Ixekizumab Citrate-Free Formulation: Results from Two Clinical Trials

Area of Science:

• Pharmacology
• Immunology
• Drug Delivery Systems

Background:

• Subcutaneous (SC) injection is a common drug administration route.
• Injection site pain (ISP) can negatively impact patient experience.
• Ixekizumab targets interleukin-17A for autoimmune conditions.

Purpose of the Study:

• Evaluate injection site pain (ISP) of a citrate-free (CF) ixekizumab formulation.
• Assess the bioequivalence of the CF ixekizumab formulation.
• Compare the overall safety profile of the CF formulation versus the original.

Main Methods:

• Two Phase 1, single-blind studies (NCT03848403, NCT04259346) in healthy participants.
• Study A: Crossover design evaluating pain via visual analog scale (VAS) after SC injection of three formulations.
• Study B: Randomized trial comparing bioequivalence of CF vs. original ixekizumab formulation (80 mg SC dose).

Main Results:

• The CF ixekizumab formulation showed significantly lower ISP (LSM VAS difference: -21.7, p<0.0001) in Study A.
• Bioequivalence of the CF formulation was confirmed in Study B (90% CIs within 0.8-1.25).
• Overall safety profiles were comparable between the CF and original formulations, apart from reduced ISP.

Conclusions:

• The citrate-free ixekizumab formulation is bioequivalent to the original.
• The CF formulation is associated with significantly reduced injection site pain.
• The CF ixekizumab formulation offers a favorable safety profile with improved patient comfort.