Literature DB >> 33135940

Neurokinin 3 receptor antagonists - prime time?

J K Prague1,2.   

Abstract

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.

Entities:  

Keywords:  Neurokinin 3 receptor antagonists; hot flushes; menopause; novel therapeutics; vasomotor symptoms

Year:  2020        PMID: 33135940     DOI: 10.1080/13697137.2020.1834530

Source DB:  PubMed          Journal:  Climacteric        ISSN: 1369-7137            Impact factor:   3.005


  3 in total

1.  Resistance training reduced luteinising hormone levels in postmenopausal women in a substudy of a randomised controlled clinical trial: A clue to how resistance training reduced vasomotor symptoms.

Authors:  Sigrid Nilsson; Moa Henriksson; Emilia Berin; David Engblom; Anna-Clara Spetz Holm; Mats Hammar
Journal:  PLoS One       Date:  2022-05-26       Impact factor: 3.752

2.  Functional Rescue of Inactivating Mutations of the Human Neurokinin 3 Receptor Using Pharmacological Chaperones.

Authors:  Ross C Anderson; Sharika Hanyroup; Yong Bhum Song; Zulfiah Mohamed-Moosa; Iman van den Bout; Alexis C Schwulst; Ursula B Kaiser; Robert P Millar; Claire L Newton
Journal:  Int J Mol Sci       Date:  2022-04-21       Impact factor: 6.208

Review 3.  Neurokinin 3 Receptor Antagonists Compared With Serotonin Norepinephrine Reuptake Inhibitors for Non-Hormonal Treatment of Menopausal Hot Flushes: A Systematic Qualitative Review.

Authors:  Sara J Menown; Javier A Tello
Journal:  Adv Ther       Date:  2021-09-12       Impact factor: 3.845

  3 in total

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