To verify the non-inferiority of KLH-2109 to leuprorelin acetate in a double-blind manner in terms of efficacy in endometriosis patients with pelvic pain.

开始日期2025-06-01

申办/合作机构

Kissei Pharmaceutical Co., Ltd.

NCT05738382

/ Unknown status临床2期

A Randomized, Double-blind, Open for Active Comparator, Parallel, Multi-center Phase II Study to Explore the Efficacy, Safety and Tolerability of BG2109 Compared With Cetrorelix During COH in Female Subjects Undergoing ART Procedures

To explore the optimal effective daily dose of BG2109 to suppress premature luteinizing hormone (LH) surge during COH in female subjects undergoing ART procedures.

开始日期2023-08-01

申办/合作机构

上海葆正医药科技有限公司

NCT05894135

/ Unknown status临床3期

A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Phase III Study to Evaluate the Efficacy and Safety of BG2109 in Chinese Subjects With Endometriosis

The objective of this study is to demonstrate the efficacy and safety of BG2109 administered orally once daily at a dose of 100 mg alone or of 200 mg in combination with add-back hormone replacement therapy (ABT: estradiol (E2) 1 mg / norethisterone acetate (NETA) 0.5 mg) versus placebo, while under randomized treatment, in the management of moderate to severe endometriosis-associated pain (EAP) in chinese women with surgically confirmed endometriosis

开始日期2023-07-14

申办/合作机构

上海葆正医药科技有限公司

100 项与林扎戈利相关的临床结果

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100 项与林扎戈利相关的转化医学

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100 项与林扎戈利相关的专利（医药）

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项与林扎戈利相关的文献（医药）

2025-10-01·FERTILITY AND STERILITY

Linzagolix with and without hormonal add-back therapy for symptomatic uterine fibroids: PRIMROSE 1 & 2 long-term extension and withdrawal study

Article

作者: Becker, Christian M ; Taylor, Hugh ; Becker, Sven ; Petraglia, Felice ; Hori, Satoshi ; Dolmans, Marie-Madeleine ; Donnez, Jacques ; Bestel, Elke ; Herrera, Francisco Carmona

OBJECTIVE:

To evaluate whether oral linzagolix administered once daily for up to 52 weeks (extension study) at a dose of 100 mg or 200 mg with or without hormonal add-back therapy (ABT) (1.0 mg estradiol; 0.5 mg norethisterone acetate) can maintain the efficacy and tolerability seen at 6 months of therapy and whether there is any recurrence of symptoms (bleeding and pain) after cessation of therapy (withdrawal study).

DESIGN:

PRIMROSE 1 and PRIMROSE 2 were essentially identical, randomized, parallel, double-blind, and placebo-controlled phase 3 trials conducted in women with uterine fibroid-associated heavy menstrual bleeding (HMB) (menstrual blood loss [MBL] of more than 80 mL per cycle over 2 menstrual cycles).

SUBJECTS:

In PRIMROSE 1 and 2, 1,012 women were included in the full analysis set. Eligible subjects were women aged 18 years or older with ultrasound-confirmed fibroids and HMB of at least 80 mL blood loss per cycle for a minimum of two cycles, as determined by the alkaline hematin method. Eligible participants had to have at least one fibroid measuring 2 cm in diameter or more (or multiple small fibroids with overall uterine volume exceeding 200 cm³), but no fibroids greater than 12 cm in diameter.

INTERVENTION:

Eligible women with uterine fibroid-associated HMB were randomly assigned at a 1:1:1:1:1 ratio to one of five masked daily treatment: placebo, 100 mg linzagolix alone, 100 mg linzagolix with hormonal ABT (1 mg estradiol and 0.5 mg norethisterone acetate), 200 mg linzagolix alone , or 200 mg linzagolix with hormonal ABT (1 mg estradiol and 0.5 mg norethisterone acetate). After 24 weeks, patients assigned to the placebo or 200 mg linzagolix alone groups were switched to 200 mg linzagolix with ABT, except in PRIMROSE 1, in which 50% of subjects on a placebo continued with the placebo (random selection) until week 52. All other women continued on the original study medication. Efficacy and safety were evaluated at week 52 (extension study) as well as week 64 (withdrawal study). Bone mineral density was also assessed at week 76 (6 months after cessation of therapy).

MAIN OUTCOME MEASURES:

The primary endpoint was decreased MBL to less than 80 mL and a reduction of more than 50% from baseline. Specifically, this study sought to determine whether the reduction in MBL and other secondary outcomes, such as uterine volume and pain, observed at 24 weeks could be maintained over an extended (52 weeks) treatment period and further withdrawal period.

