Rolapitant: a new option for chemotherapy-induced nausea and vomiting

Varuby (rolapitant) is a new NK1 antagonist licensed for the prevention of delayed nausea and vomiting associated with highly or moderately emetogenic chemotherapy.

More than half of patients treated with emetogenic chemotherapy experience delayed nausea and vomiting. | iSTOCK
More than half of patients treated with emetogenic chemotherapy experience delayed nausea and vomiting. | iSTOCK

Rolapitant is a competitive antagonist of human substance P/neurokinin 1 (NK1) receptors. It is rapidly absorbed and slowly eliminated.

Varuby is administered as a single 180mg dose (two tablets) within two hours of the start of each chemotherapy cycle, but at no less than two-week intervals, as part of a combination regimen including dexamethasone and a 5HT3 antagonist.

Highly emetogenic chemotherapy

Two phase III trials compared a rolapitant regimen (rolapitant 180mg plus iv granisetron and oral dexamethasone; n=535) with a placebo-based control regimen (placebo plus granisetron and dexamethasone; n=535) in patients receiving a highly emetogenic chemotherapy regimen including cisplatin ≥60mg/m2

The primary endpoint of both trials was complete response (defined as no emetic episodes and no use of rescue medication) in the delayed phase (>24 to 120 hours) of chemotherapy-induced nausea and vomiting.

In this phase, a significantly greater proportion of patients achieved a complete response in the rolapitant groups than in the placebo groups (71% versus 60%, p=0.0001).

Moderately emetogenic chemotherapy

Similar results were observed in a third phase III trial involving 1369 patients receiving moderately emetogenic chemotherapy including anthracycline/cyclophosphamide-based regimens, who were randomised to a rolapitant regimen (rolapitant 180mg plus oral granisetron and oral dexamethasone; n=666) or a matching placebo-based regimen (n=666).

A complete response in the delayed phase was achieved by a significantly greater proportion of patients in the rolapitant group than in the placebo group (71% versus 62%, p=0.0002).

In addition, patients who received rolapitant reported experiencing less nausea that interfered with normal daily life and fewer episodes of vomiting over multiple cycles of chemotherapy.

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