keyword
MENU ▼
Read by QxMD icon Read
search

safinamide

keyword
https://www.readbyqxmd.com/read/28579722/pharmaceutical-approval-update
#1
Mary Choy
Ribociclib (Kisqali) for HR+/HER2- advanced or metastatic breast cancer in postmenopausal women; safinamide (Xadago) as adjunctive treatment for patients with Parkinson's disease; and avelumab (Bavencio) for metastatic Merkel cell carcinoma.
June 2017: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/28537214/pharmacokinetic-drug-evaluation-of-safinamide-mesylate-for-the-treatment-of-mid-to-late-stage-parkinson-s-disease
#2
REVIEW
Thomas Müller
Patients with Parkinson's disease suffer from a heterogeneous expression of neurotransmitter deficits. They cause an individual variable expression of motor and non-motor symptoms. Thus, drugs with various mechanisms of actions are suitable to counteract these disease related neurotransmitter alterations. Areas covered: This invited review suggests safinamide as an ideal compound for therapy of Parkinson's disease, as its pharmacological profile includes reversible monoamine oxidase B inhibition, blockage of voltage-dependent sodium channels, modulation of calcium channels and abnormal glutamate release...
June 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28504022/safinamide-for-the-treatment-of-parkinson-s-disease
#3
Ruth Mary deSouza, Anthony Schapira
The major unmet needs in the medical treatment of Parkinson disease (PD) are reduction of motor side effects from dopaminergic drugs, management of non-motor symptoms and disease modification. Areas covered: Motor fluctuations and OFF periods are a significant determinant of quality of life in PD and reducing their duration and severity can significantly improve motor function. This aim may be partly facilitated by the development of effective adjunctive drugs for dopamine replacement. Safinamide (Xadago), which is a first generation anticonvulsant, has pharmacological properties which are of interest in the context of neurodegenerative diseases, leading to research into its potential as an adjunct to levodopa in PD...
June 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28150570/identification-characterization-and-quantification-of-impurities-of-safinamide-mesilate-process-related-impurities-and-degradation-products
#4
Liang Zou, Lili Sun, Hui Zhang, Wenkai Hui, Qiaogen Zou, Zheying Zhu
The characterization of process-related impurities and degradation products of safinamide mesilate (SAFM) in bulk drugand a stability-indicating HPLC method for the separation and quantification of all the impurities were investigated. Four process-related impurities (Imp-B, Imp-C, Imp-D, and Imp-E) were found in the SAFM bulk drug. Five degradation products (Imp-A, Imp-C, Imp-D, Imp-E, and Imp-F) were observed in SAFM under oxidative conditions. Imp-C, Imp-D, and Imp-E were also degradation products and process-related impurities...
February 2, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28124620/monoamine-oxidase-b-inhibitors-in-parkinson-s-disease
#5
Livia Dézsi, László Vécsei
BACKGROUND: Parkinson's disease (PD) is a neurodegenerative disorder with a prevalence increasing with age. Oxidative stress and glutamate toxicity are involved in its pathomechanism. There are still many unmet needs of PD patients, including the alleviation of motor fluctuations and dyskinesias, and the development of therapies with neuroprotective potential. OBJECTIVE: To give an overview of the pharmacological properties, the efficacy and safety of the monoamine oxidase B (MAO-B) inhibitors in the treatment of PD, with special focus on the results of randomized clinical trials...
January 24, 2017: CNS & Neurological Disorders Drug Targets
https://www.readbyqxmd.com/read/28110399/safinamide-a-review-in-parkinson-s-disease
#6
Hannah A Blair, Sohita Dhillon
Safinamide (Xadago(®)) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. In the EU, safinamide is approved for the treatment of mid- to late-stage fluctuating Parkinson's disease (PD) as add-on therapy to a stable dose of levodopa alone or in combination with other PD medications. Safinamide 50-100 mg/day administered as a fixed or flexible dose significantly increased daily 'on' time without dyskinesia (primary endpoint) in patients with mid- to late-stage PD with motor fluctuations in 24-week, placebo-controlled clinical trials...
