预约演示
更新于：2026-07-15
FPI-2265
更新于：2026-07-15
概要
基本信息
药物类型 核素偶联药物、治疗用放射药物 |
别名 225Ac-PSMA I&T、[²²⁵Ac]Ac-PSMA I&T、AZD2265 + [1] |
靶点 |
作用方式 调节剂 |
作用机制 PSMA调节剂(前列腺癌特异性膜抗原调节剂) |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构 |
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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关联
6
项与 FPI-2265 相关的临床试验NCT07590934
A Phase Ib/II, Open-label, Multi-centre, Platform Study to Assess the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Efficacy of Multiple Anti-Cancer Agents in Metastatic Prostate Cancer
NCT07611110
A Phase III, Multicentre, Randomised Controlled Study to Evaluate the Efficacy and Safety of AZD2265 (FPI-2265) ²²⁵Ac-PSMA-I&T Compared With Standard of Care in Patients With PSMA-positive Metastatic Castration-resistant Prostate Cancer (VECTRA-01)
NCT06909825
A Phase 2, Open-label, Multi-centre Study of FPI-2265 (225Ac-PSMA-I&T) and Olaparib in Participants With Metastatic Castration Resistant Prostate Cancer (mCRPC)
100 项与 FPI-2265 相关的临床结果
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100 项与 FPI-2265 相关的转化医学
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100 项与 FPI-2265 相关的专利（医药）
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9
项与 FPI-2265 相关的文献（医药）2026-04-01European Journal of Nuclear Medicine and Molecular Imaging
Review
作者: Grujić, Miloš ; Shelan, Mohamed ; Al-Ibraheem, Akram ; Afshar-Oromieh, Ali ; Mohamad, Issa ; Zilli, Thomas ; Belabaci, Zineddine ; Brignoli, Giulio
Abstract:
Background:
Targeted radionuclide therapy (TRT) has become a standard of care for patients with metastatic castration-resistant prostate cancer (mCRPC). Lutetium-177 labeled PSMA radioligand therapy ([¹⁷⁷Lu]Lu-PSMA) is an established and effective treatment option, while [²²⁵Ac]Ac-PSMA shows promise in refractory cases. The tandem use of [225Ac] Ac and [177Lu] Lu-labeled PSMA ligands is currently being explored to harness the complementary advantages of both isotopes. This meta-analysis investigates the efficacy and safety of [²²⁵Ac]Ac -/[¹⁷⁷Lu]Lu-PSMA radioligand therapy (RLT) in patients with mCRPC.
Methods:
This systematic review is reported in accordance with the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA). A comprehensive literature search was performed in PubMed, EMBASE, Web of Science (WOS), and Scopus databases, covering all records from inception through March 2025. The primary endpoints focused on therapeutic efficacy, assessed through PSA-based biochemical responses. These included any PSA decline, a PSA decline of more than 50% from baseline, stable disease (defined as a PSA increase of < 25% PSA increase or a decrease of < 50%), and progressive disease (defined as an increase of ≥ 25% PSA) following tandem 225Ac-/177Lu-PSMA tandem RLT. Secondary endpoints included overall survival (OS) and treatment-related adverse events. A random-effects model was used to generate pooled proportions through meta-analysis.
Results:
Eight studies, including a total of 323 patients treated with [²²⁵Ac]-/[¹⁷⁷Lu]-PSMA combination therapy, were analyzed. The pooled response rates showed that 47% (95% CI: 37%–56%) experienced a PSA decline greater than 50%, while 78% (95% CI: 70%–86%) had any measurable PSA decline. The estimated median OS was 11.8 months (95% CI: 9.0–14.6 months). Severe toxicities were infrequent; the most common severe grade ≥ 3 adverse events were anemia (10%) and thrombocytopenia (6%). No cases of grade ≥ 3 xerostomia were reported.
