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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, 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.
Gynaecological cancer
Published in Peter Hoskin, Peter Ostler, Clinical Oncology, 2020
Endometrial cancer is a hormone-dependent tumour and metastatic disease will respond to progestogens such as medroxyprogesterone acetate or megestrol. Response rates are between 20% and 30% and useful palliation of symptomatic metastases can be achieved. Responses to gonadotrophin-releasing hormone analogues such as leuprorelin are also recognized. There is no good evidence to support the use of these agents as adjuvant treatment.
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.
The latest advances in the pharmacological management of endometriosis
Published in Expert Opinion on Pharmacotherapy, 2023
Gabriel Hartner, Heinrich Husslein, Lorenz Kuessel, Manuela Gstoettner, Denise Tiringer, René Wenzl, Alexandra Perricos
Relugolix (TAK385), an oral GnRH-antagonist, is mainly metabolized in the liver and has a half-life of 37–42 hours. Three different doses, 10 mg, 20 mg, and 40 mg once daily, were compared to a placebo as well as to the GnRH-agonist Leuprorelin in a phase II trial. Here, relugolix showed a reduction from baseline of mean pelvic pain score, quantified using the visual analog scale (VAS), as well as a reduction in dysmenorrhea. In comparison with leuprorelin, 40 mg relugolix showed a more rapid decrease in E2 and FSH levels, as well as a comparable occurrence of side effects, such as hot flashes and changes in bone mineral density. An open-label parallel group extension trial examined safety as a primary endpoint, measured by changes in BMD and occurrence of adverse events. Similar changes in BMD were found in the relugolix 40 mg group and in the leuprorelin group, notably −4.9% and −4.4%, respectively [21,26,27]. A phase-III trial evaluating the efficacy and safety of relugolix demonstrated a good tolerability and a low incidence of adverse events, such as loss of BMD, or vasomotoric symptoms. This study compared placebo to relugolix 40 mg with add-back and relugolix-mono therapy with a delayed intake of add-back therapy [28].
Advanced delivery of leuprorelin acetate for the treatment of prostatic cancer
Published in Expert Review of Anticancer Therapy, 2022
Axel S Merseburger, Marie Christine Roesch
Initially, the release of leuprorelin acetate was higher after the IM-LA treatment (the maximum concentration was equal to 27 ± 4.9 versus 19 ± 8.0 ng/ml, respectively), with a shorter Tmax (1.0 ± 0.4 versus 2.1 ± 0.8 h). The leuprorelin acetate concentration was maintained for a longer period after the 1-month LA gel depot treatment (56 versus 42 days). The LA gel depot treatment showed a long-lasting LH suppression, with median levels remaining below 1.0 IU/l up to day 56 compared with IM-LA, where LH started to rise by day 35. Consequently, serum testosterone levels increased starting from day 42 in the IM-LA patients; levels of ≤50 ng/dL were maintained only in four patients. Most of the patients treated with the LA gel depot (13 out of 16) maintained serum testosterone levels ≤50 ng/dL for over 50 days.
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].