The goal of this study is to assess response to kisspeptin as well as the baseline patterns of luteinizing hormone (LH) secretion in individuals with polycystic ovarian syndrome (PCOS).

开始日期2023-10-06

申办/合作机构

The Schwartz Center for Compassionate Healthcare

NCT05896293 / Recruiting临床2期IIT

Kisspeptin Administration Subcutaneously to Patients With Reproductive Disorders

The goal of this study is to see whether kisspeptin, a naturally occurring hormone, can stimulate the release of other reproductive hormones in men and women with idiopathic hypogonadotropic hypogonadism (IHH). The investigators are also examining whether kisspeptin can help women release eggs from their ovaries. Kisspeptin will be administered SC for two weeks in a pulsatile fashion. Ultrasound monitoring of ovarian follicular growth (for women) and frequent blood sampling (every 10 minutes for up to 70 minutes) will be performed to assess the physiologic response to kisspeptin over time.
Funding Source: FDA OOPD

开始日期2023-02-03

申办/合作机构

The Schwartz Center for Compassionate Healthcare

NCT05633966 / Recruiting临床1期IIT

Kisspeptin Administration Subcutaneously to Patients With Reproductive Disorders

The goal of this study is to see whether kisspeptin, a naturally occurring hormone, can stimulate the release of other reproductive hormones in women with hypothalamic amenorrhea (HA). The investigators are also examining whether kisspeptin can help women release eggs from their ovaries. Kisspeptin will be administered subcutaneously (SC) for two weeks in a pulsatile fashion. Ultrasound monitoring of ovarian follicular growth and frequent blood sampling (every 10 minutes for up to two hours) will be performed to assess the physiologic response to kisspeptin over time.

开始日期2022-12-16

申办/合作机构

The Schwartz Center for Compassionate Healthcare

100 项与 Kisspeptin 112-121 相关的临床结果

登录后查看更多信息

100 项与 Kisspeptin 112-121 相关的转化医学

登录后查看更多信息

100 项与 Kisspeptin 112-121 相关的专利（医药）

登录后查看更多信息

项与 Kisspeptin 112-121 相关的文献（医药）

2022-07-14·The Journal of Clinical Endocrinology & Metabolism2区 · 医学

Kisspeptin Overcomes GnRH Neuronal Suppression Secondary to Hyperprolactinemia in Humans

2区 · 医学

Article

作者: Lippincott, Margaret F ; Nachtigall, Lisa B ; Balasubramanian, Ravikumar ; Seminara, Stephanie B ; Kayton Bryant, Nora ; Chen, Margaret E ; Hoskova, Katerina

AbstractContextHyperprolactinemia suppresses gonadotropin-releasing hormone (GnRH)-induced luteinizing hormone (LH) pulses. The hypothalamic neuropeptide kisspeptin potently stimulates the secretion of GnRH. The effects of exogenous kisspeptin administration on GnRH pulse generation in the setting of hyperprolactinemia have not previously been explored.ObjectiveThis work aimed to examine the effects of kisspeptin on GnRH secretion, as reflected by LH secretion, in women with hyperprolactinemia.MethodsWomen with hyperprolactinemia (n = 11) participated in two 12-hour visits. Before study visits, participants underwent washout of dopamine agonist and/or combined oral contraceptive. Frequent blood sampling was performed (1 sample was collected every 10 minutes). Visit 1 involved no intervention, to examine baseline LH pulsatility. During visit 2, kisspeptin 112–121 (0.24 nmol/kg) was administered every 1 hour, for 10 hours. At hour 11, one intravenous bolus of GnRH (75 ng/kg) was administered.ResultsRepetitive intravenous bolus kisspeptin administration increased the total number of LH pulses in the setting of hyperprolactinemia. The interpulse interval declined during the same time frames. LH pulse amplitude did not change, but the mean LH rose. In 6 participants with progesterone levels suggestive of an anovulatory state, mean LH and estradiol levels increased significantly at visit 2. In the entire cohort, follicle-stimulating hormone and prolactin levels did not change significantly across the 2 visits. A total of 73% of subjects exhibited an LH pulse within 30 minutes of first kisspeptin dose.ConclusionKisspeptin is capable of stimulating hypothalamic GnRH-induced LH pulses in the setting of hyperprolactinemia.

