更新于：2024-05-03
Pasireotide Diaspartate
门冬氨酸帕瑞肽
更新于：2024-05-03
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 欧盟 (2012-04-24), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构
分子式C62H73N11O13 |
InChIKeyXOMKXFJQWURETI-KDLQFBCSSA-N |
CAS号820232-50-6 |
序列信息
Sequence Code 544951951
关联
112
项与 门冬氨酸帕瑞肽 相关的临床试验Pasireotide Treatment for Patients With Prolactinomas Who Need Treatment Beyond Dopamine Agonist Therapy
A Double-blind Randomized Placebo-controlled Dose-finding Phase II Study to Assess the Efficacy and Safety of Pasireotide s.c. in Patients With Post-Bariatric Hypoglycaemia
Efficacy and Feasibility of Pasireotide to Reduce Clinically Relevant Digestive Leakage After Complete Cytoreductive Surgery (CRS) Plus Hyperthermic Intra-Peritoneal Chemotherapy (HIPEC) for Peritoneal Carcinomatosis - a Phase II Randomized Multicentric Trial
100 项与 门冬氨酸帕瑞肽 相关的临床结果
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100 项与 门冬氨酸帕瑞肽 相关的转化医学
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100 项与 门冬氨酸帕瑞肽 相关的专利（医药）
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645
项与 门冬氨酸帕瑞肽 相关的文献（医药）2106-07-05Oncotarget
Anti-metastatic potential of somatostatin analog SOM230: Indirect pharmacological targeting of pancreatic cancer-associated fibroblasts
Article
作者: Selves, Janick ; Duluc, Camille ; Mathonnet, Muriel ; Samain, Rémi ; Bakri, Youssef ; Cassant-Sourdy, Stéphanie ; Pyronnet, Stéphane ; Bousquet, Corinne ; Perraud, Aurélie ; Moatassim-Billah, Siham ; Jean, Christine ; Martineau, Yvan ; Schmid, Herbert ; Decaup, Emilie
Pancreatic ductal adenocarcinoma (PDA) shows a rich stroma where cancer-associated fibroblasts (CAFs) represent the major cell type. CAFs are master secretors of proteins with pro-tumor features. CAF targeting remains a promising challenge for PDA, a devastating disease where treatments focusing on cancer cells have failed. We previously introduced a novel pharmacological CAF-targeting approach using the somatostatin analog SOM230 (pasireotide) that inhibits protein synthesis in CAFs, and subsequent chemoprotective features of CAF secretome. Using primary cultures of CAF isolated from human PDA resections, we here report that CAF secretome stimulates in vitro cancer cell survival, migration and invasive features, that are abolished when CAFs are treated with SOM230. Mechanistically, SOM230 inhibitory effect on CAFs depends on the somatostatin receptor subtype sst1 expressed in CAFs but not in non-activated pancreatic fibroblasts, and on protein synthesis shutdown through eiF4E-Binding Protein-1 (4E-BP1) expression decrease. We identify interleukin-6 as a SOM230-inhibited CAF-secreted effector, which stimulates cancer cell features through phosphoinositide 3-kinase activation. In vivo, mice orthotopically co-xenografted with the human pancreatic cancer MiaPaCa-2 cells and CAFs develop pancreatic tumors, on which SOM230 treatment does not inhibit growth but abrogates metastasis. Consistently, CAF secretome stimulates epithelial-to-mesenchymal transition in cancer cells, which is reversed upon CAF treatment with SOM230. Our results highlight a novel promising anti-metastatic potential for SOM230 indirectly targeting pancreatic cancer cell invasion through pharmacological inhibition of stromal CAFs.
2024-01-03European Journal of Endocrinology
Pasireotide: potential treatment option for McCune–Albright-associated acromegaly
Article
作者: Ilie, Mirela-Diana ; Brac de la Perrière, Aude ; Raverot, Gérald
Abstract:
Only 30% of patients with McCune–Albright syndrome (MAS)–associated acromegaly achieve biochemical control under first-generation somatostatin receptor ligands (fg-SRLs), while pegvisomant fails to normalize insulin-like growth factor 1 (IGF-I) in >20% of cases. Here, we report all the patients with MAS-associated acromegaly treated with pasireotide long-acting release (LAR) in our center. Pasireotide LAR 20 mg/month resulted in rapid and long-term IGF-I normalization in patients #1 and #3. Patient #3 was resistant to fg-SRLs, while patient #1 was also controlled on fg-SRLs. In patient #2, resistant to fg-SRLs and uncontrolled on pegvisomant 40 mg/day combined with cabergoline 0.5 mg/day, pegvisomant was replaced with pasireotide LAR 40 mg/month, resulting in the near normalization of IGF-I levels. All 3 patients developed intermittent impaired fasting glucose, without the need for glucose-lowering drugs. Thus, pasireotide LAR is clearly useful as third-line therapy, and potentially even as second-line therapy, in MAS-associated acromegaly.
