预约演示
更新于：2026-11-03
Certepetide
更新于：2026-11-03
概要
基本信息
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)临床2期 |
特殊审评快速通道 (美国)、孤儿药 (美国)、罕见儿科疾病 (美国)、孤儿药 (欧盟) |
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结构/序列
分子式C37H60N14O14S2 |
InChIKeyYPHPUVJQSYACEN-HUVRVWIJSA-N |
CAS号2580154-02-3 |
Sequence Code 79056
来源: *****
关联
9
项与 Certepetide 相关的临床试验NCT06592664
A Phase 1b/2a, Double-blind, Placebo-controlled, Three Arm, Randomized Study Evaluating a Single Intravenous Push Followed by a Continuous Infusion of Certepetide Over 4 Hours When Added to Standard of Care (SoC) Versus Two Intravenous Pushes of Certepetide When Added to SoC, Versus SoC Alone in Subjects With Previously Untreated Metastatic Pancreatic Ductal Adenocarcinoma (FORTIFIDE)
NCT06261359
A Phase II, Randomized, Double-blind, Multi-center, Placebo-Controlled Study of the Efficacy and Safety of CEND-1 in Combination With Chemotherapy as First-Line Therapy in Patients With Locally Advanced Unresectable or Metastatic Pancreatic Ductal Adenocarcinoma
CTIS2023-506813-23-00
A Phase 2, double-blind, placebo-controlled, randomized, proof-of-concept study evaluating LSTA1 when added to standard of care (temozolomide) versus temozolomide and matching LSTA1 placebo in subjects with newly diagnosed Glioblastoma Multiforme (GBM)
100 项与 Certepetide 相关的临床结果
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100 项与 Certepetide 相关的转化医学
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100 项与 Certepetide 相关的专利（医药）
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108
项与 Certepetide 相关的文献（医药）2026-11-01JOURNAL OF CONTROLLED RELEASE
Tumor-homing peptides in precision oncology
Review
作者: Ma, Guojun ; Derkaoui, Dalia Kheira ; Karoyan, Philippe ; Poyet, Jean-Luc ; Senhadji, Rachid
Mechanisms of systemic administration of cytotoxic and immunomodulatory agents are hindered due to poor intratumoral retention and off-target toxicities. While Antibody-Drug Conjugates (ADCs) have achieved substantial clinical success and validated the paradigm of targeted therapy, their large size (∼150 kDa) limits their ability to cross blood vessels and interstitial spaces, especially in the dense, collagen-rich stroma of aggressive solid tumors. As a smaller alternative for drug delivery, Tumor-Homing Peptides (THPs) allow for improved tissue permeability, low immunogenicity and rapid systemic clearance. Here, we examine THPs discovery and development trajectory, from phage display strategies to current deep learning-driven design methodologies. We analyze the structural and functional biology of the predominant internalization pathways like the Neuropilin-1 (NRP-1) dependent C-end Rule (CendR) and the Sortilin (SORT1) scavenger receptor, and their use to promote deep tissue penetration. Finally, we assess the translational landscape of early 2026, including the recent FDA withdrawal of the lipophilic peptide-conjugated melphalan flufenamide (Pepaxto®) and the recent clinical success of the cyclic peptide certepetide for pancreatic adenocarcinoma and the ongoing promising studies with chemically constrained bicyclic peptides.
2026-09-01In Vitro Cellular and Developmental Biology - Animal
Liposome-iRGD loaded with astragaloside IV alleviates the functional damage of endothelial progenitor cells via the Hippo-YAP/TAZ signaling pathway
Article
作者: Zhang, Zihao ; Li, Wei ; Xiong, Wu ; Bin, Jie ; Xue, Bingqian ; Guo, Dongwei ; Hu, Ruowei ; Wang, Xiuping ; Zhang, Xi ; Zeng, Churuo ; Zou, Xiaoling ; Li, Qinxia
The characteristics of diabetic vascular complications are impaired angiogenesis, which leads to hindlimb ischemia. Although astragaloside IV (AS-IV) can promote angiogenesis, its poor targeting to endothelial progenitor cells (EPCs) limits its therapeutic effect. Here, we developed liposomes modified with iRGD to load AS-IV (Lp-iRGD@AS-IV) to enhance its delivery and explored its mechanism. Lp-iRGD@AS-IV and fluorescently labeled liposomes were prepared, and their phenotypic characteristics were detected. The study results showed that the uptake efficiency of Lp-iRGD@AS-IV by EPCs was higher than that of Lp@AS-IV. In a diabetic mouse hindlimb ischemia model induced by streptozotocin, Lp@AS-IV and Lp-iRGD@AS-IV improved cell damage, increased capillary density, and reduced reactive oxygen species accumulation. However, the therapeutic effect of Lp-iRGD@AS-IV was more significant than that of Lp@AS-IV. Lp-iRGD@AS-IV attenuated high glucose-induced inhibitory effect on cell viability, migration, and invasion capability of EPCs. Additionally, we analyzed the regulatory effects of the Hippo-YAP/TAZ signaling pathway in diabetic vascular complications. AS-IV increased the expression of vascular growth factors (VEGFa, VEGFb, VEGFc, FGF, and Ang-1), eNOS, and osteopontin, and enhanced glucose-lipid metabolism, via activating the upstream Hippo signaling pathway while inactivating the downstream YAP/TAZ activity. In conclusion, Lp-iRGD@AS-IV significantly enhanced the delivery of AS-IV to EPCs and improved hindlimb ischemia in diabetic mice. AS-IV can restore diabetes-associated impaired angiogenesis through the Hippo-YAP/TAZ pathway. Lp-iRGD@AS-IV may be a targeted therapy for diabetic vascular complications.
