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Varubi (ROLAPITANT)

Tersera · FDA-approved approved Small molecule Quality 65/100

Varubi works by blocking the substance-P receptor, a key player in the body's response to chemotherapy-induced nausea and vomiting.

Varubi (rolapitant) is a small molecule substance P/neurokinin-1 receptor antagonist developed by Tesaro Inc. (originally) and currently owned by Tersera. It targets the substance-P receptor to prevent chemotherapy-induced nausea and vomiting. Varubi was FDA-approved in 2015 and remains a patented medication. Key safety considerations include its long half-life of 148.5 hours.

At a glance

Generic nameROLAPITANT
SponsorTersera
Drug classSubstance P/Neurokinin-1 Receptor Antagonist
TargetSubstance-P receptor
ModalitySmall molecule
Therapeutic areaOncology
PhaseFDA-approved
First approval2015

Mechanism of action

Rolapitant is selective and competitive antagonist of human substance P/NK1 receptors. Rolapitant does not have significant affinity for the NK2 or NK3 receptors or for battery of other receptors, transporters, enzymes and ion channels. Rolapitant is also active in animal models of chemotherapy-induced emesis.

Approved indications

Common side effects

Key clinical trials

Patents

PatentExpiryType

Primary sources

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SourceUsed for
FDA labelMechanism, indications, dosing, boxed warnings, drug interactions
ClinicalTrials.govTrial enrolment, design, endpoints, results
FDA Orange BookPatents + exclusivity

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