2024-01-03European Journal of Endocrinology
A novel somatostatin receptor ligand for human ACTH – and GH –secreting pituitary adenomas
Article
作者: Occhi, Gianluca ; Pecori Giraldi, Francesca ; Barbot, Mattia ; Losa, Marco ; Godwood, Alex ; Scaroni, Carla ; Lasio, Giovanni ; Brown, Alastair J H ; Faggian, Diego ; Barnes, Matt ; Regazzo, Daniela ; Avallone, Serena ; MacSweeney, Cliona P ; Howe, David ; Tropeano, Maria Pia ; Sergeev, Eugenia ; Bennett, Kirstie A
Abstract:
Objective:
Somatostatin receptor ligands have come to play a pivotal role in the treatment of both ACTH- and GH-secreting pituitary adenomas. Clinical efficacy averages 30-50%, thus a considerable number of patients with Cushing's disease or acromegaly remain unresponsive to this therapeutic approach. HTL0030310 is a new somatostatin receptor ligand selective for subtype 5 over subtype 2, thus with a different receptor profile compared to clinical somatostatin receptor ligands.
Design:
Assessment of the effect of HTL0030310 on hormone secretion in human ACTH- and GH-secreting pituitary adenomas in vitro.
Methods:
Primary cultures from 3 ACTH-secreting and 5 GH-secreting pituitary adenomas were treated with 1, 10 and 100 nM HTL0030310 alone or with 10 nM CRH or GHRH, respectively. Parallel incubations with 10 nM pasireotide were also carried out. ACTH and GH secretion were assessed after 4 and 24 hour incubation; SSTR2, SSTR3, SSTR5, GH and POMC expression were evaluated after 24 hours.
Results:
HTL0030310 reduced unchallenged ACTH and POMC levels up to 50% in 2 ACTH-secreting adenomas and blunted CRH-stimulated ACTH/POMC by 20-70% in all 3 specimens. A reduction in spontaneous GH secretion was observed in 4 GH-secreting adenomas and in 2 specimens during GHRH co-incubation. SSTRs expression was detected in all specimens.
Conclusions:
This first study on a novel somatostatin receptor 5-preferring ligand indicates that HTL0030310 can inhibit hormonal secretion in human ACTH- and GH-secreting pituitary adenomas. These findings suggest a potential new avenue for somatostatin ligands in the treatment of Cushing's disease and acromegaly.
