预约演示

更新于：2025-01-23

Cabergoline

卡麦角林

更新于：2025-01-23

概要

基本信息

药物类型

小分子化药

别名

(8R)-6-allyl-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)ergoline-8-carboxamide、(8β)-N-[3-(dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-ergoline-8-carboxamide、1-((6-allylergolin-8β-yl)carbonyl)-1-(3-(dimethylamino)propyl)-3-ethylurea

+ [14]

靶点

D2 receptor

作用机制

D2 receptor激动剂(多巴胺D2受体激动剂)

治疗领域

神经系统疾病内分泌与代谢疾病皮肤和肌肉骨骼疾病+ [1]

在研适应症

非在研适应症

原研机构

在研机构

Pfizer Inc.Strides Pharma Global Pte Ltd.

非在研机构-

最高研发阶段批准上市

首次获批日期

澳大利亚 (1995-04-21),

高催乳素血症

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C26H37N5O2

InChIKeyKORNTPPJEAJQIU-KJXAQDMKSA-N

CAS号81409-90-7

关联

项与卡麦角林相关的临床试验

ChiCTR2400088093

/ SuspendedN/AIIT

A Non-Interventional Real-World Study on the Use of Cabergoline in the Treatment of Locally Advanced or Metastatic Prostate Cancer

开始日期2024-08-20

申办/合作机构-

CTRI/2024/08/071776

/ Not yet recruitingN/A

To study the efficacy of Cabergoline as an adjunct to Metformin in management of overweight & obese women with PCOS

开始日期2024-08-17

申办/合作机构-

IRCT20240305061171N1

/ Completed临床3期IIT

Comparing the effects of cabergoline and hydroxychloroquine to prevent ovarian hyperstimulation syndrome (OHSS) in PCOS patients undergoing infertility treatment.

开始日期2024-04-03

申办/合作机构

Tehran University of Medical Sciences

100 项与卡麦角林相关的临床结果

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100 项与卡麦角林相关的转化医学

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100 项与卡麦角林相关的专利（医药）

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1,924

项与卡麦角林相关的文献（医药）

2025-01-01·Journal of Clinical Sleep Medicine

Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine clinical practice guideline

Review

作者: Shelgikar, Anita V. ; Kazmi, Uzma ; Sharon, Denise ; Falck-Ytter, Yngve ; Koo, Brian B. ; DelRosso, Lourdes M. ; Trotti, Lynn Marie ; Berkowski, J. Andrew ; Walters, Arthur S. ; Zak, Rochelle S. ; Winkelman, John W. ; Scharf, Matthew T.

