ArticleBioorganic & medicinal chemistry2012
Riluzole prodrugs for melanoma and ALS: design, synthesis, and in vitro metabolic profiling.
Article in Bioorganic & medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
11 citing papers in PubMed, 31 citations in OpenAlex.
- A phase II trial of riluzole, an antagonist of metabotropic glutamate receptor 1 (GRM1) signaling, in patients with advanced melanoma.Pigment cell & melanoma research · 2018Trial
- Regulation of Autophagy and Metabolism in Hepatocellular Carcinoma: Involvement of Wnt-β-Catenin Pathway.Journal of cellular and molecular medicine · 2026Article
- Troriluzole inhibits methamphetamine place preference in rats and normalizes methamphetamine-evoked glutamate carboxypeptidase II (GCPII) protein levels in the mesolimbic pathway.Drug and alcohol dependence · 2023Article
- Riluzole regulates pancreatic cancer cell metabolism by suppressing the Wnt-β-catenin pathway.Scientific reports · 2022Article
- Dipeptide Prodrugs of the Glutamate Modulator Riluzole.ACS medicinal chemistry letters · 2018Article
- Current Therapy of Drugs in Amyotrophic Lateral Sclerosis.Current neuropharmacology · 2016Review
- PET imaging studies show enhanced expression of mGluR5 and inflammatory response during progressive degeneration in ALS mouse model expressing SOD1-G93A gene.Journal of neuroinflammation · 2015Article
- Intramolecular Rearrangement of α-Amino Acid Amide Derivatives of 2-Aminobenzothiazoles.Tetrahedron letters · 2014Article
- Is the risk of motor neuron disease increased or decreased after cancer? An Australian case-control study.PloS one · 2014Article
- Recent progress in the discovery of small molecules for the treatment of amyotrophic lateral sclerosis (ALS).Beilstein journal of organic chemistry · 2013Article
- Glutamate signaling in benign and malignant disorders: current status, future perspectives, and therapeutic implications.International journal of biological sciences · 2013Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
Riluzole (1) is an approved therapeutic for the treatment of ALS and has also demonstrated anti-melanoma activity in metabotropic glutamate GRM1 positive cell lines, a mouse xenograft assay and human clinical trials. Highly variable drug exposure following oral administration among patients, likely due to variable first pass effects from heterogeneous CYP1A2 expression, hinders its clinical use. In an effort to mitigate effects of this clearance pathway and uniformly administer riluzole at efficacious exposure levels, several classes of prodrugs of riluzole were designed, synthesized, and evaluated in multiple in vitro stability assays to predict in vivo drug levels. The optimal prodrug would possess the following profile: stability while transiting the digestive system, stability towards first pass metabolism, and metabolic lability in the plasma releasing riluzole. (S)-O-Benzyl serine derivative 9 was identified as the most promising therapeutically acceptable prodrug.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.