Endocrine Therapies
David E. Thurston, Ilona Pysz in Chemistry and Pharmacology of Anticancer Drugs, 2021
In the UK, leuprorelin acetate is marketed by Takeda as Prostap SRTM (a 3.75 mg prefilled syringe for monthly injection) and Prostap 3TM (an 11.25 mg prefilled syringe for three-monthly injection) for locally advanced prostate cancer as an alternative to surgical castration, adjuvant treatment to radiotherapy or radical prostatectomy in patients with high-risk localized, locally advanced, or metastatic prostate cancer. It is also approved for the treatment of endometriosis, endometrial thinning before intra-uterine surgery, reduction in size of uterine fibroids, associated bleeding before surgery, and preservation of ovarian function in women. Leuprorelin is also used to treat precocious puberty and other gender-linked disorders, and to control ovarian stimulation in In Vitro Fertilization procedures.
Bacteria and Bioactive Peptides
Prakash Srinivasan Timiri Shanmugam in Understanding Cancer Therapies, 2018
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.
Gonadotropin-releasing hormone agonist triggering
David K. Gardner, Ariel Weissman, Colin M. Howles, Zeev Shoham in Textbook of Assisted Reproductive Techniques, 2017
Very few studies have been performed to determine the optimal trigger dose that will eff ctively induce oocyte maturation and prevent OHSS by minimizing luteolysis. Diff rent doses of subcutaneous leuprorelin have been used in the literature and range from 0.5 to 4 mg (19,20,29,31,50– 52). Although some studies have used a higher dose of leuprorelin 4 mg (29) and others have used two doses 12 hours apart (53), a single dose of 1 mg is eff ctive at inducing optimal mature oocyte yield (54). The dose of triptorelin has consistently been 0.2 mg in the literature (11,15,16,20,55,56). However, a randomized dose-finding study of 0.2, 0.3, and 0.4 mg of triptorelin in oocyte donors showed similar rates of mature oocytes and top-quality embryos regardless of dose (57). Although diff rent doses have been used for intranasal buserelin, Buckett et al. showed that a dose of 50 μg is the most eff ctive minimal dose to induce an endogenous surge consistently (58). Given the overall equivalent findings, availability and cost should be considered in choosing the type and dose of GnRHa to use for trigger of oocyte maturation. As there may be diff rences in the endocrine profiles of the luteal phase due to diff rences in trigger dose, further fine-tuning of the trigger dose could enhance the function of the corpora lutea and overall outcomes.
Four consecutive minimal ovarian stimulation (TetraStim) is a feasible alternative to increase the number of oocytes and improve live birth rates in poor responders who do not accept oocyte donation
Published in Gynecological Endocrinology, 2021
Selmo Geber, Luiza P. Geber, Marcello Valle, Marcos Sampaio
For endometrial priming, patients started with subcutaneous administration of leuprorelin 3.75 mg (Lectrum, Sandoz, Brazil) on the 2nd or 21st day of the menstrual cycle. When Estradiol concentration was <30 pg/ml and the ultrasound showed an endometrial thickness of <3 mm, pituitary suppression was confirmed and treatment started with estradiol valerate (Primogyna, Bayer, Brazil) 2 mg per day from day 1–5, then the dose was increased to 4 mg per day from day 6–10, and increased to 6 mg per day from day 11. After 15 days, endometrial preparation was confirmed if Estradiol levels were >150 pg/ml and vaginal ultrasound showed an endometrial thickness >7 mm. Vaginal micronized progesterone in gel (Crinone 8%; Merck, Brazil) was started 48 h before when transfer was performed on Day 2 and 72 h before when transfer was performed on Day 3.
Spinal muscular atrophy – a revisit of the diagnosis and treatment modalities
Published in International Journal of Neuroscience, 2019
Gaurava Srivastava, Preeti Srivastava
Different studies have reported application of various drug and their specific targets under in vitro and in vivo condition along with clinical trials in SMA patients (Table 4) [94–116]. Including these drugs some historic breakthrough in the treatment of SMA are also available. The first drug approved for the treatment of SMA were nusinersen (spinraza), which was a modified antisense oligonucleotide that, administered via consecutive intrathecal injections, modulates the splicing of the SMN2 mRNA transcript to include exon 7, thereby increasing the production of full-length SMN protein [117]. Oral administration of salbutamol was found effective for the improvement of social quality of life of these patients. Salbutamol may be beneficial even in SMA type II with advanced neurological impairment cases, which are increasingly common and important in children and adolescent’s lives [118]. Leuprorelin is a drug which may provide benefit for the treatment of SBMA in humans. Beneficial effect of leuprorelin on SBMA were reported by Shimohata et al. [119].
Clinical studies investigating the use of leuprorelin in Asian women with endometriosis: a review
Published in Journal of Obstetrics and Gynaecology, 2019
Yutaka Osuga, Pao-Ling Torng, Cherng-Jye Jeng
There were very few available publications and the number of retrieved results may have been impacted on by the search strategy, limiting papers to those published in English. In the past, endometriosis research has been subject to non-publications and there has been some concern about the potential for publication bias in this area (Guo 2014). Further, the most recent research on leuprorelin that has been published (and included in this review) is from more than a decade ago. Clearly, more research on leuprorelin in an Asian population of women with endometriosis is urgently needed.
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