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Edaravone for Amyotrophic Lateral Sclerosis: Oral Formulation and Its Development Plan () - Jan 21, 2020 - Abstract #AAN2020AAN_3123; PK data indicated that an oral formulation of edaravone produces a profile similar to that of the current IV formulation. It is hoped that the clinical development plan with PK bridging and safety and tolerability of the oral formulation will provide the data needed to seek appropriate marketing authorizations.
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A Retrospective Review of Radicava Experience Across US ALS Centers () - Jan 21, 2020 - Abstract #AAN2020AAN_2791; Preliminary examination of data from 29 US ALS centers suggests administration of Radicava is predominantly home administered and associated with an infected port rate of 6.5%. A complete analysis of the data will be presented
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Edaravone Utilization and Outcomes within a Nationally Integrated Health System () - Jan 21, 2020 - Abstract #AAN2020AAN_2614; Preliminary trends show increased risk of acute and long term ALS associated hospitalization and PEG placement with edaravone compared to riluzole. Discontinuation, both acute and long-term were greater with riluzole compared to edaravone, potentially related to greater ALS progression with riluzole.
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Experience of Using Edaravone in a US-based ALS Center () - Jan 21, 2020 - Abstract #AAN2020AAN_50; The efficacy of the medication in this small sample appears reasonably comparable to the results from the original Japanese study. We would recommend that edaravone be offered to ALS patients in the early stages of disease and that US clinics continue to monitor and analyze outcomes data, as therapeutic responses across diverse populations of patients can be difficult to predict.
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Biomarker, Preclinical, Journal: Edaravone prevents memory impairment in an animal model of post-traumatic distress. (Pubmed Central) - Jan 8, 2020 Edaravone also prevented the stress-induced decrease in the ratio of reduced glutathione/oxidized glutathione and the activities of glutathione peroxidase and catalase enzymes in the hippocampus, as well as increases in the levels of oxidized glutathione and thiobarbituric acid reactive substances. In conclusion, edaravone ameliorated oxidative stress and cognitive impairment associated with a PTSD model, probably by supporting antioxidant mechanism in the hippocampus.
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[VIRTUAL] NEUROPROTECTIVE EFFICACY OF EDARAVONE AGAINST ARSENIC-INDUCED BEHAVIORAL AND NEUROCHEMICAL DEFICITS IN RATS. (EXHIBITION HALL) - Jan 6, 2020 - Abstract #AATADPD2020AAT_ADPD_722; However, chronic treatment with edaravone (10 mg/kg) significantly ameliorated the arsenic-induced behavioral deficits and neurochemical anomalies. Conclusions Thus, our current study clearly showed that edaravone confers neuroprotection against arsenic-induced memory impairment and anxiety-like behavior which may be attributed to the inhibition of oxidative-nitrosative stress and amelioration of cholinergic and mitochondrial functions.
- |||||||||| nitroprusside / Generic mfg., Radicava (edaravone) / Mitsubishi Tanabe, edaravone (MT-1186) / Mitsubishi Tanabe
Journal: Activation of anti-oxidant of curcumin pyrazole derivatives through preservation of mitochondria function and Nrf2 signaling pathway. (Pubmed Central) - Jan 5, 2020 Furthermore, compounds C1-C4 can attenuate the intracellular ROS, and compound C3 is the most effective one which can preservate the mitochondria function by inhibiting the mitochondrial membrane potential loss and enhance nuclear translocation of Nrf2 in PC12 cell. These results indicated that C3 may be a potential candidate drug for treating neurodegenerative diseases.
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Preclinical, Journal: Edaravone combined with cinepazide maleate on neurocyte autophagy and neurological function in rats with subarachnoid hemorrhage. (Pubmed Central) - Jan 1, 2020 Longa score of the combined group was significantly lower than that of the other two groups, and muscle strength score was significantly higher than that of the other two groups (P<0.05). Edaravone combined with cinepazide maleate can effectively increase the survival rate of brain cells and promote the volatilization of neurological function in the treatment of hemorrhage in the subretinal space of the omentum, which is worthy of popularization and application.
- |||||||||| Clinical, Journal: Efficacy of Neuroprotective Drugs in Acute Ischemic Stroke: Is It Helpful? (Pubmed Central) - Dec 15, 2019
Conclusion There was significant improvement in the functional outcome of patients with AIS involving MCA territory at 90 days receiving citicoline, edaravone, and cerebrolysin. However, minocycline did not offer the same efficacy as compared with other neuroprotective agents.
