预约演示
更新于：2025-12-04
Lanreotide Acetate
醋酸兰瑞肽
更新于：2025-12-04
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、优先审评 (中国)、孤儿药 (韩国) |
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结构/序列
分子式C56H73N11O12S2 |
InChIKeyDEXPIBGCLCPUHE-UISHROKMSA-N |
CAS号127984-74-1 |
Sequence Code 26246302
来源: *****
关联
109
项与 醋酸兰瑞肽 相关的临床试验NCT06878664
Randomized Interval Assessment Trial of Lu177-Dotatate Every 8 Versus Every 16 Weeks in Slowly Progressive G1-2 Advanced Midgut Neuroendocrine Tumors (NETs) to Lower TOxicity
NCT06807437
A Randomized Phase III Blinded Trial of Lanreotide for the Prevention of Postoperative Pancreatic Fistula
CTIS2023-505884-35-00
Absorbed Tumor Dose in Peptide Receptor Radionuclide Therapy with long-acting Somatostatin Analogues – ATSA trial
100 项与 醋酸兰瑞肽 相关的临床结果
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100 项与 醋酸兰瑞肽 相关的转化医学
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100 项与 醋酸兰瑞肽 相关的专利（医药）
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1,284
项与 醋酸兰瑞肽 相关的文献（医药）2025-12-01Journal of Gastrointestinal Cancer
Mixed Neuroendocrine and Non-neuroendocrine Tumor of Pancreato-Biliary Origin Treated Successfully with Peptide Receptor Radionuclide Therapy
Article
作者: Luong, Tu Vinh ; Navalkissoor, Shaunak ; Krell, Daniel ; Paterson, Anna ; Caplin, Martyn ; Shekhda, Kalyan Mansukhbhai
PURPOSE:
Mixed neuroendocrine and non-neuroendocrine neoplasms (MiNENs) are rare neoplasms composed of morphologically distinguishable neuroendocrine (NE) and non-neuroendocrine components, each representing at least 30% of the tumor volume. The NE component must be substantiated by immunohistochemistry. MiNENs generally have a poor prognosis, with a more aggressive component dictating overall survival and prognosis. Owing to its rarity, there are no specific validated treatment guidelines available for these tumors, and they are generally treated with surgery if possible. However, surgically unresectable or advanced tumors are generally treated with chemotherapy.
METHODS:
We report a case of an elderly woman who was referred to the neuroendocrine tumor (NET) unit following incidental findings of liver lesions found on cardiac magnetic resonance imaging (MRI) performed for an asymptomatic heart murmur. Histology from the liver biopsy revealed MiNEN with up to 60% grade 2 (Ki67: 19%) well-differentiated NET and up to 30% well-differentiated to moderately differentiated adenocarcinoma of possible pancreato-biliary origin; intrahepatic ductal primary could not be excluded. Her 18-fluoro-deoxyglucose positron emission tomography (FDG-PET) revealed no FDG-avid lesions, and a 68Gallium 1,4,7,10-tetraazacyclododecane-tetraacetic acid Tyr3-octreotate (68 Ga-DOTATATE)-PET scan revealed multiple areas of intensely DOTATATE-avid liver lesions. Due to the absence of any primary imaging findings, the patient was diagnosed with MiNEN of possible pancreato-biliary origin.
RESULTS:
She was started on lanreotide 120 mg every 28 days for 6 months, with no response to the treatment. Subsequently, the patient was treated with four cycles of 177Lutetium-DOTATATE (Lutathera®) peptide receptor radionuclide therapy (PRRT). She tolerated the treatment well, with no significant side effects. MRI at the end of treatment revealed a partial response to treatment.
CONCLUSION:
PRRT is currently not used in treatment protocols for the management of MiNENs; however, it could be considered a treatment option in patients with MiNENs, where there is a predominant component of well-differentiated NETs with 68 Ga-DOTATATE avid lesions.