2013-05-01·Journal of Chromatography B3区 · 医学

LC–MS/MS quantification of a neuropeptide fragment kisspeptin-10 (NSC 741805) and characterization of its decomposition product and pharmacokinetics in rats

3区 · 医学

Article

作者: Joseph M. Covey ; Ping Chen ; Zhongfa Liu ; Stephanie B. Seminara ; Yee-Ming Chan ; Kenneth K. Chan ; William Jones ; Nicola F. Smith ; Jeffrey Wang ; Chen Ren

The kisspeptins are critical regulators of mammalian reproduction. Kisspeptin-10 ((45)YNWNSFGLRF-NH2(54), kisspeptin-112-121 or metastin 45-54, NSC 741805), an active fragment of kisspeptin, has been shown to be a potent stimulator of gonadotropin-releasing hormone and secretion of luteinizing hormone in both rodents and primates. This shorter peptide fragment may have clinical utility potential and it is important to characterize its pharmacokinetic property. Recently, the pharmacokinetics of both kisspeptin-54 and kisspeptin-10 were characterized in humans using a radioimmunoassay (RIA), which measures only the immunoreactive kisspeptin (kisspeptin-IR). In this study, a highly sensitive and specific LC-MS/MS assay was developed to quantify kisspeptin-10 levels in rat plasma. The lower limit of quantitation (LLOQ) was 0.5 ng/mL, the within-day and between-day coefficient of variations (CVs) ranged from 5.2 to 15.4% and 1.3 to 14.2%, and the accuracy values ranged from 98 to 114% and 99 to 105%, respectively. With this method, stability studies demonstrated that kisspeptin-10 degraded rapidly with decomposition half-lives of 6.8 min, 2.9 min and 1.7 min at 4 °C, 25 °C, and 37 °C, respectively. The principal decomposition product was characterized as the N-terminal tyrosine deleted kisspeptin-10 (46)NWDSFGLRF-NH2(54). Pharmacokinetic study in rats showed that low ng/mL kisspeptin-10 was detected in the first few minutes, and eliminated rapidly and became undetectable 30 min after intravenous (i.v.) bolus administration of 1.0 mg/kg kisspeptin-10.

2012-08-01·The Journal of Clinical Endocrinology & Metabolism2区 · 医学

Kisspeptin Administration to Women: A Window into Endogenous Kisspeptin Secretion and GnRH Responsiveness across the Menstrual Cycle

2区 · 医学

Article

作者: Valerie F. Sidhoum ; Yee-Ming Chan ; James P. Butler ; Stephanie B. Seminara ; Nancy E. Pinnell

CONTEXTKisspeptin is the most powerful known stimulus of GnRH-induced LH secretion across mammalian species. However, the effects of kisspeptin are just being explored, and the dynamics of kisspeptin responsiveness across the menstrual cycle are incompletely understood.OBJECTIVEThe objective of the study was to characterize the effects of kisspeptin on GnRH secretion in healthy women in different phases of the menstrual cycle.PARTICIPANTS AND INTERVENTIONTen women in the early follicular phase, three women in the late follicular (preovulatory) phase, and 14 women in the midluteal phase received a bolus of kisspeptin 112-121 0.24 nmol/kg iv. An additional four women in the early to midfollicular phase received kisspeptin 112-121 0.72 nmol/kg iv.RESULTSThe response to kisspeptin varied depending on the phase of the menstrual cycle. LH pulses were observed immediately after kisspeptin administration in all luteal and preovulatory women. However, only half the women in the early follicular phase had unambiguous kisspeptin responses. Increasing the kisspeptin dose did not increase the LH response in early to midfollicular phase women. Kisspeptin did not appear to reset the GnRH pulse generator in women as it does in men.CONCLUSIONSDifferences in responses to exogenous kisspeptin across the menstrual cycle suggest that kisspeptin tone is higher in the early follicular phase compared with other cycle phases. The mechanisms that determine the timing of GnRH pulse generation in men and women appear to be distinct.

