Rolapitant: first global approval.

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Syed YY

Rolapitant: first global approval.

Drugs. 2015 Nov;75(16):1941-5. doi: 10.1007/s40265-015-0485-8.

PubMed ID

26467681 [ View in PubMed

]

Abstract

Rolapitant (Varubi) is an orally active neurokinin-1 receptor antagonist developed by TESARO and approved in the USA for use in combination with other antiemetic agents for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Unlike other approved agents in this class, rolapitant does not interact with cytochrome P450 (CYP) enzyme CYP3A4. It also has a long elimination half-life which means that a single dose could prevent CINV during the entire at-risk period (0-120 h). An intravenous formulation of rolapitant is under clinical development in the USA. Phase II development of rolapitant in postoperative nausea and vomiting, and cough appears to have been discontinued. This article summarizes the milestones in the development of rolapitant leading to the first approval for the prevention of CINV.

DrugBank Data that Cites this Article

Drugs

Rolapitant

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
Integrate drug-drug interactions in your software
Rolapitant Bexarotene	The metabolism of Rolapitant can be increased when combined with Bexarotene.
Rolapitant Bosentan	The metabolism of Rolapitant can be increased when combined with Bosentan.
Rolapitant Nafcillin	The metabolism of Rolapitant can be increased when combined with Nafcillin.
Rolapitant Efavirenz	The metabolism of Rolapitant can be increased when combined with Efavirenz.
Rolapitant Modafinil	The metabolism of Rolapitant can be increased when combined with Modafinil.