2025-12-01ACTA PHARMACOLOGICA SINICA
Somatostatin receptor 2 targeting peptide modifications for peptide-drug conjugate treatment of small cell lung cancer
Article
作者: Li, Ze-Lin ; Li, Dong-Sheng ; Tian, Chang-Lin ; Shi, Pan ; Zheng, Yan-Min ; Bo, Qing ; Wu, Fang-Ming ; Lv, Pei ; Yang, Fan ; Zhou, Li ; Wu, Yun ; Zhang, Meng-Ge ; Liang, Jun ; Zheng, Yong
Peptide-drug conjugate (PDC) represents a special therapeutic strategy to enhance drug delivery by targeting tumor cell receptors while minimizing off-target effects. Comparing the antibody-drug conjugate (ADC), the targeting peptide constitutes the pivotal component of PDC, especially with easy optimization of peptides to promote their in vivo stability, and with the agonist stimulated GPCR internalization to facilitate drug distribution into tumor cell plasma. Herein, we have optimized a highly stable peptide molecule LanTC targeting somatostatin receptor 2 (SSTR2), through amino acid substitution and disulfide bond modification from an FDA proved peptide drug Lanreotide. The LanTC based PDC was constructed through conjugation of the cytotoxic drug emtansine (DM1). The LanTC-DM1 PDC exhibited high stability and high agonist affinity to SSTR2. Subsequent in vitro and in vivo pharmacological data revealed that LanTC-DM1 PDC exhibited antitumor activity in small cell lung cancers (SCLC) which was known to have over-expressing SSTR2. The LanTC-DM1 PDC with specific targeting and antitumor activity provides a solid basis not only for advancing SSTR2-targeted PDCs as a promising therapy for SCLC, but also for other PDC developments targeting GPCRs in plasma membrane of tumor cells.
2025-10-31Drug Discoveries and Therapeutics
Paltusotine: The first selective nonpeptide agonist of somatostatin receptor 2 (SSTR2) for the treatment of acromegaly
Review
作者: Sun, Yueyi ; Lu, Daoran ; Gao, Jianjun
Acromegaly is an endocrine disorder characterized by abnormal enlargement of the extremities and internal organs resulting from excessive secretion of growth hormone (GH) by the pituitary gland, which in turn leads to elevated levels of insulin-like growth factor 1 (IGF-1). Approximately 45% of patients remain biochemically uncontrolled after surgery and require long-term treatment with injectable somatostatin analogs such as octreotide or lanreotide. These polypeptide drugs generally require monthly administration to maintain disease control; however, many patients experience recurrence of symptoms towards the end of the dosing interval. Moreover, injection-site pain and local reactions are common, significantly impacting patients' quality of life. On September 25, 2025, the U.S. Food and Drug Administration (FDA) approved paltusotine, the first once-daily oral, nonpeptide somatostatin receptor 2 (SSTR2) agonist for the treatment of acromegaly. By enabling oral rather than injectable therapy, paltusotine reduces the treatment burden and enhances patient adherence. With its rapid onset and durable biochemical control, this novel agent has the potential to reshape the current paradigm of acromegaly pharmacotherapy and offer patients a more convenient and effective treatment option. Nevertheless, its long-term safety and efficacy warrant further evaluation in real-world clinical settings.
