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更新于：2025-12-15
AZD-8205
更新于：2025-12-15
概要
基本信息
药物类型 ADC |
别名 Puxitatug Samrotecan、AZD 8205、AZD-8205 + [1] |
作用方式 抑制剂 |
作用机制 B7-H4抑制剂(含V区域T细胞激活抑制因子1抑制剂)、TOP1抑制剂(DNA拓扑异构酶I抑制剂) |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构- |
权益机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
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Sequence Code 1034096049H
来源: *****
Sequence Code 1034096050L
来源: *****
关联
4
项与 AZD-8205 相关的临床试验NCT07162480
Phase II Trial of Puxitatug Samrotecan (AZD8205) in Advanced, Recurrent or Metastatic (R/M) Aggressive Adenoid Cystic Carcinoma Subtype I (ACC-I)
NCT07044336
Puxitatug Samrotecan (AZD8205) Monotherapy vs Chemotherapy in B7-H4 Selected Advanced/Metastatic Endometrial Cancer Who Progressed On or After Platinum Based Chemotherapy and Anti-PD-1/Anti-PD-L1 Therapy (Bluestar-Endometrial01)
NL-OMON53228
Clinical Performance Study Plan for use of B7-H4 (A57.1) Assay for Patient Enrolment Into The Clinical study (D6900C00001), titled *A Phase I/IIa Multi-center, Open-label Master Protocol Dose Escalation and Expansion Study of AZD8205 as Monotherapy and in Combination with Anticancer Agents in Participants with Advanced Solid Tumors*. - AZD8205 in participants with metastatic solid malignancies
100 项与 AZD-8205 相关的临床结果
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100 项与 AZD-8205 相关的转化医学
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100 项与 AZD-8205 相关的专利（医药）
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3
项与 AZD-8205 相关的文献（医药）2025-05-01Journal of immunotherapy and precision oncology
B7 Homolog 4 (B7-H4)-Directed Agents in Oncology Clinical Trials: A Review
Review
作者: Phipps, Meave ; Falchook, Gerald S.
ABSTRACT:
B7 homolog 4 (B7-H4) is a transmembrane protein found on immune cells and is frequently overexpressed in various solid tumors, making it a promising target for cancer therapy. B7-H4–directed agents, particularly antibody-drug conjugates (ADCs) like puxitatug samrotecan (AZD8205), felmetatug vedotin (SGN-B7H4V), and GSK5733584, have demonstrated early clinical activity with promising response rates in triple-negative breast cancer (TNBC). Combination strategies, such as ADCs with anti–PD-1 or PARP inhibitor therapies, have also shown enhanced tumor regression in preclinical models and are the subject of several ongoing clinical trials. This review highlights the current landscape of B7-H4–targeted agents, their progress in clinical trials, and the potential for combination approaches to improve outcomes in B7-H4–expressing cancers.
2025-01-10ACS Pharmacology & Translational Science
Detailed Structural Elucidation of Antibody-Drug Conjugate Biotransformation Species Using High Resolution Multiple Reaction Monitoring Mass Spectrometry with Orthogonal Dissociation Methods
Article
作者: Yang, Junyan ; Huang, Yue ; Tan, Hui Yin ; Rosenbaum, Anton I. ; Yuan, Jiaqi
Antibody-drug conjugates (ADCs) are a promising drug modality substantially expanding in both the discovery space and clinical development. Assessing the biotransformation of ADCs in vitro and in vivo is important in understanding their stability and pharmacokinetic properties. We previously reported biotransformation pathways for the anti-B7H4 topoisomerase I inhibitor ADC, AZD8205, puxitatug samrotecan, that underpin its structural stability in vivo using an intact protein liquid chromatography-high resolution mass spectrometry (LC-HRMS) approach. Herein, we employed a LC-high resolution multiple reaction monitoring (LC-MRMHR) approach using both collision-induced dissociation (CID) and electron-activated dissociation (EAD) methods, confirming our earlier findings. Furthermore, we were able to obtain additional detailed structural information on the biotransformation products expanding on earlier intact analyses. We also highlight the high sensitivity of LC-MRMHR for successfully identifying minor biotransformation products at low concentrations that were not detectable using the intact protein LC-HRMS workflow. Especially, EAD aided in the confirmation of biotransformation species that contain newly formed disulfide bonds due to the preferential dissociation of disulfide bonds using this method. We observed biotransformation reactions that vary between linker-payload (PL) conjugation sites on the antibody. For example, the trend toward constitutional isomerism in thio-succinimide linker hydrolysis, and the resulting positional isomers from thiol adduct formation following linker-PL deconjugation. The reported orthogonal analytical approaches highly complement and fortify the intact protein LC-HRMS data. This study sheds further light on detailed structural characterization of various ADC species and validates the proposed biotransformation pathways explaining the stability of AZD8205 in vivo.
