Rolapitant

Rolapitant Uses, Dosage, Side Effects, Food Interaction and all others data.

Rolapitant 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 Rolapitant
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
Rolapitant
Rolapitant

Uses

Rolapitant 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.

Rolapitant is also used to associated treatment for these conditions: Delayed chemotherapy induced naused and vomiting

How Rolapitant works

Rolapitant 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.

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

Rolapitant was found to be 14.2% renally excreted and 73% fecally excreted. Of the fecally excreted compounds

Innovators Monograph

You find simplified version here Rolapitant

*** Taking medicines without doctor's advice can cause long-term problems.
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