RESULTS:

In the pooled data from PRIMROSE 1 and PRIMROSE 2 extension studies, the significantly higher proportion of women showing a reduction in HMB in all linzagolix (with or without ABT) treatment groups observed at week 24, was maintained until week 52. Percentages of women with reduced MBL at week 52 (based on the pooled week 52 full analysis set) were 55.0% in the 100 mg group, 86.1% in the 100 mg with ABT group, 76.7% in the 200 mg group/200 mg with ABT, and 89.9% in the 200 mg with ABT group. Of subjects previously treated with linzagolix and in amenorrhea by week 52, 88.8% reported their first bleed or heavy bleeding between weeks 52 and 64. In both PRIMROSE studies, the most common adverse events up to week 52 were hot flushes. Their incidence had returned to baseline values by week 64. Bone mineral density was well preserved in all groups at week 52. In women treated with 200 mg linzagolix alone up to week 24, initial bone mineral density loss (lumbar spine) recovered by week 52 after adding ABT from week 24 onwards.

CONCLUSION:

Findings at 52 weeks confirmed the benefits of treatment observed at 24 weeks. At 52 weeks, linzagolix 100 mg or 200 mg with or without ABT was found to reduce HMB, which is a burden for women with uterine fibroids. Their quality of life was improved. Risks of bone loss and vasomotor symptoms were minimized as a result of ABT administration. Partial suppression with once-daily linzagolix 100 mg without ABT potentially provides a unique option for chronic treatment of symptomatic uterine fibroids in women who do not wish to have ABT or in whom it is contraindicated. The relatively fast recurrence of uterine fibroid-associated symptoms after cessation of therapy is an argument in favor of long-term continuation of treatment.

TRIAL REGISTRATION:

PRIMROSE1 (NCT03070899) PRIMROSE 2 (NCT03070951).

2025-08-01·BJOG-AN INTERNATIONAL JOURNAL OF OBSTETRICS AND GYNAECOLOGY

Pain Reduction in Linzagolix‐Treated Patients With Uterine Fibroids: A Secondary Mediation Analysis of the PRIMROSE 1 and 2 Phase 3 Trials

Article

作者: Boolell, Mitra ; Petraglia, Felice ; Dolmans, Marie‐Madeleine ; Becker, Sven ; Bestel, Elke ; Herrera, Francisco Carmona ; Ionescu‐Ittu, Raluca ; Donnez, Jacques ; Renner, Stefan P. ; Hori, Satoshi ; St‐Pierre, Julien

ABSTRACT:

Objective:

Among women with uterine fibroids (UFs), we assess the extent to which the linzagolix effect on pain alleviation is explained by its effect on reducing heavy menstrual bleeding (HMB) and fibroid volume (FV).

Design:

Post hoc analysis on the pooled data from two randomised double‐blind placebo‐controlled phase 3 trials.

Setting:

94 sites in the US (PRIMROSE 1 trial) and 95 sites in Europe/US (PRIMROSE 2 trial).

Population:

Women aged ≥ 18 years with ultrasound‐confirmed UFs and HMB (n = 1012).

Methods:

Participants were randomised to linzagolix (100 mg and 200 mg, with and without hormonal add‐back therapy) versus placebo. A post hoc mediation analysis was conducted on the pooled PRIMROSE 1 and PRIMROSE 2 data. The effect of linzagolix versus placebo on pain reduction was divided into three components (effect explained by HMB reduction associated with linzagolix, FV reduction associated with linzagolix, and remaining [not yet explained] treatment effect), with proportions of each component reported.

Main Outcome Measures:

The mediation analysis outcome was clinically significant pain reduction, defined as a change of ≥ 2 pain categories from baseline to Week 24 using the Numeric Rating Scale (pain categories: no pain (0), and mild (1–3), moderate (4–6), severe pain (7–10)).

Results:

In the mediation analysis, 28%–51% (depending on treatment arm) of linzagolix effect on pain reduction was explained by its effect on HMB reduction, while 2%–8% was explained by its effect on FV reduction. The residual proportion ranged between 44% and 67%, depending on treatment arm, and was statistically significant only in the linzagolix 200 mg without add‐back therapy arm (p = 0.002).

Conclusions:

This analysis showed that reductions in pain were significantly mediated by reductions in HMB (all doses) and FV (200 mg alone) in linzagolix‐treated women with UFs. Further research is needed to identify additional mediating factors.

Trial Registration:

ClinicalTrials.gov: NCT03070899 and NCT03070951

2025-06-07·Human Reproduction Open

Two-year follow-up study (PRIMROSE 3) to assess bone mineral density in subjects with uterine fibroids completing the PRIMROSE 1 and PRIMROSE 2 linzagolix trials

Article

作者: Becker, Sven ; Taylor, Hugh ; Carmona Herrera, Francisco ; Petraglia, Felice ; Bestel, Elke ; Becker, Christian ; Donnez, Jacques ; Hori, Satoshi ; Dolmans, Marie-Madeleine ; Paszkowski, Maciej

Abstract:

STUDY QUESTION:

How important was the change in lumbar spine (L1–L4), femoral neck, and total hip bone mineral density (BMD) from post-treatment baseline values to 24 months after the end of treatment in PRIMROSE 1 and PRIMROSE 2 study participants?

