- Full estradiol suppression with GnRH antagonists alone can result in an increase in hypoestrogenic side effects such as vasomotor symptoms (VMS).1,2 The most common symptoms of this type are hot flushes or an increase in blood pressure, but can also include night sweats and heart palpitations1,2
- UF is an estrogen-driven disease and as per the theory, initially proposed by Barbieri et al, the focus should be on maintaining hormone levels within an optimal level.2 These optimal levels are required to ensure that the estrogen levels are not too high so that there is not good enough UF control for the patient’s needs; but conversely that they are not too low that would result in hypoestrogenic effects, such as hot flushes or hypertension. The use of add-back therapy, for example, allows the maintenance of these levels within the optimal range, which in turn results in the adequate and important balance between efficacy and safety 2-4
- The Summary of Product Characteristics for any available GnRH antagonist clearly shows the incidence of potential issues, like VMS, observed in the respective Phase 3 trials5,6
1. Osuga Y et al. Obs & Gynecol 2019; 133(3): 423-433.
2. Barbieri RL. Am J Obstet Gynecol 1992;166:740–745.
3. Elsharoud A et al. Drugs of the Future 2019; 44(2): 131-143.
4. Donnez J & Dolmans MM. J Clin Med 2021; 10: 1085.
5. Relugolix Summary of Product Characteristics. https://www.ema.europa.eu/en/documents/product-information/ryeqo-epar-product-information_en.pdf
6. Linzagolix Summary of Product Characteristics. https://www.ema.europa.eu/en/medicines/human/EPAR/yselty.