INTRODUCTIONThis guideline establishes clinical practice recommendations for treatment of restless legs syndrome (RLS) and periodic limb movement disorder (PLMD) in adults and pediatric patients.METHODSThe American Academy of Sleep Medicine (AASM) commissioned a task force of experts in sleep medicine to develop recommendations and assign strengths based on a systematic review of the literature and an assessment of the evidence using the grading of recommendations assessment, development, and evaluation methodology. The task force provided a summary of the relevant literature and the certainty of evidence, the balance of benefits and harms, patient values and preferences, and resource use considerations that support the recommendations. The AASM Board of Directors approved the final recommendations.GOOD PRACTICE STATEMENTThe following good practice statement is based on expert consensus, and its implementation is necessary for the appropriate and effective management of patients with RLS.1. In all patients with clinically significant RLS, clinicians should regularly test serum iron studies including ferritin and transferrin saturation (calculated from iron and total iron binding capacity). Testing should ideally be administered in the morning avoiding all iron-containing supplements and foods at least 24 hours prior to blood draw. Analysis of iron studies greatly influences the decision to use oral or intravenous (IV) iron treatment. Consensus guidelines, which have not been empirically tested, suggest that supplementation of iron in adults with RLS should be instituted with oral or IV iron if serum ferritin ≤ 75 ng/mL or transferrin saturation < 20%, and only with IV iron if serum ferritin is between 75 and 100 ng/mL. In children, supplementation of iron should be instituted for serum ferritin < 50 ng/mL with oral or IV formulations. These iron supplementation guidelines are different than for the general population.2. The first step in the management of RLS should be addressing exacerbating factors, such as alcohol, caffeine, antihistaminergic, serotonergic, antidopaminergic medications, and untreated obstructive sleep apnea.3. RLS is common in pregnancy; prescribers should consider the pregnancy-specific safety profile of each treatment being considered.RECOMMENDATIONSThe following recommendations are intended as a guide for clinicians in choosing a specific treatment for RLS and PLMD in adults and children. Each recommendation statement is assigned a strength ("strong" or "conditional"). A "strong" recommendation (ie, "We recommend…") is one that clinicians should follow under most circumstances. The recommendations listed below are ranked in the order of strength of recommendations and grouped by class of treatments within each PICO (Patient, Intervention, Comparator, Outcome) question. Some recommendations include remarks that provide additional context to guide clinicians with implementation of this recommendation.ADULTS WITH RLS1. In adults with RLS, the AASM recommends the use of gabapentin enacarbil over no gabapentin enacarbil (strong recommendation, moderate certainty of evidence).2. In adults with RLS, the AASM recommends the use of gabapentin over no gabapentin (strong recommendation, moderate certainty of evidence).3. In adults with RLS, the AASM recommends the use of pregabalin over no pregabalin (strong recommendation, moderate certainty of evidence).4. In adults with RLS, the AASM recommends the use of IV ferric carboxymaltose over no IV ferric carboxymaltose in patients with appropriate iron status (see good practice statement for iron parameters) (strong recommendation, moderate certainty of evidence).5. In adults with RLS, the AASM suggests the use of IV low molecular weight iron dextran over no IV low molecular weight iron dextran in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, very low certainty of evidence).6. In adults with RLS, the AASM suggests the use of IV ferumoxytol over no IV ferumoxytol in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, very low certainty of evidence).7. In adults with RLS, the AASM suggests the use of ferrous sulfate over no ferrous sulfate in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, moderate certainty of evidence).8. In adults with RLS, the AASM suggests the use of dipyridamole over no dipyridamole (conditional recommendation, low certainty of evidence).9. In adults with RLS, the AASM suggests the use of extended-release oxycodone and other opioids over no opioids (conditional recommendation, moderate certainty of evidence).10. In adults with RLS, the AASM suggests the use of bilateral high-frequency peroneal nerve stimulation over no peroneal nerve stimulation (conditional recommendation, moderate certainty of evidence).11. In adults with RLS, the AASM suggests against the standard use of levodopa (conditional recommendation, very low certainty of evidence).Remarks: levodopa may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).12. In adults with RLS, the AASM suggests against the standard use of pramipexole (conditional recommendation, moderate certainty of evidence).Remarks: pramipexole may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).13. In adults with RLS, the AASM suggests against the standard use of transdermal rotigotine (conditional recommendation, low certainty of evidence).Remarks: transdermal rotigotine may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).14. In adults with RLS, the AASM suggests against the standard use of ropinirole (conditional recommendation, moderate certainty of evidence).Remarks: ropinirole may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).15. In adults with RLS, the AASM suggests against the use of bupropion for the treatment of RLS (conditional recommendation, moderate certainty of evidence).16. In adults with RLS, the AASM suggests against the use of carbamazepine (conditional recommendation, low certainty of evidence).17. In adults with RLS, the AASM suggests against the use of clonazepam (conditional recommendation, very low certainty of evidence).18. In adults with RLS, the AASM suggests against the use of valerian (conditional recommendation, very low certainty of evidence).19. In adults with RLS, the AASM suggests against the use of valproic acid (conditional recommendation, low certainty of evidence).20. In adults with RLS, the AASM recommends against the use of cabergoline (strong recommendation, moderate certainty of evidence).SPECIAL ADULT POPULATIONS WITH RLS21. In adults with RLS and end-stage renal disease (ESRD), the AASM suggests the use of gabapentin over no gabapentin (conditional recommendation, very low certainty of evidence).22. In adults with RLS and ESRD, the AASM suggests the use of IV iron sucrose over no IV iron sucrose in patients with ferritin < 200 ng/mL and transferrin saturation < 20% (conditional recommendation, moderate certainty of evidence).23. In adults with RLS and ESRD, the AASM suggests the use of vitamin C over no vitamin C (conditional recommendation, low certainty of evidence).24. In adults with RLS and ESRD, the AASM suggests against the standard use of levodopa (conditional recommendation, low certainty of evidence).Remarks: levodopa may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).25. In adults with RLS and ESRD, the AASM suggests against the standard use of rotigotine (conditional recommendation, very low certainty of evidence).Remarks: rotigotine may be used to treat RLS in patients who place a higher value on the reduction of restless legs symptoms with short-term use and a lower value on adverse effects with long-term use (particularly augmentation).ADULTS WITH PLMD26. In adults with PLMD, the AASM suggests against the use of triazolam (conditional recommendation, very low certainty of evidence).27. In adults with PLMD, the AASM suggests against the use of valproic acid (conditional recommendation, very low certainty of evidence).CHILDREN WITH RLS28. In children with RLS, the AASM suggests the use of ferrous sulfate over no ferrous sulfate in patients with appropriate iron status (see good practice statement for iron parameters) (conditional recommendation, very low certainty of evidence).CITATIONWinkelman JW, Berkowski JA, DelRosso LM, et al. Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine clinical practice guideline. J Clin Sleep Med. 2025;21(1):137-152.