February 2017: CNS Drugs
https://www.readbyqxmd.com/read/27942720/assessment-of-safety-and-efficacy-of-safinamide-as-a-levodopa-adjunct-in-patients-with-parkinson-disease-and-motor-fluctuations-a-randomized-clinical-trial
#7
RANDOMIZED CONTROLLED TRIAL
Anthony H V Schapira, Susan H Fox, Robert A Hauser, Joseph Jankovic, Wolfgang H Jost, Christopher Kenney, Jaime Kulisevsky, Rajesh Pahwa, Werner Poewe, Ravi Anand
Importance: Although levodopa remains the most effective oral pharmacotherapy for Parkinson disease (PD), its use is often limited by wearing off effect and dyskinesias. Management of such complications continues to be a significant challenge. Objective: To investigate the efficacy and safety of safinamide (an oral aminoamide derivative with dopaminergic and nondopaminergic actions) in levodopa-treated patients with motor fluctuations. Design, Setting, and Participants: From March 5, 2009, through February 23, 2012, patients from academic PD care centers were randomized (1:1 ratio) to receive double-blind adjunctive safinamide or placebo for 24 weeks...
February 1, 2017: JAMA Neurology
https://www.readbyqxmd.com/read/27855360/benzyloxynitrostyrene-analogues-a-novel-class-of-selective-and-highly-potent-inhibitors-of-monoamine-oxidase-b
#8
Mietha M Van der Walt, Gisella Terre'Blanche, Jacobus P Petzer, Anél Petzer
This study examines a series of novel 3-benzyloxy-β-nitrostyrene analogues as a novel class of inhibitors of the monoamine oxidase (MAO) enzymes. MAO inhibitors are considered useful for the treatment of depression and Parkinson's disease, and have recently attracted attention as potential therapeutic agents for a range of disorders including Alzheimer's disease, prostate cancer and certain cardiomyopathies. This study shows that the 3-benzyloxy-β-nitrostyrene analogues are potent inhibitors of the MAO-B isoform with IC50 values in the nanomolar range (39-565 nM)...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27853355/anticonvulsant-effects-of-isomeric-nonimidazole-histamine-h3-receptor-antagonists
#9
Bassem Sadek, Ali Saad, Johannes Stephan Schwed, Lilia Weizel, Miriam Walter, Holger Stark
Phenytoin (PHT), valproic acid, and modern antiepileptic drugs (AEDs), eg, remacemide, loreclezole, and safinamide, are only effective within a maximum of 70%-80% of epileptic patients, and in many cases the clinical use of AEDs is restricted by their side effects. Therefore, a continuous need remains to discover innovative chemical entities for the development of active and safer AEDs. Ligands targeting central histamine H3 receptors (H3Rs) for epilepsy might be a promising therapeutic approach. To determine the potential of H3Rs ligands as new AEDs, we recently reported that no anticonvulsant effects were observed for the (S)-2-(4-(3-(piperidin-1-yl)propoxy)benzylamino)propanamide (1)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27803666/inhibitors-of-mao-a-and-mao-b-in-psychiatry-and-neurology
#10
REVIEW
John P M Finberg, Jose M Rabey
Inhibitors of MAO-A and MAO-B are in clinical use for the treatment of psychiatric and neurological disorders respectively. Elucidation of the molecular structure of the active sites of the enzymes has enabled a precise determination of the way in which substrates and inhibitor molecules are metabolized, or inhibit metabolism of substrates, respectively. Despite the knowledge of the strong antidepressant efficacy of irreversible MAO inhibitors, their clinical use has been limited by their side effect of potentiation of the cardiovascular effects of dietary amines ("cheese effect")...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27802242/effects-of-safinamide-on-pain-in-fluctuating-parkinson-s-disease-patients-a-post-hoc-analysis
#11
Carlo Cattaneo, Paolo Barone, Erminio Bonizzoni, Marco Sardina
BACKGROUND: Pain, a frequent non-motor symptom in Parkinson's Disease (PD), significantly impacts on quality of life. Safinamide is a new drug with dopaminergic and non-dopaminergic properties, approved in Europe as adjunct therapy to levodopa for the treatment of fluctuating PD patients. Results from two 24-month, double-blind, placebo-controlled studies demonstrated that safinamide has positive effects on both motor functions and quality of life in PD patients. OBJECTIVE: To investigate the effects of safinamide on pain management in PD patients with motor fluctuations using pooled data from studies 016 and SETTLE...