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Preclinical, Journal: Neuroprotective effects of SMTP-44D in mice stroke model in relation to neurovascular unit and trophic coupling. (Pubmed Central) - Dec 6, 2019 These effects of SMTP-44D in reducing oxidative and inflammatory stresses were similar to or stronger than those of edaravone. The present study demonstrated that SMTP-44D showed strong anti-oxidative, anti-inflammatory, and anti-apoptotic effects, moreover, the drug also significantly improved the NVU damage and NVTC in the ischemic brain.
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Journal: Disease-modifying treatment of amyotrophic lateral sclerosis. (Pubmed Central) - Nov 24, 2019 Riluzole is thought to reduce damage to motor neurons through an inhibitory effect on glutamate release, while edaravone is thought to act as a neuroprotective agent that prevents oxidative stress damage as a free radical scavenger. With the lack of treatment options, it is imperative for healthcare professionals to understand the nuances of using these 2 agents to optimize therapy and quality of life for patients with ALS.
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Review, Journal: Familial Amyotrophic Lateral Sclerosis (Pubmed Central) - Nov 23, 2019 The pathomechanism of ALS including proteostasis, RNA metabolism, and axonal pathology are discussed in detail. We also reviewed the status of development of therapeutic strategies for familial ALS based on analysis of animal models and induced pluripotent stem cells.
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Journal: Edaravone: A New Treatment for ALS (Pubmed Central) - Nov 23, 2019 Because edaravone showed a therapeutic effect in suppressing the progression of ALS symptoms, it was approved as a new therapeutic agent in Japan, in June, 2015. In this article, we discuss the recent progress of basic and clinical research for the development of new ALS treatments.
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Biomarker, Clinical, Review, Journal: Hereditary Motor Neuropathies and Amyotrophic Lateral Sclerosis: a Molecular and Clinical Update. (Pubmed Central) - Nov 22, 2019 There is a reasonable hope that the marked and continued growth in our understanding of the molecular pathophysiology of the HMNs will translate into novel therapeutic approaches in the decade to come. Such breakthroughs have already begun in ALS, where novel biomarkers and treatment strategies have translated into a new FDA-approved therapy with a number of promising agents in development and/or in definitive phase 2/3 trials.
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Clinical, Journal: Sudden onset of sleep caused by hypothalamic infarction: a case report. (Pubmed Central) - Nov 21, 2019 Such breakthroughs have already begun in ALS, where novel biomarkers and treatment strategies have translated into a new FDA-approved therapy with a number of promising agents in development and/or in definitive phase 2/3 trials. Hypothalamic stroke should be considered a cause of sudden onset of sleep.
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Clinical, P2 data, Journal: Safety and efficacy of Edaravone Dexborneol versus edaravone for patients with acute ischaemic stroke: a phase II, multicentre, randomised, double-blind, multiple-dose, active-controlled clinical trial. (Pubmed Central) - Nov 14, 2019 P2 Compared with edaravone alone, Edaravone Dexborneol was safe and well tolerated at all doses, although no significant improvement in functional outcomes was observed at 90days. NCT01929096.
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Journal: Emerging and alternative therapies for Parkinson disease: an updated review. (Pubmed Central) - Nov 8, 2019 Other rising nonpharmacotherapies incorporate microRNAs, viral vector gene therapy, stem cells transglutaminases, RTP801, and glial derived neurotrophic factor (GDNF)...While several of these therapies hold much promise in delaying the onset of the disease and slowing its progression, more pharmacotherapies and surgical interventions need to be investigated in different stages of PD. It is hoped that these emerging therapies and surgical procedures will strengthen our clinical armamentarium for improved treatment of PD.
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Clinical, Journal: Clinical observation in edaravone treatment for acute cerebral infarction. (Pubmed Central) - Nov 8, 2019 Edaravone can significantly improve the degree of neurological impairment during acute cerebral infarction, functional movement, and living quality with a definite effect and high safety. Thus, this drug has a good prospect in clinical treatment.
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Review, Journal: Complementary and alternative medicine for treating amyotrophic lateral sclerosis: A narrative review. (Pubmed Central) - Nov 7, 2019 Besides this, ALS patients treated with herbal medicine showed improved disease symptoms, but clinical trials with larger sample sizes are needed to develop a treatment with this herbal medicine. This review shows that CAM may be useful for ALS treatment, but more evidence regarding the efficacy and molecular mechanisms is required to establish CAM as a good therapy for the treatment of ALS patients.
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Clinical, Journal: Is edaravone harmful? (A placebo is not a control). (Pubmed Central) - Oct 29, 2019 In Study 19, edaravone performed better than placebo, but both placebo and edaravone likely did worse than no intervention, an interpretation more in keeping with previous trial experience of drugs with similar mechanisms of action, and with previous trial experience with edaravone. Edaravone, as presently delivered, may be both ineffective and harmful.
