rolapitant (Rx)

Brand and Other Names:Varubi
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 90mg

Chemotherapy-Induced Nausea & Vomiting

Indicated in combination with other antiemetic agents (eg, 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

See also Administration

Highly emetogenic chemotherapy

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

Moderately emetogenic chemotherapy

  • Includes anthracycline and cyclophosphamide combinations
  • Day 1
    • Rolapitant 180 mg PO 2 hr before chemotherapy PLUS
    • Dexamethasone 20 mg PO 30 minutes before chemotherapy PLUS
    • 5HT-3 antagonist according the manufacturer’s prescribing information

Dosage Modifications

Anaphylaxis or any other serious hypersensitivity reactions

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

Hepatic impairment

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

Safety and efficacy not established

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Interactions

Interaction Checker

and rolapitant

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

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            Adverse Effects

            1-10%

            Tablets

            • HEC
              • Neutropenia (9%)
              • Hiccups (5%)
              • Abdominal pain (3%)
            • MEC
              • Decreased appetite (9%)
              • Neutropenia (7%)
              • Dizziness (6%)
              • Dyspepsia (4%)
              • Urinary tract infection (4%)
              • Stomatitis (4%)
              • Anemia (3%)
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            Warnings

            Contraindications

            Coadministration with CYP2D6 substrates with a narrow therapeutic index (eg, thioridazine and pimozide)

            Hypersensitivity to any component of the product

            Cautions

            Anaphylaxis and other serious hypersensitivity reactions

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

            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 (eg, methotrexate, topotecan, or irinotecan) may result in potential adverse reactions
              • Monitor for adverse reactions related to the concomitant drug if use of rolapitant cannot be avoided
              • Use 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 (eg, digoxin) may result in potential adverse reactions
              • Monitor for adverse reactions and adjust 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 varrow therapeutic index
              • Contraindicated with CYP2D6 substrates with narrow therapeutic index (see Contraindications)
              • 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 torsades 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
              • Prior to initiating treatment, consult prescribing information for CYP2D6 substrates to obtain additional information about interactions with CYP2D6 inhibitor
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            Pregnancy

            Pregnancy

            Limited data in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcome

            Animal data

            • 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)

            Lactation

            Unknown if distributed in human breast milk and no data on effects on breastfed infant or on milk production

            Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Selective, long-acting neurokinin receptor (NK)-1 antagonist

            NK-1 receptors are highly concentrated in the vomiting center of the brain and bind a neurokinin termed substance P; activation of NK-1 receptors by substance P plays a central role in eliciting chemotherapy-induced nausea and vomiting

            Blocking the interaction of substance P at the NK-1 receptor, NK-1 receptor antagonists improve the management of nausea and vomiting

            Absorption

            Tablet

            • Peak plasma time: 4 hr; 120 hr (active metabolite)
            • Peak plasma concentration: 968 ng/mL

            Distribution

            Protein bound: 99.8%

            Vd, single-dose: 460 L (180 mg PO)

            Vd, oral: 387 L

            Metabolism

            Metabolized primarily by CYP3A4 to form a major active metabolite, M19 (C4 ­pyrrolidine-hydroxylated rolapitant)

            Exposure ratio of M19 to rolapitant was approximately 50% in plasma

            Elimination

            Eliminated primarily through the hepatic/biliary route

            Half-life, single oral doses (4.5-180 mg): 169-183 hr

            Clearance: 0.96 L/hr (oral)

            Excretion, single oral 180-mg dose: 73% feces; 14.2% urine

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            Administration

            Oral Administration

            May take with or without food

            Storage

            Tablets

            • Store at controlled room temperature 20-25ºC (68-77ºF)
            • Excursions are permitted between 15-30°C (59-86°F)
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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.