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November 7, 2025
Brand Name :
Varubi
Synonyms :
rolapitant
Class :
NK1 Receptor Antagonist, Antiemetic Agents
Dosage Forms & StrengthsÂ
TabletÂ
90 mgÂ
Chemotherapy Induced Vomiting And NauseaÂ
Highly emetogenic chemotherapy
For Day 1
Take two rolapitant tablets (180 mg) two hours before chemotherapy in combination with dexamethasone 20 mg orally half an hour before chemotherapy
For Days 2 to 4
Take dexamethasone 8 mg orally two times a day
Moderately emetogenic chemotherapy
For Day 1
Take two rolapitant tablet (180 mg) two hours before chemotherapy in combination with take dexamethasone 20 mg orally half an hour before chemotherapy
Dosage Modifications
Anaphylaxis
discontinue forever rolapitant
Hepatic impairment
Mild-to-moderate: dose modification not required
Severe: stop using it
Safety and efficacy not determined Â
Refer to adult dosingÂ
CYP3A strong enhancers of the small intestine may reduce the bioavailability of rolapitant 
antiemetics increase the hypotensive effect of apomorphine
antiemetics may enhance the serotonergic effect of serotonergic Agents
may enhance the effect of serotonergic agents
rolapitant: they may enhance the serum concentration of CYP2D6 Inhibitors
rolapitant: they may enhance the serum concentration of CYP2D6 Inhibitors
rolapitant: they may enhance the serum concentration of CYP2D6 Inhibitors
rolapitant: they may enhance the serum concentration of CYP2D6 Inhibitors
rolapitant: they may enhance the serum concentration of CYP2D6 Inhibitors
rolapitant: they may diminish the serum concentration of CYP3A4 Inducers
rolapitant: they may diminish the serum concentration of CYP3A4 Inducers
rolapitant: they may diminish the serum concentration of CYP3A4 Inducers
rolapitant: they may diminish the serum concentration of CYP3A4 Inducers
rolapitant: they may diminish the serum concentration of CYP3A4 Inducers
rolapitant: they may enhance the serum concentration of warfarin
the effect of rolapitant is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
antiemetics increase the serotonergic effect of tramadol
Actions and SpectrumÂ
rolapitant functions by inhibiting substance P, a neurotransmitter implicated in causing nausea and vomiting. The prevention of delayed chemotherapy-induced nausea and vomiting (CINV) is the only indication for the use of rolapitant. It works well against CINV in both the acute and delayed phases. Â
Frequency defined Â
1-10%Â
Neutropenia (9%)Â Â
Dyspepsia (4%)Â
Urinary tract infection (4%)Â
Decreased appetite (9%)Â
Dizziness (6%)Â Â
Anemia (3%)Â
Stomatitis (4%)Â Â
Hiccups (5%)Â
Neutropenia (7%)Â
Abdominal pain (3%)Â Â
Black Box WarningÂ
None
Contraindication/Caution:Â
Contraindication:Â
Caution:Â
Pregnancy consideration:    Â
Pregnancy category: N/AÂ
Lactation: Excretion into human milk is unknown Â
Pregnancy Categories:        Â
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.Â
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. Â
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.Â
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.Â
Category N: There is no data available for the drug under this category.Â
Pharmacology Â
rolapitant works by attaching to and inhibiting the NK1 receptor in the vomiting center of the central nervous system. It blocks the signaling process by preventing substance P from interacting with the NK1 receptor. Â
PharmacodynamicsÂ
rolapitant is used in combination with other antiemetic medications, such as 5-HT3 receptor antagonist and a corticosteroid. This combination therapy targets multiple pathways involved in the emetic process, including serotonin receptors and corticosteroid receptors.Â
PharmacokineticsÂ
Absorption  Â
rolapitant is absorbed when taken orally. It is rapidly absorbed from the gastrointestinal track. Â
DistributionÂ
The drug has a large volume of distribution throughout the body.Â
MetabolismÂ
rolapitant undergoes extensive metabolism in the liver.Â
Elimination and excretionÂ
The elimination of rolapitant and its metabolites occurs through feces.Â
AdministrationÂ
rolapitant is available as an oral tablet for administration.
Patient information leafletÂ
Generic Name: rolapitantÂ
Why do we use rolapitant?Â
rolapitant is used as an antiemetic drug for the prevention of chemotherapy-induced nausea and vomiting (CINV).