TESARO Announces Inclusion of VARUBI(TM) (rolapitant) in NCCN(R) Antiemesis Guidelines

On September 24, 2015 TESARO, Inc. (NASDAQ:TSRO), an oncology-focused biopharmaceutical company, reported the decision of the National Comprehensive Cancer Network (NCCN) to include VARUBI (rolapitant) in the NCCN Clinical Practice Guidelines in Oncology (NCCN Guidelines) Antiemesis Version 2.2015, as a recommended option in combination with other antiemetic agents for patients receiving both high emetic risk intravenous chemotherapy (HEC) and moderate emetic risk intravenous chemotherapy (MEC) (Press release, TESARO, SEP 24, 2015, View Source [SID:1234507537]). Category 1, the highest level category of evidence and consensus, was granted to rolapitant for both HEC and MEC chemotherapy.

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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. Results from three Phase 3 trials of VARUBI demonstrated a significant reduction in episodes of vomiting or use of rescue medication during the 25 to 120 hour period following administration of highly emetogenic and moderately emetogenic chemotherapy regimens.

"Patients are at the center of all that we do, and are the reason we act with a sense of urgency and passion. We are grateful that NCCN has included VARUBI in their Antiemesis Guidelines so soon after our FDA approval, and we look forward to making VARUBI available to the patients who are at risk for delayed CINV later this fall," said Mary Lynne Hedley, Ph.D., President and COO of TESARO. "The prevention of delayed CINV represents a substantial opportunity for improving the care of patients who receive HEC and MEC."

TESARO plans to launch VARUBI in the U.S. in Q4 of 2015.

The NCCN Guidelines are a comprehensive set of guidelines detailing the sequential management decisions and interventions that currently apply to 97 percent of cancers affecting patients in the United States. The intent of the NCCN Guidelines is to assist in the decision-making process of individuals involved in cancer care—including physicians, nurses, pharmacists, payers, patients and their families—with the ultimate goal of advancing patient care in the fight against cancer.

VARUBI was approved by the U.S. Food and Drug Administration (FDA) on Sept. 2, 2015 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.

About Chemotherapy-Induced Nausea and Vomiting

Chemotherapy-induced nausea and vomiting can be a debilitating, yet often preventable, side effect of chemotherapy. Up to 50% of patients undergoing highly or moderately emetogenic chemotherapy experience delayed CINV (25 to 120 hours post chemotherapy)—even when prescribed a 5-HT3 receptor antagonist and corticosteroid.

Blocking both 5-HT3 and NK-1 receptors has been shown to offer better control of nausea and vomiting than inhibiting 5-HT3 receptors alone. Because NK-1 receptors are key drivers of CINV, especially in the delayed Phase, NK-1 receptor antagonists such as VARUBI, when combined with a 5-HT3 receptor antagonist and a corticosteroid, provide enhanced protection from CINV.

About VARUBI

VARUBI is a substance P/neurokinin-1 (NK-1) receptor antagonist indicated 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. NK-1 receptors are highly concentrated in the brain and bind neurokinin substance P. Activation of NK-1 receptors plays a central role in nausea and vomiting induced by emetogenic stimuli, including certain cancer chemotherapies. A Positron Emission Tomography (PET) study with rolapitant in normal, healthy volunteers demonstrated that rolapitant crosses the blood brain barrier and occupies brain NK-1 receptors at high levels for up to 120 hours. VARUBI has a half-life of approximately 7 days, which may contribute to the ability of a single dose of VARUBI to cover the entire delayed CINV Phase (25-120 hours).

An intravenous formulation of rolapitant is also being developed. TESARO licensed exclusive rights for the development, manufacture, commercialization and distribution of VARUBI (rolapitant) from OPKO Health, Inc.

The full prescribing information for VARUBI is available at www.VarubiRx.com.

VARUBI Additional Safety Information

VARUBI is contraindicated in patients receiving thioridazine, a CYP2D6 substrate with a narrow therapeutic index.

Use of VARUBI should be avoided in patients who are receiving pimozide, a CYP2D6 substrate with a narrow therapeutic index. Adverse reactions should be monitored if concomitant use of VARUBI and other CYP2D6 substrates with a narrow therapeutic index cannot be avoided. The inhibitory effect of VARUBI on CYP2D6 lasts for at least 7 days and may last longer after administration of a single dose of VARUBI.

The most common adverse reactions (≥5%) in clinical trials were decreased appetite, neutropenia, hiccups and dizziness.

VARUBI is available by prescription only.