fosnetupitant (Akynzeo) Report issue

Small molecule Approved FDA

Active Ingredient History

NOW
  • Now
Fosnetupitant is a prodrug form of netupitant. Netupitant is a selective antagonist of human substance P/neurokinin 1 (NK-1) receptors. Upon intravenous administration, fosnetupitant is converted by phosphatases to its active form. It competitively binds to and blocks the activity of NK-1 receptors in the central nervous system, by inhibiting binding of substance P (SP) to NK-1 receptors. This prevents delayed emesis, which is associated with SP secretion. AKYNZEO® is a combination of palonosetron, a serotonin-3 receptor antagonist, and netupitant (capsules for oral use) or fosnetupitant (injections for intravenous use). AKYNZEO® for injection is indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy.   NCATS

Chemistry

  • SMILES: CN(C(=O)C(C)(C)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)C2=C(C=C(N=C2)N3CC[N+](C)(COP(O)([O-])=O)CC3)C4=C(C)C=CC=C4
  • InChIKey: HZIYEEMJNBKMJH-UHFFFAOYSA-N
  • Mol. Mass: 688.5976
  • ALogP: 5.74
  • ChEMBL Molecules:
    fosnetupitant  
    fosnetupitant chloride hydrochloride  
More Chemistry

Pharmacology

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

Organizations (3)

Research & Development (3)

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

Marketing (1)

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

Indications (4)

Approved Indications (3)


 

Nausea

Postoperative Nausea and Vomiting (approved 2018)

Vomiting

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


 

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

Overview

  • Highest Phase: Phase 3
  • # of Trials: 1
  • # of Trial Organizations: 3

Trials by Phase

Trial Phase Start Date Organizations Indications

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