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Rovatirelin is a small molecule derivative of thyrotropin-releasing hormone (TRH), developed as a TRH receptor agonist with improved central nervous system activity. It binds to the human thyrotropin-releasing hormone receptor with high affinity and promotes the release of acetylcholine and monoamine neurotransmitters such as dopamine after binding to TRH receptors in the CNS. This leads to increased spontaneous motility and enhanced noradrenergic activity, resulting in improved locomotor function. Rovatirelin has demonstrated greater potency and longer duration of action compared to taltirelin, another TRH analogue. Its primary clinical development has been for improving ataxia in patients with spinocerebellar degeneration (SCD), where it was shown to improve SARA scores in certain patient subgroups[1][4][5][6].
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