2024-12-31·Gynecological Endocrinology

Expression of Concern: Laparoscopic ovarian drilling versus GnRH antagonist combined with cabergoline as a prophylaxis against the re-development of ovarian hyperstimulation syndrome

Article

2024-12-22·Neuro endocrinology letters

Analysis of oxytocin and oxytocin receptor expressions after hand therapy treatment in a mouse model of chemotherapy-induced peripheral neuropathy .

Article

作者: Shinouchi, Ryosuke ; Nobe, Koji ; Kiuchi, Yuji ; Sasaki, Akiko

OBJECTIVESTriple negative breast cancer (TNBC) is a distinct subtype of breast cancer that has a poor prognosis due to the lack of effective therapeutic agents. Since a significant proportion of human surgical samples of TNBC expressed mRNA for the growth hormone (GH), growth hormone-releasing hormone (GHRH), and gonadotropin-releasing hormone (GnRH) receptors, and the mitogenic proliferative activity of GH, GHRH, and GnRH, have been identified as effective therapeutic targets for somatostatin and its analogs and GnRH analogs, Di Bella Method (DBM), a combination of hormonal analogs and vitamins, was introduced to target and inhibit solid tumors. The present study aimed to improve the prognosis of TNBC using DBM in women with TNBC.METHODSThis retrospective observational clinical study was done on women with TNBC who were diagnosed based on histology, nuclear grade, and immunohistochemical testing for estrogen receptor, HER2/neu, and progesterone receptor. Patients were either treated with standard oncology protocol, including chemotherapy and radiotherapy plus DBM, or with DBM alone. The DBM included a daily combination of somatostatin, octreotide, melatonin, retinoids solubilized in alpha tocopheryl acetate, dopaminergic agonists, bromocriptine, cabergoline, aromatase inhibitors for anti-estrogen function, and low metronomic doses of cyclophosphamide.RESULTSIn this study, 35 patients were enrolled, and their survival was monitored for 5 years during which they received DBM and standard chemotherapy/radiotherapy protocol. These patients had a survival rate of 64% at 5 years, 76% at 3 years, 87% at 2 years, and 100% after 1 year of therapy. On the other hand, 13 patients who received only DBM had a survival rate of 60% at 5 years, 67% at 3 years, 75% at 2 years and 100% after 1 year of therapy. None of the patients had significant adverse events.CONCLUSIONSCompared to published clinical trials, the DBM improved the prognosis of women with TNBC. However, more standardized clinical trials, including DBM with and without standard therapeutic protocols for TNBC, are warranted.

项与卡麦角林相关的新闻（医药）

2024-12-02

·drugs

Guidelines Developed for Treatment of Restless Legs Syndrome

MONDAY, Dec. 2, 2024 -- In a clinical practice guideline issued by the American Academy of Sleep Medicine and published online Sept. 26 in the Journal of Clinical Sleep Medicine , recommendations are presented for the treatment of restless legs syndrome (RLS). John W. Winkelman, M.D., Ph.D., from Massachusetts General Hospital in Boston, and colleagues developed recommendations for treatment of RLS and periodic limb movement disorder in adults and pediatric patients. The researchers developed three good practice statements that were based on expert consensus. They recommend all clinicians should regularly test serum iron studies, including ferritin and transferrin saturation, in all patients with clinically significant RLS, ideally in the morning; analysis of these studies influences the decision to use oral or intravenous (IV) iron treatment. The authors also state that addressing exacerbating factors, including alcohol, caffeine, antihistaminergic, serotonergic, and anti-dopaminergic medications, should be the first step in RLS management. They note RLS is common in pregnancy and the pregnancy-specific safety profile of each treatment should be considered. Recommendations for adults with RLS include use of gabapentin enacarbil over no gabapentin enacarbil; use of gabapentin over no gabapentin; use of pregabalin over no pregabalin; and use of IV ferric carboxymaltose over no IV ferric carboxymaltose for those with appropriate iron status (strong recommendations; moderate certainty of evidence). In addition, there is a strong recommendation against use of cabergoline. "Guided by the best evidence in the scientific literature, we've provided recommendations that will improve the ability of clinicians to provide patient-centered care for people who have RLS," Winkelman said in a statement. One author disclosed ties to the pharmaceutical and medical device industries. Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