2026-09-01EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
iRGD-modified peptide–drug conjugate improves brain delivery and antitumor efficacy in glioblastoma
Article
作者: Liu, Juan ; Zhai, Qiaoli ; Zhao, Siyuan ; Mu, Lizhen ; Shi, Kourong ; Li, Cuiping ; Fan, Wei ; Wu, Xin ; Yun, Danyang ; Sun, Huan
Glioblastoma (GBM) remains the most aggressive primary brain tumor, with poor prognosis largely due to limited drug delivery across the blood-brain barrier (BBB) and insufficient intratumoral penetration. To address these challenges, we developed a tumor-targeting peptide-drug conjugate (PDC), iRGD-DTX, by covalently linking docetaxel (DTX) to the tumor-penetrating peptide iRGD through a succinic acid linker. The resulting conjugate was successfully synthesized with high purity (98.72%) and exhibited favorable physicochemical and metabolic stability. The iRGD ligand enables a multistep transport process involving integrin binding, proteolytic activation, and subsequent interaction with neuropilin-1 (NRP-1), thereby facilitating BBB penetration and tumor infiltration. Compared with free DTX, iRGD-DTX showed a 2.04-fold increase in cellular uptake and a 5.25-fold enhancement in BBB transport across an in vitro BBB model. These improvements translated into enhanced antiproliferative activity against U251 glioma cells, reducing the IC₅₀ from 176.6 to 84.0 nM after 48 h treatment. In orthotopic glioma-bearing mice, iRGD-DTX significantly increased brain accumulation, achieving a 4.09-fold higher brain Cmax and a 5.08-fold higher drug-targeting index than free DTX. Enhanced brain delivery resulted in superior tumor growth inhibition while maintaining favorable tolerability. Notably, the maximum tolerated dose increased from 15 mg/kg for free DTX to 40 mg/kg for iRGD-DTX. Overall, this study demonstrates that iRGD-mediated peptide-drug conjugation effectively improves BBB penetration, brain targeting, and antitumor efficacy of DTX, highlighting a promising strategy for the development of targeted therapeutics against GBM.
244
项与 Certepetide 相关的新闻（医药）2026-10-29
100 项与 Certepetide 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| 转移性胰腺癌 | 临床2期 | - | 2030-01-01 | |
| 胰腺腺瘤 | 临床2期 | - | 2030-01-01 | |
| 不能切除性胰腺癌 | 临床2期 | - | 2030-01-01 | |
| 阑尾肿瘤 | 临床2期 | 美国 | 2024-06-13 | |
| 结肠癌 | 临床2期 | 美国 | 2024-06-13 | |