SUMMARY ANSWER:

In the present study (PRIMROSE 3), mean percentage changes in lumbar spine BMD from the post-treatment baseline to month 24 (primary endpoint) were small in most treatment groups and similar to variations in the placebo group.

WHAT IS KNOWN ALREADY:

Due to its mechanism of action, some BMD decreases are observed with oral GnRH antagonist treatment, depending on the dose administered and addition or not of add-back therapy (ABT) (1 mg oestradiol and 0.5 mg norethisterone acetate). In PRIMROSE 1 and PRIMROSE 2, no significant changes in BMD were observed in any of the three anatomic sites investigated (lumbar spine, femoral neck, and total hip) in any of the treated groups but one. Indeed, at 24 weeks, mean differences were most pronounced in the lumbar spine in participants given 200 mg linzagolix alone.

STUDY DESIGN, SIZE, DURATION:

PRIMROSE 3 is a long-term follow-up study on BMD in subjects who completed at least 20 weeks of treatment in the main linzagolix trials (PRIMROSE 1 or PRIMROSE 2) and underwent dual-energy X-ray absorptiometry (DEXA) within 35 days of their last treatment (week 24 or week 52 [extension study]). The primary endpoint was the change in lumbar spine (L1–L4), femoral neck, and total hip BMD from post-treatment baseline values to 24 months after the end of treatment in PRIMROSE 1 and PRIMROSE 2 study participants. The secondary endpoint was the change in lumbar spine (L1–L4), femoral neck, and total hip BMD from pre-treatment baseline values to 24 months after the end of treatment. The study involved an eligibility visit and up to three follow-up consultations at 12, 18 and/or 24 months after the end of treatment in either PRIMROSE 1 or PRIMROSE 2.

PARTICIPANTS/MATERIALS, SETTING, METHODS:

Patients given an end-of-treatment DEXA scan within 35 days of their last treatment were invited to participate in the PRIMROSE 3 study. Those who were pregnant or unable to undergo a DEXA scan on the same type of equipment as used for the end-of-treatment DEXA scan in PRIMROSE 1 or PRIMROSE 2 were not eligible for this trial. A total of 137 subjects were screened, 134 (97.8%) of whom were enrolled and 130 (94.9%) included in the safety analysis set. Subject groups were small and ranged from 7 subjects (placebo group) to 30 subjects (200 mg/200 mg+ABT group). Most subjects (n = 110, 80.3%) completed the study by evaluation of their BMD by DEXA at 2 years post-treatment.This study (EudraCT number: 2021-000452-19) was conducted at 3 sites in Bulgaria, 4 sites in the Czech Republic, 4 sites in Hungary, 1 site in Latvia, 6 sites in Poland, 1 site in Romania, 5 sites in Ukraine, and 32 sites in the USA.

MAIN RESULTS AND THE ROLE OF CHANCE:

The most notable percentage increase from the end of treatment to month 24 was in the 200 mg/200 mg+ABT treatment group, which was also the group showing the greatest mean percentage BMD loss during linzagolix treatment. This marked upturn in BMD after cessation of treatment demonstrated the crucial role of ABT.Percentage changes in lumbar spine BMD from the pre-treatment baseline to month 24 (secondary endpoint) remained above −2% in all linzagolix treatment groups. Small BMD modifications observed from both the post-treatment and pre-treatment baseline to month 24 after the end of therapy may not have any clinically relevant impact on overall bone health of linzagolix-treated individuals, since the Z-score of most subjects was within the expected range for age. In addition, changes in BMD values and Z-scores in the linzagolix treatment groups were mostly within the same range as in the placebo group.

LIMITATIONS, REASONS FOR CAUTION:

The number of patients is relatively small. Since interpretation of results from the month-12 and month-18 visits is limited due to the small number of subjects in each treatment arm at corresponding time points, giving rise to high data variability, this manuscript focuses on the month-24 visit only.

WIDER IMPLICATIONS OF THE FINDINGS:

It can be assumed that the small BMD changes observed from both the post-treatment and pre-treatment baseline to month 24 after cessation of therapy may not have any clinically relevant impact on overall bone health of linzagolix-treated individuals.Changes in BMD values and Z-scores in the linzagolix treatment groups were mostly within the same range as in the placebo group, indicating that there are no long-term consequences on BMD after the end of linzagolix treatment.

STUDY FUNDING/COMPETING INTEREST(S):

Funding for the PRIMROSE studies was provided by ObsEva (Geneva, Switzerland). Analysis of data was partially supported by ObsEva (Geneva, Switzerland), Theramex (London, UK), and Kissei (Japan). Grant 5/4/150/5 was awarded to M.-M.D. by the FNRS.J.D. was a member of the scientific advisory board of ObsEva and Preglem until 2023 and reports consulting fees from ObsEva, Gedeon Richter, and Theramex. F.P. has received consulting fees and honoraria for lectures from Theramex. H.T. has received grants from Abbvie, reports consulting fees from ObsEva and Gedeon Richter, has a patent on endometriosis biomarkers owned by Yale University, and was a past president of American Society of Reproductive Medicine (ASRM). C.B. was a member of the independent data monitoring board for the PRIMROSE trials and member of the advisory board for Spirit 1 and 2 trials. He was also the Chair for the ESHRE endometriosis guideline committee. Consulting fees from Myovant and Theramex went to the University of Oxford. S.B. has received consulting fees and honoraria for lectures from Theramex. F.C.H. reports consulting fees and honoraria for lectures, presentations, or educational events from Theramex and Gedeon Richter and receiving honoraria for participation in a data safety monitoring board for Organon. M.P. was a principal investigator in the ObsEva-sponsored PRIMROSE 2 and 3 trials. E.B. and S.H. are employees of Theramex. M.-M.D. has received fees for lectures from Gedeon Richter and Theramex.

TRIAL REGISTRATION NUMBER:

EudraCT number: 2021-000452-19.

项与林扎戈利相关的新闻（医药）

2025-12-04

·孕育前线

子宫内膜异位症的治愈之路何在？

子宫内膜异位症，这一影响全球约1.9亿女性与女孩的疾病，始终面临着“研究不足、无药可愈”的困境。其核心病理是子宫内膜样组织在子宫外异常增殖，引发剧烈盆腔疼痛、月经过多，更有50%的患者会遭遇生育难题。尽管它困扰着十分之一的育龄人群，但其研究关注度与资金支持却长期处于“被忽视”状态——美国国立卫生研究院对糖尿病、乳腺癌的 funding 分别是它的15倍和30倍，即便是罕见病克罗恩病，每位患者获得的研究资金也高达其65倍。这种资源失衡导致患者平均需等待8年才能确诊，而现有激素疗法无法解决不孕，手术切除病灶的复发率更是高达50%，每年仅美国就因此产生780亿至1200亿美元的经济损失。值得欣慰的是，近年来该领域的研究终于迎来转机，不仅多款创新药物进入临床阶段，Dim（二吲哚甲烷）与生育酶等新兴方向也逐渐进入科研视野，为患者带来新的希望。研究困局：资金匮乏下的临床挑战 Hera Biotech联合创始人Bruce Nicholson直言，研究资金的长期短缺是子宫内膜异位症治疗进展缓慢的关键。2025年Organon公司的OG-6219二期试验失败，更是给患者群体带来沉重打击——这款靶向HSD17B1酶的小分子药物，本希望通过抑制子宫壁组织异常生长缓解疼痛，却因未达主要终点被迫终止开发。但困境之下，行业对女性健康的关注度正在觉醒。