Rolapitant
Rolapitant is an antiemetic medication used to prevent nausea and vomiting, particularly delayed chemotherapy-induced nausea and vomiting, by blocking substance P/NK1 receptors in the brain.
Rolapitant is a NK1 receptor antagonist used to prevent chemotherapy-induced and postoperative nausea and vomiting.
Key facts at a glance
- ATC
- A04AD14
- RxNorm
- 1665496
- Generic
- Rolapitant
- Class
- atc-a04
- Brands
- Varubi
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- injection, tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 180mg (4 x 45mg tablets) as single dose
- Maximum
- consult physician
- Frequency
- within 2 hours before chemotherapy
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- weight-based, 1.8mg/kg (max 180mg) as single dose
- Maximum
- consult physician
- Frequency
- within 2 hours before chemotherapy
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 180mg (4 x 45mg tablets) as single dose
- Maximum
- consult physician
- Frequency
- within 2 hours before chemotherapy
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
9 groupspregnancy
generalavoid if possible
avoid use during pregnancy unless benefits outweigh risks - discuss with healthcare provider
regular fetal monitoring if used
Use with caution and monitor for adverse effects.
pregnancy
first trimesteravoid if possible
avoid use during first trimester unless benefits clearly outweigh risks
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
generaldiscontinue nursing or drug
rolapitant may be present in breast milk - decide whether to discontinue nursing or discontinue the drug considering importance of treatment to mother
monitor infant for adverse effects
geriatric
generalno adjustment needed
no specific dose adjustment required - standard adult dosing applicable
standard monitoring
pediatric_age
under 18 yearsnot recommended
safety and efficacy not established in pediatric patients - do not use in children and adolescents under 18 years
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
renal_impairment
mild moderateno adjustment needed
no dose adjustment required for mild to moderate renal impairment
standard monitoring
renal_impairment
severeuse with caution
use with caution in severe renal impairment - limited data available
enhanced monitoring recommended
Use with caution and monitor for adverse effects.
hepatic_impairment
mild moderateno adjustment needed
no dose adjustment required for mild to moderate hepatic impairment
standard monitoring
hepatic_impairment
severeuse with caution
use with caution in severe hepatic impairment - limited data available
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA approval year
FDA approval for prevention of chemotherapy-induced nausea and vomiting
Drug class
Neurokinin-1 receptor antagonist for antiemetic therapy
Primary indication
Approved for use with other antiemetics in patients receiving highly emetogenic chemotherapy
Brand name
Commercial brand name for rolapitant
Prevention of delayed nausea and vomiting associated with initial and repeat courses of chemotherapy. May also be used for prevention of postoperative nausea and vomiting in some regions.
Rolapitant is a selective and competitive antagonist at human substance P/NK1 receptors. By blocking these receptors in the central nervous system, it prevents substance P from triggering the vomiting reflex. It has minimal activity at NK2, NK3, and other receptors, transporters, and ion channels.
May interact with certain CYP3A4 substrates. Oral formulation is taken before chemotherapy. Long duration of action allows for once-per-cycle dosing. Common side effects may include decreased appetite and dizziness.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy