PDF(Pubmed)
Abstract：
An oral fixed-dose combination of relugolix/estradiol/norethisterone (also known as norethindrone) acetate [Myfembree® (USA); Ryeqo® (EU)] (hereafter referred to as relugolix combination therapy) has been approved in the USA for the management of moderate to severe pain associated with endometriosis in premenopausal women and in the EU for the symptomatic treatment of endometriosis in adult women of reproductive age with a history of previous medical or surgical treatment for their endometriosis. The gonadotropin-releasing hormone (GnRH) receptor antagonist relugolix decreases estradiol and progesterone levels, while the addition of estradiol/norethisterone acetate mitigates hypoestrogenic effects including bone mineral density (BMD) loss and vasomotor symptoms. In two pivotal phase III trials, relugolix combination therapy significantly improved dysmenorrhoea and non-menstrual pelvic pain in premenopausal women with moderate to severe endometriosis. The combination also reduced overall pelvic pain and dyspareunia, reduced analgesic and opioid use, and improved health-related quality of life. The efficacy of relugolix combination therapy was sustained over the longer term (up to 2 years). Relugolix combination therapy was generally well tolerated and BMD loss over time was minimal. With the convenience of a once daily oral dosing regimen, relugolix combination therapy is a valuable addition to the options currently available for the management of endometriosis-associated pain.
Endometriosis is a disease where tissue similar to the lining of the uterus grows outside the uterus and may reach other organs. This causes chronic pain as a result of increased inflammation and scar tissue. Women with endometriosis may experience painful menstrual periods, pelvic pain between periods, pain during sex, painful bowel movements and painful urination. Recently, a fixed-dose tablet comprising relugolix, estradiol and norethisterone (also known as norethindrone) acetate [Myfembree® (USA); Ryeqo® (EU)] (hereafter referred to as relugolix combination therapy) has been approved to treat endometriosis-associated pain. The treatment works by decreasing levels of ovarian hormones (estrogen and progesterone). In clinical trials, relugolix combination therapy improved period pain and pain between periods in women with moderate to severe pain associated with endometriosis. The treatment also improved other symptoms (overall pelvic pain and pain during sex), reduced the need for pain medications and improved health-related quality of life. Relugolix combination therapy was generally well tolerated and caused minimal bone loss, which is known to occur with some hormone therapies. With the convenience of a once daily oral pill, relugolix combination therapy is a valuable addition to the options currently available for women with endometriosis-associated pain.
Endometriosis is a disease where tissue similar to the lining of the uterus grows outside the uterus and may reach other organs. This causes chronic pain as a result of increased inflammation and scar tissue. Women with endometriosis may experience painful menstrual periods, pelvic pain between periods, pain during sex, painful bowel movements and painful urination. Recently, a fixed-dose tablet comprising relugolix, estradiol and norethisterone (also known as norethindrone) acetate [Myfembree® (USA); Ryeqo® (EU)] (hereafter referred to as relugolix combination therapy) has been approved to treat endometriosis-associated pain. The treatment works by decreasing levels of ovarian hormones (estrogen and progesterone). In clinical trials, relugolix combination therapy improved period pain and pain between periods in women with moderate to severe pain associated with endometriosis. The treatment also improved other symptoms (overall pelvic pain and pain during sex), reduced the need for pain medications and improved health-related quality of life. Relugolix combination therapy was generally well tolerated and caused minimal bone loss, which is known to occur with some hormone therapies. With the convenience of a once daily oral pill, relugolix combination therapy is a valuable addition to the options currently available for women with endometriosis-associated pain.
摘要：
relugolix/雌二醇/炔诺酮的口服固定剂量组合（也称为炔诺酮）醋酸盐[Myfembree®（USA）;Ryeqo®（EU）]（以下称为relugolix联合疗法）已在美国获得批准，用于管理与绝经前妇女子宫内膜异位症相关的中度至重度疼痛，并在EU中对其成年子宫内膜异位症进行有手术史促性腺激素释放激素（GnRH）受体拮抗剂relugolix降低雌二醇和孕酮水平，而添加雌二醇/醋酸炔诺酮可减轻雌激素低作用，包括骨矿物质密度（BMD）损失和血管舒缩症状。在两项关键的III期试验中，relugolix联合治疗可显着改善绝经前中度至重度子宫内膜异位症妇女的痛经和非月经性盆腔疼痛。该组合还减少了整体骨盆疼痛和性交困难，减少镇痛药和阿片类药物的使用，改善与健康相关的生活质量。relugolix联合治疗的疗效持续了更长时间（长达2年）。Relugolix联合治疗通常具有良好的耐受性，并且BMD随时间的损失很小。随着每日一次口服给药方案的方便，relugolix联合治疗是目前可用于治疗子宫内膜异位症相关疼痛的有价值的选择。
子宫内膜异位症是一种类似于子宫内膜的组织在子宫外生长并可能到达其他器官的疾病。由于炎症和疤痕组织增加，这会导致慢性疼痛。患有子宫内膜异位症的女性可能会经历痛苦的月经期，月经之间的骨盆疼痛，性爱时的疼痛,排便疼痛和排尿疼痛。最近,包含relugolix的固定剂量片剂，雌二醇和炔诺酮（也称为炔诺酮）醋酸盐[Myfembree®（美国）;Ryeqo®（欧盟）]（以下称为relugolix联合疗法）已被批准用于治疗子宫内膜异位症相关疼痛。治疗通过降低卵巢激素水平（雌激素和孕激素）起作用。在临床试验中,relugolix联合治疗改善了子宫内膜异位症相关中度至重度疼痛女性的经期疼痛和间期疼痛。治疗还改善了其他症状（整体盆腔疼痛和性交疼痛），减少了对止痛药的需求，改善了与健康相关的生活质量。Relugolix联合治疗通常具有良好的耐受性，并导致最小的骨丢失，这是已知发生在一些激素治疗。方便每日一次口服药丸，relugolix联合疗法是目前可用于子宫内膜异位症相关疼痛女性的有价值的选择。
子宫内膜异位症是一种类似于子宫内膜的组织在子宫外生长并可能到达其他器官的疾病。由于炎症和疤痕组织增加，这会导致慢性疼痛。患有子宫内膜异位症的女性可能会经历痛苦的月经期，月经之间的骨盆疼痛，性爱时的疼痛,排便疼痛和排尿疼痛。最近,包含relugolix的固定剂量片剂，雌二醇和炔诺酮（也称为炔诺酮）醋酸盐[Myfembree®（美国）;Ryeqo®（欧盟）]（以下称为relugolix联合疗法）已被批准用于治疗子宫内膜异位症相关疼痛。治疗通过降低卵巢激素水平（雌激素和孕激素）起作用。在临床试验中,relugolix联合治疗改善了子宫内膜异位症相关中度至重度疼痛女性的经期疼痛和间期疼痛。治疗还改善了其他症状（整体盆腔疼痛和性交疼痛），减少了对止痛药的需求，改善了与健康相关的生活质量。Relugolix联合治疗通常具有良好的耐受性，并导致最小的骨丢失，这是已知发生在一些激素治疗。方便每日一次口服药丸，relugolix联合疗法是目前可用于子宫内膜异位症相关疼痛女性的有价值的选择。
