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THE SCIENCE BEHIND ARISTADA INITIO AND ARISTADA

View the technology behind ARISTADA INITIO and ARISTADA, and their formulation and pharmacology

 

Alkermes has a deep history of developing proven, long-acting technology platforms

ARISTADA INITIO and ARISTADA are formulations made of aripiprazole lauroxil drug crystals1-4

  • ARISTADA INITIO® (aripiprazole lauroxil) and ARISTADA® (aripiprazole lauroxil) are created using the same LinkeRx® technology, and their metabolic conversion processes are the same.1-4 However, ARISTADA INITIO is not interchangeable with ARISTADA due to differing pharmacokinetic profiles1,2

ARISTADA INITIO was developed utilizing NanoCrystal® technology5

  • Drug crystals in ARISTADA INITIO are smaller than those in ARISTADA, allowing for faster dissolution5
  • ARISTADA was designed for slow dissolution from the injection site, providing extended release5,6

This proprietary LinkeRx® technology allows for consistent and sustained medication levels throughout the dosing period.3,6

LinkeRx® and the conversion of ARISTADA to aripiprazole

  • LinkeRx® is proprietary technology used to produce a non-ester prodrug of aripiprazole. Using this system, a linker attaches aripiprazole to a fatty acid, creating ARISTADA3
  • This covalently bonded modification of aripiprazole is likely converted in vivo by slow dissolution of the drug crystals and subsequent hydrolysis to release aripiprazole3

LinkeRx® technology allows for

  • Regulated absorption and a low peak-to-trough ratio6
  • Sustained release with an extended pharmacokinetic profile6
  • An aqueous suspension in a prefilled syringe that does not require reconstitution2

See the consistent and sustained medication levels provided by ARISTADA

View pharmacokinetics
References: 1. ARISTADA INITIO [package insert]. Waltham, MA: Alkermes, Inc; 2018. 2. ARISTADA [package insert]. Waltham, MA: Alkermes, Inc; 2018. 3. Hard ML, Mills RJ, Sadler BM, Turncliff RZ, Citrome L. Aripiprazole lauroxil: pharmacokinetic profile of this long-acting injectable antipsychotic in persons with schizophrenia. J Clin Psychopharmacol. 2017;37(3):289-295. 4. Hard ML, Wehr AY, Sadler BM, Mills RJ, von Moltke L. Population pharmacokinetic analysis and model-based simulations of aripiprazole for a 1-day initiation regimen for the long-acting antipsychotic aripiprazole lauroxil. Eur J Drug Metab Pharmacokinet. 2018;43(4):461-469. 5. Hard ML, Wehr AY, Du Y, Weiden PJ, Walling D, von Moltke L. Pharmacokinetic evaluation of a 1-day treatment initiation option for starting long-acting aripiprazole lauroxil for schizophrenia. J Clin Psychopharmacol. 2018;38(5):435-441. 6. Turncliff R, Hard M, Du Y, Risinger R, Ehrich EW. Relative bioavailability and safety of aripiprazole lauroxil, a novel once-monthly, long-acting injectable atypical antipsychotic, following deltoid and gluteal administration in adult subjects with schizophrenia. Schizophr Res. 2014;159(2-3):404-410.