LYNKUET® (elinzanetant) for Healthcare Professionals

Mechanism of Action

The first and only dual neurokinin (NK) targeted therapy, an NK1 and NK3 receptor antagonist, approved for the treatment of moderate to severe VMS due to menopause
¹

Kisspeptin/neurokinin B/dynorphin (KNDy) neurons located in the hypothalamus are thought to play a key role in thermoregulation.
^2-5

Thermoregulation is the maintenance of physiologic core body temperature by balancing heat generation with heat loss.⁶

During menopause, KNDy neurons can become hyperactive. This increased neuronal activity is associated with overexpression of Substance P (SP) and Neurokinin B (NKB).^1,4,7

NKB is known to be involved in the initiation of hot flashes via NK3 receptors on thermoregulatory KNDy neuronal pathways^8,9
SP, via NK1 receptors, is thought to amplify KNDy neuronal activity^10-13

KNDy neuron hyperactivity is associated with overexpression of SP and NKB during menopause.^4,7

How LYNKUET
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Works
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LYNKUET is an NK1 and NK3 receptor antagonist

Inhibition of SP and NKB through antagonism of NK1 and NK3 receptor signaling on KNDy neurons can modulate neuronal activity in thermoregulation associated with hot flashes.

LYNKUET has higher affinity for human NK1 receptors (pKi values of 8.7 to 10.2) and NK3 receptors (pKi values of 8.0 to 8.8) than for human NK2 receptors (pKi values of approximately 6.0).

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VIEW CLINICAL STUDY DESIGNS

VMS Experience

Dosing & Administration

References
1
LYNKUET (elinzanetant) [prescribing information]. Whippany, NJ: Bayer HealthCare Pharmaceuticals, Inc.; October 2025.
2
Deecher DC, Dorries K. Understanding the pathophysiology of vasomotor symptoms (hot flushes and night sweats) that occur in perimenopause, menopause, and postmenopause life stages. Arch Womens Ment Health. 2007;10(6):247-257. doi:10.1007/s00737-007-0209-5
3
Tan CL, Knight ZA. Regulation of body temperature by the nervous system. Neuron. 2018;98(1):31-48. doi:10.1016/j.neuron.2018.02.022
4
Rance NE, Dacks 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(3):211-227. doi:10.1016/j.yfrne.2013.07.003
5
Reame NK. More promising news (mostly) on manipulating neurokinin B activity as a nonhormonal treatment of hot flashes. Menopause. 2020;27(4):375-376. doi:10.1097/GME.0000000000001530
6
Hymczak H, Gołąb A, Mendrala K, et al. Core temperature measurement-principles of correct measurement, problems, and complications. Int J Environ Res Public Health. 2021;18(20):10606. doi:10.3390/ijerph182010606
7
Hager M, Goldstein T, Fitz V, Ott J. Elinzanetant, a new combined neurokinin-1/-3 receptor antagonist for the treatment of postmenopausal vasomotor symptoms. Expert Opin Pharmacother. 2024;25(7):783-789. doi:10.1080/14656566.2024.2358131
8
Christ JP, Navarro VM, Reed SD. Nonhormonal therapies for menopausal vasomotor symptoms. JAMA. 2023;330(13):1278-1279. doi:10.1001/jama.2023.15965
9
Modi M, Dhillo WS. Neurokinin 3 receptor antagonism: a novel treatment for menopausal hot flushes. Neuroendocrinology. 2019;109(3):242-248. doi:10.1159/000495889
10
Navarro VM, Bosch MA, León S, et al. The integrated hypothalamic tachykinin-kisspeptin system as a central coordinator for reproduction. Endocrinology. 2015;156:627-637. doi:10.1210/en.2014-1651
11
deCroft S, Boehm U, Herbison AE. Neurokinin B activates arcuate kisspeptin neurons through multiple tachykinin receptors in the male mouse. Endocrinology. 2013;154:2750-2760. doi:10.1210/en.2013-1231
12
Hrabovszky E, Borsay BÁ, Rácz K, et al. Substance P immunoreactivity exhibits frequent colocalization with kisspeptin and neurokinin B in the human infundibular region. PLoS ONE. 2013;8(8):e72369. doi:10.1371/journal.pone.0072369
13
Kalil B, Ramaswamy S, Plant TM. The distribution of substance P and kisspeptin in the mediobasal hypothalamus of the male rhesus monkey and a comparison of intravenous administration of these peptides to release GnRH as reflected by LH secretion. Neuroendocrinol. 2016;103(6):711-723. doi:10.1159/000442420

The first and only dual neurokinin (NK) targeted therapy, an NK1 and NK3 receptor antagonist, approved for the treatment of moderate to severe VMS due to menopause1

Kisspeptin/neurokinin B/dynorphin (KNDy) neurons located in the hypothalamus are thought to play a key role in thermoregulation.2-5

How LYNKUET® Works1

Want to learn more about LYNKUET?

The first and only dual neurokinin (NK) targeted therapy, an NK1 and NK3 receptor antagonist, approved for the treatment of moderate to severe VMS due to menopause
¹

Kisspeptin/neurokinin B/dynorphin (KNDy) neurons located in the hypothalamus are thought to play a key role in thermoregulation.
^2-5

How LYNKUET
^®
Works
¹