Rolapitant

VARUBI

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Pronunciation: roe-LA-pi-tant (va-ROO-bee)

Rolapitant ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Rolapitant ballicule

Rolapitant VARUBI mascot mnemonic cartoon — Visual mnemonic: Rolapitant mascot
**“Ruby Roller paint”**

What it isNK1 receptor antagonist; delayed chemotherapy-induced nausea.

Why this oneA very long half-life covers the whole delayed phase from a single dose.

What limits itIt inhibits CYP2D6 for weeks after one dose, which is easily forgotten. Neutropenia; the IV form was withdrawn for anaphylaxis.

Rolapitant molecular structure (skeletal formula) — Molecular structure: Rolapitant

Rolapitant prescription history

Animated chart of estimated U.S. prescriptions per year, Antiemetics (1946–2026). Rolapitant enters in 2015 (estimated).

FDA-approved for

chemo nausea (2015)

Principal riskIt inhibits CYP2D6 for weeks after a single dose

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilitySedation, QT prolongation, extrapyramidal symptoms or anticholinergic toxicity vary by receptor target.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

FDA dosing	Population	Start	Target	Max
Prevention of delayed nausea/vomiting with emetogenic chemotherapy (with a 5-HT3 antagonist and dexamethasone)	Adults	180 mg single dose	180 mg single dose	180 mg per chemotherapy cycle

Renal Undefined

Hepatic No adjustment for mild-moderate (Child-Pugh A/B); avoid in severe (Child-Pugh C)

Do not administer at intervals shorter than 2 weeks

Instructions

180 mg as a single oral dose within 2 hours before initiation of chemotherapy on Day 1
Give in combination with dexamethasone and a 5-HT3 receptor antagonist
Administer no more frequently than every 2 weeks
Take with or without meals

Available strengths

tab 90 mg

Contraindications

Concomitant CYP2D6 substrates with a narrow therapeutic index (thioridazine, pimozide) - risk of QT prolongation and Torsades de Pointes
Pediatric patients less than 2 years of age (irreversible impairment of sexual development and fertility in juvenile rats)

Cautions

Moderate CYP2D6 inhibition persists at least 28 days after a single dose - affects thioridazine, pimozide, and other CYP2D6 substrates

Adverse reactions

Neutropenia
Hiccups
Abdominal pain
Decreased appetite
Dizziness
Dyspepsia
Urinary tract infection
Stomatitis
Anemia

Pregnancy Insufficient human data; no adverse developmental effects in animals near human exposures.

Lactation No human data; present in rat milk.

Cost

Rolapitant (VARUBI)

Strength		#/mo	generic $/unit	CostPlus
90 mg	tab	per unit		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Rolapitant is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2032 est.

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Memory aids: interaction avatars

CYP2D6 inhibitor (moderate)

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Self-check

Rolapitant: Why can one dose cover delayed chemotherapy nausea?
Very long half-life.
Rolapitant: How long can CYP2D6 inhibition persist?
Weeks after one dose.