AKYNZEO® for injection

Discover the clinical data supporting AKYNZEO for injection:

The efficacy of AKYNZEO for injection for the prevention of CINV was established by demonstrating:

Safety of AKYNZEO for injection was established based on:


Palonosetron administered as an intravenous infusion was shown to be noninferior to a bolus IV push1

  • Multicenter, multinational, randomized, double-blind study
  • 425 adult cancer patients receiving a non-A/C HEC regimen received palonosetron (PALO) plus dexamethasone (DEX) to prevent CINV
    • Bolus IV push arm: Single dose of PALO 0.25 mg administered IV over 30 seconds + DEX
    • IV infusion arm: Single dose of PALO 0.25 mg administered IV over 30 minutes + DEX
  • Primary end point: Noninferiority of palonosetron IV infusion to bolus IV push
    • Complete response (CR): No emesis or rescue medication use during the acute phase (0–24 hours after chemotherapy)
    • Prespecified non-inferiority margin was set at 15%

Complete response (no emesis and no use of rescue medication) in acute phase (0–24 hours) in non-a/c HEC-Treated patients1
CR Complete Responce; Dexamethasone, Palonosetron, Oral
  • Patients achieving CR in the acute phase for IV infusion and IV bolus push were 82.7% and 86.3%, respectively. Difference of -3.4%; 99% CI -12.0% to 5.2%
  • The frequency and severity of all reported TEAEs were similar between treatment arms

Fosnetupitant in AKYNZEO for injection demonstrated bioequivalence to netupitant in AKYNZEO capsules1,2

  • AKYNZEO for injection is the only combination agent that combines palonosetron, a 5-HT3 receptor antagonist, with an NK-1 receptor antagonist
  • Netupitant, the NK-1 receptor antagonist in AKNYZEO capsules, is not water soluble, so AKYNZEO for injection includes the soluble prodrug, fosnetupitant
  • Fosnetupitant is rapidly converted to netupitant after IV administration
Plasma concentrations after single dose of fosnetupitant2
Plasma Concentration
  • The pharmacologic effects of fosnetupitant can be attributed to the activity of netupitant
  • An IV fosnetupitant dose of 235 mg (260 mg of fosnetupitant chloride hydrochloride) achieved a similar netupitant area under the curve (AUC) as 300 mg oral netupitant
Linear relationship between fosnetupitant dose and netupitant area under the curve (AUC)2
Linear Relationship between Fosnetupitant dose and Netupitant AUC

The safety profile of AKYNZEO for injection was generally similar to AKYNZEO capsules3

  • Phase 3, multinational, randomized, double-blind, multi-cycle safety study
  • 404 patients receiving a cisplatin-based HEC regimen for solid tumors received either oral or IV AKYNZEO to prevent CINV
  • Median age: 60 years; 46% women; 99.5% white; 0.3% Asian; 0.3% Hispanic
    • Oral arm: Single dose of AKYNZEO capsule + DEX (n=201)
    • IV arm: Single IV dose AKYNZEO + DEX (n=203)
    • DEX dose was PO 12 mg on Day 1, followed by 8 mg on Days 2–4 for both arms
  • Safety profile was generally similar between oral and IV formulations
    • Treatment-relates adverse reactions (TRAEs) were observed in 8.9% and 9.5% of patients in IV and PO arms, respectively
    • Severe TRAEs were observed in 0.5% and 1.0% of patients in IV and PO arms, respectively
  • There were no infusion-site reactions related to AKYNZEO for injection3

AC
=anthracycline-cyclophosphamide.
CINV
=chemotherapy-induced nausea and vomiting.
HEC
=highly emetogenic chemotherapy.
IV
=injection for intravenous use.
PO
=oral.