项与 Kisspeptin 112-121 相关的新闻（医药）

2023-02-13

·Drug Genius

Low Libido Breakthrough: New Hormonal Injection Found to Boost Sex Drive in Men and Women

Scientists announce the new hormone kisspeptin as a potential game changer for men and women distressed by their low sex drive. Both studies on men and women, which were published in the journal JAMA Network Open, found that kisspeptin was effective in treating men and women who experience Hypoactive Sexual Desire Disorder (HSDD)—one of the most common forms of low sexual desire. It’s estimated that 8 percent of men and 10 percent of women worldwide are commonly affected by Hypoactive Sexual Desire Disorder (HSDD). Despite the prevalence of the disease, treatments in men are lacking while options for women are limited, accompany side effects, or are harmful to try. Hence the lead study author, Dr. Alexander Comninos, and his colleagues at Imperial College London sought a safe and more effective alternative treatment that can help men and women seeking treatment. Findings from this study provide the first-ever clinical evidence that kisspeptin is safe and beneficial in men and women with low sexual desire. The team explains that kisspeptin is a naturally occurring hormone that works by stimulating other reproductive hormones in the body. For men, not only was the kisspeptin treatment found to have a positive impact on the brain, but it also enhanced erection. According to the authors, no particular side effects were associated with the drug overall, as it was well tolerated by both genders. For the study on women , the researchers involved a total of 32 pre-menopausal heterosexual women with an average age of 29 years. The women completed two visits to receive kisspeptin or a placebo. About half were to receive kisspeptin, and the other half were to receive a placebo on their first visit. They were also given questionnaires to fill out concerning their mood and behavior before and after taking kisspeptin and a placebo. Participants were made to watch short and long erotic videos as well as attractive male faces while the team used functional MRI to investigate their brain activity. Meanwhile, the control group just watched non-erotic workout videos. In the end, the team found that women who were more distressed by their overall sexual function and low sexual desire showed higher kisspeptin-enhanced brain activity in the hippocampus—a key structure involved in women’s sexual desire—upon watching short sexual content. In addition to that, kisspeptin administration was also found to activate the posterior cingulate cortex (another key behavioral area appearing after seeing highly attractive male faces), which was linked to reduced sexual aversion in the participants. Participants also revealed that they felt “sexy” after taking kisspeptin compared with the placebo. For the study on men , the researchers enrolled 32 right-handed heterosexual men between the ages of 21 and 52 who were troubled by their low sex drive. The team collected their blood samples before and after taking kisspeptin. Just like the study on women, they were made to watch both short and long erotic videos. Only this time, they recorded the degree of penile rigidity. The results showed that kisspeptin significantly increased brain activity in key erotic-processing brain structures as well as promoted erection by up to 56 percent more than the placebo upon watching the erotic video. Kisspeptin was also found to increase sexual desire and arousal among those with low libido similar to the women’s study. And on top of that, the men reported “happiness about sex” compared with the placebo. Conclusion Given the benefits kisspeptin has on treating men and women with distressing sexual problems, the team, however, sees the need to conduct further trials in a larger population and establish it as a more realistic treatment. Altogether, they conclude kisspeptin may offer the first safe and much-needed intervention for Hypoactive Sexual Desire Disorder (HSDD) in both genders. A patient’s story about the treatment A 44-year-old man whose name was hidden opted to be included in the trial due to previous problems with his sexual desire and performance. According to him: “The issue had always been detrimental to sustaining relationships. I would often make excuses as to why my sexual appetite was low.” “For example, I would blame stress at work or tiredness as a reason instead of being honest. I had tried other performance-supporting medication like Viagra .” He explained that it was pretty much ineffective as the case was his low desire. He also felt embarrassed and found it difficult to share with his past partners, fearing they may confuse it with a lack of attraction to them. The trial participant said: “I was keen to learn whether there was a solution to my problem and learn more about my condition.” “I received the kisspeptin infusion in June 2021 and I noticed a difference in terms of my sexual desire,” he continues. “The week I had the kisspeptin infusion we conceived our son, who was born in March 2022. I had the best possible outcome as a result of the trial.” “I also learnt a lot more about myself and my condition. I am really pleased to have contributed to this trial, which has been life-changing for me.”