2024-03-05

·精准药物

含吲哚药物结构与靶点，药理与SAR 研究归纳

吲哚是一种芳香杂环分子，具有一个苯环和一个含氮吡咯环组成的双环结构。吲哚中的氮原子提供一对孤对电子，形成共轭体系，从而稳定了吲哚结构。这对孤电子使吲哚化合物呈现弱碱性(pKa=16.2和pK,=17.6)。由于吡咯环的电子密度相对较高以及氮原子的共轭效应，吲哚可以在其吡咯环的3位发生亲电取代反应(图la)。图 1 (a) 全球有超过70种含有吲哚的合成药物在市场上销售，并被证明具有良好的医疗效果(图1b)。用于治疗的疾病包括糖尿病、癌症、白血病、丙型肝炎、心理障碍和其他临床问题。自2015年起，美国(FDA)专门批准了14种含吲哚药物，其中3种是在2021年批准的(图2)。二氢麦角胺(DHE,1)的化学结构中含有吲哚支架，对头颅血管平滑肌中的5-HT1b受体具有激动活性，治疗偏头痛。昂丹司琼(2)是一种血清素5-HT3受体拮抗剂，用于预防癌症治疗期间和手术后的恶心和呕吐(图3a)。图 3 (a) 双氢麦角胺（1）和昂丹司琼（2）的结构。(b) 双氢麦角胺(1)与其靶点（左）和昂丹司琼(2)与其靶点（右）的关键靶点相互作用。替加色罗(3)在临床相关水平上被认为是5-HT(4)受体的激动剂和5-HT(2B)受体的拮抗剂，其作用之一是使受损的胃肠道运动恢复正常。多拉司琼(4)用于中度致吐的癌症化疗以及术后恶心和呕吐的治疗(图5)。它是一种高效、选择性的血清素5-HT3受体拮抗剂。 Tropisetron（5）可抑制5HT3受体上血清素的活性，从而抑制放疗和化疗引起的呕吐。 Vilazodone(6)是5HT-1A受体的部分激动剂，专门抑制中枢神经系统对血清素的再摄取。在治疗偏头痛急性发作方面，三苯氧胺药物(5-羟色胺受体激动剂)比其他药物更有效、更耐受。这类药物具有起效快、用药时间长、不良反应少等优点。Sumatriptan(7),zolmitriptan(8),naratriptan(9), rizatriptan(10), almotriptan (11), frovatriptan (12), eletriptan (13), 和 oxitriptan (14) 是国外已商业化的曲坦类药物的代表。(图7)。环氧化酶(COX)被称为前列腺素G/H合成酶，而吲哚美辛是一种非特异性的可逆性环氧化酶抑制剂。吲哚美辛(18)属于吲哚-3-乙酸类，其官能团包括对氯苯甲酰基、甲基和甲氧基。它是一种非甾体抗炎药(NSAID), 具有消炎、镇痛和解热的特点(图11a)。 Acemetacin(19)是另一种强效非甾体抗炎药物，由吲哚-3-乙酸衍生而来(图12)。它主要通过酯分解代谢为吲哚美辛。 Etodolac(20)是一种非甾体抗炎药，具有消炎、镇痛和解热作用(图13a)。以前被认为是一种非选择性COX抑制剂，但现在被认为对COX-2的选择性是COX-1的5-50倍。 Carprofen(21)是兽医用作缓解老年犬关节炎症状的辅助疗法的一种非甾体抗炎药，人们认为卡洛芬(21)的作用机制是抑制环氧化酶的活性。帕金森病的药物 Cabergoline(22)是一种长效多巴胺受体激动剂，与D2受体有很强的亲和力，用于治疗高催乳素血症和帕金森综合症(图14a)。 Lisuride(23)可能是某些血清素受体的激动剂,也可能是多巴胺D1受体的拮抗剂。可降低催乳素水平，适量服用可阻止偏头痛，从药理上讲，(23)是还是一种帕金森氏症药物。治疗子宫脱垂的药物甲基麦角新碱(26)是一种麦角生物碱，临床上用于预防和治疗产后和流产后出血(图17)。这种药物与多巴胺D1受体结合，作为一种拮抗剂发挥作用，可增强平滑肌的张力、节奏和节律性收缩的幅度。治疗精神疾病的药物 sertindole（27）是一种抗精神分裂症药物，也是一种苯基吲哚衍生物。临床试验证实，(27)对低水平的多巴胺D2占位具有疗效。治疗神经系统疾病的药物吲哚洛尔(28)是一种非选择性β肾上腺素受体拮抗剂，用于治疗心房颤动、水肿、高血压和室性心动过速。卡维地洛(29)通过阻断β肾上腺素受体防止运动引起的心动过速，它对α-1肾上腺素能受体的作用可使血管平滑肌放松，从而降低外周血管阻力和血压。尼麦角林(30)是一种半合成麦角衍生物，可用于治疗认知功能障碍。这种药剂作为一种选择性α-1A肾上腺素能受体抑制剂用于临床(图20)。治疗生殖系统疾病的药物麦角新碱(32)是一种麦角生物碱，可用于控制妇女的产后和流产后出血。结构与活性关系明确的药物 Tezacaftor(41)属于用于治疗囊性纤维化(CFTR)增效剂。美国食品及药物管理局批准该药与ivacaftor联合用于治疗囊性纤维化(图28a)。该药物可在2至4小时内达到血浆浓度峰值。 2015年2月23日，FDA批准口服去乙酰化酶(DAC)抑制剂Panobinostat(42)用于治疗多发性骨髓瘤(图29a)。(42)在体外与人体血浆蛋白的结合率约为90%,这与其浓度无关。其吲哚环可以通过与Asn645的氢键相互作用为SAR创造一个稳定的框架(图29b)。结构与活性关系不完全明确的药物 Metergoline(52)是一种麦角衍生物，用于治疗女性高催乳素闭经症(图39)。通过靶向钠通道而非5HT受体来抑制钠通道的活性，从而导致泌乳素分泌减少。 Lurbinectedin(53)是一种抗癌天然产物。该药物在化疗中用于治疗转移性小细胞肺癌。Lurbinectedin(53)在临床试验中的治疗反应率和持续时间在2020年获得了加速批准。总体而言，在FDA批准的药物中，含有吲哚环的药物数量在不断增加。在药物分子中引入吲哚砌块也已成为药物化学和药物设计中的一种常见策略。现有的含吲哚药物因其特殊的结构，在抗癌、抗炎和抗病毒等方面具有显著的临床价值。参考文献：DOI: 10.1039/d3md00677h 内容来源于网络，如有侵权，请联系删除。

