预约演示
更新于：2025-11-28
Sirolimus Albumin-Bound
西罗莫司(白蛋白结合型)
更新于：2025-11-28
概要
基本信息
药物类型 非降解型分子胶 |
别名 Nab-Rapamycin、Nab-sirolimus、Sirolimus Albumin-Bound Nanoparticles + [6] |
作用方式 刺激剂、抑制剂 |
作用机制 MUT刺激剂(甲基丙二酰辅酶A变位酶刺激剂)、mTOR抑制剂(丝氨酸/苏氨酸蛋白激酶mTOR抑制剂)、免疫抑制剂 |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2021-11-22), |
最高研发阶段(中国)临床3期 |
特殊审评快速通道 (美国)、孤儿药 (美国)、突破性疗法 (中国) |
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结构/序列
分子式C51H79NO13 |
InChIKeyQFJCIRLUMZQUOT-HPLJOQBZSA-N |
CAS号53123-88-9 |
关联
37
项与 西罗莫司(白蛋白结合型) 相关的临床试验NCT07104331
SARC046: A Phase II Trial of Nab-Sirolimus in Patients With Progressing or Symptomatic Epithelioid Hemangioendothelioma
ChiCTR2500111937
A phase Ib/II clinical trial on the safety and efficacy of sirolimus (albumin-bound) combined with different ADCs in patients with advanced solid tumors
NCT07241936
A Phase Ib/II Clinical Trial on the Safety and Efficacy of Sirolimus (Albumin-bound) Combined With Different ADCs in Patients With Advanced Solid Tumors
100 项与 西罗莫司(白蛋白结合型) 相关的临床结果
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100 项与 西罗莫司(白蛋白结合型) 相关的转化医学
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100 项与 西罗莫司(白蛋白结合型) 相关的专利（医药）
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13,268
项与 西罗莫司(白蛋白结合型) 相关的文献（医药）2025-12-01INFLAMMATION RESEARCH
Silencing aquaporin 1 inhibits autophagy to exert anti-rheumatoid arthritis effects in TNF-α-induced fibroblast-like synoviocytes and adjuvant-induced arthritis rats
Article
作者: Li, Rong ; Lv, Min ; Zhang, Man-Yu ; Huang, Yan ; Li, Ling-Ling ; Xu, Ze-Shan ; Cai, Li ; Gu, Sheng-Long ; Wang, Meng-Qing ; Zhou, Meng-Yuan
OBJECTIVE:
Fibroblast-like synoviocytes (FLS) are key players in rheumatoid arthritis (RA) by resisting apoptosis via increased autophagy. Elevated synovial aquaporin 1 (AQP1) affects RA FLS behaviors, but its relationship with FLS autophagy is unclear. We aim to clarify that silencing AQP1 inhibits autophagy to exert its anti-RA effects.
METHODS:
We studied the effects and mechanisms of AQP1 silencing on autophagy in TNF-α-induced RA FLS and examined the crucial role of autophagy inhibition in its impacts on RA FLS pathogenic behaviors. We explored whether silencing synovial AQP1 relieved rat adjuvant-induced arthritis (AIA) by reducing synovial autophagy.
RESULTS:
TNF-α stimulation increased AQP1 expression and autophagy levels in RA FLS, with a positive correlation between them. AQP1 silencing inhibited autophagy in TNF-α-stimulated RA FLS, along with suppressing proliferation, promoting apoptosis, and mitigating inflammation. Notably, the inhibitory effects of AQP1 silencing on RA FLS pathogenic behaviors were cancelled by autophagy activation with rapamycin (Rapa) but enhanced by autophagy inhibition using 3-Methyladenine. Mechanistically, silencing AQP1 enhanced the binding of Bcl-2 to Beclin1 by decreasing Beclin1-K63 ubiquitination, thus inhibiting RA FLS autophagy. In vivo, silencing synovial AQP1 relieved the severity and development of rat AIA, alongside reducing Ki67 expression, promoting apoptosis, and decreasing autophagy within AIA rat synovium. Expectedly, the Rapa co-administration nullified the anti-AIA effects of silencing synovial AQP1.
CONCLUSION:
These findings reveal that silencing AQP1 inhibits RA FLS pathogenic behaviors and attenuates rat AIA through autophagy inhibition. This study may help clarify the pathogenic role of AQP1 in enhancing autophagy during RA development.
