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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Initial research in this area was disappointing, giving rise to modified peptides of relatively low potency, and with significant side effects due to histamine release. This delayed for some time the introduction of useful agents into clinical practice. The most useful GnRH antagonist in oncology practice worldwide is degarelix (FirmagonTM) which was developed by Ferring Pharmaceuticals and is described in detail below. A second antagonist used for prostate cancer, abarelix (PlenaxisTM) was developed and marketed by Praecis Pharmaceuticals but is only available in Germany and has limited use in clinical practice. Two other GnRH antagonists, cetrorelix (CetrotideTM) marketed by Merck Serono and ganirelix (AntagonTM, FyremadelTM) marketed by Ferring Pharmaceuticals, are approved for use in gynecological disorders and female infertility treatments but are not used in oncology practice and so are not described below.
GnRH Antagonists in the Treatment of Uterine Fibroids
Published in John C. Petrozza, Uterine Fibroids, 2020
Tejumola Adegoke, Shruthi Mahalingaiah
Adverse reactions to newer GnRH antagonists are rare and mild. They include injection site reactions (bruising, erythema, pruritus and swelling), nausea, headache, ovarian hyperstimulation syndrome, mood changes and decreased libido. Ganirelix (Antagon, Organon International) is associated with pelvic pain and vaginal bleeding [27]. Elevations of hepatobiliary enzymes were observed with use of cetrorelix acetate (Cetrotide; Serono) [28]. Use is contraindicated in anyone with known hypersensitivity to GnRH or GnRH analogues.
Novel treatment modalities
Published in Seema Chopra, Endometriosis, 2020
GnRH antagonists act by causing direct suppression of gonadotropin release from the pituitary in a dose-dependent manner; this leads to an immediate decrease in the circulating levels of gonadal steroid hormones [15], thus creating a hypoestrogenic environment to treat ectopic endometriotic implants. As compared to GnRH agonists, GnRH antagonists immediately downregulate gonadotropin secretion by competing with the endogenous GnRH for its pituitary receptors. The advantage is avoidance of initial flare usually encountered with agonist use which may improve the compliance of the patients for long-term use. Another advantage over agonists is that circulating estradiol levels in a woman on an antagonist are in a range that is sufficient to avoid menopausal symptoms because of estrogen deprivation. Available preparations include injectables (ganirelix, cetrorelix) and oral nonpeptide forms (elagolix, abarelix, ozarelix, TAK-385) [16]. Cetrorelix (3 mg subcutaneously every week for 2 months) was used in 15 patients after laparoscopic surgery of endometriosis [17]. All patients were symptom-free during the treatment; the serum level of E2 oscillated around a mean concentration of 50 pg/mL, and there was almost complete lack of adverse events related to hypoestrogenism. A minority experienced headache (20%) and irregular bleeding (20%).
Efficacy and safety of newly developed ganirelix acetate in infertile women for assisted reproductive technology: a prospective, randomised, controlled study
Published in Journal of Obstetrics and Gynaecology, 2022
E. Jung Han, Sang Woo Lyu, In Pyung Kwak, Hwang Kwon, Dong Hee Choi, Jin Young Kim, Han Moie Park, Ji Won Kim, Eun Mi Chang, Hee Jun Lee, Min Kyung Kim, Hye Nam Lee, Jeong Yun Kim, So La Park, Woo Sik Lee
Currently, premature LH secretion suppressor, which is GnRH antagonist such as cetrorelix and ganirelix is administered during COH. Thus, the ability of GnRH antagonist to inhibit premature surges of endogenous LH is very important in COH. In our study, premature LH surge was observed in 0 (0.0%) and 3 (2.5%) subjects in the test and control group, respectively. Previous three randomised studies have compared the efficacy of ganirelix with GnRH agonist (Borm and Mannaerts 2000; European and Middle East Orgalutran Study Group 2001; Fluker et al. 2001). Although these randomised studies have shown premature LH surge 1–3% of the subjects, the LH level of >10 mIU/mL was not observed in our study. Therefore considering this finding, Ganilever PFS effectively prevents the inhibition of premature LH surge.
Luteal estradiol pretreatment of poor and normal responders during GnRH antagonist protocol
Published in Gynecological Endocrinology, 2019
Omar Sefrioui, Aicha Madkour, Ismail Kaarouch, Noureddine Louanjli
All patients were stimulated with fixed antagonist protocol using the r-FSH (Orgalutran 0.25 and Gonal-F). Further r-FSH administration (Gonal-F; Serono Laboratories, Saint Cloud, France) was started by daily subcutaneously injection (150–225 IU/day) for patients with normal ovarian response and more (mean= 300 IU/day) for patients with poor ovarian response. The FSH dose was based on the woman’s age and AMH concentration that was maintained constant for 5 days and it was adjusted according to usual parameters of follicle growth determined by serum estradiol concentrations and ultrasound monitoring. A potent, third-generation GnRH antagonist, Ganirelix (Orgalutran®, MSD Schering-Plough, France) injected subcutaneously once daily starting on day 5 or day 6 of FSH administration. An intramuscular injection of 10,000 IU of human chorionic gonadotrophin (HCG, Gonadotrophines Chorioniques Endo®, Organon) was performed after obtaining follicles ≥17 mm. Embryos produced by ICSI were cultured up to day 3. Adequate embryo quality (good quality embryos; A + B) was defined based on the presence of uniformly sized and shaped blastomeres and fragmentation lower or equal to 10%. One or two good quality embryos were transferred in utero using a Frydman catheter (CCD Laboratories, Paris, France). Luteal phase was supported by vaginal administration of micronized progesterone 600 mg/day (Utrogestan®, Besins International, Montrouge, France) from the day of oocyte pick-up to the day of pregnancy test. If a pregnancy occurred, progesterone administration was extended up to the evidence of fetal heart activity at ultrasound.
The application of PGT-A for carriers of balanced structural chromosomal rearrangements
Published in Gynecological Endocrinology, 2019
Violeta Fodina, Alesja Dudorova, Baiba Alksere, Aigars Dzalbs, Natalija Vedmedovska, Santa Andersone, Conka Una, Juris Erenpreiss, Berzina Dace
Controlled ovarian stimulation was performed using recombinant follicle-stimulating hormone (Follitropin Alfa) and gonadotropin-releasing hormone antagonist (Ganirelix acetate injection or Cetrorelix acetate). All the dosages were used considering ovarian reserve and anti-mullerian hormone values in patients medical histories. When the lead follicle reached its mean diameter 18–20 mm, 6500 IU human chorionic gonadotropin agonist (hCG) were injected subcutaneously for ovulation induction. Oocyte retrieval was performed 35–36 h after hCG injection, and all metaphase II oocytes underwent intracytoplasmic sperm injection (ICSI). Before the procedure, the quality of sperm of 7 out of 10 men were analyzed with main semen analysis test, semen functional test, and semen fragmentation test.