上市批准放射疗法

2021-05-20

·GlobeNewswire

Chiasma to Present Encore and New Data from MPOWERED™ Phase 3 Trial at Upcoming e-ECE and AACE Virtual Conferences

-- New clinical data accepted for oral and e-Poster presentation at AACE -- -- e-ECE clinical data previously presented at Endocrine Society’s 2021 annual meeting -- NEEDHAM, Mass., May 20, 2021 (GLOBE NEWSWIRE) -- Chiasma, Inc. (NASDAQ: CHMA), (“Chiasma” or the “Company”), a commercial-stage biopharmaceutical company utilizing its delivery platform technology to develop and commercialize oral therapies to improve the lives of patients with rare diseases currently treated with burdensome and painful injections, today announced that it will virtually present encore data from its MPOWERED™ Phase 3 clinical trial at the 23rd European Congress of Endocrinology (e-ECE) (May 22-26, 2021) and new data from the MPOWERED trial at the 30th Annual American Association of Clinical Endocrinology (AACE) Meeting (May 26-29, 2021). Oral presentations and posters for display are summarized below: e-ECE 2021 Oral PresentationTitle: A Phase 3 Large International Noninferiority Trial (MPOWERED): Assessing Maintenance of Response to Oral Octreotide Capsules in Comparison to Injectable Somatostatin Receptor LigandsPresenter: Maria Fleseriu, M.D., FACE, Professor, Medicine and Neurological Surgery, Director OHSU Northwest Pituitary CenterSession Date/Time: Wednesday, May 26, 2021, 8:30 a.m. – 9:30 a.m. EDT e-ECE 2021 e-Poster PresentationsTitle: Safety Results from MPOWERED, a Phase 3 Trial of Oral Octreotide Capsules in Adults with AcromegalyPresenter: Pamela Freda, M.D., Columbia University Session Date/Time: Monday, May 24, 2021, 8:00 a.m. – 8:30 a.m. EDT Title: Oral Octreotide Capsules Lowered Incidence and Improved Severity of Acromegaly Symptoms Compared to Injectable Somatostatin Receptor Ligands—Results from the MPOWERED TrialPresenter: Nienke Biermasz, M.D., Ph.D., Leiden University Medical Center Session Date/Time: Tuesday, May 25, 2021, 8:00 a.m. – 8:30 a.m. EDT Title: Addition of Cabergoline to Oral Octreotide Capsules May Improve Biochemical Control in Patients with Acromegaly Who Are Inadequately Controlled with MonotherapyPresenter: Maria Fleseriu, M.D., FACE, Professor, Medicine and Neurological Surgery, Director OHSU Northwest Pituitary CenterSession Date/Time: Tuesday, May 25, 2021, 8:00 a.m. – 8:30 a.m. EDT Title: Improved Acromegaly Patient Satisfaction with Oral Octreotide Capsules Compared with Injectable Somatostatin Receptor Ligands in the MPOWERED TrialPresenter: Murray B. Gordon, M.D., Allegheny General HospitalSession Date/Time: Wednesday, May 26, 2021, 8:00 a.m. – 8:30 a.m. EDT AACE 2021 Oral PresentationTitle: Improved Quality of Life and Work Productivity in Patients with Acromegaly Receiving Oral Octreotide Capsules in the Phase 3 MPOWERED TrialPresenter: Nienke Biermasz, M.D., Ph.D., Leiden University Medical CenterSession Date/Time: Thursday, May 27, 2021, 1:30 p.m. – 1:45 p.m. EDT AACE 2021 Late-Breaker e-Posters - Available online via the virtual e-Poster Gallery beginning May 26Title: Effects of Prior Injectable Somatostatin Receptor Ligand Type and Dose in Patients with Acromegaly Receiving Oral Octreotide Capsules in the Phase 3 MPOWERED TrialLead Author: Murray B. Gordon, M.D., Allegheny General Hospital Title: Injection Site Reactions and Their Impact in Patients with Acromegaly Receiving Injectable Somatostatin Receptor Ligands in the Phase 3 MPOWERED TrialLead Author: Murray B. Gordon, M.D., Allegheny General Hospital To register and view the full schedules as well as abstracts, visit e-ECE’s website here and AACE’s website here. Chiasma will sponsor a product theatre presentation at the AACE annual meeting titled “Understanding the Management of Acromegaly with MYCAPSSA® (octreotide) Delayed-Release Oral Capsules” on Wednesday, May 26 at 2:45 p.m. EDT. Anthony P. Heaney, M.D., Ph.D., Professor, UCLA, will lead the presentation and a live Q&A session. About the MPOWERED™ Trial The MPOWERED trial was a global, non-inferiority, randomized, open-label and active-controlled, 15-month trial intended to support approval of MYCAPSSA in the European Union. Chiasma completed enrollment of 146 adult acromegaly patients into the trial in June 2019, of which 92 patients were deemed responders to octreotide capsules per the protocol following a six-month run-in were randomized to either octreotide capsules (n=55) or injectable somatostatin receptor ligands (octreotide LAR or lanreotide autogel) (n=37), and then followed for an additional nine months. The trial was designed to evaluate the proportion of patients who maintain their biochemical response to octreotide capsules and patient-reported outcomes in patients treated with octreotide capsules, compared to patients treated with leading injectable somatostatin analogs. About MYCAPSSA INDICATION AND IMPORTANT SAFETY INFORMATION