Taltirelin

1. Product Basic Information

2. Product Introduction

Taltirelin is the first approved oral thyrotropin-releasing hormone (TRH) in the world. In addition to endocrine effects, it can also exert certain central nervous system (CNS) effects, including improving motor activity, antagonizing Reserpine-induced hypothermia and antagonism of sleep.

Spinocerebellar ataxias (SCAs), formerly known as autosomal dominant ataxias, are a group of chronic degenerative diseases of the central nervous system with ataxia and dysmetria as the main clinical manifestations. Before September 2000, thyrotropin-releasing hormone (TRH) injection was the only drug used to treat this type of disease.

Tatirelin is a structurally modified drug of TRH. Pharmacological studies have shown that this product has strong and long-lasting multiple effects on the CNS through brain TRH receptors. The excitatory effect of this product on the CNS is 10 to 100 times stronger than that of TRH, and the duration of action is about 8 times longer than that of TRH. The affinity of this product to TRH receptor is about 1/11 of that of TRH, so the endocrine effect of this product is weaker than that of TRH, but this product is more stable than TRH in vivo.

In addition, the effect of this product on the release of thyrotropin (TSH) is 1/6-1/11 of that of TRH. The release of TSH is regulated by a strong negative feedback system including thyroid hormone and has a strong effect on the central nervous system. But at the same time, its hormone-like effect is small, so there are fewer side effects. Adverse reactions were mainly digestive system reactions, including vomiting, nausea and stomach upset. All adverse reactions were mild to moderate and disappeared during treatment and/or after drug withdrawal.