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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
As with the other GnRH analogues described here, goserelin works by initially stimulating the production of testosterone and estrogen which then disrupts the endogenous hormonal feedback systems resulting in down-regulation of testosterone and estrogen.
Renal Pathophysiology
Published in Manit Arya, Taimur T. Shah, Jas S. Kalsi, Herman S. Fernando, Iqbal S. Shergill, Asif Muneer, Hashim U. Ahmed, MCQs for the FRCS(Urol) and Postgraduate Urology Examinations, 2020
Herman S. Fernando, Mohamed Yehia Abdallah, Iqbal S. Shergill
Bicalutamide is an oral non-steroidal pure anti-androgen, which acts by binding to the androgen receptor (AR) and preventing the activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones. AFP is a glycoprotein of 591 amino acids with a carbohydrate moiety. Goserelin is a synthetic analogue of a naturally occurring luteinising hormone-releasing hormone (LHRH). Goserelin is poorly protein bound and has a serum elimination half-life of two to four hours in patients with normal renal function. The most common adverse effects of sildenafil use included headache, flushing, dyspepsia, nasal congestion and impaired vision, including photophobia and blurred vision. The half-lives of tadalafil, sildenafil and vardenafil are 17.50 hours, 4.0–5.0 hours, and 4.0–5.0 hours respectively. AFP and BHCG are tumour markers for testicular cancer. AFP has a half-life of 5–7 days, whilst BHCG has a half-life of 24–36 hours.
Bacteria and Bioactive Peptides
Published in Prakash Srinivasan Timiri Shanmugam, Understanding Cancer Therapies, 2018
Ameer Khusro, Chirom Aarti, Paul Agastian
Peptides comprise a few amino acids to about 40 or more amino acids coupled through amide and/or disulfide bonds, providing varied-size molecules. In the last few years, Leuprorelin, Octreotide, and Goserelin have been used against prostate cancer and breast cancer. Carfilzomib, a protease inhibitor, is used for multiple myeloma (Kaspar and Reichert 2013). The administration of peptides can be oral, subcutaneous, intravenous, or via inhalation. In spite of limited anticancer peptides, peptide therapy may have significant potential in tumor treatment. A synthetic six amino acid peptide of αC-ß4 loop region of EGFR has been known to inhibit the dimerization and signaling activity of EGFR in the presence of its ligand (Ahsan et al. 2013). Additionally, this peptide promotes EGFR interaction with the heat shock protein Hsp90, thereby catalyzing the degradation of EGFR (Ahsan et al. 2013). At present, anticancer peptides such as Cilengitide, Trebananib, NGR-hTNF, Tyroserleutide, etc., are undergoing phase III clinical trials against glioblastoma, ovarian, mesothelioma, or liver cancers (Kaspar and Reichert 2013). The lack of targeting intracellular proteins is the major limitation of currently available anticancer peptides, thereby limiting their effectiveness (Milletti 2012). Thus, an ideal anticancer peptide involves the development of cell-penetrating peptides (CPPs) that can cross the cellular membrane to modulate key intracellular proteins involved in cancer growth regulation.
Dienogest vs GnRH agonists as postoperative therapy after laparoscopic eradication of deep infiltrating endometriosis with bowel and parametrial surgery: a randomized controlled trial
Published in Gynecological Endocrinology, 2021
Marcello Ceccaroni, Roberto Clarizia, Stefano Liverani, Agnese Donati, Matteo Ceccarello, Maria Manzone, Giovanni Roviglione, Simone Ferrero
Alternatively, Strowitzki et al. compared Dienogest to Leuprolide Acetate about pelvic pain and life quality [20,21]. The reduction of pain was identical. A non-significative improvement in quality of life was found with Dienogest. Cosson et al. compared postoperative Dienogest to Triptorelin [19,22]. No difference in terms of relapse and patients’ satisfaction. Bleeding was more common with Dienogest and hot flashes with Triptorelin. Granese et al. compared postoperative Dienogest to Leuprorelin [19,23]. Pain and quality-of-life scores were identical. No difference in imaging recurrence. Takaesu et al. compared postoperative Dienogest to Goserelin [24]. The pain was significantly lowered with both. The recurrence rate demonstrated no significant difference. Side-effects were observed more within Goserelin. Abdou et al. compared postoperative Dienogest to LA [25]. Reduction in pain was highly significant with both. Spotting and weight gain more common with Dienogest, hot flashes, and vaginal dryness with LA. A meta-analysis valued postoperative Dienogest on recurrence after surgery, compared to no treatment. The chances of recurrence appeared to be significantly lower with Dienogest (p < .001) [26].
Investigational luteinizing hormone releasing hormone (LHRH) agonists and other hormonal agents in early stage clinical trials for prostate cancer
Published in Expert Opinion on Investigational Drugs, 2019
Nirmish Singla, Rashed A. Ghandour, Ganesh V. Raj
The isolation and structural identification of the LHRH molecule was performed in 1971, and LHRH analogs were first tested in humans in 1981 [16,17]. Since then, thousands of LHRH agonists have been synthesized. Substitutions at various positions of NH2 and COOH resulted in the current forms of LHRH agonists, with prolonged duration of action and 50–100 times greater activity than the native endogenous LHRH [18–20]. In 1986, triptorelin was the first sustained-release formulation of an LHRH agonist to be commercially available. Its effect lasted for 28 days [21]. Currently the most widely used LHRH agonists are leuprolide, triptorelin, and goserelin. Leuprolide and triptorelin are available as slow-release formulations, administered intramuscularly (or subcutaneously for leuprolide) at intervals of 1–12 months. Goserelin is administered subcutaneously at intervals of 1–3 months. Various formulations of LHRH agonists are often used, as very few comparative head-to-head trials have been performed.
Unsafe testosterone-based dosing regimen of androgen deprivation therapy in patients with locally advanced or metastatic prostate cancer: a prematurely ended randomized controlled trial (MIDAS-trial)
Published in Acta Oncologica, 2021
Midas B. Mulder, Erwin Birnie, Caroline van Dijck – van Boetzelaer, Gert-Jan van de Geijn, Egbert Boevé, Elsbeth M. Westerman, Paul Hamberg
Despite the fact that LHRH agonists have been available over the past 30 years, so far no research has been done to determine whether efficiently dosing LHRH agonists reduces costs. In the Netherlands, approximately 8000 patients per year are considered for starting ADT. The majority of these patients (95%) choose chemical castration by a LHRH agonist [1]. Our study shows that for all patients in the intervention group the next injection of goserelin 10.8 mg could be postponed safely with at least 1 month. Based on the available literature and this study, if we start dosing goserelin 10.8 mg injections every 4 months instead of 3 months, total health care costs will drop with 2 million euros per year just in the Netherlands.