Small Effects, Questionable Outcomes: Bremelanotide for Hypoactive Sexual Desire Disorder
Efficacy outcomes are only informative to the extent that they are validated. We examined the measurement properties of efficacy measures from the phase III ("RECONNECT") bremelanotide trials for hypoactive sexual desire disorder (HSDD) in women. ...
Spielmans GI, Ellefson EM — Journal of sex research
An evaluation of bremelanotide injection for the treatment of hypoactive sexual desire disorder
Female sexual response implies a deep intertwining between psychosocial and neurobiological mediators. Regulation of central melanocortin signaling may enhance sexual desire. In premenopausal women with hypoactive sexual desire disorder (HSDD), me...
Cipriani S, Alfaroli C, Maseroli E et al. — Expert opinion on pharmacotherapy
Estradiol regulates leptin sensitivity to control feeding via hypothalamic Cited1
Until menopause, women have a lower propensity to develop metabolic diseases than men, suggestive of a protective role for sex hormones. Although a functional synergy between central actions of estrogens and leptin has been demonstrated to protect...
González-García I, García-Clavé E, Cebrian-Serrano A et al. — Cell metabolism
Targeting the central melanocortin system for the treatment of metabolic disorders
A large body of preclinical and clinical data shows that the central melanocortin system is a promising therapeutic target for treating various metabolic disorders such as obesity and cachexia, as well as anorexia nervosa. Setmelanotide, which fun...
Sweeney P, Gimenez LE, Hernandez CC et al. — Nature reviews. Endocrinology
Melanocortin receptor agonist melanotan-II microinjected in the nucleus accumbens decreases appetitive and consumptive responding for food
Obesity is a major health problem worldwide. An understanding of the factors that drive feeding behaviors is key to the development of pharmaceuticals to decrease appetite and consumption. Proopiomelanocortin (POMC), the melanocortin peptide precu...
Eliason NL, Martin L, Low MJ et al. — Neuropeptides
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists
The pleiotropic role played by melanocortin receptors (MCRs) in both physiological and pathological processes has stimulated medicinal chemists to develop synthetic agonists/antagonists with improved potency and selectivity. Here, by deploying the...
Tomassi S, Dimmito MP, Cai M et al. — Journal of medicinal chemistry
Safety Profile of Bremelanotide Across the Clinical Development Program
Background: Bremelanotide, a melanocortin receptor agonist, is Food and Drug Administration (FDA)-approved for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder. Methods: Review of bremelanotide's sa...
Clayton AH, Kingsberg SA, Portman D et al. — Journal of women's health (2002)
Medical Treatment of Female Sexual Dysfunction
Female sexual dysfunction (FSD) comprises multiple overlapping sexual disorders with a multifaceted cause within the frame of the biopsychosocial model. Health care providers can screen for FSD according to their level of expertise and deliver at ...
Nappi RE, Tiranini L, Martini E et al. — The Urologic clinics of North America
The neurobiology of bremelanotide for the treatment of hypoactive sexual desire disorder in premenopausal women
Hypoactive sexual desire disorder (HSDD) is a common female sexual dysfunction and is estimated to affect approximately 10% of women in the United States. It has been suggested that HSDD is associated with an imbalance of hormone and neurotransmit...
Pfaus JG, Sadiq A, Spana C et al. — CNS spectrums
Prespecified and Integrated Subgroup Analyses from the RECONNECT Phase 3 Studies of Bremelanotide
Background: Hypoactive sexual desire disorder (HSDD), the most prevalent female sexual dysfunction, is characterized as persistent diminished desire for sexual activity accompanied by distress. The efficacy and safety of bremelanotide, a melanocor...
Simon JA, Kingsberg SA, Portman D et al. — Journal of women's health (2002)
Pharmacologic therapeutic options for sexual dysfunction
Sexual problems are reported by up to 45% of individuals assigned female at birth. Although sexual function is a complex biopsychosocial construct, there are a number of pharmacologic treatment options aimed at addressing the changing vaginal horm...
Burton CS, Mishra K — Current opinion in obstetrics & gynecology
Bremelanotide for Treatment of Female Hypoactive Sexual Desire
Hypoactive sexual desire disorder (HSDD) is a persistent deficiency or absence of sexual fantasies and desire resulting in significant distress or interpersonal difficulty. Women with this disorder may display a lack of motivation for sexual activ...
Edinoff AN, Sanders NM, Lewis KB et al. — Neurology international
Pharmacotherapy for Sexual Dysfunction in Women
This review article discusses the controversy in the DSM-5 conceptualization and diagnostic criteria for female sexual dysfunction (FSD). An overview of recent studies on available treatments for hypoactive sexual desire disorder (HSDD), female se...
Lee JH, Lee JE, Harsh V et al. — Current psychiatry reports
Re-Analyzing Phase III Bremelanotide Trials for "Hypoactive Sexual Desire Disorder" in Women
Kingsberg et al. described results from two 24-week Phase III trials of bremelanotide for treating hypoactive sexual desire disorder (HSDD) in women. 72.72% of protocol-listed outcomes were not reported by Kingsberg et al., who provided results of...
