Version July 2025
Chemotherapy-induced nausea and vomiting (prevention): Note: Do not administer rolapitant at less than 2-week intervals. No dosage adjustment for concomitant dexamethasone is required. For highly emetogenic chemotherapy and for anthracycline/cyclophosphamide combinations, the antiemetic regimen should also include olanzapine on days 1 to 4 (Ref).
Highly emetogenic chemotherapy (cisplatin-based): Oral: 180 mg within 2 hours prior to initiation of chemotherapy on day 1 only (in combination with dexamethasone given on days 1 to 4 and a 5-HT3 receptor antagonist on day 1).
Moderately emetogenic chemotherapy and anthracycline/cyclophosphamide combinations: Oral: 180 mg within 2 hours prior to initiation of chemotherapy on day 1 only (in combination with dexamethasone on day 1 and a 5-HT3 receptor antagonist as appropriate based on the agent selected).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl 30 to 90 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling; however, based on pharmacokinetics, dosage adjustment is not likely necessary.
CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
End-stage kidney disease requiring hemodialysis: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Child-Pugh classes A and B: No dosage adjustment is necessary.
Child-Pugh class C: Avoid use if possible (has not been studied); if use cannot be avoided, monitor closely for adverse reactions related to rolapitant.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults as part of combination regimens.
1% to 10%:
Gastrointestinal: Abdominal pain (3%), decreased appetite (9%), dyspepsia (4%), hiccups (5%), stomatitis (4%)
Genitourinary: Urinary tract infection (4%)
Hematologic & oncologic: Anemia (3%), neutropenia (7% to 9%)
Nervous system: Dizziness (6%)
Postmarketing: Hypersensitivity: Anaphylactic shock (FDA Safety Alert, Jan 16, 2018), anaphylaxis (FDA Safety Alert, Jan 16, 2018)
Concurrent use of CYP2D6 substrates with a narrow therapeutic index, such as thioridazine or pimozide; pediatric patients <2 years of age.
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no relevant warnings listed in the manufacturer's labeling.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet Therapy Pack, Oral:
Varubi (180 MG Dose): 90 mg (2 ea) [contains fd&c blue #2 (indigo carm) aluminum lake]
No
Tablet Therapy Pack (Varubi (180 MG Dose) Oral)
2 x 90 mg (per each): $397.68
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Oral: Administer within 2 hours prior to initiation of chemotherapy (on day 1 only). May be administered without regard to meals.
Chemotherapy-induced nausea and vomiting, prevention: Prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including, but not limited to highly emetogenic chemotherapy (in combination with other antiemetic agents).
Rolapitant may be confused with aprepitant, fosaprepitant, fosnetupitant, netupitant.
Varubi may be confused with valrubicin.
Substrate of CYP3A4 (Major with inducers), CYP3A4 (Minor with inhibitors); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits BCRP, CYP2B6 (Weak), CYP2D6 (Moderate), P-glycoprotein;
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Afatinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Afatinib. Management: If combined, administer the P-gp inhibitor simultaneously with, or after, the dose of afatinib. Monitor closely for signs and symptoms of afatinib toxicity and if the combination is not tolerated, reduce the afatinib dose by 10 mg. Risk D: Consider Therapy Modification
Ajmaline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Ajmaline. Risk C: Monitor
Aliskiren: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Aliskiren. Risk C: Monitor
Alpelisib: BCRP/ABCG2 Inhibitors may increase serum concentration of Alpelisib. Management: Avoid coadministration of BCRP/ABCG2 inhibitors and alpelisib due to the potential for increased alpelisib concentrations and toxicities. If coadministration cannot be avoided, closely monitor for increased alpelisib adverse reactions. Risk D: Consider Therapy Modification
Amitriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Amitriptyline. CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Amitriptyline. Risk C: Monitor
Amoxapine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Amoxapine. Risk C: Monitor
Amphetamines: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Amphetamines. Management: Monitor for amphetamine toxicities (including serotonin syndrome) if used with a moderate CYP2D6 inhibitor. Initiate amphetamine therapy at lower doses, monitor frequently, and adjust doses as needed. Discontinue amphetamines if serotoinin syndrome occurs Risk C: Monitor
ARIPiprazole Lauroxil: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of ARIPiprazole Lauroxil. Risk C: Monitor
ARIPiprazole: CYP2D6 Inhibitors (Moderate) may increase serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy, indication, or dosage form. Consult full interaction monograph for specific recommendations. Risk C: Monitor
Atomoxetine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Atomoxetine. Risk C: Monitor
BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors): Rolapitant may increase serum concentration of BCRP/ABCG2 Substrates (Clinically Relevant with Inhibitors). Management: Monitor patients receiving rolapitant for increased exposure to and/or effects of BCRP/ABCG2 substrates. Use the lowest effective rosuvastatin dose when used in combination with rolapitant. Risk C: Monitor
Beta-Acetyldigoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Beta-Acetyldigoxin. Risk C: Monitor
Bilastine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Bilastine. Risk X: Avoid
Brexpiprazole: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Brexpiprazole. Management: If brexpiprazole is to be used together with both a moderate CYP2D6 inhibitor and a strong or moderate CYP3A4 inhibitor, the brexpiprazole dose should be reduced to 25% of the usual dose when treating indications other than major depressive disorder. Risk C: Monitor
BuPROPion: CYP2B6 Inhibitors (Weak) may increase serum concentration of BuPROPion. Risk C: Monitor
Carvedilol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Carvedilol. Risk C: Monitor
Celiprolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Celiprolol. Risk C: Monitor
Cladribine: BCRP/ABCG2 Inhibitors may increase serum concentration of Cladribine. Management: Avoid concomitant use of BCRP inhibitors during the 4 to 5 day oral cladribine treatment cycles whenever possible. If combined, consider dose reduction of the BCRP inhibitor and separation in the timing of administration. Risk D: Consider Therapy Modification
ClomiPRAMINE: CYP2D6 Inhibitors (Moderate) may increase serum concentration of ClomiPRAMINE. CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of ClomiPRAMINE. Risk C: Monitor
CloZAPine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of CloZAPine. Risk C: Monitor
Codeine: CYP2D6 Inhibitors (Moderate) may decrease therapeutic effects of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Risk C: Monitor
Colchicine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: This combination is often contraindicated, but combined use may be permitted with dose adjustment and monitoring. Recommendations vary based on brand, indication, use of CYP3A4 inhibitors, and hepatic/renal function. See interaction monograph for details. Risk D: Consider Therapy Modification
CycloSPORINE (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of CycloSPORINE (Systemic). Risk C: Monitor
CYP3A4 Inducers (Moderate): May decrease serum concentration of Rolapitant. Risk C: Monitor
CYP3A4 Inducers (Strong): May decrease serum concentration of Rolapitant. Risk X: Avoid
Dabigatran Etexilate: P-glycoprotein/ABCB1 Inhibitors may increase active metabolite exposure of Dabigatran Etexilate. Risk C: Monitor
Desipramine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Desipramine. Risk C: Monitor
Deutetrabenazine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Deutetrabenazine. Risk C: Monitor
Dextromethorphan: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Dextromethorphan. Risk C: Monitor
Digitoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Digitoxin. Risk C: Monitor
Digoxin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Digoxin. Management: Measure digoxin serum concentrations before initiating treatment with these P-glycoprotein (P-gp) inhibitors. Reduce digoxin concentrations by either reducing the digoxin dose by 15% to 30% or by modifying the dosing frequency. Risk D: Consider Therapy Modification
Doxepin (Systemic): CYP2D6 Inhibitors (Moderate) may increase serum concentration of Doxepin (Systemic). Risk C: Monitor
Doxepin (Topical): CYP2D6 Inhibitors (Moderate) may increase serum concentration of Doxepin (Topical). Risk C: Monitor
DOXOrubicin (Conventional): CYP2D6 Inhibitors (Moderate) may increase serum concentration of DOXOrubicin (Conventional). Risk X: Avoid
DOXOrubicin (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Conventional). Risk X: Avoid
DOXOrubicin (Liposomal): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of DOXOrubicin (Liposomal). Risk C: Monitor
Edoxaban: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Edoxaban. Risk C: Monitor
Eliglustat: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Eliglustat. Management: Eliglustat dose is 84 mg daily with CYP2D6 inhibitors. Use is contraindicated (COI) when also combined with strong CYP3A4 inhibitors. When also combined with a moderate CYP3A4 inhibitor, use is COI in CYP2D6 EMs or IMs and should be avoided in CYP2D6 PMs. Risk D: Consider Therapy Modification
Ensartinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ensartinib. Risk X: Avoid
Etoposide Phosphate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide Phosphate. Risk C: Monitor
Etoposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Etoposide. Risk C: Monitor
Everolimus: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Everolimus. Risk C: Monitor
Flecainide: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Flecainide. Risk C: Monitor
Glecaprevir and Pibrentasvir: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Glecaprevir and Pibrentasvir. Risk C: Monitor
