Improving levodopa delivery: IPX203, a novel extended-release carbidopa-levodopa formulation.

IPX203 is a novel oral extended-release (ER) formulation of carbidopa (CD) and levodopa (LD) developed to address the short half-life and limited area for absorption of LD in the gastrointestinal tract. This paper presents the formulation strategy of IPX203 and its relationship to the pharmacokinetics (PK) and pharmacodynamic profile of IPX203 in Parkinson's disease (PD) patients. IPX203 was developed with an innovative technology containing immediate-release (IR) granules and ER beads that provides rapid LD absorption to achieve desired plasma concentration and maintaining it within the therapeutic range for longer than can be achieved with current oral LD formulations. The PK and pharmacodynamics of IPX203 were compared with IR CD-LD in a Phase 2, open-label, rater-blinded, multicenter, crossover study in patients with advanced PD. Pharmacokinetic data showed that on Day 15, LD concentrations were sustained above 50% of peak for 6.2 h with IPX203 vs. 3.9 h with IR CD-LD ( These data confirm that the unique design of IPX203 addresses some of the limitations of oral LD delivery.

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© 2023 The Author(s).

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The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: P.L. has served as a consultant or investigator in clinical trials sponsored by Acorda Therapeutics, Amneal, Appello, Axovant, Aptinyx, Biogen, Biotie, Bukwang Pharmaceutical, Cavion, Cerevel, Denali Therapeutics, F. Hoffmann-LaRoche, Impax Laboratories Inc., Impel Neuropharma, Ipsen, Kyowa Hakko Kirin, Lundbeck A/S, the Michael J. Fox Foundation for Parkinson’s Research, Mitsubishi Tanabe Pharma, Neurocrine Biosciences, NeuroDerm Ltd, Noven, Parkinson Study Group, Pharma Two B, Prexton Therapeutics, Revance Therapeutics, Saccadous, Sun Pharma, and US WorldMeds. He has received speaking fees from Acorda Therapeutics, Britannia, the American Academy of Neurology, the International Parkinson and Movement Disorder Society, Kyowa Hakko Kirin, Neurocrine Biosciences, Paladin Labs, US WorldMeds, and the World Parkinson Congress. He is compensated for services as editor-in-chief of Clinical Neuropharmacology and serves without compensation on the editorial boards of Journal of Neural Transmission, Translational Neurodegeneration, and Journal of Parkinson’s Disease. A.E. has received speaking and consulting fees from AbbVie/Allergan, Acadia, Acorda Therapeutics, Adamas, Affiris, Amneal, Biohaven, Cerevel, Ipsen, NeuroDerm, Teva, US WorldMeds, and XW Labs. D.B. has received research support for clinical trials from AbbVie, Amneal, Athira Pharma, Axial Biotherapeutics, Cerevel, Enterin, Jazz Pharmaceuticals, Merck, Neuraly, Pharma Two B, and Praxis. S.G. has received research funding from the NIH and has participated in clinical studies funded by Biogen, Amneal, Parkinson Foundation, and the Michael J. Fox Foundation. R.G. has received speaking and consulting fees, as well as payment for his participation in clinical research trials as principal investigator, from companies including, but not limited to: Allergan, Adamas, Teva, Ipsen, US WorldMeds, Impax, Sunovion, AbbVie, Kyowa, Cynapsus, Neurocrine, Pharma Two B, Lundbeck, Novartis, Boehringer Ingelheim, GlaxoSmithKline, Amneal, Merz, Acadia, Medtronic, Merz, Abbott, and NeuroDerm. R.D. has participated as a clinical trial investigator in clinical studies funded by Amneal, Pharma Two B, AbbVie, NeuroDerm, Cerevel, Neurocrine/HSG, Neuraly, Alexion, Global Kinetics, AEON Biopharma, Praxis, and Sage Therapeutics. He has received grants from UAMS Translational Research Institute. He has served as a consultant for Best Doctors Inc. and Synergic Medical Technologies. He owns stock in Biogen, Gilead Sciences, Imara, Atea Pharmaceuticals, and Compass Pathways. G.B. and R.D. are employees of Amneal Pharmaceuticals, LLC.