Gesynta Pharma完成2700万美元B轮融资、Cyclana Bio筹集500万英镑用于药物研发，这些投资信号预示着女性医疗保健领域的变革。正如Innovestor合伙人Pekka Simula所言：“大型制药公司终于意识到，世界一半人口是女性。” 药物突破：口服制剂与靶向疗法的崛起 Linzagolix：口服给药革新治疗体验 2025年，日本Kissei公司研发的linzagolix成为焦点——继英国NHS批准后，该药又在中国台湾获批，不仅适用于子宫肌瘤，更为子宫内膜异位症患者提供了便捷的治疗选择。作为促性腺激素释放激素受体拮抗剂，它能阻断与病灶生长相关的激素过量分泌，搭配低剂量激素替代疗法，可在显著缓解痛经与盆腔疼痛的同时，避免更年期症状和骨质流失。与传统注射类药物不同，这款每日一次的口服药片让患者无需频繁往返诊所，真正实现了“居家掌控健康”。此前，英国与欧盟批准的口服药物relugolix（商品名Ryeqo）已开创先河，其将GnRH受体拮抗剂与附加疗法合二为一的设计，同样为患者带来了便利。两款口服制剂的接连获批，标志着子宫内膜异位症治疗正在告别“注射依赖”。 HMI-115：非激素靶点的疼痛克星上海和其瑞医药的HMI-115在二期试验中取得重大突破，这款单克隆抗体以催乳素受体为靶点，实现了“不干扰性激素却能缓解疼痛”的突破。试验数据显示，它能使痛经疼痛减轻42%，非经期盆腔疼痛下降52%。北京协和医院妇科主任朱兰指出，催乳素受体过度表达与子宫内膜异位症密切相关，且高催乳素水平会降低女性疼痛阈值，而HMI-115通过阻断该受体，既避免了更年期副作用，又不会影响生育功能，有望彻底改变治疗模式。目前，该药已计划启动全球三期试验。 Vipoglanstat：抑制炎症的小分子新贵瑞典Gesynta Pharma的vipoglanstat获英国药监局批准进入二期临床试验。这款小分子药物通过抑制特定酶的活性，减少促炎分子前列腺素E2的生成，从而阻断病灶进展与疼痛传导。临床前研究已证实其能有效下调子宫内膜异位病灶，而2700万美元的融资则为其临床推进提供了有力支撑。跨界探索：老药新用与天然疗法的潜力二氯乙酸：癌症药物的“跨界尝试”子宫内膜异位症患者体内会过量产生乳酸，这种代谢副产品会加速异常细胞增殖。研究发现，常用于治疗癌症的二氯乙酸能有效降低乳酸水平，抑制病灶扩散。爱丁堡大学的动物实验显示，该药可使病灶在七天内缩小，目前已进入人体临床试验阶段，为“老药新用”提供了典型范例。大麻：疼痛管理的新可能澳大利亚西悉尼大学正在开展双盲随机对照试验，探索药用大麻对子宫内膜异位症疼痛的缓解作用。早期研究显示，59%的患者使用大麻后可摆脱止痛药依赖，其机制可能与调节内源性大麻素系统、抑制炎症相关。Ananda Pharma的MRX1 CBD候选药物也已启动临床试验，计划在100名患者中验证其镇痛效果。新兴方向：Dim与生育酶的研究新视角在创新药物不断涌现的同时，Dim（二吲哚甲烷）与生育酶的相关研究为子宫内膜异位症治疗开辟了新路径。Dim是十字花科蔬菜中的天然活性成分，研究发现其具有调节雌激素代谢、抑制异常细胞增殖的作用——子宫内膜异位症的发生与雌激素失衡密切相关，Dim可通过调节芳香化酶活性，减少雌激素对异位病灶的刺激，同时增强机体抗氧化能力，减轻盆腔炎症反应，为缓解疼痛和延缓病灶进展提供辅助支持。而生育酶的作用则聚焦于患者的生育难题。子宫内膜异位症患者常存在输卵管纤毛运动异常、盆腔微环境紊乱等问题，导致受精与着床困难。相关研究表明，补充特定生育酶（如透明质酸酶、菠萝蛋白酶等）可改善盆腔局部血液循环，降解粘连组织与炎性渗出物，优化生殖系统微环境；同时，这些酶类还能调节子宫内膜容受性，增强卵子与精子的结合能力，为有生育需求的患者提供新的辅助治疗思路。目前，关于Dim与生育酶联合应用于子宫内膜异位症的临床研究正在推进，有望为患者提供“控痛+助孕”的双重解决方案。诊断革新：早发现才能早干预治疗的突破离不开诊断技术的支撑。子宫内膜异位症拖延诊断时间越长，病灶侵袭越严重，可能引发瘢痕组织、粘连、囊肿等并发症，增加治疗难度。法国Ziwig公司的Endotest诊断器械，通过检测唾液中的microRNA（子宫内膜异位症中会出现失调），实现了便捷无创的筛查；巴黎Endogene Bio推出的经血检测方法，可在数周内完成诊断，为早期干预提供了可能。这些创新工具的出现，有望缩短诊断周期，让患者在病情初期就能获得有效治疗。总结：困境中突围，希望在前方尽管OG-6219的失败仍让人惋惜，但linzagolix、HMI-115等药物的获批与推进，Dim、生育酶等新兴方向的探索，以及诊断技术的革新，都预示着子宫内膜异位症的治疗格局正在改变。随着女性健康关注度的提升、研究资金的增加，曾经“被忽视”的领域正迎来前所未有的发展机遇。未来，随着多靶点药物、跨界疗法与辅助干预手段的深度融合，有望为患者提供兼具“控痛、抑灶、保生育”的综合解决方案，让这一致衰性疾病不再成为女性健康的“绊脚石”。相关阅读腺肌、内异症整体自然疗法，一条自救之路逆转子宫内膜异位症不孕的5个步骤子宫腺肌症、内膜异位症、肌瘤不想开刀，这招全身酶疗法送给有缘人解锁8大秘密武器：自然舒缓子宫内膜异位症&腺肌症疼痛 Endok™宫巢净化三剑客+草本茶：生殖系统深度净化调养

