Varubi
Varubi Uses, Dosage, Side Effects, Food Interaction and all others data.
Varubi is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist approved for the prevention of delayed chemotherapy-induced nausea and vomiting (CINV) in adults. Delayed-phase CINV typically occurs >24 hours after chemotherapy treatment and is principally mediated by Neurokinin-1 and its ligand Substance P, which is released in the gut following chemotherapy administration. Neurokinin-1 is also known as Tachykinin Receptor 1 (TACR1), Neurokinin 1 Receptor (NK1R), and Substance P Receptor (SPR).By blocking Substance P from interacting with NK-1 receptors in the gut and the central nervous system, rolapitant prevents late-phase CINV. Unlike other available NK-1 receptor antagonists, rolapitant is not an inhibitor of Cytochrome P450 enzyme CYP3A4 and has a long elimination half-life, allowing a single dose to prevent both acute and late-phase CINV during the first 120 hours post-chemotherapy.
Trade Name | Varubi |
Availability | Prescription only |
Generic | Rolapitant |
Rolapitant Other Names | Rolapitant |
Related Drugs | lorazepam, ondansetron, Zofran, dexamethasone, Ativan, metoclopramide |
Weight | 90mg, |
Type | Oral Tablet, Intravenous |
Formula | C25H26F6N2O2 |
Weight | Average: 500.485 Monoisotopic: 500.189847063 |
Protein binding | Rolapitant is 99.8% bound to human plasma protein. |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | United States, |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Varubi is a neurokinin-1 (NK-1) receptor antagonist used in combination with other antiemetics for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy.
This drug is indicated in adults in combination with other antiemetics for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy.
Varubi is also used to associated treatment for these conditions: Delayed chemotherapy induced naused and vomiting
How Varubi works
Varubi is an orally active, highly selective Neurokinin-1 Receptor (NK1R) antagonist. NK1 receptors are located primarily in the gut and central nervous system and are activated by Substance P following chemotherapy administration. By binding to the NK1 receptor, rolapitant prevents binding of its ligand Substance P, which is released in the gut following chemotherapy administration.
Toxicity
Most common adverse reactions occurring in >3% of patients receiving moderately emetogenic chemotherapy and combinations of anthracycline and cyclophosphamide included decreased appetite, neutropenia, dizziness, dyspepsia, urinary tract infection, stomatitis, and anemia. Most common adverse reactions occurring in patients receiving cisplatin-based highly emetogenic chemotherapy included neutropenia, hiccups, and abdominal pain.
Food Interaction
- Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of rolapitant.
- Take with or without food.
Varubi Drug Interaction
Moderate: amphetamine / dextroamphetamine, doxorubicin, meclizine, sulfasalazine, diphenhydramineUnknown: lactobacillus acidophilus, nifedipine, aspirin / dipyridamole, lubiprostone, cyclobenzaprine, trihexyphenidyl, lorazepam, amoxicillin / clavulanate, multivitamin, multivitamin, sulfamethoxazole / trimethoprim, dicyclomine, loratadine, docusate, escitalopram
Varubi Disease Interaction
Major: hepatic impairmentModerate: lactose intolerance, renal impairment
Volume of Distribution
460 L
Elimination Route
Following administration of rolapitant, plasma concentrations reached peak levels in about 4 hours.
Half Life
Mean terminal half life ranged from 169 to 183 hours (~7 days).
Clearance
0.96 L/hour
Elimination Route
Varubi was found to be 14.2% renally excreted and 73% fecally excreted. Of the fecally excreted compounds
Innovators Monograph
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