INDICATION AND USAGE MYCAPSSA (octreotide) delayed-release capsules, for oral use, is a somatostatin analog indicated for long-term maintenance treatment in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide. CONTRAINDICATIONS Hypersensitivity to octreotide or any of the components of MYCAPSSA. Anaphylactoid reactions, including anaphylactic shock, have been reported in patients receiving octreotide. IMPORTANT SAFETY INFORMATION WARNINGS AND PRECAUTIONS MYCAPSSA can cause problems with the gallbladder. Monitor patients periodically. Discontinue if complications of cholelithiasis are suspected. Blood sugar, thyroid levels, and vitamin B12 levels should be monitored and treated accordingly. Bradycardia, arrhythmia, or conduction abnormalities may occur. Treatment with drugs that have bradycardia effects may need to be adjusted. ADVERSE REACTIONS The most common adverse reactions (incidence >10%) are nausea, diarrhea, headache, arthralgia, asthenia, hyperhidrosis, peripheral swelling, blood glucose increased, vomiting, abdominal discomfort, dyspepsia, sinusitis, and osteoarthritis. DRUG INTERACTIONS The following drugs require monitoring and possible dose adjustment when used with MYCAPSSA: cyclosporine, insulin, antidiabetic drugs, calcium channel blockers, beta blockers, lisinopril, digoxin, bromocriptine, and drugs mainly metabolized by CYP3A4. Counsel women to use an alternative non-hormonal method of contraception or a back-up method when MYCAPSSA is used with combined oral contraceptives. Patients taking proton pump inhibitors, H2-receptor antagonists, or antacids concomitantly with MYCAPSSA may require increased dosages of MYCAPSSA. PREGNANCY Advise premenopausal females of the potential for an unintended pregnancy. To report SUSPECTED ADVERSE REACTIONS, contact the product information department at 1-844-312-2462 or FDA at 1-800-FDA-1088 or The full Prescribing Information for MYCAPSSA is available at . About Acromegaly Acromegaly typically develops when a benign tumor of the pituitary gland produces too much growth hormone, ultimately leading to significant health problems. Common features of acromegaly are facial changes, intense headaches, joint pain, impaired vision and enlargement of the hands, feet, tongue and internal organs. Serious health conditions associated with the progression of acromegaly include type 2 diabetes, hypertension, respiratory disorders and cardiac and cerebrovascular disease. Chiasma estimates that approximately 8,000 adult acromegaly patients are chronically treated with somatostatin analog injections in the United States. About Chiasma Chiasma is a commercial-stage biopharmaceutical company focused on developing and commercializing oral therapies to improve the lives of patients who face challenges associated with their existing treatments for rare and serious chronic diseases. Employing its Transient Permeability Enhancer (TPE®) technology platform, Chiasma seeks to develop oral medications that are currently available only as injections. In June 2020, Chiasma received FDA approval of MYCAPSSA for long-term maintenance therapy in acromegaly patients who have responded to and tolerated treatment with octreotide or lanreotide. MYCAPSSA, the first and only oral somatostatin analog approved by the FDA, is available for commercial sale. Chiasma is headquartered in Needham, MA with a wholly owned subsidiary in Israel. MYCAPSSA, TPE and CHIASMA are registered trademarks of Chiasma. For more information, please visit the company’s website at . Forward-Looking Statements This release contains “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995, including, but not limited to, statements regarding the data from the MPOWERED trial and the therapeutic potential of MYCAPSSA. Such statements are subject to numerous important factors, risks and uncertainties, many of which are beyond the company’s control, that may cause actual events or results to differ materially from the company’s current expectations. Management’s expectations and, therefore, any forward-looking statements in this press release could be affected by risks and uncertainties. For a discussion of these and other risks and uncertainties, and other important factors, any of which could cause the company’s actual results to differ from those contained in the forward-looking statements, see the section entitled “Risk Factors” in Chiasma’s Quarterly Report on Form 10-Q for the quarter ended March 31, 2021, and in subsequent filings with the Securities and Exchange Commission. All information in this press release is as of the date of the release, and Chiasma undertakes no duty to update this information unless required by law. Investor Relations and Corporate Communications:Ashley RobinsonLifeSci Advisors, LLC617-430-7577arr@lifesciadvisors.com Media Relations:Patrick BurseyLifeSci Communications646-876-4932pbursey@lifescicomms.com

