"Give with a free hand, but give only your own."
 -- J.R.R. Tolkien The Children of Hurin
- Nypta -

General Information:

Wikipedia entry:
Dr. Ray Shahelien entry: 


Nypta (NP-12, Tideglusib, Zentylor)

See also Tau Busters

NOTE: Nypta has reportedly failed a clinical trial for PSP in 2012.

GSK-3 inhibitor drugs lithium and "NP-12" (Noscira, Spain), may also prevent tau protein corruption.  Lithium has side effects that make it difficult to use.  Clinical trials of NP-12 are ongoing (as of 3/6/2010).  In the clinical trials, the drug is referred to as "NP031112"  NP-12 is the commonly used name for NP031112. The drug is also known as Nypta®. The active ingredient is 4-benzyl-2-naphtalen-1-yl-1,2,4-thiadiazolidine-3,5-dione.

More about Nypta:

From the PSP Association (Europe):  http://www.pspeur.org/news_and_events/detail.html?id=245

From ClinicalTrials.gov "Safety, Tolerability, and Efficacy of Two Different Oral Doses of NP031112 Versus Placebo in the Treatment of Patients With Mild-to-Moderate Progressive Supranuclear Palsy (Tauros)" http://www.clinicaltrial.gov/ct2/show/NCT01049399

NP031112, a thiadiazolidinone compound, prevents inflammation and neurodegeneration under excitotoxic conditions: potential therapeutic role in brain disorders.

Luna-Medina R, Cortes-Canteli M, Sanchez-Galiano S, Morales-Garcia JA, Martinez A, Santos A, Perez-Castillo A.

Instituto de Investigaciones Biomédicas, Consejo Superior de Investigaciones Científicas, Universidad Autónoma de Madrid, 28029 Madrid, Spain.

Inflammation and neurodegeneration coexist in many acute damage and chronic CNS disorders (e.g., stroke, Alzheimer's disease, Parkinson's disease). A well characterized animal model of brain damage involves administration of kainic acid, which causes limbic seizure activity and subsequent neuronal death, especially in the CA1 and CA3 pyramidal cells and interneurons in the hilus of the hippocampus. Our previous work demonstrated a potent anti-inflammatory and neuroprotective effect of two thiadiazolidinones compounds, NP00111 (2,4-dibenzyl-[1,2,4]thiadiazolidine-3,5-dione) and NP01138 (2-ethyl-4-phenyl-[1,2,4]thiadiazolidine-3,5-dione), in primary cultures of cortical neurons, astrocytes, and microglia. Here, we show that injection of NP031112, a more potent thiadiazolidinone derivative, into the rat hippocampus dramatically reduces kainic acid-induced inflammation, as measured by edema formation using T2-weighted magnetic resonance imaging and glial activation and has a neuroprotective effect in the damaged areas of the hippocampus. Last, NP031112-induced neuroprotection, both in vitro and in vivo, was substantially attenuated by cotreatment with GW9662 (2-chloro-5-nitrobenzanilide), a known antagonist of the nuclear receptor peroxisome proliferator-activated receptor gamma, suggesting that the effects of NP031112 can be mediated through activation of this receptor. As such, these findings identify NP031112 as a potential therapeutic agent for the treatment of neurodegenerative disorders.
J Neurosci. 2007 May 23;27(21):5766-76.
PMID: 17522320 [PubMed]
Free article:  Journal of Neuroscience http://www.jneurosci.org/cgi/content/full/27/21/5766

Efficacy, Safety and Tolerability of Tideglusib to Treat Mild-to-Moderate Alzheimer's Disease Patients (ARGO)

The main purpose of this study is to evaluate the cognitive changes after administration of tideglusib versus placebo at two oral doses and two treatment regimes for 26 weeks in patients with mild to moderate Alzheimer's disease.

After the 26 week core treatment period, the patients may continue in the study under blinded conditions for an optional extension period up to a maximum of 39 additional weeks (total study duration up to 65 weeks), until the last patient in the study has completed the 26 week of treatment.

FDA Grants Fast Track Status to Tideglusib (Zentylor) for Progressive Supranuclear Palsy

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Updated: July 2, 2012
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