临床结果

2023-02-08

·药研

2023年全球最值得关注的10大III期临床研究

Scrip Pharma Intelligence日前展望了2023年10项最值得关注的临床III 期试验。[1]在临床方面看起来特别强劲的是阿斯利康，诺和诺德和诺华，它们今年的峰值潜力读数都在 50 亿美元至 60 亿美元之间。罗氏、辉瑞、礼来、葛兰素史克、赛诺菲、默克和拜耳旗下的III期临床研究也上榜。以下的排名按照预计的临床完成的时间顺序排列。 01 Tusamitamab Ravtansine （CARMEN-LC03研究） ·开发商：赛诺菲/ ImmunoGen, Inc联合开发 ·药物：tusamitamab ravtansine ·药物类型：ADC（抗体-药物偶联物） ·适应症：NSCLC（非小细胞肺癌） ·阶段: III期·时间：2023年上半年 ·背景：赛诺菲的Tusamitamab Ravtansine是处于后期开发阶段的众多抗体-药物偶联物 (ADC) 之一，是靶向 CEACAM5 的最先进药物。 ·机制：CEACAM5（Carcinoembryonic antigen-related cell adhesion molecule 5，癌胚抗原相关细胞粘附分子5，亦称CD66e），是 CEA （Carcinoembryonic antigen，癌胚抗原）蛋白家族的成员，在细胞迁移、细胞侵袭和细胞粘附中起着关键作用，并被多种癌细胞类型过度表达。在给予抗体-药物偶联物tusamitamab ravtansine 后，其抗体部分将靶向肿瘤细胞上的 CEACAM5。在抗体/抗原结合以及内化后，ADC偶联物将释放细胞毒剂，导致肿瘤细胞死亡（图1）。图1. ravtansine化学结构以及细胞毒素释放过程 ·临床研究状态：来自 CEACAM5 阳性二线和三线非小细胞肺癌 (NSCLC) 患者的 III 期 CARMEN-LC03 研究的顶线数据将于上半年到期。它有两个主要终点：与多西他赛docetaxel相比，无进展生存期 (PFS) 提高长达 15 个月，总生存期 (OS) 与多西他赛相比提高长达两年。 02 Datopotamab Deruxtecan（TROPION-LUNG01研究） ·开发商：AstraZeneca/Daiichi Sankyo联合开发 ·药物：Datopotamab Deruxtecan ·药物类型：ADC（抗体-药物偶联物） ·适应症：NSCLC（非小细胞肺癌） ·阶段: III期·时间：2023年上半年 ·背景：Datopotamab deruxtecan 正在临床试验TROPION-LUNG01中进行研究（Datopotamab与多西紫杉醇在既往治疗过的晚期或转移性非小细胞肺癌中无可操作基因组改变的研究。 ·机制：Datopotamab Deruxtecan以TROP2（trophoblast cell-surface antigen 2，滋养层细胞表面抗原 2）蛋白为靶点。TROP2是一种跨膜糖蛋白，在多种类型的实体瘤中广泛表达，包括非小细胞肺癌NSCLC。[2] ·临床研究状态：目前尚没有 TROP2 定向疗法被批准用于治疗 NSCLC 患者。[3]但Gilead已在市场上推出首个靶向TROP2 的ADC Trodelvy (sacituzumab govitecan)，用于二线或之后的局部晚期或转移性三阴性乳腺癌 (TNBC)，以及作为局部晚期或转移性尿路上皮癌的后期治疗。TROPION-LUNG01将评估Datopotamab vs多西紫杉醇，对于先前接受过治疗的晚期或转移性非小细胞肺癌 (NSCLC) 患者中的疗效、安全性和药代动力学表现。 03 Belantamab mafodotin（DREAMM-8和DREAMM-7研究） ·开发商：葛兰素史克 ·药物：Belantamab mafodotin（商品名：Blenrep） ·药物类型：ADC ·适应症：二线多发性骨髓瘤·时间：2023年上半年 ·背景：葛兰素史克的靶向 BCMA （B细胞成熟抗原，B-cell maturation antigen）的重磅药物Blenrep® (belantamab mafodotin) 的去年遭受打击，因为该药物未能在 III 期 DREAMM-3 验证性研究中显示出显著的 PFS（无进展生存期）益处，去年年底应FDA的要求从美国市场撤出该产品。 