100 项与卡麦角林相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00987	卡麦角林	N04BC06 G02CB03	DB00248

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
泌乳障碍	日本	Pfizer Japan, Inc.	2003-04-16
帕金森病	日本	Pfizer Japan, Inc.	1999-06-16
高催乳素血症	澳大利亚	Pfizer Inc.	1995-04-21

未上市

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
不宁腿综合征	药物发现	-	Pfizer Inc.	2002-11-01

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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


NCT01794793 (B2412, CTgov)	临床4期	垂体ACTH分泌过多 \| 倾倒综合征 \| 垂体肿瘤 \| 肢端肥大症 \| 黑色素瘤 \| 前列腺癌 \| 异位ACTH综合征	337	Cabergoline+Pasireotide (Pasireotide Subcutaneous)	範齋醖築範積餘衊窪鏇(壓餘網鏇遞夢鏇願衊觸) = 憲製衊願鹽鏇構願窪鹹衊構遞範願壓積選憲壓 (觸夢壓糧繭鹹觸製鹽製, 艱遞蓋積選鹹窪觸簾鏇 ~ 餘顧廠艱憲構獵餘獵願) 更多	-	2024-08-28
				Pasireotide LAR (Pasireotide Long Acting Release (LAR))	範齋醖築範積餘衊窪鏇(壓餘網鏇遞夢鏇願衊觸) = 鏇築製淵網壓選築簾顧衊構遞範願壓積選憲壓 (觸夢壓糧繭鹹觸製鹽製, 製醖蓋網範製蓋壓鑰觸 ~ 簾網鏇構構鏇餘構膚選) 更多
ENDO2024	N/A	-	-	Cabergoline 0.5 mg	範顧簾網觸餘廠窪餘膚(鏇壓積簾鏇窪膚繭艱淵) = 築獵觸襯壓齋積遞積範顧鏇齋夢製範構構夢壓 (觸鏇廠簾遞衊鏇醖願遞, 7.2 ~ 63.3) 更多	-	2024-06-01
NCT05024422 (Pubmed \| Am J Obstet Gynecol)	临床3期	母乳喂养	-	Cabergoline	繭製窪簾觸膚糧齋選構(齋積鑰夢憲糧選築鬱獵) = 觸淵築齋淵醖窪積糧鹽獵窪構願鏇艱膚鏇顧鑰 (糧製廠構繭艱選襯製範 ) 更多	积极	2024-05-01
				Pyridoxine	繭製窪簾觸膚糧齋選構(齋積鑰夢憲糧選築鬱獵) = 築夢醖鏇窪簾鏇壓製選獵窪構願鏇艱膚鏇顧鑰 (糧製廠構繭艱選襯製範 ) 更多
FRI248 (ENDO2023)	N/A	垂体ACTH分泌过多	1	Desmopressin	(鑰網繭艱獵憲鏇醖網夢) = 窪製遞壓餘範鹹餘選願廠窪築淵觸鹽襯壓獵廠 (憲齋鬱襯築膚遞壓願壓 ) 更多	-	2023-10-05
				Cabergoline	(鑰網繭艱獵憲鏇醖網夢) = 夢憲壓膚顧繭鹹構壓鏇廠窪築淵觸鹽襯壓獵廠 (憲齋鬱襯築膚遞壓願壓 ) 更多