2017: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/27713822/population-pharmacokinetic-and-pharmacodynamic-analyses-of-safinamide-in-subjects-with-parkinson-s-disease
#12
Luca Loprete, Chiara Leuratti, Carlo Cattaneo, Mita M Thapar, Colm Farrell, Marco Sardina
Safinamide is an orally administered α-aminoamide derivative with both dopaminergic and non-dopaminergic properties. Nonlinear mixed effects models for population pharmacokinetic (PK) and pharmacokinetic-pharmacodynamic (PKPD) analyses were developed using records from, respectively, 623 and 668 patients belonging to two Phase 3, randomized, placebo-controlled, double-blind efficacy studies. The aim was to estimate safinamide population PK parameters in patients with Parkinson's disease (PD) on stable levodopa therapy, and to develop a model of safinamide effect on the PD phase of normal functioning (ON-time)...
October 2016: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/27665574/clinical-pharmacokinetics-and-pharmacodynamics-of-safinamide
#13
REVIEW
Thomas Müller, Paul Foley
The symptoms of Parkinson's disease (PD) reflect disruptions of a number of brain neurotransmitter systems of varying type and degree. Pharmacological agents with multiple neurochemical mechanisms of action are therefore promising candidates for countering these problems and providing comprehensive symptomatic relief for patients. The pharmacological profile of safinamide includes reversible monoamine oxidase B inhibition, blockage of voltage-dependent Na(+) channels, modulation of Ca(2+) channels, and inhibition of glutamate release...
March 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27536120/emerging-approaches-in-parkinson-s-disease-adjunctive-role-of-safinamide
#14
REVIEW
Thomas Müller
Ongoing neuronal death in Parkinson's disease (PD) causes an altered neurotransmission of various biogenic amines, particularly dopamine. As these changes do not follow a distinct pattern, they vary individually, and are differently pronounced. As a result, a heterogeneous onset of motor and nonmotor features occurs in each patient with PD during the whole course of the disease. PD actually describes a set of distinct diseases that manifest themselves in clinical syndromes with certain similarities but also great differences...
2016: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/26917951/adjuvant-therapies-for-parkinson-s-disease-critical-evaluation-of-safinamide
#15
REVIEW
Fabrizio Stocchi, Margherita Torti
Safinamide (SAF) is a new drug developed for the treatment of Parkinson's disease (PD). It is a benzylamino derivative with multiple mechanisms of action and antiparkinsonian, anticonvulsant, and neuroprotective properties. SAF inhibits monoamine oxidase B and dopamine reuptake and glutamate release, blocks voltage-dependent sodium channels, and modulates calcium channels. Although the antiparkinsonian effect can be ascribed in part to the inhibition of the monoamine oxidase B, which is complete at 50 mg, the enhanced benefit seen at the 100 mg dose is probably due to nondopaminergic mechanisms...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/26889632/safinamide-as-add-on-therapy-to-levodopa-in-mid-to-late-stage-parkinson-s-disease-fluctuating-patients-post-hoc-analyses-of-studies-016-and-settle
#16
RANDOMIZED CONTROLLED TRIAL
Carlo Cattaneo, Marco Sardina, Ermino Bonizzoni
BACKGROUND: Studies 016 and SETTLE showed that safinamide was safe and effective as adjunct therapy in patients with advanced Parkinson's disease (PD) and motor fluctuations. The addition of safinamide to a stable dose of levodopa alone or with other antiparkinsonian medications significantly increased ON time with no/non-troublesome dyskinesia, decreased OFF time and improved Parkinson's symptoms. OBJECTIVE: To evaluate the clinical effects of safinamide 100 mg/day on motor fluctuations and cardinal Parkinson's symptoms in specific patient subgroups using pooled data from Studies 016 and SETTLE...
