• To prevent delayed nausea and vomiting associated with initial/repeat courses of emetogenic cancer chemotherapy (in combination with dexamethasone and a 5-HT₃ antagonist).

Contraindicated in:

• Concurrent use of CYP2D6 substrates with a narrow therapeutic index.

Use Cautiously in:

• Concurrent use of other CYP2D6 substrates
• Severe hepatic impairment (avoid if possible; if unavoidable, monitor carefully)
• OB: Safety not established in pregnancy
• Lactation: Safety not established in breastfeeding
• Pedi: Safety and effectiveness not established in children
• Geri: Older adults may be more sensitive to drug effects.

CV: dizziness.

GI: ↓ appetite, abdominal pain, dyspepsia, hiccups, stomatitis.

GU: ↓ fertility (females).

Hemat: anemia, neutropenia.

Misc: infusion reactions.

Drug-Drug:

• ↑ levels and risk of serious cardiac toxicity with CYP2D6 substrates with a narrow therapeutic index, including thioridazine and pimozide; concurrent use contraindicated.
• May ↑ levels and risk of toxicity of other CYP2D6 substrates for an extended period of time (≥28 days).
• May ↑ levels and risk of toxicity of breast cancer resistance protein (BCRP) substrates, including irinotecan, methotrexate, rosuvastatin, and topotecan; dose reduction may be necessary.
• May ↑ levels and risk of toxicity of P-glycoprotein (P-gp) substrates, including digoxin; avoid concurrent use with P-gp substrates with a narrow therapeutic index.
• Strong CYP3A4 inducers, including rifampin, may ↓ levels and effectiveness; avoid concurrent use.

• Tablets: 90 mg;

• PO (Adults): 180 mg administered within 2 hr prior to start of chemotherapy.

Varubi

• Acts as a selective antagonist at substance P/neurokinin 1 (NK₁) receptors in the brain.

• Decreased nausea and vomiting associated with chemotherapy.
• Augments the antiemetic effects of dexamethasone and 5-HT₃ antagonists.

Therapeutic Classification: antiemetics

Pharmacologic Classification: neurokinin antagonists

Absorption: Well absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Protein Binding: 99.8%.

Metabolism/Excretion: Mostly metabolized, primarily by the CYP3A4 isoenzyme; one metabolite, C4–pyrrolidine-hydroxylated rolapitant (M19), has antiemetic activity. Excretion is mainly via hepatic/biliary elimination. 14% excreted in urine (8% as metabolites), 73% in feces (38% as unchanged drug).

Half-life: Rolapitant: 7 days; M19: 7 days.

(plasma concentrations)

• Instruct patient to take rolapitant as directed. Direct patient to read the Patient Package Insert before starting therapy and each time Rx renewed in case of changes.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
• Advise patient and family to use general measures to decrease nausea (begin with sips of liquids and small, nongreasy meals; provide oral hygiene; remove noxious stimuli from environment).
• Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding. May impair fertility in females; impairment is reversible.

rol-AP-i-tant

NDC Code^*

• 69656- Tesaro, Inc.
  • 69656-101- Varubi
    • 69656-101-02- 2 TABLET in 1 BLISTER PACK (69656-101-02)

• 69656- Tesaro, Inc.
  • 69656-102- Varubi
    • 69656-102-10- 1 VIAL, SINGLE-DOSE in 1 CARTON (69656-102-10) > 92.5 mL in 1 VIAL, SINGLE-DOSE

• 70720- TerSera Therapeutics LLC
  • 70720-101- Varubi
    • 70720-101-02- 2 TABLET in 1 BLISTER PACK (70720-101-02)