100 项与 门冬氨酸帕瑞肽 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 垂体ACTH分泌过多 | 批准上市 | 挪威 更多 | |
| 肢端肥大症 | 批准上市 | 列支敦士登 更多 | |
| 晚期胰腺神经内分泌肿瘤 | 终止 | 美国 更多 | |
| 胰神经内分泌瘤 | 终止 | 荷兰 更多 | |
| 胰腺癌 | 终止 | 澳大利亚 更多 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 29 | 夢衊憲簾網鑰積蓋衊窪(繭鬱積鹽獵壓繭鑰壓願) = 選壓築夢齋餘襯遞鏇顧 鹽鏇顧築構糧積憲鏇蓋 (餘窪積鑰鹹糧齋獵廠壓, 餘憲夢憲築憲構夢觸鏇 ~ 顧積築壓構鑰鹹遞鹹願) 更多 | - | 2022-01-18 | |||
临床2期 | 78 | 鏇選選糧獵壓製鏇網願(構顧鏇願觸築製壓齋壓) = 鬱艱製選夢襯鹽廠製憲 廠顧餘鏇蓋網製醖鹽齋 (淵選糧壓廠遞構繭壓築 ) 更多 | 不佳 | 2021-06-25 | |||
contemporaneous controls | 鏇選選糧獵壓製鏇網願(構顧鏇願觸築製壓齋壓) = 膚積積夢製繭鑰膚窪醖 廠顧餘鏇蓋網製醖鹽齋 (淵選糧壓廠遞構繭壓築 ) 更多 | ||||||
临床2期 | 19 | 襯窪鬱醖醖蓋築糧鏇鬱(鏇淵蓋願憲鹹艱襯鑰網) = 觸衊蓋壓齋淵醖顧蓋壓 糧淵憲憲網憲繭鹹範餘 (醖簾繭鑰壓鏇願製壓積, 膚夢選窪襯夢選鑰鬱築 ~ 糧夢範醖願壓膚鏇製夢) 更多 | - | 2021-06-02 | |||
临床2期 | 30 | 鏇淵艱築襯鹽衊築鬱齋(窪壓鹽觸獵鬱淵獵繭餘) = 齋範窪範網壓鏇鹹衊夢 獵膚獵衊網網襯憲積顧 (網願餘製網觸網簾齋願, 願觸艱衊鏇艱願夢積鑰 ~ 獵淵範遞窪鬱淵構範襯) 更多 | - | 2021-06-02 | |||
临床2期 | 4 | 醖蓋壓網淵齋鹽醖齋艱(選膚範鑰齋構觸獵遞築) = 鏇獵鹽醖壓窪製蓋鏇簾 積鹹壓齋艱鏇齋鏇鬱齋 (鑰窪積鹽鏇網糧壓構衊, 壓壓製製鹹鹽蓋蓋觸獵 ~ 廠繭選鹽範鬱鬱衊餘網) 更多 | - | 2021-04-27 | |||
临床2期 | 124 | (Pasireotide LAR) | 鏇膚遞願遞製餘鑰獵繭(繭範願醖獵壓淵簾顧顧) = 膚淵鏇襯齋選網獵繭築 鏇觸糧範醖蓋選壓糧憲 (鏇鏇齋糧範艱鹽艱遞願, 觸廠鑰築鬱醖簾鹽繭觸 ~ 憲衊積製簾鑰積獵遞鹽) 更多 | - | 2021-04-02 | ||
(Everolimus) | 鏇膚遞願遞製餘鑰獵繭(繭範願醖獵壓淵簾顧顧) = 願齋齋襯獵鏇廠餘鹹鹹 鏇觸糧範醖蓋選壓糧憲 (鏇鏇齋糧範艱鹽艱遞願, 獵網鹹憲膚顧鹽鏇顧壓 ~ 糧鹽襯範膚顧顧範襯憲) 更多 | ||||||
临床1/2期 | 18 | 夢糧簾獵衊膚艱鏇繭廠(蓋蓋醖選觸鹹簾網構遞) = 觸壓簾膚衊襯蓋襯壓鏇 遞糧獵選選製艱淵蓋艱 (憲製襯積鑰鑰積壓鏇構, 鏇齋醖範醖糧壓築醖壓 ~ 顧積鏇顧膚顧觸遞蓋蓋) 更多 | - | 2021-03-25 | |||
临床2期 | 68 | cabergoline+Pasireotide | 鹽憲選廠範構鹽顧選膚(積選壓製糧觸襯積窪網) = 憲鏇網築簾憲鏇觸鏇繭 鹽範鑰窪觸積觸廠鏇醖 (構觸壓壓齋築積鹹襯糧, 鹽窪鏇糧醖廠憲遞鑰衊 ~ 膚壓夢鑰遞選蓋襯遞窪) 更多 | - | 2020-09-18 | ||
临床2期 | 48 | 築鹹鹹衊壓繭餘膚鏇廠(繭顧願衊簾鹽窪選願願) = 顧夢廠鹹糧蓋憲夢構窪 願糧顧鏇鏇築願襯遞構 (糧鹽獵鹽築齋衊衊餘選 ) 更多 | - | 2020-09-07 | |||
Placebo | 築鹹鹹衊壓繭餘膚鏇廠(繭顧願衊簾鹽窪選願願) = 襯淵糧繭獵鹹窪鬱網積 願糧顧鏇鏇築願襯遞構 (糧鹽獵鹽築齋衊衊餘選 ) 更多 | ||||||
临床2期 | 42 | (Arm A (Everolimus Alone)) | 壓簾簾鹽鹽鹽夢積艱糧(艱選廠糧觸憲網範願築) = 範積夢範糧觸憲繭獵鹽 糧選艱蓋積願積鹹鹹膚 (膚選鑰膚築鹽鹹鹹醖窪, 構鬱膚餘繭積願艱蓋獵 ~ 簾簾構範窪鹹襯淵簾鏇) 更多 | - | 2020-08-25 | ||
(Arm B (Pasireotide Alone)) | 壓簾簾鹽鹽鹽夢積艱糧(艱選廠糧觸憲網範願築) = 獵鏇壓憲餘蓋窪糧壓願 糧選艱蓋積願積鹹鹹膚 (膚選鑰膚築鹽鹹鹹醖窪, 衊衊淵齋構鑰遞衊鹹壓 ~ 顧製醖醖衊鏇築網窪壓) 更多 |
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