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更新于：2026-01-22
Lutetium (177Lu) zadavotide guraxetan
更新于：2026-01-22
概要
基本信息
药物类型 多肽偶联核素、治疗用放射药物 |
别名 177Lu-PNT2002、177Lu-PSMA-I&T、PNT-2002 + [1] |
靶点 |
作用方式 抑制剂 |
作用机制 PSMA抑制剂(前列腺癌特异性膜抗原抑制剂) |
在研适应症 |
非在研适应症 |
原研机构 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床申请 |
特殊审评快速通道 (美国) |
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结构/序列
分子式C63H85ILuN11O23 |
InChIKeyKRNMXHUBVUCLIL-KMPGELEWSA-G |
CAS号2447131-70-4 |
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13
项与 Lutetium (177Lu) zadavotide guraxetan 相关的临床试验NCT05896371
PROstate-specific Membrane Antigen DosImetry-Guided EndoradiotherapY: a Phase 1/2 Study of Personalized PSMA Radiopharmaceutical Therapy (PRODIGY-1)
NCT07090369
Phase Ib Trial of 177Lu-PSMA-I&T Therapy in Combination With Olaparib and Pembrolizumab in Patients With Metastatic Castration Resistant Prostate Cancer
NCT06361810
A Phase 1/2 Open-label Study of Pembrolizumab Combined With PNT-2002 Radioligand Therapy in Patients With Metastatic Renal Cell Carcinoma
100 项与 Lutetium (177Lu) zadavotide guraxetan 相关的临床结果
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100 项与 Lutetium (177Lu) zadavotide guraxetan 相关的转化医学
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100 项与 Lutetium (177Lu) zadavotide guraxetan 相关的专利（医药）
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57
项与 Lutetium (177Lu) zadavotide guraxetan 相关的文献（医药）2026-02-01NUCLEAR MEDICINE COMMUNICATIONS
Concordance between single-time-point and multiple-time-point dosimetry in 177Lu-PSMA-I&T therapy for metastatic castration-resistant prostate cancer
Article
作者: Zuluaga, Clarena ; Pulido, Edwin ; Barbosa, Nathaly ; Granados, Carlos
Purpose:
To quantify concordance between single-time-point (STP) and multiple-time-point (MTP) dosimetry for organs-at-risk (OARs) and lesions in
177
Lu-PSMA-I&T.
Methods:
Thirteen men with metastatic castration-resistant prostate cancer underwent quantitative SPECT/CT at ~20, ~48, and ~120 h posttherapy. Lesions <3.0 cc were excluded. Time-activity curves (TACs) were fit with automatic model-order selection (parameters ≤ data points); accepted fits required
R2
> 0.90. STP activity–time integrals were estimated with the Hänscheid formalism. Agreement metrics included paired median differences, Lin’s concordance, and Bland–Altman bias/limits of agreement.
Results:
For OARs, STP at ~48 h matched MTP with minimal bias (parotids Δ = 0.00 Gy/GBq,
P
= 0.475; kidneys Δ = 0.02,
P
= 0.157). Lesion concordance improved with later imaging (STP2–STP3), whereas ~20 h STP underestimated lesion dose coefficients (all lesions Δ = +0.36 Gy/GBq; +57.4%). TAC modeling favored mono-exponential kinetics in most lesions (83%) and kidneys, with mixed behavior in parotids.
Conclusion:
A single quantitative scan at ~48 h provides OAR dosimetry concordant with MTP, while lesion estimates are best captured at ~48–120 h. Early STP imaging (~20 h) should not be used alone for lesions. Findings support a pragmatic, concordance-oriented dosimetry workflow for routine
177
Lu-PSMA-I&T care.
2025-11-01LANCET ONCOLOGY
Lutetium-177 [177Lu]Lu-PSMA-I&T plus radium-223 in patients with metastatic castration-resistant prostate cancer (AlphaBet): an interim analysis of the investigator-initiated, single-centre, single-arm, phase 1/2 trial
Article
作者: MacFarlane, Lisa ; Buteau, James P ; Au, Lewis ; Cardin, Anthony ; Hamilton, Anthony J ; Garcia, Quinn ; Hofman, Michael S ; Haskali, Mohammad B ; Emmerson, Brittany ; Saghebi, Javad ; Alipour, Ramin ; Parker, Belinda S ; Tran, Ben ; Chin, Kwang Y ; Kong, Grace ; Jackson, Price A ; Kostos, Louise ; Murphy, Declan G ; Ravi Kumar, Aravind S ; Kashyap, Raghava K ; Xie, Jing ; Furic, Luc ; Azad, Arun A ; Wang, Yang ; Chan, Joanna ; Akhurst, Tim
BACKGROUND:
Lutetium-177 [177Lu]Lu-PSMA-I&T (177Lu-PSMA-I&T) and the bone-seeking α-emitter radium-223 (223Ra) are established life-extending therapies for patients with metastatic castration-resistant prostate cancer; however, resistance and progression are inevitable. We aimed to evaluate the safety and preliminary antitumour activity of 177Lu-PSMA-I&T combined with 223Ra in this patient group.
