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Updating {{chembox}} (changes to verified fields - added verified revid - updated 'DrugBank_Ref', 'ChEBI_Ref', 'KEGG_Ref') per Chem/Drugbox validation (report errors or [[user talk:CheMoBot...
m Added Huntington's disease as one of the diseases for which laquinimod's effect is being studied.
 
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'''Laquinimod''' is an experimental [[immunomodulator]] developed by [[Active Biotech]] and [[Teva Pharmaceutical Industries|Teva]]. It is currently being investigated as an oral treatment for [[multiple sclerosis]] (MS).
'''Laquinimod''' is an experimental [[immunomodulator]] developed by Active Biotech and [[Teva Pharmaceutical Industries|Teva]]. It is being investigated as an oral treatment for [[multiple sclerosis]] (MS) and [[Huntington's disease]].


Laquinimod is the successor of Active Biotech's failed experimental immunomodulator [[Roquinimex|linomide]].<ref>{{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 |year=2000 |month=April |pmid=10773855 |author-separator=, |author2=Lycklama à Nijeholt GJ |author3=Polman CH |display-authors=3 |last4=Adèr |first4=HJ |last5=Barkhof |first5=F}}</ref>
Laquinimod is the successor of Active Biotech's failed experimental immunomodulator [[Roquinimex|linomide]].<ref>{{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-style=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}}</ref>


The compound has been investigated in two Phase II trials using successive [[magnetic resonance imaging|magnetic resonance scans]] (MRI). Laquinimod seems to be able to reduce the MS disease activity on MRI.<ref name="pmid18572078">{{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 |year=2008 |month=June |pmid=18572078 |doi=10.1016/S0140-6736(08)60918-6 |author-separator=, |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}}</ref><ref name="pmid15781813">{{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 |year=2005 |month=March |pmid=15781813 |doi=10.1212/01.WNL.0000154520.48391.69 |author-separator=, |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}}</ref> However, the response to a given dose was discrepant between both studies.<ref>{{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 |year=2008 |month=June |pmid=18572062 |doi=10.1016/S0140-6736(08)60894-6}}</ref>
The compound has been investigated in two Phase II trials using successive [[magnetic resonance imaging|magnetic resonance scans]] (MRI). Laquinimod seems to be able to reduce the MS disease activity on MRI.<ref name="pmid18572078">{{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-style=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}}</ref><ref name="pmid15781813">{{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-style=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}}</ref><ref>{{Cite journal|last=He|first=Dian|last2=Han|first2=Kai|last3=Gao|first3=Xiangdong|last4=Dong|first4=Shuai|last5=Chu|first5=Lan|last6=Feng|first6=ZhanHui|last7=Wu|first7=Shan|editor1-first=Lan|editor1-last=Chu|date=2013-08-06|title=Laquinimod for multiple sclerosis|journal=The Cochrane Database of Systematic Reviews|issue=8|pages=CD010475|doi=10.1002/14651858.CD010475.pub2|issn=1469-493X|pmid=23922214}}</ref> However, the response to a given dose was discrepant between both studies.<ref>{{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}}</ref>


Phase III studies for Multiple Sclerosis started in December 2007 <ref>{{ClinicalTrialsGov|NCT00509145|Safety and Efficacy of Orally Administered Laquinimod Versus Placebo for Treatment of Relapsing Remitting Multiple Sclerosis (RRMS) (ALLEGRO)}}</ref> but in 2011 Teva announced that its clinical trials involving Laquinimod had failed, being unable to significantly reduce relapses into multiple sclerosis among patients beyond what a placebo was.<ref>{{cite news|last=Kresege|first=Naomi|title=Teva’s Copaxone Successor Fails in Latest Clinical Trial|url=http://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 L.P.{{!}}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.}}</ref>
Phase III studies for MS started in December 2007.<ref>{{ClinicalTrialsGov|NCT00509145|Safety and Efficacy of Orally Administered Laquinimod Versus Placebo for Treatment of Relapsing Remitting Multiple Sclerosis (RRMS) (ALLEGRO)}}</ref> In 2011, Teva announced its clinical trials involving laquinimod had failed, being unable to significantly reduce relapses in MS among patients beyond a placebo.<ref>{{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|access-date=2 August 2011|newspaper=[[Bloomberg L.P.|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.}}</ref> 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.<ref name="Comi2012">{{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| hdl = 10459.1/65687 | hdl-access = free }}</ref>
{{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 (Russia)|Ministry of Health]] (the [[Food and Drug Administration|FDA]] analog) as a treatment for relapsing-remitting multiple sclerosis (RRMS) under the brand name '''Nerventra'''.<ref>{{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|access-date=21 October 2015|language=ru}}</ref>
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== External links ==

