherapy-induced nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (including high-dose cisplatin), as well as moderately emetogenic cancer chemotherapy.

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With this approval, Emend becomes the first and only NK1 receptor antagonist to be approved for the prevention of the acute and delayed phases of chemotherapy-induced nausea and vomiting in patients ages 12 to 17, and those younger than 12 who weigh at least 30 kg.

Emend was previously approved for adults for use in combination with other anti-nausea and anti-vomiting drugs for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of chemotherapy known to cause these problems (OT 5/10/03 issue).

The drug is known to have little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting.

The safety and efficacy for this expanded approval for Emend were evaluated in a randomized, double-blind, active-comparator-controlled clinical study that assessed Emend used in combination with ondansetron compared with ondansetron alone in 63 patients age 12 to 17 and 69 patients younger than 12 who weighed at least 30 kg, all of whom were receiving either highly or moderately emetogenic chemotherapy.

The most common adverse reactions were neutropenia, headache, diarrhea, decreased appetite, cough, fatigue, hemoglobin decreased, dizziness, and hiccups.

Emend is contraindicated in patients with any known sensitivity to any component of this drug, as well as in patients taking pimozide.

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Clinical Quick Facts: Varubi

Drug: Varubi (rolapitant)

Approved Indication: Use in combination with other antiemetic agents for adults to prevent delayed-phase chemotherapy-induced nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, both emetogenic and highly emetogenic

Common Side Effects: Neutropenia, hiccups, decreased appetite, and dizziness

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Clinical Quick Facts: Emend

Drug: Emend (aprepitant)

Approved Indication: Treatment in combination with other antiemetic agents for the prevention of acute and delayed chemotherapy-induced nausea and vomiting in patients as young as 12, as well as for patients younger than 12 who weigh at least 30 kg (i.e., about 66 pounds)

Common Side Effects: Neutropenia, headache, diarrhea, decreased appetite, cough, fatigue, hemoglobin decreased, dizziness, and hiccups

Copyright © 2015 Wolters Kluwer Health, Inc. All rights reserved.
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