Rolapitant

Reviewed on 8/27/2021

Brand Name and Other Names: Varubi

Generic Name: Rolapitant

Drug Class: Antiemetic Agents; NK1 Receptor Antagonists

What Is Rolapitant Used For and How Does it Work?

Rolapitant is used in combination with other antiemetic agents (e.g., dexamethasone and 5HT-3 antagonist) in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

Rolapitant is available under the following different brand names: Varubi.

What Are the Dosages of Rolapitant?

Dosages of Rolapitant:

Dosage Forms and Strengths

Tablet

  • 90mg

Dosage Considerations – Should be Given as Follows:

Chemotherapy-Induced Nausea and Vomiting

Indicated in combination with other antiemetic agents (e.g., dexamethasone and 5HT-3 antagonist) in adults for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.

Highly emetogenic chemotherapy

  • Includes cisplatin-based highly emetogenic cancer chemotherapy
  • Day 1
    • Rolapitant 180 mg orally 2 hours before chemotherapy PLUS
    • Dexamethasone 20 mg orally 30 minutes before chemotherapy PLUS
    • 5HT-3 antagonist according to the manufacturer’s prescribing information
  • Days 2-4
    • Dexamethasone 8 mg orally twice daily
    • Rolapitant 180 mg orally 2 hours before chemotherapy PLUS
    • Dexamethasone 20 mg orally 30 minutes before chemotherapy PLUS
    • 5HT-3 antagonist according to the manufacturer’s prescribing information

Dosage Modifications

Anaphylaxis or any other serious hypersensitivity reactions

  • Immediately discontinue treatment and appropriate medical management (e.g., initiate epinephrine and/or antihistamines)
  • Permanently discontinue rolapitant

Hepatic impairment

  • Mild-to-moderate (Child-Pugh A to B): No dosage adjustment is necessary
  • Severe (Child-Pugh C): Avoid use; if use cannot be avoided, monitor for drug-related adverse reactions

Safety and efficacy not established in pediatric patients

SLIDESHOW

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What Are Side Effects Associated with Using Rolapitant?

Common side effects of rolapitant include:

Tablets

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

What Other Drugs Interact with Rolapitant?

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

  • Severe interactions of rolapitant include:
  • Rolapitant has serious interactions with at least 27 different drugs.
  • Rolapitant has moderate interactions with at least 76 different drugs.
  • Mild interactions of rolapitant include:

What Are Warnings and Precautions for Rolapitant?

Warnings

  • This medication contains rolapitant. Do not take Varubi if you are allergic to rolapitant or any ingredients contained in this drug.

Contraindications

  • Coadministration with CYP2D6 substrates with a narrow therapeutic index (e.g., thioridazine and pimozide)
  • Hypersensitivity to any component of the product

Effects of Drug Abuse

  • No information is available.

Short-Term Effects

  • See "What Are Side Effects Associated with Using Rolapitant?"

Long-Term Effects

  • See "What Are Side Effects Associated with Using Rolapitant?"

Cautions

Anaphylaxis and other serious hypersensitivity reactions

  • Anaphylaxis, anaphylactic shock, and other serious hypersensitivity reactions, some requiring hospitalization have been reported

Drug interactions overview

  • Avoid the use of rolapitant in patients who require chronic administration of strong CYP3A4 inducers
  • Monitor INR and prothrombin time and adjust warfarin dose, to maintain INR target range, when used concomitantly with rolapitant
  • BCRP substrates with a narrow therapeutic index
    • Oral rolapitant is an inhibitor of breast cancer resistance protein (BCRP); increased plasma concentrations of BCRP substrates (e.g., methotrexate, topotecan, or irinotecan) may result in potential adverse reactions
    • Monitor for adverse reactions related to the concomitant drug if the use of rolapitant cannot be avoided
    • Use a lowest effective dose of rosuvastatin (see prescribing information for additional information on recommended dosing)
  • P-gp substrates with a narrow therapeutic index
    • Oral rolapitant is an inhibitor of p-glycoprotein (P-gp)
    • Increased plasma concentrations of P-gp substrates (e.g., digoxin) may result in potential adverse reactions
    • Monitor for adverse reactions and adjust the dose if concomitant use of rolapitant tablets with digoxin or other P-gp substrates with a narrow therapeutic index cannot be avoided
  • CYP2D6 substrates with a narrow therapeutic index
    • Contraindicated with CYP2D6 substrates with a narrow therapeutic index
    • Monitor for adverse reactions if coadministration with other CYP2D6 substrates with a narrow therapeutic index cannot be avoided
    • Rolapitant can significantly increase plasma concentrations of thioridazine and pimozide, which may result in QT prolongation and torsade de pointes; if patients require pimozide or thioridazine, use an alternative antiemetic to rolapitant or an alternative to thioridazine or pimozide that is not metabolized by CYP2D6
  • Other CYP2D6 substrates
    • May increase plasma concentrations of CYP2D6 substrates for at least 28 days following rolapitant administration and may result in adverse reactions
    • Before initiating treatment, consult prescribing information for CYP2D6 substrates to obtain additional information about interactions with a CYP2D6 inhibitor

Pregnancy and Lactation

  • The limited data regarding the use of rolapitant in pregnant women are insufficient to inform a drug-associated risk of adverse developmental outcomes. In animal reproduction studies, no teratogenic or embryo-fetal effects were observed with oral administration in rats and rabbits during the period of organogenesis at doses up to 1.3 times and 2.9 times, respectively, the maximum recommended human dose (MRHD). Consult your doctor.
  • It is unknown if rolapitant is distributed in human breast milk and there is no data on its effects on breastfed infants or milk production. Consider the developmental and health benefits of breastfeeding along with the mother's clinical need for rolapitant, and any potential adverse effects on the breastfed infant from the drug or underlying maternal condition.
References
https://reference.medscape.com/drug/varubi-rolapitant-1000029

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