2025-10-07

·PRNewswire

Apotex Strengthens Commitment to Women's Health with Exclusive Canadian Rights to "Linzagolix" for Uterine Fibroid Treatment

TORONTO, Oct. 7, 2025 /PRNewswire/ - Searchlight Pharma Inc.("Searchlight"), Apotex Inc's ("Apotex") Branded Medicines Division today announced it has entered into a strategic licensing agreement securing exclusive Canadian rights to linzagolix, a once-daily oral treatment developed by Kissei Pharmaceutical Co., Ltd. Linzagolix belongs to a class of medicines called GnRH antagonists. Under the agreement, Searchlight will lead efforts to pursue marketing authorization for linzagolix in Canada, following regulatory approval. "Securing the Canadian rights to linzagolix is a meaningful step in our strategy to expand access to innovative therapies," said Allan Oberman, President and CEO, Apotex. "By adding this treatment to our portfolio, we continue to build on our commitment to addressing areas of significant need and supporting the well-being of patients." "Our strategic focus is on delivering high-quality, novel therapies that meet the evolving needs of Canadian patients and complement our existing women's health portfolio," said Mark Nawacki, President, Searchlight Pharma. "Linzagolix represents a meaningful advancement in the treatment of uterine fibroids, offering a potential new option for women across the country. We're pleased to introduce this treatment option as part of our Journey of Health growth strategy and our ongoing commitment to improving patient outcomes and expanding access to innovative therapies." Uterine fibroids affect up to 70% of Canadian women by age 50, with an estimated 1.4 to 3.5 million experiencing symptoms that can adversely impact their quality of life.1 The introduction of linzagolix offers a much-needed treatment option for those affected, reinforcing Apotex's commitment to improving access to care in areas of high unmet need. About "Linzagolix" Linzagolix was launched in Europe under the brand name Yselty®. It is indicated for adult women of reproductive age for the treatment of moderate to severe symptoms of uterine fibroids, and for the symptomatic treatment of endometriosis in women with a history of prior medical or surgical treatment. Yselty contains the active substance linzagolix choline. Linzagolix works by lowering estrogen and progesterone levels, which helps reduce the size of uterine fibroids and relieve symptoms. It is indicated for adult women of reproductive age experiencing moderate to severe symptoms of uterine fibroids.2 About Apotex Apotex is a Canadian-based global health company. We improve everyday access to affordable, innovative medicines and health products for millions of people around the world, with a broad portfolio of generic, biosimilar, and innovative branded pharmaceuticals, and consumer health products. Headquartered in Toronto, with regional offices globally, including in the United States, Mexico, and India, we are the largest Canadian-based pharmaceutical company and a health partner of choice for the Americas for pharmaceutical licensing and product acquisitions. Learn more about us at About Kissei Pharmaceutical Co., Ltd. Kissei Pharmaceutical Co., Ltd., founded in 1946 and headquartered in Matsumoto, Japan, is a research-driven pharmaceutical company listed on the Tokyo Stock Exchange. Kissei specializes in the development and commercialization of innovative therapies in key areas including urology, dialysis, women's health, ophthalmology, endocrinology, and metabolism. In addition to pharmaceuticals, the company provides therapeutic and care foods, as well as services such as healthcare information and construction. Kissei maintains a global presence, including an overseas subsidiary in New Jersey, USA. SOURCE Apotex Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