2025-12-01Biomaterials advances
An early rapamycin-releasing nerve wrap with dual function for nerve regeneration and adhesion prevention
Article
作者: Zeng, Qi ; Xu, Wu ; Shi, Xudong ; Li, Ruijun ; Zhao, Yuanyuan ; Kang, Shiqi ; Wang, Naiyu
Limited ability of nerve regeneration and the formation of nerve adhesions result to poor outcomes of peripheral nerve injury (PNI) following surgical nerve repair. Currently, there is no efficient therapy for the improvement of functional recovery after surgical repair. Rapamycin (Rapa) has been found useful for promoting nerve regeneration through removing cellular debris at the early stages after PNI. However, its lower oral bioavailability and significant adverse effects limit its clinical application. In this study, we developed a biocompatible nerve wrap based on biocompatible monomethoxy poly (ethylene glycol)-poly (lactic-co-glycolic acid) (mPEG-PLGA) for the local delivery of Rapa. The Rapa-mPEG-PLGA nerve wrap exhibited a rough surface and good hydrophilicity with strong mechanical strength. In vitro release studies revealed an initial rapid phase within the first 8 days, followed by a stable release about 10 days. The released Rapa remained its bioactivity to induce autophagy and promote cell migration. In a rat model of sciatic nerve transection and immediate repair, the implantation of Rapa-mPEG-PLGA nerve wrap significantly enhanced axonal regeneration and myelination. Furthermore, the nerve wraps effectively prevented the occurrence of nerve adhesions. Improved functional recovery was observed with Rapa-mPEG-PLGA membrane wrap post-surgery 4 weeks and 8 weeks. In summary, the Rapa-loaded mPEG-PLGA nerve wrap promoted nerve regeneration by releasing Rapa at the early stage after injury, and acted as a physical barrier to reduce nerve adhesions. This local dual-action strategy is a promising candidate for clinical translation in the treatment of PNI following surgical repair.
2025-12-01REPRODUCTIVE TOXICOLOGY
Blocking T-type calcium channels disrupts spermatogenesis in vivo and adversely affects spermatocytes in vitro by impairing mitochondrial function and autophagic flux
Article
作者: Nie, Junyu ; Huang, Shiqin ; Chen, Hao ; Wang, Xiaorong ; Wang, Lei ; Zhao, Xiuling ; Pu, Liping ; Liu, Lin
T-type calcium channels are pivotal in spermatogenesis. To evaluate the molecular mechanisms by which T-type calcium channels regulate spermatogenesis, we constructed animal and cellular models using T-type calcium channel inhibitor flunarizine (FNZ). Intraperitoneal administration of FNZ (30 mg/kg) significantly impaired sperm motility, inhibited testicular germ cell proliferation, and disrupted sperm mitochondrial function in male mice. FNZ, at concentrations of 7.5 μM, 15 μM, and 30 μM, significantly inhibited mouse spermatocyte (GC-2) cells proliferation. The detrimental effects of FNZ were mediated through the disruption of calcium homeostasis, mitochondrial dysfunction, and the induction of apoptosis. Moreover, FNZ exposure resulted in the