Relugolix for the treatment of uterine fibroids

Barra, Fabio; Seca, Marta; Corte, Luigi Della; Giampaolino, Pierluigi; Ferrero, Simone

doi:10.1358/dot.2019.55.8.3020179

Cited by 29 publications

(19 citation statements)

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“…42,43 The US Food and Drug Administration (FDA) has recently approved the use of the first oral gonadotropin-releasing hormone antagonist coupled with estradiol and norethindrone for the treatment of fibroids, 44 which has shown to effectively reduce heavy menstrual bleeding in patients. [45][46][47] These medications produce a hormonal milieu similar to the early follicular phase and reduce associated symptoms, but a perpetual regimen is required to maintain disease management, which can become quite costly for the patient.…”

Section: Medical Therapymentioning

confidence: 99%

Uterine Fibroids: Assessing Unmet Needs from Bench to Bedside

Aninye

Laitner

2021

Journal of Women's Health

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Section: Medical Therapymentioning

confidence: 99%

Uterine Fibroids: Assessing Unmet Needs from Bench to Bedside

Aninye

Laitner

2021

Journal of Women's Health

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“…However, the benefits of medical treatment, such as lower costs or better acceptance in patients, are tempered with average efficacy [93]. Recent publications have shed light on new interesting hormonal compounds, such as selective progesterone receptor modulators (SPRMs): ulipristal acetate (UPA) [92], vilaprisan (VPR) [94] and new oral gonadotropin-releasing hormone (GnRH) analogs, like elagolix [95,96], relugolix [97] or linzagolix [98]. However, UPA might cause negative effect on the liver [99] and VPR studies were discontinued due to the negative findings in its long-term use in animals [94].…”

Section: Pharmacological Treatment Of Uterine Fibroids -Hormonal Vs Non-hormonal Agentsmentioning

confidence: 99%

Non-hormonal mediators of uterine fibroid growth

Cetin¹,

Al-Hendy

Ciebiera

2020

Current Opinion in Obstetrics &Amp; Gynecology

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Purpose of the review-Uterine fibroids (UFs) are the most common benign neoplasms of the female reproductive tract and one of the major public health concerns. Although most women with UFs are asymptomatic, over 30% of them will present with varying symptoms. This review focuses on the role of non-hormonal mediators and pathways in UF biology. Furthermore, it provides data regarding the most recent findings in the field of compounds which use those non-hormonal pathways in the medical therapy of UFs.Recent findings-Complex signaling pathway alterations are crucial for UF development. The topic of the pathophysiology of UFs focuses mostly on steroids and other hormones. However, other very important pathways exist which are independent of hormones. Some of the most important pathways which are non-hormonal, but in some cases still hormone-depended, include growth factors, cytokines and inflammation, Smad proteins, wingless type/β-catenin and others.Summary-Much more is known about hormonal than about non-hormonal signaling in UFs. Growth factors, early life exposure and inflammation are key factors in UF biology. Numerous agents depend on those pathways and may find their place in the current and future therapy of UFs.

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“…Bayer AG halted the further clinical development of its candidate drug for the treatment of uterine fibroids containing vilaprisan, a compound closely resembling ulipristal and mifepristone [50]. Meanwhile, Elagolix (AbbVie Inc, North Chicago, ILL, USA) and Relagulix (Myovant Sciences Inc, Brisbane, CA, USA), drugs containing a gonadotropin-releasing hormone antagonist as the active agent, are nearing approval in the U.S. and elsewhere for the same indication (Relagulix already having been approved in Japan) [51][52][53]. Therefore, it appears more likely than not that in a few years' time, antiprogestin-containing drugs will no longer be prescribed for the treatment of uterine fibroids.…”

Section: Additional Thoughts On the Antiprogestin Co-control Of Rccvsmentioning

confidence: 99%

Herpes Simplex Viruses Whose Replication Can Be Deliberately Controlled as Candidate Vaccines

Voellmy¹,

Bloom

Vilaboa

2020

Vaccines

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Over the last few years, we have been evaluating a novel paradigm for immunization using viruses or virus-based vectors. Safety is provided not by attenuation or inactivation of vaccine viruses, but by the introduction into the viral genomes of genetic mechanisms that allow for stringent, deliberate spatial and temporal control of virus replication. The resulting replication-competent controlled viruses (RCCVs) can be activated to undergo one or, if desired, several rounds of efficient replication at the inoculation site, but are nonreplicating in the absence of activation. Extrapolating from observations that attenuated replicating viruses are better immunogens than replication-defective or inactivated viruses, it was hypothesized that RCCVs that replicate with wild-type-like efficiency when activated will be even better immunogens. The vigorous replication of the RCCVs should also render heterologous antigens expressed from them highly immunogenic. RCCVs for administration to skin sites or mucosal membranes were constructed using a virulent wild-type HSV-1 strain as the backbone. The recombinants are activated by a localized heat treatment to the inoculation site in the presence of a small-molecule regulator (SMR). Derivatives expressing influenza virus antigens were also prepared. Immunization/challenge experiments in mouse models revealed that the activated RCCVs induced far better protective immune responses against themselves as well as against the heterologous antigens they express than unactivated RCCVs or a replication-defective HSV-1 strain. Neutralizing antibody and proliferation responses mirrored these findings. We believe that the data obtained so far warrant further research to explore the possibility of developing effective RCCV-based vaccines directed to herpetic diseases and/or diseases caused by other pathogens.

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Relugolix for the treatment of uterine fibroids

Cited by 29 publications

References 0 publications

Uterine Fibroids: Assessing Unmet Needs from Bench to Bedside

Uterine Fibroids: Assessing Unmet Needs from Bench to Bedside

Non-hormonal mediators of uterine fibroid growth

Herpes Simplex Viruses Whose Replication Can Be Deliberately Controlled as Candidate Vaccines

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