Clinical trial evaluating apomorphine oromucosal solution in Parkinson's disease patients

• DOI: 10.1111/cts.13796
• Publication Date: 2024-05-07T10:48:32Z
• Authors: Eva Thijssen; Bert Tuk; Michel Cakici; Veerle van Velze; Erica Klaassen; Frans Merkus; Teus van Laar; Philip Kremer; Geert Jan Groeneveld
• Keywords: Apomorphine; Tolerability; Pramipexole

Abstract Apomorphine, used to treat OFF episodes in patients with Parkinson's disease (PD), is typically administered via subcutaneous injections. Administration of an oromucosal solution could offer a non‐invasive and user‐friendly alternative. This two‐part clinical study evaluated the safety, tolerability, pharmacokinetics (PK), dose proportionality novel apomorphine hydrochloride solution, as well its relative bioavailability injection sublingual film. In part A study, 12 PD received 2 mg (4% weight/volume) randomized order, followed by 4 8 apomorphine. B 13 7 (7% 30 14 Washout between administrations both parts was at least days. Safety, PK were assessed pre‐ post‐dose. Both showed that generally well‐tolerated. Observed side effects typical for administration included asymptomatic orthostatic hypotension, yawning, fatigue, somnolence. Oromucosal exposure increased dose, although less than proportional. The mean (SD) maximum reached 753.0 (298.6) ng*min/mL (area under plasma concentration–time curve from zero infinity) 8.0 (3.3) ng/mL (maximum concentration). comparable after approximately half observed summary, clinically relevant concentrations be without tolerability issues.