Elinzanetant: a phase III therapy for postmenopausal patients with vasomotor symptoms

Элинзанетант: терапия III фазы для пациенток в постменопаузе с вазомоторными симптомами
Jenifer Sassarini, Richard A. Anderson
2024-01-02

ElinzanetantNK1 and NK3 receptorsneurokinin receptor antagonistsnon-hormonal therapyvasomotor symptoms
INTRODUCTION: Menopausal vasomotor symptoms (VMS) are experienced by most women and are often debilitating and can last for years. While hormone replacement therapy is effective, it carries risks that have impacted its wider use, and it can be contraindicated. There is a large unmet need for a safe, effective non-hormonal therapy. AREAS COVERED: The importance of the neurokinin (NK) system in the hypothalamic regulation of the vasomotor center has become clear. NK antagonists, previously developed for other indications, have therefore been investigated for the treatment of VMS. Elinzanetant is a potent antagonist at both NK1 (endogenous ligand Substance P) and NK3 (neurokinin B) receptors, whereas other related drugs in development are selective NK3 antagonists. Elinzanetant has been investigated in 2 Phase II trials for menopausal VMS, demonstrating rapid onset and dose-dependant efficacy for the relief of VMS and improvement in quality of life for up to 12 weeks. Phase III trials are underway in women both with physiological menopause and after treatment for breast cancer. EXPERT OPINION: Elinzanetant is a very promising non-hormonal approach to a highly prevalent symptom constellation, with rapid onset and high efficacy. Wider indications are being explored in current Phase III trials.
1
Elinzanetant addresses the unmet need for effective non-hormonal therapy when hormone replacement therapy is contraindicated or undesirable.
2
Elinzanetant is a potent dual antagonist of neurokinin-1 and neurokinin-3 receptors for non-hormonal treatment of menopausal vasomotor symptoms.
3
Phase III trials are evaluating elinzanetant in women with physiological menopause and in women treated for breast cancer.
4
The therapy is characterized as promising, with rapid onset and high efficacy, while broader indications remain under investigation.
5
Two Phase II trials showed rapid, dose-dependent relief of vasomotor symptoms and improved quality of life for up to 12 weeks.

Elinzanetant therapy in postmenopausal women with menopausal vasomotor symptoms

The efficacy, rapidity of onset, safety, and quality-of-life benefits of dual NK1/NK3 receptor antagonism for relieving menopausal vasomotor symptoms

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2024-01-02
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Jenifer Sassarini
Richard A. Anderson
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