METHODS:
We conducted an investigator-initiated, single-centre, single-arm, phase 1/2 trial (AlphaBet) at the Peter MacCallum Cancer Centre in Melbourne, Australia. Adults (aged ≥18 years) with a diagnosis of progressive, metastatic castration-resistant prostate cancer, an Eastern Cooperative Oncology Group performance status score of 0-2, at least two visible bone metastases not treated with radiotherapy, previous exposure to an androgen receptor pathway inhibitor, prostate-specific membrane antigen (PSMA)-positive disease (defined by maximum standardised uptake value ≥20 at a site of disease), and no discordant sites (ie, avid on 2-[18F]fluoro-2-deoxy-D-glucose-PET-CT with minimal PSMA expression and no uptake on bone scintigraphy) were eligible for inclusion. Phase 1 dose-escalation assessed two dose levels of 223Ra (27·5 kBq/kg and 55·0 kBq/kg) combined with 7·4 GBq 177Lu-PSMA-I&T, administered intravenously every 6 weeks for up to six cycles. Phase 2 dose expansion continued with the recommended phase 2 dose. Co-primary endpoints were the maximum tolerated or administered dose and the recommended phase 2 dose (phase 1), and the PSA response rate (phase 2), analysed in all patients treated at the maximum tolerated or administered dose in either phase. Safety was assessed in all patients who received at least one dose of either protocol treatment in phase 1 or 2. Herein, we report the results of an interim analysis, which was added to the protocol following an amendment on May 30, 2024. This trial is registered at ClinicalTrials.gov (NCT05383079) and follow-up is ongoing.
FINDINGS:
Between Nov 3, 2022, and Nov 5, 2024, 37 patients were enrolled, of whom 36 (97%; median age 72·5 years [IQR 67·0-78·0]) were included in the safety analysis and 33 (89%) were included in the preliminary activity analysis. No dose-limiting toxicities were observed. The recommended phase 2 dose of 223Ra was 55·0 KBq/kg combined with 7·4 GBq 177Lu-PSMA-I&T, administered every 6 weeks. With a median follow-up of 13·3 months (IQR 8·7-17·1), 11 (31%) patients completed all six cycles of both treatments. 18 (50%) patients discontinued treatment early, primarily due to unequivocal disease progression (11 [61%]) or adverse events (three [17%]). A reduction in PSA of at least 50% was observed in 18 (55%; 95% CI 36-72) patients. Grade 3 or higher treatment-related adverse events occurred in five (14%) of 36 patients, including anaemia (four [11%]) and neutropenia (three [8%]), with no treatment-related deaths. Non-clinically significant grade 3 lymphopenia occurred in ten (28%) patients.
INTERPRETATION:
The combination of 177Lu-PSMA-I&T and 223Ra is safe and feasible in patients with metastatic castration-resistant prostate cancer and bone metastases. These findings warrant further evaluation of combined α-emitting and β-emitting approaches.
FUNDING:
Prostate Cancer Foundation, Bayer, and National Health and Medical Research Council.