Spielmans GI — Journal of sex research
Bremelanotide and flibanserin for low sexual desire in women: the fallacy of regulatory precedent
The US Food and Drug Administration (FDA) has approved two drugs for 'hypoactive sexual desire disorder' in women, flibanserin (Addyi) in 2015 and bremelanotide (Vyleesi) in 2019. In this paper we examine the outcome measures and clinical trial da...
Mintzes B, Tiefer L, Cosgrove L — Drug and therapeutics bulletin
Hypoactive Sexual Desire Disorder in Women: Physiology, Assessment, Diagnosis, and Treatment
Nearly half of women in the United States report problems with sexual function. Many health care providers do not ask about sexual concerns during routine clinical encounters because of personal discomfort, lack of familiarity with treatment, or t...
Pettigrew JA, Novick AM — Journal of midwifery & women's health
Bremelanotide: First Approval
Bremelanotide (Vyleesi™) is a melanocortin receptor agonist recently approved in the USA for the treatment of premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD), as characterized by low sexual desire tha...
Dhillon S, Keam SJ — Drugs
Bremelanotide: New Drug Approved for Treating Hypoactive Sexual Desire Disorder
Objective: To review data regarding bremelanotide, a recently approved therapy for hypoactive sexual desire disorder (HSDD). Data Sources: Literature search of Medline, SCOPUS, and EMBASE was performed using the search terms bremelanotide, bremela...
Mayer D, Lynch SE — The Annals of pharmacotherapy
Long-Term Safety and Efficacy of Bremelanotide for Hypoactive Sexual Desire Disorder
To evaluate the long-term safety and efficacy of bremelanotide as treatment for hypoactive sexual desire disorder in premenopausal women.
Simon JA, Kingsberg SA, Portman D et al. — Obstetrics and gynecology
Melanocortin 5 receptor signaling pathway in health and disease
Melanocortin hormone system plays a key role in maintaining the homeostasis of our body via their neuro-immune-endocrine activities and regulates a diverse array of physiological functions, including melanogenesis, inflammation, immunomodulation, ...
Xu Y, Guan X, Zhou R et al. — Cellular and molecular life sciences : CMLS
A glimpse into the underground market of melanotan
Melanotan-I and melanotan-II are alpha-melanocyte stimulating hormone (a-MSH) analogues that can be purchased illicitly online with relative ease and are injected subcutaneously to stimulate a tan. Little is known about the use of these unregulate...
Callaghan Iii DJ — Dermatology online journal
Melanoma associated with the use of melanotan-II
Unlicensed use of melanotan-II (MT-II) to promote skin pigmentation has become prevalent amongst young people attending fitness centres. We present a case where the melanocyte stimulation of MT-II in combination with the use of sun tanning beds co...
Hjuler KF, Lorentzen HF — Dermatology (Basel, Switzerland)
An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist
Melanocortins affect multiple physiological responses, including sexual behaviors. Bremelanotide is a synthetic peptide melanocortin analog of alpha-melanocyte-stimulating hormone that is an agonist at melanocortin receptors MC3R and MC4R.
Diamond LE, Earle DC, Heiman JR et al. — The journal of sexual medicine
The use of telemetry technology to test the proerectile effect of melanotan-II (MT-II) in conscious rats
The aim of this study is to demonstrate that monitoring, by means of telemetry technology, the increases in intracavernosal pressure (ICP) in freely moving rats using melanotan-II (MT-II) as a proerectile inducer compound is a relevant experimenta...
Giuliano F, Rössler AS, Clément P et al. — European urology
PT-141 Palatin
Palatin, under license from Competitive Technology, is developing the peptide PT-141, a synthetically modified analog of PT-14, as a nasal spray for the potential treatment of erectile dysfunction (ED) and female sexual dysfunction. In September 2...
Hedlund P — Current opinion in investigational drugs (London, England : 2000)
The potent melanocortin receptor agonist melanotan-II promotes peripheral nerve regeneration and has neuroprotective properties in the rat
The neurotrophic and neuroprotective potential of the alpha-melanocyte-stimulating hormone (alpha-MSH) analog cyclo-[Ac-Nle(4),Asp(5),D-Phe(7),Lys(10)]alpha-MSH-(4-10) amide (melanotan-II), a potent melanocortin receptor agonist, was investigated....
Ter Laak MP, Brakkee JH, Adan RA et al. — European journal of pharmacology
Co-treatment with melanotan-II, a potent melanocortin, does not protect against cisplatin ototoxicity
Cisplatin, an important chemotherapeutic agent, has severe dose-limiting side effects including peripheral neurotoxicity and ototoxicity. Peripheral neurotoxicity can be delayed or prevented by simultaneous treatment with a class of neuropeptides ...
Wolters FL, de Vocht TF, Klis SF et al. — Hearing research
Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study
A pilot phase I study was conducted with a cyclic heptapeptide analog of alpha-melanocyte stimulating hormone (alpha-MSH). The lactam-bridged molecule, called Melanotan-II (MT-II), has the structure Ac-Nle4-Asp5-His6-D-Phe7-Arg8-Trp9-Lys10 alpha-M...
Dorr RT, Lines R, Levine N et al. — Life sciences