rolapitant (varubi) Report issue

Small molecule Approved FDA
AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

Active Ingredient History

NOW
  • Now
Rolapitant (VARUBI) is neurokinin 1 (NK1) receptor antagonist. Rolapitant does not have significant affinity for the NK2 or NK3 receptors. Drug is indicated 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. Most common adverse reactions are: neutropenia and hiccups at Cisplatin Based Highly Emetogenic Chemotherapy; decreased appetite, neutropenia and dizziness at Moderately Emetogenic Chemotherapy and Combinations of Anthracycline and Cyclophosphamide. Inhibition of BCRP and P-gp by rolapitant can increase plasma concentrations of the concomitant drug and potential for adverse reactions. Strong CYP3A4 Inducers (e.g., rifampin) can significantly reduce plasma concentrations of rolapitant and decrease the efficacy of VARUBI.   NCATS

Chemistry

  • SMILES: C[C@@H](OC[C@@]1(c2ccccc2)CC[C@]2(CCC(=O)N2)CN1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1
  • InChIKey: FIVSJYGQAIEMOC-ZGNKEGEESA-N
  • Mol. Mass: 500.48
  • ALogP: 5.73
  • ChEMBL Molecules:
    rolapitant  
    rolapitant hydrochloride  
More Chemistry

Pharmacology

  • Mechanism of Action:
  • Multi-specific: Missing data
  • Black Box: No
  • Availability: Prescription Only
  • Delivery Methods: Oral
  • Pro Drug: No

Drug Pricing (per unit)

United States

$164.4150 - $256.8600
More Pricing Detail

Note: This drug pricing data is preliminary, incomplete, and may contain errors.

Alternative names

8-((1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro(4,5)decan-2-one | rolapitant | rolapitant hcl | rolapitant hydrochloride | sch619734 | sch 619734 | sch-619734 | varubi

Organizations (8)

Research & Development (7)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Marketing (2)

Organization Org Type FDA approvals Clinical Trials involvement Org ID Force Sort

Indications (7)

Approved Indications (3)


 

Drug-Related Side Effects and Adverse Reactions (approved 2015)

Nausea

Postoperative Nausea and Vomiting

Experimental Indications - Clinical Trial Phases 1-4 (7)


 

Cough (Phase 2)

Drug-Related Side Effects and Adverse Reactions (Phase 3)

Nausea ()

Neoplasms, Germ Cell and Embryonal (Phase 2)

Postoperative Nausea and Vomiting (Phase 2)

Sarcoma (Phase 2)

Vomiting (Phase 2)

Overview

  • Highest Phase: Phase 3
  • # of Trials: 12
  • # of Trial Organizations: 7

Trials by Phase

Trial Phase Start Date Organizations Indications

Feedback

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