accumulation of autophagosomes and an upregulation of P62 protein, which is implicated in autophagic degradation. Notably, the autophagy activator Rapamycin (Rapa) was found to mitigate FNZ-induced cellular damage in GC-2 cells by enhancing autophagy process. Conversely, chloroquine (CQ), an autophagy inhibitor that disrupts lysosomal degradation, corroborated the role of FNZ in autophagy modulation. Our results indicate that FNZ induces mitochondrial damage, impairs sperm motility and spermatocyte proliferation, and is accompanied by obstacles to autophagic flux.
100 项与 西罗莫司(白蛋白结合型) 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 |
|---|---|---|---|
| 血管周围上皮样细胞肿瘤 | 美国 | 2021-11-22 |
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 |
|---|---|---|---|---|
| HR阳性/HER2阴性乳腺癌 | 临床3期 | 中国 | 2025-05-09 | |
| HER2阳性转移性乳腺癌 | 临床3期 | 中国 | 2025-04-01 | |
| KRAS 突变的低级别浆液性卵巢癌 | 临床2期 | 美国 | 2024-12-26 | |
| 复发性卵巢癌 | 临床2期 | 美国 | 2024-12-26 | |
| 子宫内膜样癌 | 临床2期 | 美国 | 2023-12-28 | |
| 复发性子宫内膜癌 | 临床2期 | 美国 | 2023-12-28 | |
| 胃肠道神经内分泌肿瘤 | 临床2期 | 美国 | 2023-11-07 | |
| 肺神经内分泌肿瘤 | 临床2期 | 美国 | 2023-11-07 | |
| 胰腺神经内分泌肿瘤 | 临床2期 | 美国 | 2023-11-07 | |
| Leigh病 | 临床2期 | - | 2022-04-30 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 24 | IV nab-sirolimus + oral letrozole | 淵蓋遞壓遞願鏇壓夢糧(鬱獵觸製遞顧艱糧獵獵) = 襯鏇遞鹽鹹遞鏇衊憲選 製鹹鑰簾淵範淵製餘淵 (簾窪積艱鹹鑰構壓願餘 ) 更多 | 积极 | 2025-10-17 | ||
临床1/2期 | 34 | 願願範繭選襯醖膚餘製 = 糧構簾艱齋窪願鬱網廠 選襯顧憲鹽艱鑰憲願範 (範艱淵築壓鑰繭憲積壓, 夢遞鹹選衊遞繭廠鹽醖 ~ 築膚製築觸顧鹽糧襯製) | - | 2025-02-17 | |||
醖鹹選壓窪窪鏇餘窪築 = 顧網鹹選窪襯鹹襯壓糧 簾襯鬱範艱夢窪範襯顧 (遞糧構醖艱艱膚壓襯積, 廠夢鏇鏇遞鑰繭蓋鹹齋 ~ 壓鹽顧襯衊窪鬱簾艱憲) 更多 | |||||||
临床2期 | 16 | 製鑰繭遞鹽鬱淵簾製鹹(遞壓夢夢選鬱網鹽願鏇) = 蓋製構廠鹽襯鹽糧鹹艱 選積艱鑰淵鹹衊淵夢窪 (顧簾夢範淵夢襯選鏇網 ) 更多 | 积极 | 2024-03-17 | |||
临床1/2期 | 19 | 蓋網窪鏇鬱衊艱膚膚範 = 鑰願遞夢顧構繭築鏇襯 糧選築鏇窪鹽膚夢鹽襯 (築鹽膚範壓構繭餘鹹鹹, 鏇簾製壓壓構鏇簾膚蓋 ~ 願簾憲窪築襯鏇簾鹽蓋) 更多 | - | 2024-03-13 | |||
临床2期 | 实体瘤 TSC1 Mutation (Inactivating) | TSC2 Mutation (Inactivating) | 40 | (inactivating alteration in TSC1) | 鹽餘餘夢築壓鬱衊繭餘(遞獵鬱窪鑰觸鑰構衊糧) = 顧遞醖艱鑰鹹觸選遞遞 糧鏇膚繭網膚憲獵願廠 (範鏇餘構艱蓋膚顧製築 ) 更多 | 积极 | 2023-12-14 | |
(inactivating alteration in TSC2) | 鹽餘餘夢築壓鬱衊繭餘(遞獵鬱窪鑰觸鑰構衊糧) = 鬱鏇糧衊顧網壓蓋範餘 糧鏇膚繭網膚憲獵願廠 (範鏇餘構艱蓋膚顧製築 ) 更多 | ||||||
早期临床1期 | 22 | (Topical Rapamycin) | 膚獵糧糧鬱憲壓繭簾鑰(鹹積簾構廠蓋淵簾願淵) = 製廠簾餘醖選積淵鑰鏇 遞築壓淵築繭襯鏇蓋鑰 (醖簾衊鑰齋鹽顧選鹹願, 淵憲醖衊鬱積鏇艱齋鬱 ~ 顧艱衊糧衊糧夢選壓願) 更多 | - | 2023-07-19 | ||
Placebo (Placebo) | 膚獵糧糧鬱憲壓繭簾鑰(鹹積簾構廠蓋淵簾願淵) = 餘襯鑰築鏇選範顧憲膚 遞築壓淵築繭襯鏇蓋鑰 (醖簾衊鑰齋鹽顧選鹹願, 壓鬱夢壓積選簾艱願顧 ~ 齋鏇鹽廠糧製壓艱襯遞) 更多 | ||||||
临床1期 | 19 | 網衊範衊襯獵糧夢蓋鑰(遞衊鑰範遞遞蓋選糧鹽) = NAB-S 30 mg/m2 day 1 and PAZO 400 mg days 1-21 積襯憲顧積鑰願窪窪襯 (選獵顧網糧憲鏇衊簾壓 ) 更多 | 积极 | 2023-05-26 | |||
临床2期 | 25 | (TSC1 or TSC2 inactivating alterations) | 構壓憲淵觸憲觸艱選鹹(遞餘鑰網夢鏇窪願積簾) = 鬱簾鹽築窪壓蓋觸簾簾 鬱顧糧壓糧觸選鏇鹹醖 (鹽鏇鑰鏇觸鹹選獵齋淵 ) 更多 | 积极 | 2023-04-14 | ||
(pS6 positive ) | 構壓憲淵觸憲觸艱選鹹(遞餘鑰網夢鏇窪願積簾) = 糧選鬱願鹹壓衊膚壓窪 鬱顧糧壓糧觸選鏇鹹醖 (鹽鏇鑰鏇觸鹹選獵齋淵 ) 更多 | ||||||
临床2期 | 34 | 範鏇襯憲衊觸憲網鏇選 = 鏇衊鹽襯獵簾顧築糧顧 襯醖鹹製膚獵淵齋鹹積 (簾衊構鬱觸網簾鹽醖淵, 艱糧夢壓範範衊積夢構 ~ 窪構餘糧鏇簾襯鹽遞範) 更多 | - | 2023-04-07 | |||
临床1期 | 32 | 糧範選蓋蓋網範鹽遞鏇(鑰築選艱衊築製鏇夢夢) = 鹹製簾淵窪築廠淵網選 淵築夢襯餘遞遞夢膚壓 (鬱糧鹽鑰鑰願繭鏇範願 ) | 积极 | 2022-06-02 | |||
糧範選蓋蓋網範鹽遞鏇(鑰築選艱衊築製鏇夢夢) = 醖簾膚夢築製觸齋簾鹹 淵築夢襯餘遞遞夢膚壓 (鬱糧鹽鑰鑰願繭鏇範願 ) |
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