2016: Journal of Parkinson's Disease
https://www.readbyqxmd.com/read/26849427/the-safety-and-efficacy-of-safinamide-mesylate-for-the-treatment-of-parkinson-s-disease
#17
REVIEW
Santiago Perez-Lloret, Olivier Rascol
Safinamide (brand name Xadago®, Zambon S.p.A) is a third-generation reversible MAO-B inhibitor, which also blocks sodium voltage-sensitive channels and modulates stimulated release of glutamate. Safinamide was recently licensed by EMA for the treatment of PD as add-on therapy to a stable dose of levodopa alone or in combination with other PD medicinal products in mid-to advanced-stage fluctuating patients. It is also under review by the US FDA. Studies in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys and 6OHDA-lesioned rats suggest antiparkinsonian efficacy and antidyskinesic effects...
2016: Expert Review of Neurotherapeutics
https://www.readbyqxmd.com/read/26825389/mitochondrial-permeability-transition-pore-a-promising-target-for-the-treatment-of-parkinson-s-disease
#18
REVIEW
Md Zeeshan Rasheed, Heena Tabassum, Suhel Parvez
Among the neurodegenerative diseases (ND), Parkinson's disease affects 6.3 million people worldwide characterized by the progressive loss of dopaminergic neurons in substantia nigra. The mitochondrial permeability transition pore (mtPTP) is a non-selective voltage-dependent mitochondrial channel whose opening modifies the permeability properties of the mitochondrial inner membrane. It is recognized as a potent pharmacological target for diseases associated with mitochondrial dysfunction and excessive cell death including ND such as Parkinson's disease (PD)...
January 2017: Protoplasma
https://www.readbyqxmd.com/read/26744740/safinamide-for-symptoms-of-parkinson-s-disease
#19
REVIEW
T Müller
Chronic and slow progression of neuronal death in Parkinson's disease is responsible for an altered neurotransmission of various biogenic amines, such as dopamine. Therefore, an individually different pronounced heterogeneity of motor and nonmotor symptoms characterizes each Parkinson's disease patient. Ideal candidates for the balance of these neurotransmitter deficits are compounds like safinamide with broad mechanisms of action such as reversible monoamine oxidase type B inhibition, blockage of voltage-dependent sodium channels, modulation of calcium channels and of glutamate release...
November 2015: Drugs of Today
https://www.readbyqxmd.com/read/26587996/clinical-pharmacology-review-of-safinamide-for-the-treatment-of-parkinson-s-disease
#20
REVIEW
Margherita Fabbri, Mario M Rosa, Daisy Abreu, Joaquim J Ferreira
Safinamide (Xadago™) is an oral α-aminoamide derivative marketed for the treatment of Parkinson's disease (PD). The drug has both dopaminergic properties, namely highly selective and reversible inhibition of monoamine oxidase B, and nondopamimetic properties, namely selective sodium channel blockade and calcium channel modulation, with consequent inhibition of excessive glutamate release. In 2014, safinamide was approved in the European Economic Area, as "an add-on therapy to stable dose levodopa, alone or in combination with other PD therapies in mid- to late-stage-fluctuating PD patients...
December 2015: Neurodegenerative Disease Management
keyword
keyword
94106
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"