Conclusion:
[²²⁵Ac]Ac-/[¹⁷⁷Lu]Lu-PSMA RLT shows encouraging activity and manageable safety in patients with advanced mCRPC. Given the retrospective nature of the available evidence and limited data, these findings should be further evaluated in prospective trials to determine long-term efficacy and survival outcomes.
2025-12-01JOURNAL OF NUCLEAR MEDICINE
[
225
Ac]Ac-PSMA I&T: A Preclinical Investigation on the Fate of Decay Nuclides and Their Influence on Dosimetry of Salivary Glands and Kidneys
Article
作者: Sebastian Fischer ; Wolfgang Weber ; Alfred Morgenstern ; Kerstin Hürkamp ; Alexander Wurzer ; Wei Bo Li ; Frank Bruchertseifer ; Samaah Saleh ; Baiqing Sun ; Susanne Kossatz ; Matthias Eiber ; Calogero D’Alessandria ; Julia Brosch-Lenz
α-therapy with 225Ac-labeled radioligands targeting prostate-specific membrane antigen (PSMA) has emerged as a promising treatment option for advanced metastatic castration-resistant prostate cancer. Because of α-recoil, the progeny is released from the PSMA-targeted molecule and can undergo redistribution, contributing to off-target toxicity. Here, we report on biodistribution and dosimetry studies of [225Ac]Ac-PSMA I&T performed in mice to investigate the pharmacokinetics of the radioligand compared with unbound progeny. Moreover, the cellular uptake and externalization kinetics of [225Ac]Ac-PSMA I&T were compared with those of its 177Lu-labeled analog. Methods: In vitro studies were performed on LNCaP and PC3 PIP cells. Biodistribution studies (performed 10 min to 7 d after injection) were conducted in LNCaP tumor-bearing and healthy mice. Equilibrium uptake was determined 24 h after dissection by quantification of 221Fr (218 keV) and 213Bi (440 keV). Tissues of interest (kidneys, salivary glands, and tumor tissue) were measured immediately after dissection until reaching equilibrium to determine the time-dependent activity distribution of 221Fr and 213Bi. Absorbed doses were calculated using MIRDcalc, assuming decay of the progeny at the site of the first decay versus taking into account redistribution of unbound progeny. Results: [225Ac]Ac-PSMA I&T demonstrated cell-binding characteristics and cellular retention similar to those of [177Lu]Lu-PSMA I&T. In biodistribution studies, no redistribution of 221Fr and 213Bi was measured from tumor tissue. Higher uptake of 213Bi was found in the kidneys (2-fold higher at 10 min and at 1 h after injection) and salivary glands (1.7-fold and 8.5-fold higher at 10 min and 1 h after injection, respectively) at the time of death compared with equilibrium. This contribution increased the absorbed dose in the kidneys and salivary glands by a factor of 1.3 and 2.5, respectively, assuming uptake of 221Fr and in situ formation of 213Bi. Conclusion: The PSMA-targeting characteristics and pharmacokinetics of [225Ac]Ac-PSMA I&T are similar to those of [177Lu]Lu-PSMA I&T. The progeny of [225Ac]Ac-PSMA I&T is trapped in tumor tissue. Uptake of liberated decay products into the salivary glands and kidneys was identified as an additional factor explaining the increased side effects of 225Ac therapy compared with 177Lu-based radioligands.
2024-07-01European Journal of Nuclear Medicine and Molecular Imaging
Article
作者: Unterrainer, Lena M ; Liubchenko, Grigory ; Ziegler, Sibylle I ; Rumiantcev, Mikhail ; Brendel, Matthias ; Gildehaus, Franz Josef ; Resch, Sandra ; Zacherl, Mathias ; Böning, Guido ; Delker, Astrid ; Bartenstein, Peter
Abstract:
Purpose:
Although 221Fr and 213Bi have sufficient gamma emission probabilities, quantitative SPECT after [225Ac]Ac-PSMA-I&T therapy remains challenging due to low therapeutic activities. Furthermore, 221Fr and 213Bi may underlie a different pharmacokinetics due to alpha recoil. We conducted a quantitative SPECT study and a urine analysis to investigate the pharmacokinetics of 221Fr and 213Bi and the impact on image-based lesion and kidney dosimetry.
