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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Buserelin is a synthetic nonapeptide agonist analog of GnRH (molecular weight 1,239.42) (Figure 8.27). It was first synthesized and patented by Hoechst in 1976, although it is presently marketed as an injection (SuprecurTM) and nasal spray (SuprefactTM) by Sanofi-Aventis. Buserelin is now off-patent, and several generic versions are available. Like the other GnRH agonists described in this chapter, buserelin is used for the treatment of advanced prostate cancer, endometriosis, pituitary desensitization before induction of ovulation by gonadotrophins for in vitro fertilization, and a number of other sex-hormone-related medical conditions.
Clinical Endocrinology of Pregnant Mares
Published in Juan Carlos Gardón, Katy Satué, Biotechnologies Applied to Animal Reproduction, 2020
It has been reported, that administration of a singular dose of 20–40 μg buserelin between day 9 and 10 after ovulation increase the embryo numbers in multiple ovulating and pregnancy rates up to 5–10% (Newcombe et al., 2001; Kanitz et al., 2007; Newcombe and Peters, 2014). Buserelin does not increase circulating P4 levels or preventing the luteolysis, acting independently of CL in the mare (Stout et al., 2002). These effects prevent EPL that operate between day 9–10 and day 13–14 of pregnancy.
Principles of treatment
Published in Caroline Overton, Colin Davis, Lindsay McMillan, Robert W Shaw, Charles Koh, An Atlas of ENDOMETRIOSIS, 2020
Caroline Overton, Colin Davis, Lindsay McMillan, Robert W Shaw, Charles Koh
Medical treatment of endometriosis produces no improvement in pregnancy rates compared to expectant treatment. Medical treatment with danazol1, buserelin2, medroxyprogesterone acetate1, and gestrinone3 was no more effective than placebo or expectant management in improving pregnancy rates.
Meta-analysis of the relation between irritable bowel syndrome and antibodies against endogenous gonadotropin-releasing hormone and its receptor
Published in Baylor University Medical Center Proceedings, 2023
Karam R. Motawea, Joseph Varney, Mohamed Gamal, Kirellos Said Abbas, Fatma A. Monib, Mhd Kutaiba Albuni, Elias Battikh, Bisher Sawaf, Lina Taha Khairy, Agyad Bakkour, Ali Hadi Hussein Muwaili, Fatima Abubaker Abdalla Abdelmajid, Eman Mohammed Sharif Ahmed, Dhuha Hadi Hussein Muwaili, Safaa M. A. Ahmed, Sarya Swed
Endometriosis treated with GnRH and GnRH analogs is associated with gastrointestinal tract function.10,19 One study found that some women treated with GnRH analogs for endometriosis developed GnRH antibodies and gastrointestinal dysmotility. This led to the loss of nearly all GnRH neurons of their enteric system.19 During treatment with buserelin, gastrointestinal side effects were reported,21 including constipation, nausea, and vomiting, reaffirming past ideas about the enteric nervous system and gastrointestinal motor control regulated by GnRH.22 The levels of stomach discomfort 5 years after buserelin medication were higher than they were throughout treatment. Buserelin, on the other hand, does not increase the formation of antibodies against GnRH, LH, or receptors.11 Additionally, LH receptor expression was recently discovered on human enteric neurons,20 and it was found to be lowered in rats following recurrent buserelin treatment.23
Buserelin Inhibits the Immunosuppressive Activity of Regulatory T Cells through the Protein Kinase A Signaling in a Central Precocious Puberty Model
Published in Immunological Investigations, 2022
Hua Li, Xiao-Xia Zhu, Jin-Bo Xiang, Lei Jian
The first question is why buserelin can impact Treg function. Buserelin is a GnRH agonist used in the treatments of CPP and hormone-responsive cancers such as prostate cancer or breast cancer (Brogden et al. 1990; Klijn et al. 2000). It binds to GnRHR on target cells to exert its efficacy. Under the steady condition, the expression of GnRHR in peripheral organs/tissues including lymphoid organs is very low. This is perhaps why the effect of buserelin on peripheral immune cells is overlooked by most researchers. Several studies noticed that peripheral blood mononuclear cells or T lymphocytes were affected by GnRH or GnRHas (Chen et al. 1999; Sung et al. 2015; Tanriverdi et al. 2005), but none of these studies were conducted in vivo. However, these studies suggest the presence of GnRHR on the surface of immune cells and GnRHas-induced functional changes upon ligation to GnRHR. Therefore, we were interested in whether buserelin modulates Treg activity to influence immune homeostasis. We found that Tregs constitutively expressed GnRHR, though at a relatively low level. This GnRHR expression is the molecular basis for buserelin and perhaps other GnRHas to alter Treg function.
Single-administered GnRH agonist as luteal phase support in insemination cycles: a randomized controlled trial
Published in Gynecological Endocrinology, 2022
Riikka Leppänen, Helena Tinkanen, Heini Huhtala, Katja Ahinko
Our study population represents real-life IUI patients in the fertility clinic. Because of the various ovarian stimulations and etiologies of infertility, our study population is heterogeneous, which may bear an influence on the results. The subgroups with different ovarian stimulation protocols were quite small but there was a significant difference between the live birth rates in the triptorelin and the control group among the patients using letrozole (0 vs 14.7%, p = .020). It may be possible that somehow during the same cycle, the letrozole in the early follicle phase and the triptorelin in the luteal phase have a harmful impact on the embryo-endometrium interaction, the embryo or the corpus luteum. The result could also be coincidence because of the quite small subgroups using letrozole (n = 38 vs n = 34). Conversely, the administration of the GnRH agonist buserelin in the luteal phase during the aromatase inhibitor stimulated cycle resulted in promising pregnancy rates in the study with 24 patients [12]. It is possible that the GnRH agonist at the time of implantation may require progesterone luteal support to maintain the corpus luteum function in IUI cycles.