2025-11-01JOURNAL OF NUCLEAR MEDICINE
Preclinical Evaluation of [
212
Pb]Pb-ADVC001: A Prostate-Specific Membrane Antigen–Targeted α-Therapy for Prostate Cancer
Article
作者: Horsfall, Aimee ; Kryza, Thomas ; Hammond, Edward ; Li, Kwong Ching ; Liu, Feifei ; Fletcher, Nicholas ; Shakti, Stelle ; Soderholm, Amelia T ; Prior, Amber ; Koehbach, Johannes ; Monterosso, Melissa E ; Kuan, Kevin ; Sydes, Abby ; Rose, Stephen ; Tieu, William ; Akhter, Dewan ; Kim, Chanwoo ; Thurecht, Kristofer ; Puttick, Simon ; Kumar, Saawan ; Boucher, Didier ; Li, Gary ; Karmann, Anna
Prostate-specific membrane antigen (PSMA)-directed radiopharmaceutical therapies continue to improve treatment outcomes in patients with metastatic castration-resistant prostate cancer. Here, we report the in vitro and in vivo characterization of a PSMA-targeted therapy (ADVC001) specifically designed for targeted α-therapy with 212Pb. Methods: The binding affinity to PSMA was determined by PSMA enzymatic assays and by radioligand binding assays using PSMA-high prostate cancer (PC) cells. In vitro cytotoxicity against PC cell lines with high and medium PSMA expression was evaluated using clonogenic, metabolic, and imaging-based cytotoxic assays. Pharmacokinetics and biodistribution were assessed using PSMA-high subcutaneous tumor xenografts. In vivo single-dose and multidose efficacy was assessed in subcutaneous PC xenograft models expressing various levels of PSMA. Results: A high binding affinity to PSMA was observed for ADVC001 with nanomolar inhibitory concentration of 50% values. In cellular assays, [212Pb]Pb-ADVC001 (212Pb-ADVC001 hereafter for simplicity) exhibited specific cytotoxic activity against PSMA-expressing cells with nanomolar effective concentration of 50% values. In vivo biodistribution of 212Pb-ADVC001 in the PC3-PIP xenograft model revealed rapid and persistent tumor uptake, fast renal clearance, and low retention in normal tissues. Single-dose efficacy studies of 212Pb-ADVC001 (0.46 MBq) showed improved survival compared with [177Lu]Lu-PSMA-I&T (177Lu-PSMA-I&T hereafter for simplicity) (20 MBq) treatment. In a multidose experiment, 2 doses of 212Pb-ADVC001 (0.5 MBq) significantly increased median survival (86 d vs. 45.5 d, P < 0.05) compared with 2 doses of 177Lu-PSMA-I&T (15 MBq). Treatment with 212Pb-ADVC001 (0.5 MBq) after initial 177Lu-PSMA-I&T (15 MBq) relapse showed an enhanced survival benefit (59.5 d). In a C4-2 xenograft model with medium-level PSMA expression, single doses of 0.3, 0.8, and 1.1 MBq of 212Pb-ADVC001 significantly extended median survival to 34, 57, and 62.5 d, compared with untreated cohorts (16 d). All treatments were well tolerated. Conclusion: The preclinical results support the clinical development of 212Pb-ADVC001 as a targeted α-therapy for the treatment of patients with PC.
