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This thyrotropin-releasing hormone (TRH) analog is designed to protect the pyroglutamyl peptide bond in TRH from enzymatic hydrolysis [33]. Taltirelin (exhibits higher stability in the blood and brain compared to TRH, which leads to an increase of 10–100 fold in its CNS stimulatory action compared to TRH, accompanied by a much longer half-life (t½) [33]. However, taltirelin induces lower thyrotropin (TSH) release in rodents compared to TRH, suggesting a low affinity for receptors in the TSH-secreting cells of the pituitary [34]. Following oral administration to rats and dogs, taltirelin was absorbed through all regions of the small intestine and was detected intact in brain tissue up to 6 h after administration [33]. PK studies in man showed dose-dependent plasma levels, and no evidence of accumulation [33]. Oral taltirelin has been on the Japanese market for 15 years [35], and oral disintegrating tablets containing taltirelin were recently marketed there as “Ceredist®OD Tablets 5” (Mitsubishi) [35]. There is some evidence for efficacy of this TRH analog in the treatment of spinocerebellar ataxia and other neurodegenerative disorders [36,37]. A new TRH analog with potential for oral delivery is in preclinical development targeting neurodegenerative conditions [38].