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MedKoo product information:
Talampanel
Description of
Talampanel:
Talampanel is a glutamate receptor inhibitor with anti-seizure
activity. Talampanel is also an orally active, potent and selective
AMPA-receptor
antagonist, and can noncompetitively bind to the AMPA subtype of
glutamate excitatory amino acid receptors and may inhibit the growth of gliomas by interfering with neurotransmitters involved in brain tumor
growth. This agent may also protect against traumatic brain injury.
Talampanel (GYKI 53405) is being investigated for the treatment of
epilepsy, malignant gliomas and amyotrophic lateral sclerosis (ALS). As
of May 2010, results from the trial for ALS have been found negative. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
Current developer: Teva
Pharmaceuticals Inc.
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MedKoo Code#:
202740
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Name:
Talampanel
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CAS#:
161832-65-1
Synonym:
LY300164；GYKI-53773；Gyki 53405；Gyki-53405；LY 293606.
IUPAC/Chemical name: (8R)-7-Acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine
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Chemical structure
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Theoretical analysis
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MedKoo Code#: 202740
Name: Talampanel
CAS#: 161832-65-1
Chemical Formula: C19H19N3O3
Exact Mass: 337.14264
Molecular Weight: 337.37
Elemental Analysis: C, 67.64; H, 5.68; N, 12.46; O, 14.23
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Availability and price:
Talampanel (99%) is in stock.
Price reduced on 4/5/2013
10 mg / $250.00
20 mg / $390.00
50 mg / $650.00
100 mg / $980.00
200 mg / $1,650.00
500 mg / $2,650.00
Grams in available, please ask for
price.
For order and questions, please send email to
sales@medkoo.com. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Quality control data:
Product will be shipped with supporting
analytical data.
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Information about this agent
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Talampanel is currently being
investigated for the treatment of epilepsy, malignant gliomas and
amyotrophic lateral sclerosis (ALS). It is a noncompetitive antagonist
of the AMPA receptor, a type of glutamate receptor in the central
nervous system. (source:
http://en.wikipedia.org/wiki/Talampanel).
Teva has exclusive worldwide rights to develop and
market talampanel for the treatment of neurological disorders. Based on
talampanel',s anti-glutamate excitatory activity, Teva believes that
talampanel can significantly delay the functional deterioration of ALS
patients. Based on the scientific, mechanistic rationale and a positive
signal from a small Phase II study in ALS, Teva is proceeding with the
development of talampanel for the latter indication, and a Phase II
study has been initiated in centers in the U.S., Canada, Europe, and
Israel. to evaluate the efficacy, tolerability and safety of an oral
administration of 75mg and 150mg daily doses of talampanel for 52
weeks.The recruitment of 559 ALS patients has been completed and the
study is scheduled to end by the second quarter of 2010. (source:
http://www.tevapharm.com/research/products_ni.asp#Talampanel).
On May 17, 2010, Teva announced the results of the recently
completed trial of Talampanel for people with ALS. The results were
conclusively negative. The ALS Functional Rating scale, a tool
instrument used to assess changes in physical functioning in people with
ALS over time, was the primary outcome measure; both this measure and
the other measures investigated showed no difference in the rate of
progression in participants with ALS treated with placebo or either of 2
doses of the study medication. While there were more side effects seen
in participants treated with the Talampanel, the dropout rates were very
similar in all groups, making the negative results more convincing.
While this is a very disappointing result for patients, caregivers, and
physicians, the convincing nature of the results provides a clear answer
to the effectiveness of this treatment for people with ALS. Fortunately,
there are many other promising drugs now being tested; it is important
for all to remain hopeful and committed to finding improved therapies
for ALS. (sourcing:
http://www.alsa.org/patient/drug.cfm?id=1370).
1: Wang C, Niu L. Mechanism of
Inhibition of the GluA2 AMPA Receptor Channel Opening by Talampanel and
Its Enantiomer: The Stereochemistry of the 4-Methyl Group on the
Diazepine Ring of 2,3-Benzodiazepine Derivatives. ACS Chem Neurosci.
2013 Feb 12. [Epub ahead of print] PubMed PMID: 23402301.
2: Paizs M, Tortarolo M, Bendotti C, Engelhardt JI, Siklós L. Talampanel
reduces the level of motoneuronal calcium in transgenic mutant SOD1 mice
only if applied presymptomatically. Amyotroph Lateral Scler. 2011
Sep;12(5):340-4. doi: 10.3109/17482968.2011.584627. Epub 2011 May 30.
PubMed PMID: 21623665; PubMed Central PMCID: PMC3231880.
3: Iwamoto FM, Kreisl TN, Kim L, Duic JP, Butman JA, Albert PS, Fine HA.
Phase 2 trial of talampanel, a glutamate receptor inhibitor, for adults
with recurrent malignant gliomas. Cancer. 2010 Apr 1;116(7):1776-82. doi:
10.1002/cncr.24957. PubMed PMID: 20143438; PubMed Central PMCID:
PMC2846997.