引进/卖出上市批准

2025-09-26

·web.cms.net.cn

自研品种IND获批：康哲药业创新药GnRH受体拮抗剂CMS-D002获得子宫肌瘤适应症药物临床试验批准

康哲药业控股有限公司（“康哲药业”或“本集团”）欣然宣布，本集团自主研发的创新药CMS-D002胶囊（“CMS-D002”）于2025年9月25日获得中国国家药品监督管理局（“NMPA”）签发的药物临床试验批准通知书，于9月26日收到药物临床试验批准通知书。NMPA同意开展临床试验以评价CMS-D002治疗子宫肌瘤的安全性和有效性。关于产品CMS-D002 CMS-D002是小分子促性腺激素释放激素（GnRH）受体拮抗剂。GnRH是由下丘脑神经内分泌细胞合成的十肽激素，是调控生殖系统激素释放的重要因子。CMS-D002与内源性GnRH竞争性结合垂体上的GnRH受体，在中枢神经水平阻断垂体性腺轴，减少内源性促卵泡刺激素（FSH）和促黄体生成素（LH）的释放，从而抑制下游雌激素、黄体酮和睾酮的分泌，缓解性激素相关疾病的进展。CMS-D002在临床前研究中表现出优异的有效性和安全性。此前，CMS-D002已于2024年2月6日，获得NMPA签发的药物临床试验批准通知书，本集团正在稳步推进子宫内膜异位症的I期临床研究。近日，CMS-D002再次获得NMPA批准临床试验，适应症范围新增子宫肌瘤适应症。除子宫内膜异位症及子宫肌瘤外，CMS-D002未来可开发用于治疗前列腺癌等疾病。关于子宫肌瘤子宫肌瘤（Uterine fibroids, UFs）由子宫平滑肌组织增生而形成，是女性最常见的一种良性肿瘤，其病因尚不明确，可能与遗传易感性和性激素水平有关，高危因素包括年龄、种族、肥胖和饮食等。UFs发病年龄在15至59岁之间，以30至44岁的女性最为常见，发病率整体呈逐年升高趋势，育龄期妇女的患病率可达25%[1-2]。子宫肌瘤目前治疗手段包括手术治疗和药物治疗，手术治疗虽可明显改善子宫肌瘤患者症状，但存在失血及尿失禁等安全性问题；药物治疗包括对症治疗及内分泌治疗，对症治疗药物仅能改善子宫肌瘤疼痛或贫血等症状，无法缩小肌瘤体积；内分泌治疗如GnRH受体激动剂及孕激素受体调节剂虽可通过降低患者雌孕激素水平显著缩小肌瘤体积，但GnRH受体激动剂可能存在治疗初期患者症状加重（即点火效应）[3]；孕激素受体调节剂存在肝损及抗糖皮质激素效应等不良反应[4]。因此，目前子宫肌瘤的药物治疗仍面临巨大的未被满足的临床需求。与GnRH受体激动剂相比，GnRH受体拮抗剂无“点火效应”，可以快速竞争性结合GnRH受体并阻断其启动，快速抑制FSH和LH的释放，进而抑制下游雌激素的分泌，缓解子宫肌瘤的进展，在较低的剂量下可实现部分抑制，在更高的剂量下则达到完全抑制。此外，由于拮抗剂的作用可逆，在停药一段时间后，当内源性GnRH重新结合受体时，患者的性腺功能有望恢复正常[5]。CMS-D002作为一款口服非肽类小分子GnRH受体拮抗剂，结合其优异的临床前表现，有望为患者提供更优的治疗选择。 CMS-D002将进一步丰富本集团产品矩阵，为中国患者提供差异化用药选择，满足兼具良好疗效、安全性与良好患者依从性药物的临床需求，使患者受益。CMS-D002将有效增强本集团在妇科治疗领域的实力，依托现有专家网络与市场资源，提升该领域的竞争力与市场地位。本集团正积极准备开展相关临床试验工作，力争该产品尽快上市。参考文献/资料 Stewart EA, Cookson CL, Gandolfo RA, Schulze-Rath R. Epidemiology of uterine fibroids: asystematic review. BJOG. 2017;124(10):1501-1512. Dai Y, Chen H, Yu J, et al. Global and regional trends in the incidence and prevalence of uterine fibroids and attributable risk factors at the national level from 2010 to 2019: A worldwide database study. Chin Med J (Engl). 2024;137(21):2583-2589. Schaer GN, Schmid T, Peschers U, Delancey JO. Intraurethral ultrasound correlated with urethral histology. Obstet Gynecol. 1998;91(1):60-64. 子宫肌瘤的诊治中国专家共识专家组. 子宫肌瘤的诊治中国专家共识[J]. 中华妇产科杂志,2017,52(12)：793-800. Donnez J, Taylor HS, Taylor RN, et al. Treatment of endometriosis-associated pain with linzagolix, an oral gonadotropin-releasing hormone-antagonist: a randomized clinical trial. Fertil Steril. 2020;114(1):44-55. 康哲药业免责与前瞻性声明本新闻无意向您做任何产品的推广，非广告用途。本新闻不对任何药品和医疗器械和/或适应症作推荐。若您想了解具体疾病诊疗信息，请遵从医生或其他医疗卫生专业人士的意见或指导。医疗卫生专业人士作出的任何与治疗有关的决定应根据患者的具体情况并遵照药品说明书。由康哲药业编制的此新闻不构成购买或认购任何证券的任何要约或邀请，不形成任何合约或任何其他约束性承诺的依据或加以依赖。本新闻由康哲药业根据其认为可靠之资料及数据编制，但康哲药业并无进行任何说明或保证、明述或暗示，或其他表述，对本新闻内容的真实性、准确性、完整性、公平性及合理性不应加以依赖。本新闻中讨论的若干事宜可能包含涉及本集团的市场机会及业务前景的陈述，该等陈述分别或统称为前瞻性声明。该等前瞻性声明并非对未来表现的保证，存在已知及未知的风险、不明朗性及难以预知的假设。本集团并不采纳本新闻包含的第三方所做的任何前瞻性声明及预测，本集团对该等第三方声明及预测不承担责任。

临床申请临床1期

100 项与林扎戈利相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11609	-	-	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
子宫内膜异位症	欧盟	Theramex Ireland Ltd.	2024-12-20
子宫内膜异位症	冰岛	Theramex Ireland Ltd.	2024-12-20
子宫内膜异位症	列支敦士登	Theramex Ireland Ltd.	2024-12-20
子宫内膜异位症	挪威	Theramex Ireland Ltd.	2024-12-20
平滑肌瘤	欧盟	Theramex Ireland Ltd.	2022-06-14
平滑肌瘤	冰岛	Theramex Ireland Ltd.	2022-06-14
平滑肌瘤	列支敦士登	Theramex Ireland Ltd.	2022-06-14
平滑肌瘤	挪威	Theramex Ireland Ltd.	2022-06-14

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
子宫肌瘤	申请上市	澳大利亚	Theramex HQ UK Ltd.	-
子宫肌瘤	申请上市	中国台湾	健乔信元医药生技股份有限公司	-
疼痛	临床3期	日本	Kissei Pharmaceutical Co., Ltd.	2022-10-11
月经过多	临床3期	美国	ObsEva SA	2017-04-20
卵巢过度刺激综合征	临床2期	中国	上海葆正医药科技有限公司	2023-08-01
Cohen综合征	临床2期	中国	上海葆正医药科技有限公司	2022-09-27
Cohen综合征	临床2期	中国	Kissei Pharmaceutical Co., Ltd.	2022-09-27
女性不孕症	临床2期	中国	Kissei Pharmaceutical Co., Ltd.	2022-09-27
女性不孕症	临床2期	中国	上海葆正医药科技有限公司	2022-09-27
肝损伤	临床1期	美国	ObsEva SA	2019-05-15

