Rolapitant IV is a potent, highly selective, long-acting NK-1 receptor antagonist being developed for the prevention of delayed CINV.


TESARO is investigating whether a single dose of intravenous (IV) rolapitant is equivalent to oral rolapitant.

Mechanism of Action

Neurokinin-1 (NK-1) receptors are highly concentrated in the vomiting center of the brain, and bind a neurokinin called Substance P. Activation of NK-1 receptors by Substance P plays a central role in eliciting CINV. By blocking the interaction of Substance P at the NK-1 receptor, NK-1 receptor antagonists have demonstrated improvement in the management of nausea and vomiting experienced by patients receiving chemotherapy.

Chemotherapy-Induced Nausea and Vomiting

CINV can affect up to 90% of patients receiving chemotherapy without appropriate prevention, and can lead to dehydration, weight loss, malnutrition, hospitalization and delays in or even discontinuation of treatment.

Various antiemetic treatment guidelines recommend that NK-1 receptor antagonists be used in patients receiving highly emetogenic (cisplatin or anthracycline/cyclphosphamide) and moderately emetogenic (carboplatin) regimens.

Intravenous (IV) rolapitant is an investigational agent and, as such, has not been approved by any regulatory agencies.