Haloperidol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Haloperidol. Risk C: Monitor
Iboga: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Iboga. Risk C: Monitor
Iloperidone: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Iloperidone. CYP2D6 Inhibitors (Moderate) may decrease active metabolite exposure of Iloperidone. Specifically, concentrations of the metabolite P95 may be decreased. CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Iloperidone. Specifically, concentrations of the metabolite P88 may be increased. Risk C: Monitor
Imipramine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Imipramine. Concentrations of desipramine may be increased. CYP2D6 Inhibitors (Moderate) may increase serum concentration of Imipramine. Risk C: Monitor
Indoramin: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Indoramin. Risk C: Monitor
Lapatinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Lapatinib. Risk C: Monitor
Larotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Larotrectinib. Risk C: Monitor
Lefamulin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Lefamulin. Management: Avoid concomitant use of lefamulin tablets with P-glycoprotein/ABCB1 inhibitors. If concomitant use is required, monitor for lefamulin adverse effects. Risk D: Consider Therapy Modification
Lofepramine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Lofepramine. The active metabolite of lofepramine is desipramine. Risk C: Monitor
Mavorixafor: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Mavorixafor. Risk C: Monitor
Mequitazine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Mequitazine. Risk X: Avoid
Methadone: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Methadone. Risk C: Monitor
Metoclopramide: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Metoclopramide. Risk C: Monitor
Metoprolol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Metoprolol. Risk C: Monitor
Morphine (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Morphine (Systemic). Risk C: Monitor
Nadolol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Nadolol. Risk C: Monitor
Naldemedine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Naldemedine. Risk C: Monitor
Naloxegol: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Naloxegol. Risk C: Monitor
Nebivolol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Nebivolol. Risk C: Monitor
Nortriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Nortriptyline. Risk C: Monitor
Oliceridine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Oliceridine. Risk C: Monitor
Olmutinib: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Olmutinib. Risk C: Monitor
PARoxetine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of PARoxetine. Risk C: Monitor
PAZOPanib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of PAZOPanib. Risk X: Avoid
Perhexiline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Perhexiline. Risk C: Monitor
Perphenazine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Perphenazine. Risk C: Monitor
Pimozide: Rolapitant may increase serum concentration of Pimozide. Risk X: Avoid
Pitolisant: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Pitolisant. Risk C: Monitor
Pralsetinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Pralsetinib. Management: If this combo cannot be avoided, decrease pralsetinib dose from 400 mg daily to 300 mg daily; from 300 mg daily to 200 mg daily; and from 200 mg daily to 100 mg daily. Risk D: Consider Therapy Modification
Propafenone: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Propafenone. Risk C: Monitor
Propranolol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Propranolol. Risk C: Monitor
Protriptyline: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Protriptyline. Risk C: Monitor
Ranolazine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ranolazine. Risk C: Monitor
Relugolix, Estradiol, and Norethindrone: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix, Estradiol, and Norethindrone. Management: Avoid use of relugolix/estradiol/norethindrone with P-glycoprotein (P-gp) inhibitors. If concomitant use is unavoidable, relugolix/estradiol/norethindrone should be administered at least 6 hours before the P-gp inhibitor. Risk D: Consider Therapy Modification
Relugolix: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Relugolix. Management: Avoid coadministration of relugolix with oral P-gp inhibitors whenever possible. If combined, take relugolix at least 6 hours prior to the P-gp inhibitor and monitor patients more frequently for adverse reactions. Risk D: Consider Therapy Modification
Repotrectinib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Repotrectinib. Risk X: Avoid
RifAXIMin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RifAXIMin. Risk C: Monitor
Rimegepant: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Rimegepant. Management: Avoid administration of another dose of rimegepant within 48 hours if given concomitantly with a P-glycoprotein (P-gp) inhibitor. Risk D: Consider Therapy Modification