==See also==
* [[Management of multiple sclerosis]]

⚫
==References==
{{Reflist}}

⚫
==External links==
* [http://clinicaltrials.gov/search/intervention=laquinimod Entries in NIH Study Registry]
* [http://clinicaltrials.gov/search/intervention=laquinimod Entries in NIH Study Registry]


⚫
== References ==
{{reflist}}


{{Multiple sclerosis}}
{{Multiple sclerosis}}
{{Immunosuppressants}}
{{Immunosuppressants}}

[[Category:Immunosuppressants]]
[[Category:Immunosuppressants]]
[[Category:S1P receptor modulators]]




{{antineoplastic-drug-stub}}
{{antineoplastic-drug-stub}}

[[cs:Laquinimod]]
[[sr:Lakvinimod]]

Latest revision as of 10:25, 25 January 2024

Laquinimod
Names
Preferred IUPAC name
5-Chloro-N-ethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
ECHA InfoCard 100.220.145 Edit this at Wikidata
UNII
  • InChI=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 checkY
    Key: GKWPCEFFIHSJOE-UHFFFAOYSA-N checkY
  • 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
    Key: GKWPCEFFIHSJOE-UHFFFAOYAW
  • CCN(c1ccccc1)C(=O)C\3=C(/O)c2c(Cl)cccc2N(C)C/3=O
Properties
C19H17ClN2O3
Molar mass 356.803 g/mol
Pharmacology
N07XX10 (WHO)
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)

Laquinimod is an experimental immunomodulator developed by Active Biotech and Teva. It is being investigated as an oral treatment for multiple sclerosis (MS) and Huntington's disease.

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][4] However, the response to a given dose was discrepant between both studies.[5]

Phase III studies for MS started in December 2007.[6] In 2011, Teva announced its clinical trials involving laquinimod had failed, being unable to significantly reduce relapses in MS among patients beyond a placebo.[7] 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.[8][clarification needed]

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.[9]

See also

[edit]

References

[edit]
  1. ^ Tan IL, Lycklama à Nijeholt GJ, Polman CH, et al. (April 2000). "Linomide in the treatment of multiple sclerosis: MRI results from prematurely terminated phase-III trials". Mult Scler. 6 (2): 99–104. doi:10.1191/135245800678827626. PMID 10773855.
  2. ^ Comi G, Pulizzi A, Rovaris M, et al. (June 2008). "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". Lancet. 371 (9630): 2085–2092. doi:10.1016/S0140-6736(08)60918-6. PMID 18572078.
  3. ^ Polman C, Barkhof F, Sandberg-Wollheim M, et al. (March 2005). "Treatment with laquinimod reduces development of active MRI lesions in relapsing MS". Neurology. 64 (6): 987–91. doi:10.1212/01.WNL.0000154520.48391.69. PMID 15781813.
  4. ^ He, Dian; Han, Kai; Gao, Xiangdong; Dong, Shuai; Chu, Lan; Feng, ZhanHui; Wu, Shan (2013-08-06). Chu, Lan (ed.). "Laquinimod for multiple sclerosis". The Cochrane Database of Systematic Reviews (8): CD010475. doi:10.1002/14651858.CD010475.pub2. ISSN 1469-493X. PMID 23922214.
  5. ^ Keegan BM, Weinshenker BG (June 2008). "Laquinimod, a new oral drug for multiple sclerosis". Lancet. 371 (9630): 2059–2060. doi:10.1016/S0140-6736(08)60894-6. PMID 18572062.
  6. ^ Clinical trial number NCT00509145 for "Safety and Efficacy of Orally Administered Laquinimod Versus Placebo for Treatment of Relapsing Remitting Multiple Sclerosis (RRMS) (ALLEGRO)" at ClinicalTrials.gov
  7. ^ Kresege, Naomi (1 August 2011). "Teva's Copaxone Successor Fails in Latest Clinical Trial". Bloomberg. Retrieved 2 August 2011. 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.
  8. ^ Comi, G.; Jeffery, D.; Kappos, L.; Montalban, X.; Boyko, A.; Rocca, M. A.; Filippi, M.; Allegro Study, G. (2012). "Placebo-Controlled Trial of Oral Laquinimod for Multiple Sclerosis". New England Journal of Medicine. 366 (11): 1000–1009. doi:10.1056/NEJMoa1104318. hdl:10459.1/65687. PMID 22417253.
  9. ^ "Nerventra (laquinimod) Capsules 0,6 mg. Registration certificate". State Register of Medicines (in Russian). Retrieved 21 October 2015.
[edit]



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