2024-10-22ANALYTICAL CHEMISTRY
Extensive Biotransformation Profiling of AZD8205, an Anti-B7-H4 Antibody-Drug Conjugate, Elucidates Pathways Underlying Its Stability In Vivo
Article
作者: Liang, Meina ; Vijayakrishnan, Balakumar ; Kinneer, Krista ; Rosenbaum, Anton I. ; Tan, Hui Yin ; Luheshi, Nadia ; Yang, Junyan ; Yuan, Jiaqi ; Mu, Ruipeng ; Masterson, Luke ; Huang, Yue ; Ball, Kathryn
What happens to macromolecules in vivo? What drives the structure-activity relationship and in vivo stability for antibody-drug conjugates (ADCs)? These interrelated questions are increasingly relevant due to the re-emerging importance of ADCs as an impactful therapeutic modality and the gaps that exist in our understanding of ADC structural determinants that underlie ADC in vivo stability. Complex macromolecules, such as ADCs, may undergo changes in vivo due to their intricate structure as biotransformations may occur on the linker, the payload, and/or at the modified conjugation site. Furthermore, the dissection of ADC metabolism presents a substantial analytical challenge due to the difficulty in the identification or quantification of minor changes on a large macromolecule. We employed immunocapture-LCMS methods to evaluate in vivo changes in the drug-antibody ratio (DAR) profile in four different lead ADCs. This comprehensive characterization revealed that a critical structural determinant contributing to the ADC design was the linker, and competition of the thio-succinimide hydrolysis reaction over retro-Michael deconjugation can result in superb conjugation stability in vivo. These data, in conjunction with additional factors, informed the selection of AZD8205, puxitatug samrotecan, a B7-H4-directed cysteine-conjugated ADC bearing a novel topoisomerase I inhibitor payload, with durable DAR, currently being studied in the clinic for the potential treatment of solid malignancies (NCT05123482). These results highlight the relevance of studying macromolecule biotransformation and elucidating the ADC structure-in vivo stability relationship. The comprehensive nature of this work increases our confidence in the understanding of these processes. We hope this analytical approach can inform future development of bioconjugate drug candidates.
100 项与 AZD-8205 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 子宫内膜癌 | 临床3期 | 中国 | 2025-11-17 | |
| 子宫内膜癌 | 临床3期 | 澳大利亚 | 2025-11-17 | |
| 子宫内膜癌 | 临床3期 | 中国台湾 | 2025-11-17 | |
| 恶性实体肿瘤 | 临床3期 | 美国 | 2025-08-01 | |
| 恶性实体肿瘤 | 临床3期 | 中国 | 2025-08-01 | |
| 恶性实体肿瘤 | 临床3期 | 日本 | 2025-08-01 | |
| 恶性实体肿瘤 | 临床3期 | 阿根廷 | 2025-08-01 | |
| 恶性实体肿瘤 | 临床3期 | 澳大利亚 | 2025-08-01 | |
| 恶性实体肿瘤 | 临床3期 | 奥地利 | 2025-08-01 | |
| 恶性实体肿瘤 | 临床3期 | 比利时 | 2025-08-01 |
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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1/2期 | HR阳性/HER2低表达乳腺癌 B7-H4 | 57 | 廠鏇淵觸網構範網窪鑰(窪鬱積餘簾蓋蓋繭願襯) = 淵鹽壓醖築獵製鏇衊繭 範獵窪襯選觸淵窪壓遞 (簾膚糧夢顧餘鑰觸願顧 ) 更多 | 积极 | 2025-05-15 | ||
廠鏇淵觸網構範網窪鑰(窪鬱積餘簾蓋蓋繭願襯) = 鹹鹽鹹糧鑰獵獵製壓築 範獵窪襯選觸淵窪壓遞 (簾膚糧夢顧餘鑰觸願顧 ) 更多 | |||||||
BLUESTAR (NEWS) 人工标引  | 临床1/2期 | 52 | Puxitatug samrotecan 2.0 mg/kg | 衊製窪築積簾憲簾鏇憲(窪憲淵膚積蓋鹹壓蓋鬱) = 鏇窪範繭獵鏇廠網夢艱 願鹹窪網遞願觸顧蓋艱 (醖願簾鹹鏇範襯衊觸範 ) 更多 | 积极 | 2025-03-16 | |
Puxitatug samrotecan 2.4 mg/kg | 衊製窪築積簾憲簾鏇憲(窪憲淵膚積蓋鹹壓蓋鬱) = 選醖窪鑰願鑰壓窪簾蓋 願鹹窪網遞願觸顧蓋艱 (醖願簾鹹鏇範襯衊觸範 ) 更多 | ||||||
临床1/2期 | 实体瘤 二线 | 46 | 齋淵艱鏇鹹壓餘艱築鹹(選齋顧齋鏇衊鏇膚窪糧) = 構築餘選獵鑰範獵網繭 廠範製選糧觸獵餘淵選 (構夢蓋廠膚網顧範鹽範 ) 更多 | 积极 | 2024-09-13 | ||
临床1期 | - | 夢膚製鬱壓鹽鹹鑰鏇糧(構繭壓鑰鬱選餘襯顧餘) = 簾衊簾願餘鑰膚鏇艱願 壓壓顧艱淵選鑰遞壓壓 (遞鹹夢蓋鹽鹹蓋壓壓選 ) | - | 2023-03-14 |
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