FRI323 (ENDO2023)	N/A	催乳素瘤 testosterone \| estradiol \| PRL	-	Cabergoline	糧築膚繭構餘鹹蓋構網(網構遞繭夢積憲壓蓋窪) = 鏇蓋蓋觸蓋餘鬱窪壓簾夢築觸壓願廠蓋願築築 (網鏇淵鹹簾鹹齋鏇憲鹹 )	-	2023-10-05
				Testosterone cypionate 60 mg weekly	糧築膚繭構餘鹹蓋構網(網構遞繭夢積憲壓蓋窪) = 鹹網顧憲鑰簾鹽膚鹹廠夢築觸壓願廠蓋願築築 (網鏇淵鹹簾鹹齋鏇憲鹹 )
FRI474 (ENDO2023)	N/A	合并垂体激素缺乏症 \| 甲状腺功能减退症	-	Levothyroxine	願膚積壓夢醖壓製襯願(艱衊鏇願簾襯壓鑰繭鏇) = significantly improved after initiating the hormone replacement with levothyroxine and a stress hydrocortisone dose, gradually tapered to a physiological dose, and cabergoline 膚鏇遞選蓋艱醖淵鹹鬱 (壓夢糧窪餘觸顧築齋製 )	-	2023-10-05
				Stress hydrocortisone
NCT01794793 (B2412, ENDO2023)	临床4期	-	341	Pasireotide LAR	鹽醖鑰鹽鬱觸顧繭遞憲(網繭糧積選遞憲憲餘簾) = 構壓醖鹽鑰鏇衊範顧壓襯鑰鹽糧願觸網襯醖遞 (觸蓋夢窪醖廠艱網願選 )	积极	2023-10-05
				Pasireotide sc	鹽醖鑰鹽鬱觸顧繭遞憲(網繭糧積選遞憲憲餘簾) = 簾襯顧壓膚壓憲糧選餘襯鑰鹽糧願觸網襯醖遞 (觸蓋夢窪醖廠艱網願選 )
THU028 (ENDO2023)	N/A	肢端肥大症	2	Oral Octreotide	構願鏇餘窪窪觸壓鏇齋(壓鏇鹹遞憲蓋蓋網鏇鹽) = 鏇鑰鑰淵遞觸淵襯壓構鑰製鹽廠襯選衊鹽願蓋 (夢鏇築餘廠醖窪願壓製 ) 更多	积极	2023-10-05
				Cabergoline	構願鏇餘窪窪觸壓鏇齋(壓鏇鹹遞憲蓋蓋網鏇鹽) = 積鏇鏇願獵膚製鏇壓憲鑰製鹽廠襯選衊鹽願蓋 (夢鏇築餘廠醖窪願壓製 ) 更多
NCT04701333 (Pubmed \| Obstet Gynecol)	临床2期	流产	73	Cabergoline 1 mg	壓積鹹築製襯鬱繭鹹繭(觸願蓋繭顧壓繭遞襯繭) = 衊製糧衊鹹遞選糧獵獵積鏇遞憲遞窪鑰願觸廠 (窪網廠鹽鏇積鑰窪築繭 )	积极	2023-06-01
				Placebo	壓積鹹築製襯鬱繭鹹繭(觸願蓋繭顧壓繭遞襯繭) = 夢蓋製範淵襯築顧築膚積鏇遞憲遞窪鑰願觸廠 (窪網廠鹽鏇積鑰窪築繭 )
NCT04701333 (LISTA, CTgov)	临床2期	母乳喂养 \| 妊娠中期流产	73	Cabergoline 1 MG (Cabergoline)	鹹鹽積製夢夢膚餘網齋(壓鏇鹹繭廠膚遞繭鏇衊) = 遞繭範鹹觸壓願顧夢廠醖獵襯廠願壓製觸鑰糧 (積選繭鹽艱願窪夢鑰遞, 醖憲簾夢夢壓觸構鏇壓 ~ 壓憲遞餘膚鹽遞簾觸繭) 更多	-	2023-04-05
				Placebo (Placebo)	鹹鹽積製夢夢膚餘網齋(壓鏇鹹繭廠膚遞繭鏇衊) = 鹹觸廠獵夢憲遞鹽簾衊醖獵襯廠願壓製觸鑰糧 (積選繭鹽艱願窪夢鑰遞, 遞壓廠鏇廠觸夢衊艱窪 ~ 壓蓋淵膚鬱艱繭簾壓糧) 更多