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Neurokinin 3 receptor antagonists – prime time?

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Pages 25-31 | Received 06 Aug 2020, Accepted 30 Sep 2020, Published online: 02 Nov 2020

References

  • Stearns V, Ullmer L, Lopez JF, Smith Y, Isaacs C, Hayes D. Hot flushes. Lancet 2002;360:1851–61
  • Avis NE, Crawford SL, Greendale G, et al. Duration of menopausal vasomotor symptoms over the menopause transition. JAMA Intern Med 2015;175:531–9
  • Carpenter JS, Woods NF, Otte JL, et al. MsFLASH participants’ priorities for alleviating menopausal symptoms. Climacteric 2015;18:859–66
  • Drewe J, Bucher KA, Zahner C. A systematic review of non-hormonal treatments of vasomotor symptoms in climacteric and cancer patients. Springerplus 2015;4:65-015-0808-y. eCollection 2015
  • Ayers B, Smith M, Hellier J, Mann E, Hunter MS. Effectiveness of group and self-help cognitive behavior therapy in reducing problematic menopausal hot flushes and night sweats (MENOS 2): a randomized controlled trial. Menopause 2012;19:749–59
  • Bray F, Ferlay J, Soerjomataram I, Siege RL, Torre LA, Jemal A. Global Cancer Statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 Cancers in 185 Countries. CA Cancer J Clin 2018;68:394–424
  • National Institute for Health and Care Excellence. Menopause: diagnosis and management. NG23, published Nov 2015, available at nice.org.uk/guidance/NG23 [last accessed 8 Oct 2020].
  • Marjoribanks J, Farquhar C, Roberts H, Lethaby A, Lee J. Long-term hormone therapy for perimenopausal and postmenopausal women. Cochrane Database Syst Rev 2017;1:CD004143
  • Rance NE, Dack PA, Mittelman-Smith MA, Romanovsky AA, Krajewski-Hall SJ. Modulation of body temperature and LH secretion by hypothalamic KNDy (Kisspeptin, Neurokinin B and Dynorphin) neurons: a novel hypothesis on the mechanism of hot flushes. Front Neuroendocrinol 2013;34:211–27
  • Prague JK, Dhillo WS. Neurokinin 3 receptor antagonism – the magic bullet for hot flushes? Climacteric 2017;20:505–9
  • Costanian C, Zangiabadi S, Bahous SA, Deonandan R, Tamim H. Reviewing the evidence on vasomotor symptoms: the role of traditional and non-traditional factors. Climacteric 2020;23:213–23
  • Rance NE, Young WS. 3rd,. Hypertrophy and increased gene expression of neurons containing neurokinin-B and substance-P messenger ribonucleic acids in the hypothalami of postmenopausal women. Endocrinology 1991;128:2239–47
  • Rometo AM, Krajewski SJ, Voytko ML, Rance NE. Hypertrophy and increased kisspeptin gene expression in the hypothalamic infundibular nucleus of postmenopausal women and ovariectomized monkeys. J Clin Endocrinol Metab 2007;92:2744–50
  • Mittelman-Smith MA, Williams H, Krajewski-Hall SJ, et al. Arcuate kisspeptin/neurokinin B/dynorphin (KNDy) neurons mediate the estrogen suppression of gonadotropin secretion and body weight. Endocrinology 2012;153:2800–12
  • Jayasena CN, Comninos AN, De Silva A, et al. Effects of neurokinin B administration on reproductive hormone secretion in healthy men and women. J Clin Endocrinol Metab 2014;99:E19–27
  • Crandall C, Manson J, Hohensee C, et al. Association of genetic variation in the tachykinin receptor 3 locus with hot flashes and night sweats in the Women’s Health Initiative Study. Menopause 2017;24:252–61
  • Nakamura K, Morrison SF. A thermosensory pathway mediating heat-defense responses. Proc Natl Acad Sci USA 2010;107:8848–53
  • Dacks PA, Krajewski SJ, Rance NE. Activation of neurokinin 3 receptors in the median preoptic nucleus decreases core temperature in the rat. Endocrinology 2011;152:4894–905
  • Mittelman-Smith MA, Krajewski-Hall SJ, McMullen NT, Rance NE. Neurokinin 3 receptor-expressing neurons in the median preoptic nucleus modulate heat-dissipation effectors in the female rat. Endocrinology 2015;156:2552–62
  • Pragu JK, Roberts RE, Comninos AN, et al. Neurokinin 3 receptor antagonism as a novel treatment for menopausal hot flushes: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet 2017;389:1809–20
  • Depypere H, Timmerman D, Donders G, et al. Treatment of menopausal vasomotor symptoms with fezolinetant, a neurokinin 3 receptor antagonist: a phase 2a trial. J Clin Endocrinol Metab 2019;104:5893–905
  • Fraser GL, Lederman S, Waldbaum A, et al. A phase 2b, randomized, placebo-controlled, double-blind, dose-ranging study of the neurokinin 3 receptor antagonist fezolinetant for vasomotor symptoms associated with menopause. Menopause 2020;27:382–92
  • Trower M, Anderson RA, Ballantyne E, Joffe H, Kerr M, Pawsey S. Effects of NT-814, a dual neurokinin 1 and 3 receptor antagonist, on vasomotor symptoms in postmenopausal women: a placebo-controlled, randomized trial. Menopause 2020;27:498–505