4: Pascuzzi RM, Shefner J, Chappell AS, Bjerke JS, Tamura R, Chaudhry V,
Clawson L, Haas L, Rothstein JD. A phase II trial of talampanel in
subjects with amyotrophic lateral sclerosis. Amyotroph Lateral Scler.
2010 May 3;11(3):266-71. doi: 10.3109/17482960903307805. PubMed PMID:
19961264.
5: Grossman SA, Ye X, Chamberlain M, Mikkelsen T, Batchelor T, Desideri
S, Piantadosi S, Fisher J, Fine HA. Talampanel with standard radiation
and temozolomide in patients with newly diagnosed glioblastoma: a
multicenter phase II trial. J Clin Oncol. 2009 Sep 1;27(25):4155-61. doi:
10.1200/JCO.2008.21.6895. Epub 2009 Jul 27. PubMed PMID: 19636006;
PubMed Central PMCID: PMC2734427.
6: Aujla PK, Fetell MR, Jensen FE. Talampanel suppresses the acute and
chronic effects of seizures in a rodent neonatal seizure model.
Epilepsia. 2009 Apr;50(4):694-701. doi:
10.1111/j.1528-1167.2008.01947.x. Epub 2009 Feb 12. PubMed PMID:
19220413; PubMed Central PMCID: PMC2672962.
7: Howes JF, Bell C. Talampanel. Neurotherapeutics. 2007 Jan;4(1):126-9.
Review. PubMed PMID: 17199027.
8: Denes L, Szilágyi G, Gál A, Nagy Z. Talampanel a non-competitive
AMPA-antagonist attenuates caspase-3 dependent apoptosis in mouse brain
after transient focal cerebral ischemia. Brain Res Bull. 2006 Jul
31;70(3):260-2. Epub 2006 Mar 31. PubMed PMID: 16861112.
9: Sólyom S, Pallagi I, Abrahám G, Kertész M, Horváth G, Berzsenyi P.
New features in synthesis of talampanel related 2,3-benzodiazepines. Med
Chem. 2005 Sep;1(5):481-5. PubMed PMID: 16787333.
10: Buchwald P, Juhász A, Bell C, Pátfalusi M, Kovács P, Hochhaus G,
Howes J, Bodor N. Influence of the N-acetylation polymorphism on the
metabolism of talampanel: an investigation in fasted and fed subjects
genotyped for NAT2 variants. Pharmazie. 2006 Feb;61(2):125-34. PubMed
PMID: 16526560.
11: Erdo F, Berzsenyi P, Német L, Andrási F. Talampanel improves the
functional deficit after transient focal cerebral ischemia in rats. A
30-day follow up study. Brain Res Bull. 2006 Jan 15;68(4):269-76. Epub
2005 Sep 19. PubMed PMID: 16377432.
12: Buchwald P, Juhász A, Bell C, Pátfalusi M, Howes J, Bodor N. Unified
pharmacogenetics-based parent-metabolite pharmacokinetic model
incorporating acetylation polymorphism for talampanel in humans. J
Pharmacokinet Pharmacodyn. 2005 Aug;32(3-4):377-400. PubMed PMID:
16320099.
13: Erdo F, Berzsenyi P, Andrási F. The AMPA-antagonist talampanel is
neuroprotective in rodent models of focal cerebral ischemia. Brain Res
Bull. 2005 Jul 15;66(1):43-9. Epub 2005 Apr 21. PubMed PMID: 15925143.
14: Andrási F, Berzsenyi P, Farkas L, Körösi J, Hámori T, Botka P, Ling
I, Láng T. Omeprazole and talampanel as two examples of retrometabolic
drug design. Pharmazie. 2004 May;59(5):365-6. PubMed PMID: 15212302.
15: Langan YM, Lucas R, Jewell H, Toublanc N, Schaefer H, Sander JW,
Patsalos PN. Talampanel, a new antiepileptic drug: single- and
multiple-dose pharmacokinetics and initial 1-week experience in patients
with chronic intractable epilepsy. Epilepsia. 2003 Jan;44(1):46-53.
PubMed PMID: 12581229.
16: Világi I, Takács J, Gulyás-Kovács A, Banczerowski-Pelyhe I, Tarnawa
I. Protective effect of the antiepileptic drug candidate talampanel
against AMPA-induced striatal neurotoxicity in neonatal rats. Brain Res
Bull. 2002 Oct 15;59(1):35-40. PubMed PMID: 12372546.
17: Chappell AS, Sander JW, Brodie MJ, Chadwick D, Lledo A, Zhang D,
Bjerke J, Kiesler GM, Arroyo S. A crossover, add-on trial of talampanel
in patients with refractory partial seizures. Neurology. 2002 Jun
11;58(11):1680-2. PubMed PMID: 12058100.
18: Belayev L, Alonso OF, Liu Y, Chappell AS, Zhao W, Ginsberg MD, Busto
R. Talampanel, a novel noncompetitive AMPA antagonist, is
neuroprotective after traumatic brain injury in rats. J Neurotrauma.
2001 Oct;18(10):1031-8. PubMed PMID: 11686490.
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