Rolapitant

What is Rolapitant?

• Rolapitant (Varubi) is a substance P/neurokinin 1 (NK1) receptor antagonist called an "antiemetic." Varubi is used with other medicines in adults to help prevent nausea and vomiting that happens later with certain anti-cancer medicines (chemotherapy).

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What are the uses of this medicine?

• This medicine is used in combination with other antiemetic agents 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.

How does this medicine work?

• Rolapitant (roe la' pi tant) is a substance P/neurokinin 1 (NK-1) receptor antagonist which has potent and prolonged antiemetic activity. Rolapitant acts as a substance P antagonist blocking the neurokinin 1 (NK1) receptor, which is found in the central nervous system and induces the vomiting reflex when activated by substance P. Rolapitant has been shown to inhibit both acute and delayed nausea and vomiting associated with cancer chemotherapy and surgical procedures, and appears to act synergistically with serotonin type 3 (5-HT3) receptor blockers.
• Because of its delayed half-life, rolapitant is particularly potent in preventing delayed (>24 hours after chemotherapy) nausea and vomiting.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who are hypersensitive to any component of the product (including soybean oil).
• taking CYP2D6 substrates with a narrow therapeutic index, such as thioridazine and pimozide.

What drug interactions can this medicine cause?

• Varubi is contraindicated in patients taking CYP2D6 substrates with a narrow therapeutic index such as thioridazine and pimozide.
• Varubi can also increase plasma concentrations of other CYP2D6 substrates for at least 28 days following administration of Varubi and may result in adverse reactions.
• Avoid the use of Varubi in patients who require chronic administration of strong CYP3A4 inducers (eg: rifampin, carbamazepine, phenytoin, St. John’s wort).
• Oral Varubi is an inhibitor of BCRP and P-gp and can increase plasma concentrations of the concomitant drug and potential for adverse reactions. ncreased 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 use of Varubi tablets cannot be avoided.
• Monitor for adverse reactions if concomitant use of Varubi tablets with other P-gp substrates with a narrow therapeutic index cannot be avoided.

Is this medicine FDA approved?

• It was approved for use in the United States in 2015.

How should this medicine be used?

Recommended Dosage:

• Administer in combination with dexamethasone and a 5-HT3 receptor antagonist.
• No dosage adjustment for dexamethasone is required.
• Tablets: The recommended dosage is 180 mg as a single dose.
• Injectable emulsion: The recommended dosage is 166.5 mg administered as an intravenous infusion over 30 minutes.

Administration Take Varubi exactly as your doctor tells you to take it. There are 2 ways your doctor may prescribe Varubi for you:

Varubi tablets:

• Varubi tablets are taken on Day 1 of chemotherapy. Take 2 Varubi tablets by mouth within 2 hours before you receive your anti-cancer medicine (chemotherapy).
• Varubi tablets can be taken with or without food.
• Do not take Varubi more than 1 time every 14 days.
• If you take too much Varubi, call your doctor or go to the nearest hospital emergency room right away.

Varubi injectable emulsion:

• Varubi injectable emulsion is given on Day 1 of chemotherapy.
• It will be given to you in your vein (intravenously) over 30 minutes, within 2 hours before you receive your anti-cancer medicine (chemotherapy).

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 90 mg of rolapitant
• Injectable emulsion: 166.5 mg/92.5 mL (1.8 mg/mL) of rolapitant in a single-dose vial

This medicine is available in fallowing brand namesː

• Varubi

What side effects can this medication cause?

The most common side effects of Varubi in people who take Varubi and receive Cisplatin chemotherapy medicine include:

• low white blood cell count
• hiccups
• stomach (abdominal) pain

The most common side effects of Varubi in people who take Varubi and receive Anthracycline and Cyclophosphamide chemotherapy medicines include:

• decreased appetite
• low white blood cell count
• dizziness
• indigestion
• urinary tract infection
• mouth sores
• low red blood cell count

Varubi may cause serious side effects, including:

• Serious allergic reactions
• Change in the level of some medicines in your blood

What special precautions should I follow?

• Anaphylaxis, anaphylactic shock and other serious hypersensitivity reactions have been reported. Most occur immediately following initiation of infusion. If symptoms occur, stop Varubi injectable emulsion, initiate appropriate medical management including epinephrine and/or an antihistamine. Permanently discontinue Varubi injectable emulsion.

Rolapitant is a moderate inhibitor of CYP2D6 and significantly increases the plasma concentrations of CYP2D6 substrates for at least 28 days following single dose administration of Varubi. Before starting Varubi, consider if patients require:

• thioridazine or pimozide; if so, use an alternative antiemetic to Varubi or an alternative to thioridazine or pimozide that is not metabolized by CYP2D6.
• other CYP2D6 substrates; if so, consult the prescribing information for the CYP2D6 substrate for additional information about interactions with CYP2D6 inhibitors

What to do in case of emergency/overdose?

• There are no data on overdose with Varubi.

Manangement for overdosage:

• There is no antidote for Varubi overdose.
• Discontinue Varubi in the event of overdose, and institute general supportive measures and close observation.

Can this medicine be used in pregnancy?

• The limited data with Varubi use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes.

Can this medicine be used in children?

• Safety and efficacy of Varubi have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: rolapitant
• Inactive ingredients (tablet): colloidal silicon dioxide, croscarmellose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, and pregelatinized starch. The tablets are coated in non-functional blue and clear coats.
• The tablet coating comprises the following inactive ingredients: FD&C Blue No. 2-Indigo Carmine Lake, polyethylene glycol, polysorbate 80, polyvinyl alcohol, talc, and titanium dioxide.
• Inactive ingredients (injectable emulsion): dibasic sodium phosphate, anhydrous (2.8 mg/mL), medium chain triglycerides (11 mg/mL), polyoxyl 15 hydroxystearate (44 mg/mL), sodium chloride (6.2 mg/mL), soybean oil (6.6 mg/mL), water for injection and may contain hydrochloric acid and/or sodium hydroxide to adjust pH to 7.0 to 8.0.

Who manufactures and distributes this medicine?

• Manufactured for: Tesaro a GSK Company Winter St., Waltham

What should I know about storage and disposal of this medication?

• Store Varubi at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Varubi and all medicines out of the reach of children.

• Dailymed label info on Rolapitant
• FDA Rolapitant

Rolapitant Resources
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