AKYNZEO^® injection

Discover the clinical data supporting AKYNZEO injection

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

• Noninferiority of IV palonosetron bolus vs IV Infusion
• Bioequivalence of fosnetupitant to netupitant

Safety of AKYNZEO injection was established based on:

• Adverse event profile of AKYNZEO injection compared with AKYNZEO capsules

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

• Multicenter, multinational, randomized, double-blind study
• 425 adult cancer patients receiving a non-AC 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 endpoint: 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 noninferiority margin was set at -15%

• 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 injection demonstrated bioequivalence to netupitant in AKYNZEO capsules^1,2

• AKYNZEO injection is the only combination agent that includes a 5-HT₃ RA (palonosetron) with an NK-1 RA (netupitant)
• Netupitant, the NK-1 RA in AKYNZEO capsules, is not water soluble, so AKYNZEO injection includes the soluble prodrug, fosnetupitant
• Fosnetupitant is rapidly converted to netupitant after IV administration

Fosnetupitant plasma concentrations decreased rapidly, while netupitant plasma concentrations remained steady over time²

• 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

The safety profile of AKYNZEO injection was generally similar to AKYNZEO capsules^1,3

• Phase III, multinational, randomized, double-blind, multicycle safety study³
• 404 patients receiving a cisplatin-based HEC regimen for solid tumors received either oral or IV AKYNZEO to prevent CINV^1,3
• Median age: 60 years; 46% women; 99.5% white; 0.3% Asian; 0.3% Hispanic¹
  • Oral arm: Single dose of AKYNZEO capsule + DEX (n=201)
  • IV arm: Single IV dose of 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^1,3
  • 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 injection³

Warnings and Precautions

• Hypersensitivity reactions, including anaphylaxis, have been reported in patients receiving palonosetron, one of the components of AKYNZEO, with or without known hypersensitivity to other 5-HT₃ receptor antagonists.

• 5HT₃ RA=5HT₃ receptor antagonist; AC=anthracycline-cyclophosphamide; CINV=chemotherapy-induced nausea and vomiting; HEC=highly emetogenic chemotherapy; NK-1 RA=neurokinin-1 receptor antagonist; PO=oral; QTc=corrected QT interval; TRAE=treatment-related adverse event.
• *AKYNZEO for Injection has not been studied for the prevention of nausea and vomiting associated with anthracycline plus cyclophosphamide chemotherapy.