Blenrep® 之前于 2020 年 8 月在美国被有条件地批准用于复发/难治性多发性骨髓瘤。该药物是第一个获得批准用于治疗骨髓瘤的 BCMA 靶向药物，但对眼睛毒性的担忧已经导致其上市表现不佳，它在 2022 年第三季度的收入仅达到 4280 万美元。 ·临床研究状态：该产品的未来主要取决于 DREAMM-7 和 DREAMM-8 的数据，这两个数据都将在2023年上半年发布。DREAMM-7 正在评估 belantamab mafodotin 联合硼替佐米和地塞米松vs daratumumab 联合硼替佐米和地塞米松的安全性和有效性。DREAMM-8 正在评估 belantamab mafodotin 联合泊马度胺和地塞米松vs泊马度胺、硼替佐米和地塞米松联合治疗复发/难治性多发性骨髓瘤患者的疗效和安全性。 04 Ribociclib（NATALEE研究） ·开发商：诺华 ·药物：Ribociclib （商品名Kisqali®） ·药物类型：小分子 ·适应症：乳腺癌 ·时间： 2023年下半年 ·背景：Kisqali 经 FDA 2017年批准，与芳香酶抑制剂或氟维司群联合，作为初始内分泌治疗，用于治疗 HR+/HER2- 晚期或转移性乳腺癌。诺华希望通过NATALEE 研究，将 Kisqali 用于早期患者。诺华公司正在测试它作为 HR+/HER2- 早期乳腺癌的辅助疗法，可能为该产品开辟新的患者群体。 ·机制：Ribociclib 是一种选择性细胞周期蛋白依赖性激酶抑制剂 (cyclin-dependent kinase inhibitor)，是一类通过抑制细胞周期蛋白依赖性激酶 4 和 6 (CDK4/6, cyclin-dependent kinase 4 and 6) ，来减缓癌症进展的药物。这些激酶在过度激活时，会使癌细胞生长和分裂过快。靶向 CDK4/6 可能确保癌细胞不会继续不受控制地复制。Ribociclib 于 2017 年 3 月被美国 FDA 批准。目前是唯一一种在一线 HR+/HER2- 晚期乳腺癌中具有总体生存获益的 CDK4/6 抑制剂。 ·临床研究状态：诺华的目标是通过其 CDK4/6 抑制剂 Kisqali (ribociclib) 获得同类药物最佳地位，它瞄准了辉瑞市场领先的 Ibrance (palbociclib)，并寻求在早期乳腺癌中赶上礼来 (Lilly) 的 Verzenio (abemaciclib)。诺华正在测试Ribociclib作为 HR+/HER2- 早期乳腺癌的辅助疗法，该研究（NATALEE）已经通过了对 70% 事件的第一次中期分析，预计将在上半年进行第二次中期分析（对 85%事件）。最终分析将在2023年下半年给出。分析师认为该药物的总销售额预测为 100 亿美元。 05 Semaglutide （SELECT CVOT研究） ·开发商：诺和诺德 ·药物：Semaglutide（商品名Wegovy®） ·药物类型：多肽·适应症：肥胖症·时间： 2023年中 ·机制：Semaglutide属于胰高血糖素样肽-1类似物（GLP-1），是GLP-1受体的激动剂。GLP-1可以诱发分泌胰岛素，从而降低血糖，是II型糖尿病的治疗剂。Semaglutide的另一个功效是针对肥胖症患者，它对于GLP-1受体的激动剂作用，可以降低食欲，增加饱腹感，从而实现体重管理的目标。 ·背景：礼来的 GLP1/GIP 双重受体激动剂 Mounjaro®（tirzepatide）在肥胖症（临床III期中）追赶诺和诺德的 GLP1多肽 Wegovy®（semaglutide 注射液 2.4mg）。在此前的头对头研究中，Mounjaro® 已经在II糖尿病治疗中取得了对 semaglutide (Ozempic®) 的胜利，礼来公司也提出要在肥胖症中进行类似的比较试验。