100 项与 醋酸兰瑞肽 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 垂体肿瘤 | 日本 | 2021-01-15 | |
| 巨人症 | 日本 | 2013-01-08 | |
| 胃肠胰神经内分泌肿瘤 | 澳大利亚 | 2003-09-11 | |
| 类癌 | 韩国 | 2002-08-08 | |
| 神经内分泌肿瘤 | 韩国 | 2002-08-08 | |
| 肢端肥大症 | 中国 | 2002-03-14 | |
| 恶性类癌综合征 | 中国 | 2002-03-14 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 肺神经内分泌肿瘤 | 临床3期 | 美国 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 奥地利 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 加拿大 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 丹麦 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 法国 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 德国 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 意大利 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 荷兰 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 波兰 | 2017-03-06 | |
| 肺神经内分泌肿瘤 | 临床3期 | 西班牙 | 2017-03-06 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 310 | (Ki67 <10%) | 積鹽膚醖積膚鏇窪鏇觸(糧蓋鹹構顧艱醖艱繭積) = 窪夢鹽鹽窪繭壓獵壓獵 鏇壓獵淵製糧積積網鬱 (網構遞鏇遞糧鏇築鏇膚 ) 更多 | 积极 | 2025-10-17 | ||
(Ki67 ≥10%) | 積鹽膚醖積膚鏇窪鏇觸(糧蓋鹹構顧艱醖艱繭積) = 餘窪糧網廠範艱製遞齋 鏇壓獵淵製糧積積網鬱 (網構遞鏇遞糧鏇築鏇膚 ) 更多 | ||||||
临床1/2期 | 42 | 網憲積糧願齋壓襯構繭(糧壓襯構齋範獵製齋繭) = 選壓膚網蓋艱簾鑰築襯 遞觸遞繭鏇衊艱鹹齋築 (廠膚觸餘壓艱遞壓願築, 11.0 ~ 18.3) 更多 | 积极 | 2025-10-17 | |||
(pancreatic NET (panNET)) | 網憲積糧願齋壓襯構繭(糧壓襯構齋範獵製齋繭) = 淵窪艱蓋廠廠淵鹹積範 遞觸遞繭鏇衊艱鹹齋築 (廠膚觸餘壓艱遞壓願築 ) | ||||||
临床3期 | 178 | 鬱鏇選艱壓廠廠繭齋憲(淵顧醖築艱艱製繭壓膚) = 簾築壓鹹鑰範範網積壓 網蓋壓顧鹽壓製蓋蓋簾 (襯壓顧鹹膚蓋構衊願衊 ) 更多 | 积极 | 2025-10-17 | |||
鬱鏇選艱壓廠廠繭齋憲(淵顧醖築艱艱製繭壓膚) = 鹽糧選襯糧餘鹽遞鹽憲 網蓋壓顧鹽壓製蓋蓋簾 (襯壓顧鹹膚蓋構衊願衊 ) 更多 | |||||||
N/A | 一线 Ki67 proliferation index | 314 | 範積築願觸顧鬱壓鹹繭(憲顧憲遞繭網醖願壓齋) = 壓範鬱簾夢範壓鬱範鏇 顧網窪獵廠繭鹽簾構壓 (範窪衊積醖遞構憲蓋顧 ) | - | 2025-07-03 | ||
临床2期 | 18 | 獵繭繭艱齋繭襯廠範範(顧簾鬱夢獵鹹範鬱願壓) = 繭鬱糧願醖鹽製鬱製鏇 齋築齋淵遞獵鹹網淵顧 (觸襯艱淵衊鬱選膚襯顧 ) 更多 | 积极 | 2025-05-30 | |||
临床4期 | 51 | Octreotide+LAR Lanreotide (Octreotide Then Lanreotide) | 鏇壓範壓遞膚構顧餘獵(膚積衊餘鏇繭憲襯顧餘) = 鏇鹽獵網壓襯蓋獵積餘 網網壓醖鏇衊鏇鑰鹽製 (製壓憲淵膚築夢選構蓋, 襯鏇獵鹹廠鹽窪鹹鏇憲 ~ 顧築鑰築襯膚齋廠鬱艱) 更多 | - | 2025-05-09 | ||
Octreotide+LAR Lanreotide (Lanreotide Then Octreotide) | 願鏇艱製築鑰鹽製網壓(積積鹹顧繭築築繭鏇鑰) = 淵膚鹽廠淵餘鹹膚窪壓 齋壓餘齋積夢醖願鬱窪 (憲獵築簾淵製鬱製網醖, 範繭淵遞醖餘醖鏇鏇夢 ~ 淵憲願觸鏇糧製窪鏇鹽) 更多 | ||||||
N/A | 35 | Somatostatin analogs (long-acting releasing octreotide 30 mg) | 構願淵鬱鹽簾構蓋構構(積鹹繭簾糧廠鏇遞壓艱) = 壓繭鑰製繭鹽顧選製衊 顧憲鬱鬱製願繭糧壓鑰 (獵醖憲鑰構憲餘顧窪憲, 67 ~ NR) | 积极 | 2025-01-23 | ||
構願淵鬱鹽簾構蓋構構(積鹹繭簾糧廠鏇遞壓艱) = 繭膚鹽構網構夢淵鏇鹽 顧憲鬱鬱製願繭糧壓鑰 (獵醖憲鑰構憲餘顧窪憲, 67 ~ NR) | |||||||
临床3期 | 178 | 膚艱獵簾鏇廠廠衊繭襯(願築積鬱繭獵製艱淵顧) = 築齋鏇衊遞選齋鏇餘憲 夢築糧醖淵鹽網鏇鏇觸 (顧鑰夢選糧蓋鹽獵築觸 ) 更多 | 积极 | 2025-01-23 | |||
膚艱獵簾鏇廠廠衊繭襯(願築積鬱繭獵製艱淵顧) = 醖積獵壓觸膚廠壓餘範 夢築糧醖淵鹽網鏇鏇觸 (顧鑰夢選糧蓋鹽獵築觸 ) 更多 | |||||||
临床3期 | 43 | 鑰蓋醖簾壓獵夢憲築蓋 = 蓋鏇網蓋廠醖鹽憲窪壓 蓋齋糧製簾築憲構網糧 (憲糧範憲願築壓觸糧獵, 築築廠憲鑰網觸鹹鏇遞 ~ 製廠範衊憲願顧遞蓋夢) 更多 | - | 2024-10-01 | |||
临床2期 | 类癌 | 胃肠胰神经内分泌肿瘤 | 6 | Y-90 microspheres+Lanreotide | 艱鹹膚構繭範鹽淵選憲 = 壓觸獵齋蓋艱齋衊憲網 襯壓願構簾糧繭膚鹽範 (窪鏇鹹顧獵餘選夢觸顧, 壓製膚壓遞壓廠範選繭 ~ 醖選鹹膚簾獵壓製構鏇) 更多 | - | 2023-07-27 |
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