| 词条 | Laquinimod |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 462089089 | ImageFile=Laquinimod.svg | IUPACName=5-chloro-N-ethyl-4-hydroxy-1-methyl-2-oxo- | OtherNames= |Section1={{Chembox Identifiers | IUPHAR_ligand = 7639 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 908SY76S4G | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 11444966 | InChI = 1/C19H17ClN2O3/c1-3-22(12-8-5-4-6-9-12)19(25)16-17(23)15-13(20)10-7-11-14(15)21(2)18(16)24/h4-11,23H,3H2,1-2H3 | InChIKey = GKWPCEFFIHSJOE-UHFFFAOYAW | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 66092 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C19H17ClN2O3/c1-3-22(12-8-5-4-6-9-12)19(25)16-17(23)15-13(20)10-7-11-14(15)21(2)18(16)24/h4-11,23H,3H2,1-2H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = GKWPCEFFIHSJOE-UHFFFAOYSA-N | CASNo_Ref = {{cascite|changed|??}} | CASNo=248281-84-7 | PubChem=216469 | SMILES=CCN(c1ccccc1)C(=O)C\\3=C(/O)c2c(Cl)cccc2N(C)C/3=O |Section2={{Chembox Properties | Formula=C19H17ClN2O3 | MolarMass=356.803 g/mol | Appearance= | Density= | MeltingPt= | BoilingPt= | Solubility= |Section6={{Chembox Pharmacology | ATCCode_prefix = N07 | ATCCode_suffix = XX10 |Section7={{Chembox Hazards | MainHazards= | FlashPt= | AutoignitionPt = }} Laquinimod is an experimental immunomodulator developed by Active Biotech and Teva. It is being investigated as an oral treatment for multiple sclerosis (MS). Laquinimod is the successor of Active Biotech's failed experimental immunomodulator linomide.[1] The compound has been investigated in two Phase II trials using successive magnetic resonance scans (MRI). Laquinimod seems to be able to reduce the MS disease activity on MRI.[2][3] However, the response to a given dose was discrepant between both studies.[4] Phase III studies for MS started in December 2007.[5] In 2011, Teva announced its clinical trials involving laquinimod had failed, being unable to significantly reduce relapses in MS among patients beyond a placebo.[6] However, the final results of above-mentioned phase III trial proved oral laquinimod administered once daily slowed the progression of disability and reduced the rate of relapse in patients with relapsing–remitting multiple sclerosis.[7] {{huh?|The previous sentence says in this trial the drug failed to significantly reduce relapses versus placebo, but this sentence says the trial proved that the drug reduced relapses. Can someone familiar with the data please clarify this contradiction? - October 2015|date=October 2015}}On May 7, 2013 laquinimod was approved by the Russian Ministry of Health (the FDA analog) as a treatment for relapsing-remitting multiple sclerosis (RRMS) under the brand name Nerventra.[8] See also
References1. ^{{cite journal |author=Tan IL |title=Linomide in the treatment of multiple sclerosis: MRI results from prematurely terminated phase-III trials |journal=Mult Scler |volume=6 |issue=2 |pages=99–104 |date=April 2000 |pmid=10773855 |name-list-format=vanc|author2=Lycklama à Nijeholt GJ |author3=Polman CH |display-authors=3 |last4=Adèr |first4=HJ | author-link4 = Herman J. Adèr |last5=Barkhof |first5=F |doi=10.1191/135245800678827626}} 2. ^{{cite journal |author=Comi G |title=Effect of laquinimod on MRI-monitored disease activity in patients with relapsing-remitting multiple sclerosis: a multicentre, randomised, double-blind, placebo-controlled phase IIb study |journal=Lancet |volume=371 |issue=9630 |pages=2085–2092 |date=June 2008 |pmid=18572078 |doi=10.1016/S0140-6736(08)60918-6 |name-list-format=vanc|author2=Pulizzi A |author3=Rovaris M |display-authors=3 |last4=Abramsky |first4=O |last5=Arbizu |first5=T |last6=Boiko |first6=A |last7=Gold |first7=R |last8=Havrdova |first8=E |last9=Komoly |first9=S}} 3. ^{{cite journal |author=Polman C |title=Treatment with laquinimod reduces development of active MRI lesions in relapsing MS |journal=Neurology |volume=64 |issue=6 |pages=987–91 |date=March 2005 |pmid=15781813 |doi=10.1212/01.WNL.0000154520.48391.69 |name-list-format=vanc|author2=Barkhof F |author3=Sandberg-Wollheim M |display-authors=3 |last4=Linde |first4=A |last5=Nordle |first5=O |last6=Nederman |first6=T |author7=Laquinimod in Relapsing MS Study Group}} 4. ^{{cite journal |author=Keegan BM, Weinshenker BG |title=Laquinimod, a new oral drug for multiple sclerosis |journal=Lancet |volume=371 |issue=9630 |pages=2059–2060 |date=June 2008 |pmid=18572062 |doi=10.1016/S0140-6736(08)60894-6}} 5. ^{{ClinicalTrialsGov|NCT00509145|Safety and Efficacy of Orally Administered Laquinimod Versus Placebo for Treatment of Relapsing Remitting Multiple Sclerosis (RRMS) (ALLEGRO)}} 6. ^{{cite news|last=Kresege|first=Naomi|title=Teva’s Copaxone Successor Fails in Latest Clinical Trial|url=https://www.bloomberg.com/news/2011-08-01/teva-s-oral-multiple-sclerosis-drug-fails-to-meet-goal-of-clinical-trial.html|accessdate=2 August 2011|newspaper=Bloomberg|date=1 August 2011|quote=Teva Pharmaceutical Industries Ltd. (TEVA)’s experimental multiple sclerosis pill failed to reduce relapses more than placebo in a clinical trial, dealing a blow to the company’s effort to find a successor to an older drug.}} 7. ^{{Cite journal | last1 = Comi | first1 = G. | last2 = Jeffery | first2 = D. | last3 = Kappos | first3 = L. | last4 = Montalban | first4 = X. | last5 = Boyko | first5 = A. | last6 = Rocca | first6 = M. A. | last7 = Filippi | first7 = M. | last8 = Allegro Study | first8 = G. | title = Placebo-Controlled Trial of Oral Laquinimod for Multiple Sclerosis | doi = 10.1056/NEJMoa1104318 | journal = New England Journal of Medicine | volume = 366 | issue = 11 | pages = 1000–1009 | year = 2012 | pmid = 22417253| pmc = }} 8. ^{{cite web|title=Nerventra (laquinimod) Capsules 0,6 mg. Registration certificate|url=http://grls.rosminzdrav.ru/Grls_View_v2.aspx?idReg=64645&t=|website=State Register of Medicines|accessdate=21 October 2015|language=Russian}} External links
1 : Immunosuppressants |
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