Methods:
Five patients (7.7 ± 0.2 MBq [225Ac]Ac-PSMA-I&T) underwent an abdominal SPECT/CT (1 h) at 24 and 48 h (Siemens Symbia T2, high-energy collimator, 440 keV/218 keV (width 20%), 78 keV (width 50%)). Quantitative SPECT was reconstructed using MAP-EM with attenuation and transmission-dependent scatter corrections and resolution modelling. Time-activity curves for kidneys (CT-based) and lesions (80% isocontour 24 h) were fitted mono-exponentially. Urine samples collected along with each SPECT/CT were measured in a gamma counter until secular equilibrium was reached.
Results:
Mean kidney and lesion effective half-lives were as follows: 213Bi, 27 ± 6/38 ± 10 h; 221Fr, 24 ± 6/38 ± 11 h; 78 keV, 23 ± 7/39 ± 13 h. The 213Bi-to-221Fr kidney SUV ratio increased by an average of 9% from 24 to 48 h. Urine analysis revealed an increasing 213Bi-to-225Ac ratio (24 h, 0.98 ± 0.15; 48 h, 1.08 ± 0.09). Mean kidney and lesion absorbed doses were 0.17 ± 0.06 and 0.36 ± 0.1 $${{\text{Sv}}}_{{\text{RBE}}=5}$$Sv RBE = 5 Sv RBE = 5
Conclusion:
SPECT/CT imaging and urine analysis showed minor differences of up to 10% in the daughter-specific pharmacokinetics. These variances had a minimal impact on the lesion and kidney dosimetry which remained within 8%.
100 项与 FPI-2265 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 |
|---|---|---|---|---|
| 转移性去势抵抗性前列腺癌 | 临床3期 | 美国 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 中国 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 日本 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 澳大利亚 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 奥地利 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 巴西 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 加拿大 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 法国 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 德国 | 2026-05-04 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 印度 | 2026-05-04 |
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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 | 25 | 製鹽繭襯壓積鹽襯願醖(製鹹餘餘遞糧襯淵鏇網) = 獵遞積膚鏇鏇顧選選選 鬱襯醖淵鑰顧廠築積鑰 (遞獵積憲獵膚願選夢願 ) 更多 | 积极 | 2024-04-09 | |||
临床2期 | 转移性去势抵抗性前列腺癌 Prostate specific antigen | 30 | 衊願夢構鬱選顧醖鏇獵(遞構積遞構襯憲壓鹹獵) = dry mouth (18/21 [86%]), fatigue (10/21 [48%]) dry eye (6/21 [28%]), and anemia (6/21 [28%]). All were Grade 1-2 in severity, expect anemia Grade 3 which was observed in (5/21 [24%]). Other Grade 3 TRAEs included decreased platelet count (3/21 [14%]). No Grade 4 or 5 TRAEs were reported. Dry mouth was primarily Grade 1 (13/21 [62%]) with only 5 patients (24%) experiencing Grade 2 dry mouth; 鹹鏇獵艱壓觸遞壓衊衊 (鹹選窪壓蓋獵夢鹹鏇積 ) | 积极 | 2024-04-05 | ||
N/A | 17 | Ac-225-PSMA I&T | 觸夢觸夢餘鹽廠艱願憲(選膚簾壓糧鹹艱鹽醖膚) = Grade 3-4 anemia was observed in 6 out of 12 patients. 淵構糧繭糧衊繭襯廠積 (蓋獵憲觸鏇淵顧襯顧鑰 ) 更多 | 积极 | 2020-09-18 |
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