Rolapitant hydrochloride

Rolapitant Hydrochloride is the hydrochloride salt form of Rolapitant. It is a centrally-acting, selective, neurokinin 1 receptor antagonist with potent antiemetic activity. It also prevents both SP-induced emesis and chemotherapy-induced nausea and vomiting. It also plays a key role in inducing nausea and vomiting caused by emetogenic cancer chemotherapy. It has both, rapid onset of action and a significantly longer half-life. Rolapitant hydrochloride is sold under the trade name Varubi in the US and Varuby in the European Union. Tesoro inc originally developed and licensed Rolapitant hydrochloride for clinical development to act as a selective NK1 receptor antagonist in 2015. It has been approved for treating chemotherapy-induced nausea and vomiting and is equally safe and effective as other medicines of its class. Rolapitant hydrochloride liquid for intravenous use has been discontinued in the United States.

Dosage and Administration

Rolapitant hydrochloride is given before starting each cycle but at no less than 2-week intervals. In the cases of highly emetogenic cisplatin-based chemotherapy, the dose is 180mg, given 2hrs prior to chemotherapy with dexamethasone 20mg, given 30mins prior to chemotherapy, and a 5-HT3 receptor ­antagonist on Day 1. This is followed by a dose of dexamethasone 8mg, taken twice daily, on Days 2–4 of the chemotherapy. For treating moderately emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide, the dose is set at 180mg, given 2hrs prior to chemotherapy with dexamethasone 20mg, given 30mins prior to chemotherapy on Day 1, and a 5-HT3 receptor antagonist on Days 1–4 of the chemotherapy. The Price of Rolapitant hydrochloride In the USA, the consumer pays around $317 for an intravenous emulsion containing166.5 mg per 92.5 mL, for a supply of 92.5 milliliters and the average cost of 90mg tablet is USD280.

How does it work?

Rolapitant blocks the activity of the NK1-receptor by competitively binding to it the central nervous system. By blocking receptors in the body that play a role in vomiting and nausea called neurokinin (NK)-1 receptors located in the brain stem, thus providing relief from the symptoms.

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