诺和诺德Wegovy的肥胖症研究SELECT CVOT正在进行中，预计于今年年中取得结果。诺和诺德在 Wegovy 的 17500 名患者参加的 SELECT 研究中，进行心血管方面的分析，加上口服semaglutide的 OASIS 1 研究，这些结果对于巩固其 semaglutide 特许经营权意义重大。分析师非常相信 SELECT-CVOT 最终将在年中进行的最终分析中取得成功。他们将 Wegovy 的最高销售额定在 114 亿美元左右。 06 Donanemab（RAILBLAZER-ALZ2研究） ·开发商：礼来 ·药物：Donanemab ·药物类型：单克隆抗体 ·适应症：阿尔茨海默病 ·阶段：III期·时间： 2023年中 ·机制：Donanemab (LY3002813) 是一种人源化 IgG1 单克隆抗体，靶向特定类型淀粉样蛋白 β (Aβ) ，即焦谷氨酸 Aβ （pyroglutamate Aβ）的N 末端的表位，这种靶标为仅存在于与阿尔茨海默病相关的脑淀粉样蛋白斑块中。[4]它的作用是诱导小胶质细胞介导的现有 Aβ 斑块的清除，目的是减缓与阿尔茨海默病相关的认知功能的进行性下降。 ·背景：礼来公司2022 年底向 FDA 发起了Donanemab生物制剂许可申请 (BLA)，但由于在 II 期 TRAILBLAZER-ALZ 临床试验中，至少12 个月的药物暴露数据的患者数量有限，FDA刚刚发布了一份完整的回复函。 ·临床研究状态：2021 年 3 月，礼来公司宣布了一项名为 TRAILBLAZER-ALZ 2 的扩展III期试验，该试验将寻求在扩大的患者群体中确认之前试验的结果，以解决原始试验的一些缺陷。[5]礼来目前正在准备针对早期疾病的III期RAILBLAZER-ALZ2研究，以应对这一问题，并计划2023年中公布顶线结果。分析师指出，这些数据对礼来的未来很重要。 07 mRNA 流感疫苗PF-07252220 ·开发商：辉瑞 ·药物：PF-07252220·药物类型：疫苗 ·适应症：流感 ·阶段：III期 ·时间：2023年下半年 ·背景与临床研究状态：辉瑞公司于去年 9 月开始了基于 mRNA 的流感疫苗 PF-07252220 的第一个 III 期功效研究，美国 25000 名患者的试验结果预计将于2023年中公布。四价修饰 RNA (modRNA) 候选流感疫苗是 2018 年与 BioNTech SE 达成的全球合作和许可协议的一部分。辉瑞估计其 mRNA 疫苗产品组合的年收入潜力在 100 亿美元至 150 亿美元之间。他们表示，针对 COVID-19 的 mRNA 疫苗已显示出与传统重组蛋白疫苗相当或更好的功效，而且 PF-07252220 的初始数据显示出令人乐观的结果。 08 SRP-9001（EMBARK研究） ·开发商：罗氏/Sarepta ·药物：SRP-9001 (delandistrogene moxeparvovec) ·药物类型：基因疗法·适应症：杜氏肌营养不良症 ·阶段：III期 ·时间：2023年下半年 ·背景：SRP-9001正在开发用于治疗罕见病杜氏肌营养不良症。它通过肌肉内和静脉内途径给药。该疗法通过重组腺相关病毒载体血清型 74 (AAV74)，携带微抗肌萎缩蛋白基因实现治疗目的。 ·临床研究状态：来自罗氏和 Sarepta Therapeutics, Inc. 的 Duchenne 肌营养不良基因疗法 SRP-9001 (delandistrogene moxeparvovec) 的 EMBARK III 期研究数据将于 10 月到期，但FDA 已决定通过优先审查尽早审查药物数据，并将 PDUFA 日期定为 5 月 29 日。该研究纳入了 125 名年龄在 4-7 岁之间的患者，该年龄组的肌肉已经开始退化，但仍然能够行走。其主要终点是北极星动态评估总分相对于基线的变化，以衡量在第 52 周时的进展情况。 