Laquinimod

Laquinimod
IUPAC name

5-chloro-N-ethyl-4-hydroxy-1-methyl-2-oxo-
N-phenyl-1,2-dihydroquinoline-3-carboxamide
Identifiers
CAS number 248282-07-7 N
PubChem 216469
ChemSpider 11444966 Y
UNII 908SY76S4G Y
ChEMBL CHEMBL66092 Y
Jmol-3D images Image 1
Properties
Molecular formula C19H17ClN2O3
Molar mass 356.803 g/mol
 N (verify) (what is: Y/N?)
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Infobox references

Laquinimod is an experimental immunomodulator developed by Active Biotech and Teva. It is currently 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 Multiple Sclerosis started in December 2007 [5] 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.[6]

External links

References

  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. 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. ^ 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. 
  5. ^ ClinicalTrials.gov NCT00509145 Safety and Efficacy of Orally Administered Laquinimod Versus Placebo for Treatment of Relapsing Remitting Multiple Sclerosis (RRMS) (ALLEGRO)
  6. ^ Kresege, Naomi (1 August 2011). "Teva’s Copaxone Successor Fails in Latest Clinical Trial". Bloomberg. http://www.bloomberg.com/news/2011-08-01/teva-s-oral-multiple-sclerosis-drug-fails-to-meet-goal-of-clinical-trial.html. 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." 
Signs and symptoms
Diagnosis and evolution following
Investigation
Treatment
Borderline forms
Other

M: CNS

anat(n/s/m/p/4/e/b/d/c/a/f/l/g)/phys/devp

noco(m/d/e/h/v/s)/cong/tumr, sysi/epon, injr

proc, drug(N1A/2AB/C/3/4/7A/B/C/D)
Intracellular
(initiation)
Macrolides/
other IL-2 inhibitors
TNF-α inhibitor
Intracellular
(reception)
Extracellular
Serum target
(noncellular)
Cellular target
Unsorted
-cept (Fusion)

M: LMC

cell/phys/auag/auab/comp, igrc

imdf/ipig/hyps/tumr

proc, drug(L3/4)