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Endocrine Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Toremifene (FarestonTM), also known as 4-chlorotamoxifen, is an orally available nonsteroidal SERM similar in structure to tamoxifen but with the addition of a chlorine substituent on the terminal carbon of the ethyl substituent (Figure 8.6). It is a mixed antagonist-agonist of the estrogen receptor, with antiestrogenic effects in breast tissue but estrogenic effects in the bone, liver, and uterus. Toremifene was introduced into medical use in 1997, and was the first antiestrogen agent to be approved since tamoxifen in 1978. Interestingly, the small structural change of the addition of a chlorine atom reduces the potency compared to tamoxifen by approximately one-third, and a dose of 60 mg daily is equivalent to a 20 mg daily of tamoxifen in the treatment of breast cancer. Structure of toremifene (FarestonTM).
Formulated Natural Selective Estrogen Receptor Modulators: A Key To Restoring Women’s Health
Published in Megh R. Goyal, Durgesh Nandini Chauhan, Plant- and Marine-Based Phytochemicals for Human Health, 2018
A. Anita Margret, S. Aishwarya, J. Theboral
Tamoxifene is widely used for this indication and is a reference compound for prevention and treatment.25, 41, 108 Toremifene has been also marketed for breast cancer treatment.16 Tamoxifene induces positive effects on bone density, whereas toremifene use is accompanied by slight reductions in bone density.59 Both toremifene and tamoxifene have an estrogen-agonistic effect on the endometrium.71, 87 Raloxifene is the chief molecule of benzothiophenes and is widely used for osteoporosis treatment and prevention. This class of SERMs is antiresorptive on bone.
Luteinized thecomatosis and other conditions associated with sclerosing peritonitis: a problem in causation, management, and nomenclature
Published in Expert Review of Anticancer Therapy, 2021
Mitigation or cure of the sclerosing peritonitis through removal of the ovaries is the most important objective for those cases that are of ovarian origin. Future studies may result in more effective treatment for peritoneal sclerosis, perhaps through the blocking of inflammatory cytokines. We are aware of two cases in which medical therapy was successful in the treatment of sclerosing peritonitis. Regarding the first patient, treatment with the anti-estrogen leuprolide and the gonadotropin-releasing hormone (GnRH) inhibitor toremifene led to a complete remission for 5 years [7]. Leuprolide is a selective estrogen receptor modulator and hence is a mixed agonist-antagonist of the estrogen receptor. It is the biological target of estrogens such as estradiol. In the second patient, a five-year complete remission of the sclerosing peritonitis was observed following therapy with the anti-estrogenic medication tamoxifin and the gonadotropin-releasing hormone (GnRH) agonist goserelin [8].
Safety of sugammadex for reversal of neuromuscular block
Published in Expert Opinion on Drug Safety, 2019
GHM Honing, CH Martini, A Bom, M van Velzen, M Niesters, LPHJ Aarts, A Dahan, M Boon
Cyclodextrins are theoretically capable of interacting with other drugs besides aminosteroidal NMBDs. This could result in dissociation of the NMBD from sugammadex, resulting in prolonged reversal times or recurrence of neuromuscular block. This was investigated by Zwiers et al., who developed a pharmacokinetic-pharmacodynamic model that took into account the binding affinity for sugammadex of NMBDs and 300 other commonly used drugs [65]. Their model indicated that toremifene and fusidic acid have a displacement potential, albeit in concentrations that are unlikely to be achieved during routine administration of these drugs [65]. In addition, flucloxacillin was found to be able to interact with sugammadex, however a subsequent clinical study could not confirm a significant displacement interaction [66]. The model of Zwiers et al. also indicated that corticosteroids were unlikely to interact with sugammadex [65]. This contrasted with in vitro findings, indicating that high-dose dexamethasone could reduce the efficacy of sugammadex in a human muscle cell model [67], but agrees with a human study which found no effect of sugammadex 4 mg/kg on serum cortisol levels [68].
The use of selective estrogen receptor modulators on bone health in men
Published in The Aging Male, 2019
Sok Kuan Wong, Nur-Vaizura Mohamad, Putri Ayu Jayusman, Ahmad Nazrun Shuid, Soelaiman Ima-Nirwana, Kok-Yong Chin
In another randomized, double-blind, placebo-controlled, phase-III trial, the effects of second generation SERMs, toremifene (80 mg/kg) on BMD were evaluated in men (n = 197; aged: ≥50 years) with serum prostate-specific antigen (PSA) of 4 ng/ml or less [48]. After 12 months of treatment, there was a significant increase in BMD at lumbar spine, total hip and femoral neck by 1.6%, 0.7% and 0.2% respectively when compared with control group [48]. Interestingly, another study carried out in a larger sample population of men (n = 1284) for 2 years showed that toremifene (80 mg/kg) treatment caused a reduction in relative risk for new fracture by 50% (95% CI –1.5 to 75.0, p = 0.05) [49]. Besides, a significant increase in BMD at the lumbar spine, hip and femoral neck, as well as concomitant decrease in bone turnover markers, were observed [49]. In a similar study of toremifene (80 mg/kg) treatment in men treated with androgen deprivation therapy (ADT) (n = 647), toremifene significantly increased BMD in all measured sites after 24 months, causing a decrease in relative risk of new fracture by 79.5% (95% CI 29.8–94.0, p < 0.005) and an absolute risk reduction of 3.8% [50]. Levels of bone-specific ALP, CTX and OC were also significantly decreased when compared with the baseline which indicated low bone turnover. Besides a variation in age gap for phase-III trial of toremifene in men younger than 80 years is warranted to confirm these findings as they found that older age appears to be a potentially important risk factor for toremifene treatment [50].