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Captisol® and Nexterone®

Solvent-Free Amiodarone Injection

In 2001, CyDex (now Ligand) began development of Amiodarone HCL, brand name Cordarone® I.V. This work led to a Patent being granted in 2005 and in 2006, CyDex licensed Captisol to Prism.

Cordarone I.V. is an FDA-approved drug that prolongs the duration of the action potential of all cardiac fibers while causing minimal reduction of dV/dt (maximal upstroke velocity of the action potential).

Cordarone I.V. Side-Effects and Incompatibilities

  • PolySorbate 80 (or Tween 80)
  • Hepatotoxicity, severe hypotension, cardiac depression
  • BzAlcohol: CNS depression, acidosis, respiratory failure
  • Foams –complicating required dilution and delivery
  • Irritating, phlebitis
  • Incompatible with plastics 

Goal of Program

  • Eliminate undesirable excipients
  • Reduce side-effects
  • 505b2 filing with bioequivalence bridging data, i.e. pharmacodynamics and pharmacokinetics required in 80-120% range 

Captisol-enabled® Results

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  • Study showing amiodarone plasma concentration-time profile along with its major metabolite, desethylamiodarone
  • Comparison study in normal: PM101 (Captisol-enabled® Amiodarone) vs AIV (existing commercial product).
  • Study demonstrates bioequivalence in same concentration in plasma with Captisol-enabled® Amiodarone compared to Cordarone I.V.
  • No change in pharmacodynamics and PK
  • Captisol-enabled® 100% of pharmacodynamics and pharmacokinetics required for 5052b filin 

  • Captisol® replaced polysorbate 80, thereby alleviating blood pressure changes due to this co-solvent
  • A study of Captisol-enabled® Amiodarone demonstrated no changes in blood pressure

In 2008, Prism received approval for Amiodarone (Nexterone) in a vial presentation. Prism's initial submission supported vial and syringe presentations 

In 2010, Prism received approval for an sNDA for a pre-mixed bag or ready-to-use bag presentation

  • Faster
  • Easier administration
  • Time saver in emergency room setting
  • Cost saver

Then, in 2011, Baxter acquired Prism Pharmaceuticals and the Nexterone® product line. The deal included upfront and milestones fees that could potentially total up to $338M.