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Mesoscale Nanoparticles Treat Cisplatin-Induced AKI and Avoid Tumor Accumulation (Exhibit Hall, Walter E. Washington Convention Center) - Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_3278; We anticipate that these studies will constitute the basis for the development of novel strategies for the treatment and prevention of cisplatin induced AKI in humans. Funding NIDDK Support
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Journal: Simultaneous Blood-Brain Barrier Crossing and Protection for Stroke Treatment Based on Edaravone-Loaded Ceria Nanoparticles. (Pubmed Central) - Oct 10, 2019 The as-designed E-A/P-CeO features highly effective BBB-crossing via receptor-mediated transcytosis to access brain tissues and synergistic elimination of ROS by both the loaded edaravone and ceria nanoparticles. Resultantly, the E-A/P-CeO with low toxicity and excellent hemo/histocompatibility, can be used to effectively treat strokes by great intracephalic uptake enhancement and in the meantime effective BBB protections, holding great potentials in the stroke therapy with much mitigated harmful side-effects and sequelae.
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Clinical, PK/PD data, Review, Journal: Two Decades-Long Journey from Riluzole to Edaravone: Revisiting the Clinical Pharmacokinetics of the Only Two Amyotrophic Lateral Sclerosis Therapeutics. (Pubmed Central) - Oct 9, 2019 The key objectives of the review were to (i) tabulate the clinical pharmacokinetics of riluzole and edaravone with emphasis on absorption, distribution, metabolism and excretion (ADME) properties; (ii) provide a comparative scenario of the pharmacokinetics of the two drugs wherever possible; and (iii) provide perspectives and introspection on the gathered clinical pharmacokinetic data of the two drugs with appropriate conjectures to quench scientific curiosity. Based on this review, the following key highlights were deduced: (i) as a result of both presystemic metabolism and polymorphic hepatic cytochrome P450 (CYP) metabolism, the oral drug riluzole exhibited more inter-subject variability than that of intravenous edaravone; (ii) using various parameters for comparison, including the published intravenous data for riluzole, it was apparent that edaravone was achieving the desired systemic concentrations to possibly drive the local brain concentrations for its efficacy in ALS patients with lesser variability than riluzole; (iii) using scientific conjectures, it was deduced that the availability of intravenous riluzole may not be beneficial in therapy due to its fast systemic clearance; (iv) on the contrary, however, there appeared to be an opportunity for the development of an oral dosage form of edaravone, which may potentially benefit the therapy option for ALS patients by avoiding hospitalization costs; and (v) because of the existence of pharmaco-resistance for the brain entry in ALS patients, it appeared prudent to consider combination strategies of edaravone and/or riluzole with suitable P-glycoprotein efflux-blocking drugs to gain more favorable outcomes in ALS patients.
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Journal: Protective effect of edaravone on blood-brain barrier by affecting NRF-2/HO-1 signaling pathway. (Pubmed Central) - Sep 27, 2019 Compared with the model group of cerebral infarction, the expression of MDA and GSH in the three edaravone groups was significantly decreased, GSH and SOD was increased (P<0.05), in a dose-dependent manner. Edaravone might play a protective role in the BBB by activating the NRF-2/HO-1 signaling pathway.
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A GOOD DISGUISE: RESPIRATORY FAILURE AS A RARE INITIAL PRESENTATION OF AMYOTROPHIC LATERAL SCLEROSIS (Ernest N. Morial Convention Center - Exhibit Hall - Poster Area 2) - Sep 25, 2019 - Abstract #CHEST2019CHEST_2818; Although uncommon, physicians should keep motor neuron diseases in the differential for patients who present with chronic respiratory failure of unclear etiology. Increased awareness can lead to earlierdiagnosis, treatment, and improved quality of life in ALS patients.
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Clinical, Journal: Bioavailability of Edaravone Sublingual Tablet Versus Intravenous Infusion in Healthy Male Volunteers. (Pubmed Central) - Sep 20, 2019 Compared with IV administration, C with SL administration was ∼17% lower and T was statistically significantly longer. The exposure differences can be addressed by modifying the strength of the SL tablet, and then conducting a second study to demonstrate the pharmacokinetic bioavailability of the sublingually administered new strength versus IV infusion of edaravone.
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Journal: Synthesis, Characterization and Antioxidant Properties of a New Lipophilic Derivative of Edaravone. (Pubmed Central) - Aug 3, 2019 Moreover, since oxidative stress is involved in numerous retinal degenerative diseases, the ability of C18-edaravone to contrast 2,2-azobis (2-amidinopropane hydrochloride) (AAPH)-induced cell death was assessed in adult retinal pigmented epithelium (ARPE-19) cells. Overall, the results demonstrated that the newly synthesized molecule has a high affinity for lipid membrane, increasing the efficacy of the unmodified edaravone under stress conditions.
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