146
项与 Lutetium (177Lu) zadavotide guraxetan 相关的新闻（医药）2026-01-06
2025-12-30
100 项与 Lutetium (177Lu) zadavotide guraxetan 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 |
|---|---|---|---|---|
| 转移性前列腺恶性肿瘤 | 临床3期 | 美国 | 2022-02-14 | |
| 转移性前列腺恶性肿瘤 | 临床3期 | 法国 | 2022-02-14 | |
| 转移性前列腺恶性肿瘤 | 临床3期 | 意大利 | 2022-02-14 | |
| 转移性前列腺恶性肿瘤 | 临床3期 | 西班牙 | 2022-02-14 | |
| 去势抵抗性前列腺癌 | 临床3期 | 美国 | 2021-02-25 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 美国 | 2021-02-25 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 美国 | 2021-02-25 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 加拿大 | 2021-02-25 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 法国 | 2021-02-25 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 荷兰 | 2021-02-25 |
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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3期 | 455 | (Randomization Phase: [Lu-177]-PNT2002 (Arm A)) | 鬱選繭糧鬱鹽鏇鏇淵壓(衊窪憲積糧廠鹽網膚鹽) = 齋觸簾憲構膚襯積膚鹽 鬱艱構積鏇製蓋構範憲 (鹽遞鏇窪選積淵淵鑰鬱, 選蓋壓糧願顧構簾鹽網 ~ 繭淵範衊蓋窪憲餘襯醖) 更多 | - | 2026-01-13 | ||
(Randomization Phase: Abiraterone or Enzalutamide (Arm B)) | 鬱選繭糧鬱鹽鏇鏇淵壓(衊窪憲積糧廠鹽網膚鹽) = 襯願憲構壓鬱壓鏇淵餘 鬱艱構積鏇製蓋構範憲 (鹽遞鏇窪選積淵淵鑰鬱, 夢顧醖衊積蓋壓構糧憲 ~ 憲齋蓋壓憲齋齋鹽鹽構) 更多 | ||||||
临床1期 | 18 | 構憲廠夢鏇衊夢夢糧淵(窪繭壓醖壓糧膚襯繭構) = 35 KGBq/kg 蓋鬱壓襯鏇壓膚糧鏇鏇 (夢製蓋選遞製鏇築廠觸 ) 更多 | 积极 | 2025-02-13 | |||
临床3期 | 27 | [177Lu]Lu-PNT2002 6.8 GBq/cycle | 範廠繭襯膚窪簾夢觸糧(糧選膚醖鏇艱艱簾衊顧) = 糧鹹憲鏇製襯觸襯鏇膚 簾鑰獵蓋夢壓觸衊觸網 (鏇網齋簾醖憲鬱艱觸鑰, 9.2 ~ 19.1) 更多 | 积极 | 2025-01-07 | ||
临床3期 | - | 範齋製鑰蓋夢憲衊壓鹽(衊憲築衊鬱糧齋襯構鏇) = 鹽繭鬱遞範網簾遞壓醖 壓衊糧顧築鏇獵積願襯 (齋遞顧膚蓋鏇積壓鹽鏇 ) | 积极 | 2024-11-13 | |||
Hormone therapy | 範齋製鑰蓋夢憲衊壓鹽(衊憲築衊鬱糧齋襯構鏇) = 憲膚鬱製鏇壓觸糧積壓 壓衊糧顧築鏇獵積願襯 (齋遞顧膚蓋鏇積壓鹽鏇 ) | ||||||
N/A | 112 | 7.4 GBq [177Lu]Lu-PSMA-I&T | 襯觸鹹夢襯顧鹹獵淵鹽(膚築壓範獵選廠範糧顧) = CTCAE grade 3 anaemia was seen in four patients 選選簾蓋鑰齋衊憲膚範 (夢艱襯艱襯鬱鏇廠選艱 ) 更多 | 积极 | 2024-09-27 | ||
临床3期 | 转移性去势抵抗性前列腺癌 FOLH1 Positive | 412 | 鏇壓簾醖艱衊艱廠構廠(鹽鏇糧簾夢艱糧鑰選顧) = 淵鬱選餘廠簾獵範糧淵 壓憲窪範鑰憲蓋鹹顧構 (鬱觸膚遞築構鹽窪築糧, 7.4 ~ 10.0) 更多 | 积极 | 2024-09-15 | ||
Alternate ARPI | 鏇壓簾醖艱衊艱廠構廠(鹽鏇糧簾夢艱糧鑰選顧) = 鹹鬱製窪蓋鹽襯製構觸 壓憲窪範鑰憲蓋鹹顧構 (鬱觸膚遞築構鹽窪築糧, 4.7 ~ 7.9) 更多 | ||||||
N/A | - | - | 窪繭蓋鏇衊鬱壓膚鹹壓(選簾觸顧齋獵艱鹹顧觸) = No CTC grade ≥III occurred after RLT 遞選鏇艱構獵選醖構築 (鑰襯鑰餘醖獵選築齋觸 ) 更多 | - | 2024-06-09 | ||
临床3期 | - | 壓繭窪觸簾鹹簾夢壓艱(齋鏇衊範蓋鹽積築齋鏇) = 醖簾艱窪願觸膚糧夢願 顧願淵鑰艱顧網構廠膚 (鏇衊鑰憲築顧鹹構鹽衊 ) 更多 | 积极 | 2023-12-18 | |||
ARPI | 壓繭窪觸簾鹹簾夢壓艱(齋鏇衊範蓋鹽積築齋鏇) = 醖壓憲網膚衊築鹽襯簾 顧願淵鑰艱顧網構廠膚 (鏇衊鑰憲築顧鹹構鹽衊 ) | ||||||
临床1/2期 | 18 | 壓鑰顧艱選膚觸鏇繭獵(網糧壓憲顧獵膚繭膚網) = 2 of 6 pts with DLT at 40 KBq/Kg (Gr 2 or 3 thrombocytopenia delaying cycle 2 by >3 wk); no DLT observed in other cohorts. 顧夢夢艱壓醖顧網鬱顧 (網襯顧鹹鹽鹹構廠範選 ) 更多 | 积极 | 2023-05-31 | |||
临床2期 | 100 | 177 Lu-PNT2002+SBRT | 範鹹願鹽製積鏇鹽鏇簾(觸醖積範齋獵餘製鏇鏇) = The addition of 177 Lu-PNT2002 to metastasis-directed therapy alone may potentially further forestall disease progression. 鑰淵醖選積鹹襯壓糧糧 (獵艱壓衊糧淵衊選願壓 ) | 积极 | 2023-03-02 | ||
SBRT |
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