Trade name Varubi.
A drug which acts as a selective NK1 receptor antagonist (antagonist for the NK1 receptor).
Approved as a medication for the treatment of chemotherapy-induced nausea and vomiting (CINV) after clinical trials showed it to have similar or improved efficacy and some improvement in safety over existing drugs.
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.
An injectable emulsion in combination with other antiemetics in adults to prevent delayed emetogenic chemotherapy-induced nausea and vomiting 25 to 120 hours after chemotherapy dosing.
A highly selective and competitive antagonist of human substance P/neurokinin 1 (NK-1) receptors.
This receptor is involved in delayed CINV,
It has a 7-day half-life in plasma.
IV formulation is comparable to the oral formulation.
Adding oral rolapitant at 180 mg to an antiemetic regimen of granisetron and dexamethasone significantly improved complete response rates in the delayed phase of CINV among patients undergoing highly emetogenic cisplatin-based chemotherapy, compared with granisetron and dexamethasone without rolapitant, 73% vs 58%.
Associated with a significant reduction in the number of episodes of vomiting and the use of rescue medication during the delayed phase following chemotherapy administration.
Associated with less disruption of daily life by nausea.
Most NK-1 receptor antagonist doses are administered intravenously
In the bioequivalence study of patients assigned to receive 166.5-mg IV rolapitant or 180-mg oral rolapitant, the safety profile was similar.
The most common adverse events are: neutropenia, hiccups, loss of appetite, and dizziness.
Infusion-related symptoms included warm sensations, abdominal pain, dizziness, and peripheral paresthesia.
Should not be used in patients treated with CYP3A4 inducers like rifampin, and digoxin concentrations should be monitored when administered concomitantly, in case dosage adjustments are required.