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- Levomet (melevodopa) / Chiesi
Axon terminal hypertrophy of striatal projection neurons with levodopa-induced dyskinesia priming () - Aug 30, 2023 - Abstract #MDSCongress2023MDS_Congress_1273;
Increased GABA storage in axon terminals of the direct pathway neurons represents the priming process of LID.
- | Levomet (melevodopa) / Chiesi
Journal: Human aromatic amino acid decarboxylase is an asymmetric and flexible enzyme: implication in AADC deficiency. (Pubmed Central) - Jul 31, 2023
Increased GABA storage in axon terminals of the direct pathway neurons represents the priming process of LID. Here, for the first time, we solved the crystal structure of human holoAADC in the internal aldimine (1.9?
- | Levomet (melevodopa) / Chiesi
Journal: Axon terminal hypertrophy of striatal projection neurons with levodopa-induced dyskinesia priming. (Pubmed Central) - Jun 23, 2023
The AIM score increased with levodopa treatment, as did the hypertrophy of axon terminals in the GPi, showing an increased number of synaptic vesicles in hypertrophied terminals. Increased GABA storage in axon terminals of the direct pathway neurons represents the priming process of LID.
- | Levomet (melevodopa) / Chiesi
Journal: Development and Validation of a New LC-MS/MS Bioanalytical Method for the Simultaneous Determination of Levodopa, Levodopa Methyl Ester, and Carbidopa in Human Plasma Samples. (Pubmed Central) - Jun 14, 2023
Reinjection reproducibility was assessed. The described method was successfully applied to a 45-year-old male patient to compare the pharmacokinetic behavior of an L-DOPA-based medical treatment involving commercially available Mucuna pruriens extracts and an LDME/carbidopa (100/25 mg) formulation.
- | Levomet (melevodopa) / Chiesi
Journal: Coupling between GPR143 and dopamine D2 receptor is required for selective potentiation of dopamine D2 receptor function by L-3,4-dihydroxyphenylalanine in the dorsal striatum. (Pubmed Central) - Apr 18, 2023
Administration of non-effective dose of L-DOPA methyl ester augmented the quinpirole-induced hypolocomotion in WT mice but not in Gpr143 mice...Intracerebroventricular administration of a peptide that disrupted the interaction mitigated quinpirole-induced behavioral changes in WT mice but not in Gpr143 mice. These findings provide evidence that coupling between GPR143 and DRD2 is required for selective DRD2 modulation by L-DOPA in the dorsal striatum.
- | Levomet (melevodopa) / Chiesi
Journal: A Bio-Based Supramolecular Adhesive: Ultra-High Adhesion Strengths at both Ambient and Cryogenic Temperatures and Excellent Multi-Reusability. (Pubmed Central) - Oct 12, 2022
Herein, castor oil, melevodopa, and iron ions are used as building blocks to construct a novel bio-based supramolecular adhesive (BSA) with outstanding adhesion performances...In addition, the BSA displays excellent multi-reusability with more than 87% of the original adhesion strength remaining even after reuse for ten times. It is highly anticipated that this line of research will provide a new insight into designing bio-based adhesives with outstanding adhesion performances and excellent multi-reusability.
- | Levomet (melevodopa) / Chiesi
Journal: Preparation and detailed characterization of the thiomer chitosan-cysteine as a suitable mucoadhesive excipient for nasal powders. (Pubmed Central) - Sep 30, 2022
Thereafter, nasal powder formulations were prepared using the polymer and the antiparkinsonian drug levodopa methyl ester hydrochloride by freeze-drying to investigate their nasal applicability. Based on the in vitro studies, these powders might be suitable for reducing the off periods of Parkinson's disease because of their expected higher in vivo mucoadhesion.
- | Levomet (melevodopa) / Chiesi
Journal: Phosphodiesterase 9 inhibition prolongs the antiparkinsonian action of l-DOPA in parkinsonian non-human primates. (Pubmed Central) - May 20, 2022
PDE9i was administered as monotherapy and co-administration with l-DOPA at two predetermined doses (suboptimal and threshold s.c. doses of l-Dopa methyl ester plus benserazide) using a controlled blinded protocol to assess motor disability, l-DOPA -induced dyskinesias (LID), and other neurologic drug effects...These results indicate that cGMP upregulation interacts with dopamine signaling to enhance the l-DOPA reversal of parkinsonian motor disability. Therefore, striatal PDE9 inhibition may be further explored as a strategy to improve motor responses to l-DOPA in PD.
- | Levomet (melevodopa) / Chiesi
Journal: Development of a Novel MR Colonography via Iron-Based Solid Lipid Nanoparticles. (Pubmed Central) - Mar 3, 2022
SLNs were prepared with the simultaneous loading of trivalent Fe ions (Fe), levodopa methyl ester (DM), and fluorescein isothiocyanate (FITC)...Confocal fluorescence microscopy confirmed that FeDM-FITC-SLNs were mainly distributed in the intestinal mucosa and tumor capsule. Iron-based SLNs are promising alternatives for contrast enhancement at T1-weighted MRI and will help in the differential diagnosis of intestinal bowel diseases (IBDs).
- | Levomet (melevodopa) / Chiesi
Journal: Development of a Hydrophobicity-Controlled Delivery System Containing Levodopa Methyl Ester Hydrochloride Loaded into a Mesoporous Silica. (Pubmed Central) - Aug 11, 2021
The release studies indicated that the release rate significantly decreased (p < 0.05) with increasing hydrophobicity. The products with controlled release can reduce the off period frequency.
- | Levomet (melevodopa) / Chiesi
Journal: Kinetic characterization of the oxidation of catecolamines and related compounds by laccase. (Pubmed Central) - Apr 22, 2021
The addition of a methyl group (α-methyl dopa) increases the rate but decreases the affinity for catalysis. l-Epinephrine and l-norepinephrine have an affinity similar to isoprenaline, but faster catalysis, probably due to the greater nucleophilic power of their phenolic hydroxyl.
- | Levomet (melevodopa) / Chiesi
Journal: Partial Tablet Coating by 3D Printing. (Pubmed Central) - Jan 29, 2021
The percentage of the tablet surface coated, the number of coating layers as well as the coated sides of the tablet where the parameters which controlled the release profile for both APIs. Different dissolution profiles have been achieved by tuning these simple parameters, which revealed a non-Fickian release mechanism regardless of the API.
- || Levomet (melevodopa) / Chiesi, Sirio (carbidopa/melevodopa) / Chiesi, Ligand
Clinical, Review, Journal: A systematic review on the clinical experience with melevodopa/carbidopa fixed combination in patients with Parkinson disease. (Pubmed Central) - Feb 14, 2020
Data from literature have shown that melevodopa/carbidopa in a highly soluble formulation as effervescent oral tablets is effective in improving control of motor complications in PD patients compared to conventional levodopa. Further research is needed to confirm this evidence in large controlled trials and to explore if melevodopa/carbidopa may have a potential role in the earlier phases of the disease or in special PD populations.