Macleod Diabetes and Endocrine Centre, Royal Devon and Exeter Hospital, Exeter, UK.
College of Medicine and Health, University of Exeter, Exeter, UK.
Climacteric. 2021 Feb;24(1):25-31. doi: 10.1080/13697137.2020.1834530. Epub 2020 Nov 2.
Vasomotor symptoms (hot flushes, flashes, night sweats) occur in the majority of menopausal women, and are reported as being of the highest symptom priority as they often persist over many years and can be highly disruptive. Hormone therapy is the most effective available treatment but is not without risk if taken long term, and is sometimes contraindicated; for example, in women with a personal or family history of breast cancer, which is the most common female cancer worldwide. Other treatment alternatives are not as efficacious, can cause side effects, and/or are not widely available. A new, effective, targeted treatment could therefore benefit millions of women worldwide. This became possible to investigate after accumulated evidence from both animal and human models implicated heightened signaling of a hypothalamic neuropeptide together with its receptor (neurokinin B/NK3R) in the etiology of sex-steroid-deficient vasomotor symptoms. Four clinical trials of three chemically distinct oral NK3R antagonists for the treatment of menopausal flushes have since completed and published, which consistently demonstrate efficacy and tolerability of these agents. These suggest great promise to change practice in the future if ongoing further larger-scale studies of longer duration confirm the same; as, estrogen exposure will no longer be required to effectively and safely treat vasomotor symptoms.
血管舒缩症状（热潮红、阵发性发热、盗汗）发生在大多数绝经后妇女中，据报道，这些症状是最高的症状优先级，因为它们往往会持续多年，并且可能会高度干扰日常生活。激素治疗是最有效的可用治疗方法，但如果长期使用，并非没有风险，并且有时是禁忌的；例如，对于有个人或家族乳腺癌病史的妇女，乳腺癌是全球最常见的女性癌症。其他治疗选择的疗效不如激素治疗，会引起副作用，而且/或者无法广泛获得。因此，一种新的、有效的、有针对性的治疗方法可能会使全世界数以百万计的妇女受益。这是在动物和人类模型的累积证据表明，下丘脑神经肽及其受体（神经激肽 B/NK3R）的信号传导增强与绝经后血管舒缩症状的病因有关之后，才有可能进行研究。此后，已经完成并发表了四项针对绝经热潮红治疗的三种化学上不同的口服 NK3R 拮抗剂的临床试验，这些试验一致证明了这些药物的疗效和耐受性。如果正在进行的更大规模、更长时间的研究证实了同样的效果，这些结果表明它们很有希望在未来改变治疗实践；因为不再需要雌激素暴露来有效地、安全地治疗血管舒缩症状。
