Fezolinetant

Fezolinetant is a first-in-class NK3 receptor antagonist and certified reference standard developed for the treatment of moderate-to-severe menopausal vasomotor symptoms. As the active pharmaceutical ingredient marketed as Veozah®, Fezolinetant received FDA approval for this indication, representing a novel non-hormonal therapeutic option. In pharmaceutical quality control contexts, Fezolinetant serves as the primary reference standard for impurity profiling, analytical method development, and regulatory submissions. Fezolinetant is recognized through multiple regulatory designations including INN, USAN, and WHO-DD, making it indispensable for ANDA filings and quality control testing. The drug substance Fezolinetant exhibits excellent stability when stored under recommended conditions, with powder stable for 3 years at –20°C and 2 years at 4°C. Furthermore, Fezolinetant demonstrates a well-characterized mechanism of action—blocking NKB binding to KNDy neurons in the hypothalamus—demonstrating the therapeutic potential of this novel molecular scaffold.

Product Parameters

Mechanism Of Action

Fezolinetant targets thermoregulatory abnormalities induced by declining estrogen levels during menopause: estrogen deficiency leads to excessive release of neurokinin B (NKB) from KNDy neurons in the hypothalamus (which express kisspeptin, neuropeptide B, and enkephalin), thereby activating NK3 receptors and subsequently stimulating neurons in the medial preoptic nucleus (MnPO) of the hypothalamus, resulting in abnormal heat dissipation. Fezolinetant works by selectively blocking the binding of NKB to the NK3 receptor, thereby inhibiting this signaling pathway and restoring thermoregulatory homeostasis. As the first non-hormonal treatment for vasomotor symptoms (VMS), it fills a therapeutic gap for populations contraindicated for hormone therapy (e.g., patients with cardiovascular disease or those at risk of hormone-dependent cancer), avoids the potential carcinogenic and thrombotic risks associated with traditional hormone replacement therapy, and provides a novel, precisely targeted option for the management of menopausal symptoms.

Synthetic Route

Application

Fezolinetant is an oral selective neurokinin receptor type 3 (NK3) antagonist indicated for the treatment of menopausal-related moderate to severe vasomotor symptoms (VMS).

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Reach out to Cosperpharm for Fezolinetant that combines exceptional purity with the documentation and supply reliability your research program demands. Whether you are advancing NK3 receptor research, developing analytical methods, or scaling up production, our team is ready to partner with you.