RisperiDONE: CYP2D6 Inhibitors (Moderate) may increase serum concentration of RisperiDONE. Risk C: Monitor
RisperiDONE: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RisperiDONE. Risk C: Monitor
RomiDEPsin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of RomiDEPsin. Risk C: Monitor
Rosuvastatin: BCRP/ABCG2 Inhibitors may increase serum concentration of Rosuvastatin. Risk C: Monitor
Saquinavir: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Saquinavir. Risk C: Monitor
Seladelpar: BCRP/ABCG2 Inhibitors may increase serum concentration of Seladelpar. Risk C: Monitor
Sertindole: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Sertindole. Risk C: Monitor
Silodosin: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Silodosin. Risk C: Monitor
Sirolimus (Conventional): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Sirolimus (Conventional). Management: Avoid concurrent use of sirolimus with P-glycoprotein (P-gp) inhibitors when possible and alternative agents with lesser interaction potential with sirolimus should be considered. Monitor for increased sirolimus concentrations/toxicity if combined. Risk D: Consider Therapy Modification
Sirolimus (Protein Bound): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Sirolimus (Protein Bound). Risk X: Avoid
Sofpironium: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Sofpironium. Risk C: Monitor
Tacrolimus (Systemic): P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Tacrolimus (Systemic). Risk C: Monitor
Talazoparib: BCRP/ABCG2 Inhibitors may increase serum concentration of Talazoparib. Risk C: Monitor
Talazoparib: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Talazoparib. Risk C: Monitor
Tamoxifen: CYP2D6 Inhibitors (Moderate) may decrease active metabolite exposure of Tamoxifen. Specifically, CYP2D6 inhibitors may decrease the metabolic formation of highly potent active metabolites. Management: Consider alternatives to the use of moderate CYP2D6 inhibitors with tamoxifen when possible, as the combination may be associated with reduced clinical effectiveness of tamoxifen. Risk D: Consider Therapy Modification
Tamsulosin: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Tamsulosin. Risk C: Monitor
Teniposide: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Teniposide. Risk C: Monitor
Tenofovir Disoproxil Fumarate: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Tenofovir Disoproxil Fumarate. Risk C: Monitor
Tetrabenazine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Tetrabenazine. Specifically, concentrations of the active alpha- and beta-dihydrotetrabenazine metabolites may be increased. Risk C: Monitor
Thioridazine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Thioridazine. Risk X: Avoid
Timolol (Systemic): CYP2D6 Inhibitors (Moderate) may increase serum concentration of Timolol (Systemic). Risk C: Monitor
Topotecan: BCRP/ABCG2 Inhibitors may increase serum concentration of Topotecan. Risk X: Avoid
Topotecan: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Topotecan. Risk X: Avoid
TraMADol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of TraMADol. CYP2D6 Inhibitors (Moderate) may decrease active metabolite exposure of TraMADol. Risk C: Monitor
Trimipramine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Trimipramine. Risk C: Monitor
Ubrogepant: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 50 mg and second dose (at least 2 hours later if needed) of 50 mg when used with a P-gp inhibitor. Risk D: Consider Therapy Modification
Valbenazine: CYP2D6 Inhibitors (Moderate) may increase active metabolite exposure of Valbenazine. Risk C: Monitor
Venetoclax: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring concomitant treatment with P-glycoprotein (P-gp) inhibitors. Resume the previous venetoclax dose 2 to 3 days after discontinuation of a P-gp inhibitor. Risk D: Consider Therapy Modification
VinCRIStine: P-glycoprotein/ABCB1 Inhibitors may increase serum concentration of VinCRIStine. Risk X: Avoid
Vortioxetine: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Vortioxetine. Risk C: Monitor
Warfarin: Rolapitant may increase serum concentration of Warfarin. Risk C: Monitor
Zuclopenthixol: CYP2D6 Inhibitors (Moderate) may increase serum concentration of Zuclopenthixol. Risk C: Monitor
Adverse events were observed in some animal reproduction studies.
It is not known if rolapitant is present in breast milk. According to the manufacturer, the decision to breastfeed during therapy should take into account the risk of exposure to the infant and the benefits of treatment to the mother.
Monitor for adverse reactions, particularly in patients with severe hepatic impairment.
Rolapitant prevents delayed nausea and vomiting associated with emetogenic chemotherapy by selectively and competitively inhibiting the substance P/neurokinin 1 (NK1) receptor.
Distribution: Vd/F: 387 L (patients with cancer).
Protein binding: 99.8%.
Metabolism: Hepatic; primarily by CYP3A4 to form active metabolite M19 (major).
Half-life elimination: ~7 days (range: 169 to 183 hours).
Time to peak: ~4 hours.
Excretion: Feces (73%); urine (~14%; primarily as metabolites).