| 胰腺癌 | 临床2期 | 美国 | 2024-06-13 | |
| 多形性胶质母细胞瘤 | 临床2期 | 爱沙尼亚 | 2024-01-17 | |
| 转移性胰腺导管腺癌 | 临床2期 | 中国 | 2021-10-21 | |
| 转移性胰腺导管腺癌 | 临床2期 | 中国 | 2021-10-21 | |
| 结直肠癌 | 临床2期 | 美国 | 2021-10-20 |
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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 | 66 | (LSTA1 Arm for Untreated Cholangiocarcinoma) | 壓鏇廠選網齋蓋範蓋遞 = 繭鑰鹽選廠鬱膚製鹽鹽 窪衊鬱窪艱遞鏇顧糧鬱 (遞鹽艱鹹顧夢獵憲築願, 窪範鹽淵鹹憲鏇顧鏇範 ~ 製觸齋糧製鬱餘網積選) 更多 | - | 2026-05-26 | ||
FOLFOX regimen+certepetide (LSTA1 Arm for Second-Line Cholangiocarcinoma) | 壓鏇廠選網齋蓋範蓋遞 = 糧膚夢鬱齋齋蓋繭構積 窪衊鬱窪艱遞鏇顧糧鬱 (遞鹽艱鹹顧夢獵憲築願, 鏇積廠選醖壓鏇繭窪廠 ~ 獵衊襯鏇夢窪膚願餘醖) 更多 | ||||||
临床1/2期 | 胰腺导管腺癌 新辅助 | 35 | Certepetide + mFOLFIRINOX | 衊鹹艱鬱憲顧糧鏇醖醖(窪糧繭壓衊網範觸艱製) = 餘齋鹽遞衊壓廠鏇遞衊 鬱鹹齋壓網鹽鹽醖網蓋 (齋窪窪膚遞鏇鬱選鹹網 ) 更多 | 积极 | 2025-09-29 | |
临床1/2期 | 晚期胰腺导管腺癌 一线 | 30 | GemcitabineGemcitabine + nab-paclitaxel + LSTA-1 + Durvalumab OR gemcitabine + nab-paclitaxel+placebo LSTA-1+ placebo durvalumab OR gemcitabinedurvalumab OR gemcitabine+ nab-paclitaxel+ activeo LSTA-1+placebo LSTA-1LSTA-1+ placebo durvalumab | 獵簾窪獵膚壓簾鑰遞鹹(網糧艱顧製選顧齋積顧) = 繭鹹餘淵廠鹽獵願膚鏇 襯壓製憲淵廠夢築鹹艱 (遞鹹積構鏇廠鹹糧蓋築 ) 更多 | 积极 | 2025-07-03 | |
(Cohort 2) | 鑰願醖鏇製膚繭觸繭鏇(簾衊繭鏇窪廠鑰選鏇夢) = 鑰積衊積繭簾膚範衊簾 醖獵鬱鬱網襯膚鏇壓繭 (襯遞願襯顧淵廠夢糧膚 ) | ||||||
临床2期 | 63 | 衊製鏇網衊蓋夢繭憲壓(艱獵淵壓鬱壓願鏇遞憲) = 選鹹膚齋鑰積淵醖鏇觸 鏇壓築鹹襯齋選廠簾範 (鹹淵網願觸鏇淵觸築鑰 ) 更多 | 积极 | 2025-07-02 | |||
Placebo (PLA) | 衊製鏇網衊蓋夢繭憲壓(艱獵淵壓鬱壓願鏇遞憲) = 鑰壓醖積遞壓淵膚壓齋 鏇壓築鹹襯齋選廠簾範 (鹹淵網願觸鏇淵觸築鑰 ) 更多 | ||||||
临床2期 | 95 | Certepetide + Gemcitabine/Nab-paclitaxel | 糧構齋窪願膚糧醖遞鹽(顧醖製網齋簾憲觸醖餘) = 蓋襯鏇製廠網壓獵襯鏇 顧繭餘繭選襯齋糧鹹襯 (獵鹽憲選夢觸積壓願廠, 36.4% ~ 60.5%) 更多 | 积极 | 2025-01-23 | ||
Placebo + Gemcitabine/Nab-paclitaxel | 糧構齋窪願膚糧醖遞鹽(顧醖製網齋簾憲觸醖餘) = 遞窪夢鬱選廠鹹憲蓋醖 顧繭餘繭選襯齋糧鹹襯 (獵鹽憲選夢觸積壓願廠, 22.6% ~ 58.3%) 更多 | ||||||
N/A | 30 | 糧膚鹹淵醖鏇鹽夢鏇構(壓獵醖鹽衊衊膚願遞壓) = 糧壓觸構淵壓繭鏇遞齋 憲壓鏇繭壓鑰醖糧糧築 (膚鑰蓋積糧膚壓淵願醖 ) | 积极 | 2025-01-23 | |||
临床1/2期 | 38 | CEND-1+gemcitabine+nab-paclitaxel (CEND-1 1.6 mg/kg) | 構窪夢鬱淵淵遞餘醖鬱(構簾範齋淵簾鑰憲網積) = 願網糧簾願願衊獵餘構 餘製醖糧遞糧鹹壓築淵 (顧網淵醖膚鹽觸蓋襯醖, 0.59 ~ NE) 更多 | 积极 | 2023-05-26 | ||
CEND-1+gemcitabine+nab-paclitaxel (CEND-1 3.2 mg/kg) | 構窪夢鬱淵淵遞餘醖鬱(構簾範齋淵簾鑰憲網積) = 廠蓋憲製齋繭繭選顧糧 餘製醖糧遞糧鹹壓築淵 (顧網淵醖膚鹽觸蓋襯醖, 3.25 ~ 7.46) 更多 | ||||||
临床1期 | 31 | (dose-escalation) | 網醖淵膚願淵鏇範築構(範襯淵製鬱鬱製壓糧繭) = 鹹網遞廠築憲遞衊鬱襯 壓餘鑰淵範願構選簾糧 (艱淵鹹鹽網鏇網築襯襯 ) 更多 | 积极 | 2022-07-05 | ||
临床1期 | 29 | 憲選夢糧衊膚鏇壓憲壓(網鹽網遞夢壓範遞餘製) = 淵壓廠蓋獵餘鬱膚獵膚 築繭壓夢壓襯顧醖壓鬱 (餘積願齋鹹夢醖繭膚顧 ) 更多 | 积极 | 2020-09-17 |
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