The launch of opicapone for Parkinson’s disease: negatives versus positives

Caldas, Ana Castro; Teodoro, Tiago; Ferreira, Joaquim J.

doi:10.1080/14740338.2018.1433659

Cited by 23 publications

(30 citation statements)

References 16 publications

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“…In line with data from clinical trials [3-7], opicapone was globally beneficial in patients with advanced PD and motor fluctuations under levodopa and other adjunct PD therapies. The therapeutic impact of this drug was soon perceived by both clinicians and patients.…”

supporting

confidence: 55%

Opicapone in Parkinson’s Disease: Real-World Data from a Portuguese Center

2021

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Dear Editor, Opicapone is a novel treatment option for patients with Parkinson's disease (PD) and motor fluctuations, with proven efficacy and safety in clinical trials [1][2][3][4]. Nevertheless, it is fundamental to capture the benefit and risk after a product has received regulatory approval and increase its role in health-care decisions based on realworld data.We carried out a retrospective study to evaluate the therapeutic benefits, safety, and tolerability of opicapone in day-to-day clinical practice. All 2019 clinical registries from movement disorder outpatient visits to the Neurology Department of our center were reviewed. All the patients with a PD diagnosis that initiated opicapone from January to December 2019 were included. All these patients had been managed by one of the three movement disorder specialists of our center.We documented sociodemographic (age and sex) and historical relevant data (total daily levodopa equivalent dose (LED), time since PD diagnosis, time since motor fluctuations, and time under opicapone therapy). Before and after introducing opicapone, levodopa and other adjunct PD therapies were recorded as the daily LED (Table 1), by using described conversion factors [1]. Addi-

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supporting

confidence: 55%

Opicapone in Parkinson’s Disease: Real-World Data from a Portuguese Center

2021

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“…Nevertheless, these data disclose precious information concerning possible adverse reactions that otherwise would be lost. Excluding the hepatic concern, the safety profile of tolcapone can be considered comparable to other COMT inhibitors, including a low drop-out rate for dyskinesia, being the most frequent cause of treatment discontinuation in patients under opicapone 50 mg/day [43].…”

Section: Discussionmentioning

confidence: 99%

Safety and efficacy of tolcapone in Parkinson’s disease: systematic review

Artusi

Sarro

Imbalzano

et al. 2021

Eur J Clin Pharmacol

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Purpose Tolcapone is an efficacious catechol-O-methyltransferase inhibitor for Parkinson’s disease (PD). However, safety issues hampered its use in clinical practice. We aimed to provide evidence of safety and efficacy of tolcapone by a systematic literature review to support clinicians’ choices in the use of an enlarging PD therapeutic armamentarium. Methods We searched PubMed for studies on PD patients treated with tolcapone, documenting the following outcomes: liver enzyme, adverse events (AEs), daily Off-time, levodopa daily dose, unified Parkinson’s disease rating scale (UPDRS) part-III, quality of life (QoL), and non-motor symptoms. FAERS and EudraVigilance databases for suspected AEs were interrogated for potential additional cases of hepatotoxicity. Results Thirty-two studies were included, for a total of 4780 patients treated with tolcapone. Pertaining safety, 0.9% of patients showed liver enzyme elevation > 2. Over 23 years, we found 7 cases of severe liver injury related to tolcapone, 3 of which were fatal. All fatal cases did not follow the guidelines for liver function monitoring. FAERS and EudraVigilance database search yielded 61 reports of suspected liver AEs possibly related to tolcapone. Pertaining efficacy, the median reduction of hours/day spent in Off was 2.1 (range 1–3.2), of levodopa was 108.9 mg (1–251.5), of “On” UPDRS-III was 3.6 points (1.1–6.5). Most studies reported a significant improvement of QoL and non-motor symptoms. Conclusion Literature data showed the absence of relevant safety concerns of tolcapone when strict adherence to hepatic function monitoring is respected. Given its high efficacy on motor fluctuations, tolcapone is probably an underutilized tool in the therapeutic PD armamentarium.

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“…However, of these, only tolcapone can cross the BBB and inhibit brain COMT activity, but its clinical use is limited because of its high hepatoxicity [139]. Even with the improvements that these inhibitors brought to PD treatment, researchers and pharmaceutical companies are still focused on the development of more effective and safer COMT inhibitors to improve PD therapy [140]. Structurally, the COMT catalytic Even with the improvements that these inhibitors brought to PD treatment, researchers and pharmaceutical companies are still focused on the development of more effective and safer COMT inhibitors to improve PD therapy [140].…”

Section: Catechol-o-methyltransferase Inhibitorsmentioning

confidence: 99%

“…Even with the improvements that these inhibitors brought to PD treatment, researchers and pharmaceutical companies are still focused on the development of more effective and safer COMT inhibitors to improve PD therapy [140]. Structurally, the COMT catalytic Even with the improvements that these inhibitors brought to PD treatment, researchers and pharmaceutical companies are still focused on the development of more effective and safer COMT inhibitors to improve PD therapy [140]. Structurally, the COMT catalytic site is surrounded by the "gatekeeper" residues Trp43 and Pro174, which ensure the correct orientation of the substrate, the magnesium ion and the S-(5 -Adenosyl)-L-methionine (SAM) cofactors, as well as residues Trp143, Lys144, and Glu199, which are involved in substrate binding [141].…”

Section: Catechol-o-methyltransferase Inhibitorsmentioning

confidence: 99%

Recent Developments in New Therapeutic Agents against Alzheimer and Parkinson Diseases: In-Silico Approaches

et al. 2021

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Neurodegenerative diseases (ND), including Alzheimer’s (AD) and Parkinson’s Disease (PD), are becoming increasingly more common and are recognized as a social problem in modern societies. These disorders are characterized by a progressive neurodegeneration and are considered one of the main causes of disability and mortality worldwide. Currently, there is no existing cure for AD nor PD and the clinically used drugs aim only at symptomatic relief, and are not capable of stopping neurodegeneration. Over the last years, several drug candidates reached clinical trials phases, but they were suspended, mainly because of the unsatisfactory pharmacological benefits. Recently, the number of compounds developed using in silico approaches has been increasing at a promising rate, mainly evaluating the affinity for several macromolecular targets and applying filters to exclude compounds with potentially unfavorable pharmacokinetics. Thus, in this review, an overview of the current therapeutics in use for these two ND, the main targets in drug development, and the primary studies published in the last five years that used in silico approaches to design novel drug candidates for AD and PD treatment will be presented. In addition, future perspectives for the treatment of these ND will also be briefly discussed.

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The launch of opicapone for Parkinson’s disease: negatives versus positives

Cited by 23 publications

References 16 publications

Opicapone in Parkinson’s Disease: Real-World Data from a Portuguese Center

Opicapone in Parkinson’s Disease: Real-World Data from a Portuguese Center

Safety and efficacy of tolcapone in Parkinson’s disease: systematic review

Recent Developments in New Therapeutic Agents against Alzheimer and Parkinson Diseases: In-Silico Approaches

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