  • Loprinzi CL, Dueck AC, Khoyratty BS, et al. A phase iii randomized, double-blind, placebo-controlled trial of gabapentin in the management of hot flashes in men (N00CB). Ann Oncol 2009;20:542–9
  • Gordon PR, Kerwin JP, Boesen KG, Senf J. Sertraline to treat hot flashes: a randomized controlled, double-blind, crossover trial in a general population. Menopause 2006;13:568–75
  • Sloan JA, Loprinzi CL, Novotny PJ, Barton DL, Lavasseur BI, Windschitl H. Methodologic lessons learned from hot flash studies. J Clin Oncol 2001;19:4280–90
  • Prague JK, Roberts RE, Comninos AN, et al. Neurokinin 3 receptor antagonism rapidly improves vasomotor symptoms with sustained duration of action. Menopause 2018;25:862–9
  • Prague JK, Abbara A, Comninos AN, et al. Neurokinin 3 receptor antagonists do not increase FSH or estradiol secretion in menopausal women. J Endocr Soc 2020;4:bvz009
  • U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER) Center for Biologics Evaluation and Research (CBER). Guidance for industry drug-induced liver injury: premarketing clinical evaluation. 2009. http://www.fda.gov/media/116737/download [last accessed 6 Aug 2020]
  • Ratti E, Bellew K, Bettica P, et al. Results from 2 randomized, double-blind, placebo-controlled studies of the novel NK1 receptor antagonist casopitant in patients with major depressive disorder. J Clin Psychopharmacol 2011;31:727–33
  • Ratti E, Carpenter D, Zamuner S, et al. Efficacy of vestipitant, a neurokinin-1 receptor antagonist, in primary insomnia. Sleep 2013;36:1823–30
  • Skorupskaite K, George JT, Veldhuis JD, Millar RP, Anderson RA. Neurokinin 3 receptor antagonism reveals roles for neurokinin B in the regulation of gonadotropin secretion and hot flashes in postmenopausal women. Neuroendocrinology 2018;106:148–57
  • Maclennan AH, Broadbent JL, Lester S, Moore V. Oral oestrogen and combined oestrogen/progestogen therapy versus placebo for hot flushes. Cochrane Database Syst Rev 2004;2004:CD002978
  • Franco OH, Chowdhury R, Troup J, et al. Use of plant-based therapies and menopausal symptoms: a systematic review and meta-analysis. JAMA 2016;315:2554–63
  • Cholanian M, Krajewski-Hall SJ, Levine RB, McMullen NT, Rance NE. Electrophysiology of arcuate neurokinin B neurons in female Tac2-EGFP transgenic mice. Endocrinology 2014;155:2555–65
  • Cholanian M, Krajewski-Hall SJ, McMullen NT, Rance NE. Chronic oestradiol reduces the dendritic spine density of KNDy (kisspeptin/neurokinin b/dynorphin) neurones in the arcuate nucleus of ovariectomised Tac2-enhanced green fluorescent protein transgenic mice. J Neuroendocrinol 2015;27:253–63
  • Cvetkovic V, Poncet F, Fellmann D, Griffond B, Risold PY. Diencephalic neurons producing melanin-concentrating hormone are influenced by local and multiple extra-hypothalamic tachykininergic projections through the neurokinin 3 receptor. Neuroscience 2003;119:1113–45
  • Li N, Nattie E, Li A. The role of melanin concentrating hormone (MCH) in the central chemoreflex: a knockdown study by siRNA in the lateral hypothalamus in rats. PLoS One 2014;9:e103585
  • Chao OY, Huston JP, Nikolaus S, de Souza Silva MA. Concurrent assessment of memory for object and place: evidence for different preferential importance of perirhinal cortex and hippocampus and for promnestic effect of a neurokinin-3 R agonist. Neurobiol Learn Mem 2016;130:149–58
  • Andero R, Dias B, Ressler K. A role for Tac2, NkB, and Nk3 receptor in normal and dysregulated fear memory consolidation. Neuron 2014;83:444–54
  • Noel S, Sorlet C, Hospied S, et al. Suppression of weight gain in ovariectomized high-fat diet rats and in female monkeys by treatment with ESN364 (NK3 antagonist). Endocrine Rev 2017;38:OR19-6
  • Lessard A, Campos MM, Neugebauer W, Couture R. Implication of nigral tachykinin NK3 receptors in the maintenance of hypertension in spontaneously hypertensive rats: a pharmacologic and autoradiographic study. Br J Pharmacol 2003;138:554–63
  • De Brito Gariepy H, Couture R. Blockade of tachykinin NK3 receptor reverses hypertension through a dopaminergic mechanism in the ventral tegmental area of spontaneously hypertensive rats. Br J Pharmacol 2010;161:1868–84
  • Litman RE, Smith MA, Desa DG, Simpson T, Sweitzer D, Kanes SJ. The selective neurokinin 3 antagonist AZD2624 does not improve symptoms or cognition in schizophrenia: a proof-of-principle study. J Clin Psychopharmacol 2014;34:199–204
  • Meltzer H, Prus A. NK3 receptor antagonists for the treatment of schizophrenia. Drug Discov Today: Therapeut Strateg 2006;3:555–60

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