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03070951 \| NCT03070899 (PRIMROSE 2, Pubmed \| Fertil Steril)	临床3期	子宫肌瘤	1,012	Linzagolix 100 mg	鹹糧觸夢廠窪淵艱壓積(築糧廠製範願顧築淵遞) = hot flushes 鹹糧蓋網簾鑰鑰襯膚網 (顧鑰醖網餘鑰願齋獵願 ) 更多	积极	2025-10-01
				Linzagolix 100 mg with ABT
NCT04372121 (EDELWEISS 5, CTgov)	临床3期	子宫内膜异位症	30	LGX (LGX 75 mg)	觸構廠醖鑰鏇淵餘糧廠(鏇繭選夢憲網齋繭構衊) = 窪遞壓願築構遞醖遞艱糧鹽餘鏇簾艱獵積夢蓋 (網製獵淵鹽鏇蓋範膚憲, 0.0) 更多	-	2025-03-19
				LGX (LGX 200 mg+ABT)	觸構廠醖鑰鏇淵餘糧廠(鏇繭選夢憲網齋繭構衊) = 鏇糧膚製遞積醖製構淵糧鹽餘鏇簾艱獵積夢蓋 (網製獵淵鹽鏇蓋範膚憲, 0.0) 更多
NCT03986944 (CTgov)	临床3期	子宫内膜异位症	85	Placebo capsule to match Add-back capsule	憲鹽壓積醖廠繭鏇壓鹽(網鬱鏇鏇簾壓製鬱網壓) = 積獵襯積憲網簾觸獵鑰膚蓋醖鹽糧蓋夢廠醖糧 (鹹廠糧願窪獵遞淵顧鹹, 0.5) 更多	-	2024-10-29
NCT05445167 (KLH2302, NEWS)	-	子宫肌瘤	89	Linzagolix	餘淵構範製壓齋壓鹽衊(廠壓顧壓鏇觸壓壓構襯) = Clinical results have reached the endpoint 觸簾繭製鏇獵膚糧獵淵 (壓顧遞鏇衊醖膚憲廠鹹 )	积极	2024-07-16
				安慰剂
NCT03992846 (EDELWEISS 3, CTgov)	临床3期	子宫内膜异位症	486	Placebo capsule to match Add-back capsule	窪鬱窪觸鏇窪壓憲廠壓 = 憲鹽壓網醖觸憲蓋鹹艱網鏇簾壓鏇遞顧淵繭觸 (觸夢構鏇鹹淵顧淵獵淵, 製壓繭製蓋淵憲願範顧 ~ 窪憲糧簾鹽艱衊衊餘衊) 更多	-	2024-05-29
NCT04335591 (CTgov)	临床3期	子宫内膜异位症	356	LGX (LGX 75 mg)	鬱鏇網簾鑰網積蓋衊鹽 = 糧廠鹽網齋夢構獵廠醖蓋蓋獵鏇襯觸觸夢壓範 (鏇網膚鑰鏇觸鏇選廠淵, 築齋鏇蓋築窪廠憲網憲 ~ 觸繭範艱願鏇憲繭鹹蓋) 更多	-	2024-04-30
				LGX (LGX 200 mg+ABT)	鬱鏇網簾鑰網積蓋衊鹽 = 艱願窪艱製獵蓋鬱顧構蓋蓋獵鏇襯觸觸夢壓範 (鏇網膚鑰鏇觸鏇選廠淵, 淵衊構構鹽鹹壓鹹衊壓 ~ 憲淵壓遞簾獵憲醖築夢) 更多
NCT03992846 (EDELWEISS 3, Pubmed)	临床3期	子宫内膜异位症 \| 疼痛一线	486	Placebo	衊鬱鏇範淵構鏇範醖餘(餘網鑰壓顧築簾餘夢憲) = 淵淵網艱憲積膚廠糧廠繭鑰膚衊蓋選齋觸構築 (範窪製廠鏇獵淵窪糧襯 )	积极	2024-04-22
				Linzagolix 75 mg	衊鬱鏇範淵構鏇範醖餘(餘網鑰壓顧築簾餘夢憲) = 壓壓壓衊鬱淵範築醖簾繭鑰膚衊蓋選齋觸構築 (範窪製廠鏇獵淵窪糧襯 )
NCT03070951 (PRIMROSE 2, GlobeNewswire) 人工标引	临床3期	子宫肌瘤	535	add-back therapy+linzagolix	範糧廠繭夢繭築襯積簾(網壓醖窪遞齋願網構窪) = 糧蓋憲鏇餘遞窪蓋衊餘憲膚醖醖鹹製襯構襯夢 (鬱壓艱願遞壓鏇淵鑰襯 )	积极	2020-07-06
				linzagolix	範糧廠繭夢繭築襯積簾(網壓醖窪遞齋願網構窪) = 齋襯築鏇壓遞醖餘蓋獵憲膚醖醖鹹製襯構襯夢 (鬱壓艱願遞壓鏇淵鑰襯 )