09 Elinzanetant（OASIS研究） ·开发商：拜耳 ·药物：Elinzanetant ·药物类型：小分子药物 ·适应症：更年期血管舒缩症状 ·阶段：III期 ·机制：Elinzanetant是一种口服活性小分子神经激肽 NK1 受体和 NK3 受体拮抗剂，这种双重作用机制可能会降低参与体温调节的 kisspeptin（调控女性生殖内分泌功能的重要肽激素）、神经激肽 B 和强啡肽神经元回路的过度活跃。已发现它可以缓解绝经后妇女的潮热，并以剂量依赖性方式抑制绝经前妇女的黄体生成素、雌二醇和黄体酮水平。[6] ·时间： 2023 年下半年·背景：拜耳的 OASIS 研究 Elinzanetant 治疗更年期血管舒缩症状。护理标准，激素疗法，由于禁忌症或个人偏好，对于更年期症状的治疗的选择是有限的。相比之下，Elinzanetant 在 II 期研究中显示出显著且快速的血管舒缩症状改善，并且耐受性良好。数据结果显示，Elinzanetant可能比竞争对手 Astellas Pharma, Inc.的fezolinetant（一种口服神经激肽 3 受体拮抗剂）更具优势。 ·临床研究状态：Elinzanetant III 期 OASIS 研究计划的第一批结果预计将于 2023 年下半年公布。FDA正在对其进行优先审查，预计将于 2 月 22 日做出决定。拜耳寄希望于在峰值销售额中带来总计 120 亿欧元销售额。 10 Evobrutinib（EVOLUTION RMS 1 和2研究） ·开发商：默克 ·药物：Evobrutinib ·药物类型：小分子药物 ·适应症：复发性多发性硬化症 ·阶段：III期 ·机制：Evobrutinib是一款酪氨酸激酶小分子抑制剂，靶向BTK (布鲁顿氏酪氨酸激酶, Bruton tyrosine kinase) 。BTK 在 B 细胞发育中起着至关重要的作用，它们的激活是抗原受体信号传导的第一步。BTK 由 B 细胞和骨髓细胞表达，这两种细胞都被认为是多发性硬化症的驱动因素。 ·时间： 2023 年第4季度 ·背景：BTK 抑制剂将成为多发性硬化症的下一个大战场，许多候选药物处于后期开发阶段。目前领先的是默克的 evobrutinib 和赛诺菲的 tolebrutinib，紧随其后的是罗氏的fenebrutinib和诺华remibrutinib。 BTK 抑制剂具有高选择性，仅针对某些 B 细胞，与靶向 CD20 的单克隆抗体相比，例如罗氏的Ocrevus（ocrelizumab）和诺华的Kesimpta（ofatumumab），具有更高的安全性。此外，BTK 抑制剂可以穿过血脑屏障，因此它们可以抑制驱动多发性硬化症发展的 B 细胞和小胶质细胞。 ·临床研究状态：默克公司的 evobrutinib 在复发性多发性硬化症中的 EVOLUTION RMS 1 和 2 III 期试验，可能会在 2023 年最后一个季度的某个时候首先报告，其结果可能与赛诺菲的 tolebrutinib 的 III 期读数不相上下。 ------------THE END------------ 内容来源于网络，如有侵权，请联系删除。

抗体药物偶联物临床结果临床成功引进/卖出

100 项与 Kisspeptin 112-121 相关的药物交易

登录后查看更多信息

研发状态

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
特发性低促性腺素性功能减退症	临床2期	美国	The Schwartz Center for Compassionate Healthcare	2023-02-03
生殖道疾病 NOS	临床2期	美国	The Schwartz Center for Compassionate Healthcare	2023-02-03
继发性睾丸衰竭	临床2期	美国	The Schwartz Center for Compassionate Healthcare	2023-02-03
性腺机能减退	药物发现	美国	Mass General Brigham, Inc.	2020-12-02