We have located links that may give you full text access.
Comparison of novel PSMA-targeting [ 177 Lu]Lu-P17-087 with its albumin binding derivative [ 177 Lu]Lu-P17-088 in metastatic castration-resistant prostate cancer patients: a first-in-human study.
PURPOSE: Prostate-specific membrane antigen (PSMA) is a promising target for diagnosis and radioligand therapy (RLT) of prostate cancer. Two novel PSMA-targeting radionuclide therapy agents, [177 Lu]Lu-P17-087, and its albumin binder modified derivative, [177 Lu]Lu-P17-088, were evaluated in metastatic castration-resistant prostate cancer (mCRPC) patients. The primary endpoint was dosimetry evaluation, the second endpoint was radiation toxicity assessment (CTCAE 5.0) and PSA response (PCWG3).
METHODS: Patients with PSMA-positive tumors were enrolled after [68 Ga]Ga-PSMA-11 PET/CT scan. Five mCRPC patients received [177 Lu]Lu-P17-087 and four other patients received [177 Lu]Lu-P17-088 (1.2 GBq/patient). Multiple whole body planar scintigraphy was performed at 1.5, 4, 24, 48, 72, 120 and 168 h after injection and one SPECT/CT imaging was performed at 24 h post-injection for each patient. Dosimetry evaluation was compared in both patient groups.
RESULTS: Patients showed no major clinical side-effects under this low dose treatment. As expected [177 Lu]Lu-P17-088 with longer blood circulation (due to its albumin binding) exhibited higher effective doses than [177 Lu]Lu-P17-087 (0.151 ± 0.036 vs. 0.056 ± 0.019 mGy/MBq, P = 0.001). Similarly, red marrow received 0.119 ± 0.068 and 0.048 ± 0.020 mGy/MBq, while kidney doses were 0.119 ± 0.068 and 0.046 ± 0.022 mGy/MBq, respectively. [177 Lu]Lu-P17-087 demonstrated excellent tumor uptake and faster kinetics; while [177 Lu]Lu-P17-088 displayed a slower washout and higher average dose (7.75 ± 4.18 vs. 4.72 ± 2.29 mGy/MBq, P = 0.018). After administration of [177 Lu]Lu-P17-087 and [177 Lu]Lu-P17-088, 3/5 and 3/4 patients showed reducing PSA values, respectively.
CONCLUSION: [177 Lu]Lu-P17-088 and [177 Lu]Lu-P17-087 displayed different pharmacokinetics but excellent PSMA-targeting dose delivery in mCRPC patients. These two agents are promising RLT agents for personalized treatment of mCRPC. Further studies with increased dose and frequency of RLT are warranted to evaluate the potential therapeutic efficacy.
TRIAL REGISTRATION: 177 Lu-P17-087/177 Lu-P17-088 in Patients with Metastatic Castration-resistant Prostate Cancer (NCT05603559, Registered at 25 October, 2022). URL OF REGISTRY: https://classic.
CLINICALTRIALS: gov/ct2/show/NCT05603559 .
METHODS: Patients with PSMA-positive tumors were enrolled after [68 Ga]Ga-PSMA-11 PET/CT scan. Five mCRPC patients received [177 Lu]Lu-P17-087 and four other patients received [177 Lu]Lu-P17-088 (1.2 GBq/patient). Multiple whole body planar scintigraphy was performed at 1.5, 4, 24, 48, 72, 120 and 168 h after injection and one SPECT/CT imaging was performed at 24 h post-injection for each patient. Dosimetry evaluation was compared in both patient groups.
RESULTS: Patients showed no major clinical side-effects under this low dose treatment. As expected [177 Lu]Lu-P17-088 with longer blood circulation (due to its albumin binding) exhibited higher effective doses than [177 Lu]Lu-P17-087 (0.151 ± 0.036 vs. 0.056 ± 0.019 mGy/MBq, P = 0.001). Similarly, red marrow received 0.119 ± 0.068 and 0.048 ± 0.020 mGy/MBq, while kidney doses were 0.119 ± 0.068 and 0.046 ± 0.022 mGy/MBq, respectively. [177 Lu]Lu-P17-087 demonstrated excellent tumor uptake and faster kinetics; while [177 Lu]Lu-P17-088 displayed a slower washout and higher average dose (7.75 ± 4.18 vs. 4.72 ± 2.29 mGy/MBq, P = 0.018). After administration of [177 Lu]Lu-P17-087 and [177 Lu]Lu-P17-088, 3/5 and 3/4 patients showed reducing PSA values, respectively.
CONCLUSION: [177 Lu]Lu-P17-088 and [177 Lu]Lu-P17-087 displayed different pharmacokinetics but excellent PSMA-targeting dose delivery in mCRPC patients. These two agents are promising RLT agents for personalized treatment of mCRPC. Further studies with increased dose and frequency of RLT are warranted to evaluate the potential therapeutic efficacy.
TRIAL REGISTRATION: 177 Lu-P17-087/177 Lu-P17-088 in Patients with Metastatic Castration-resistant Prostate Cancer (NCT05603559, Registered at 25 October, 2022). URL OF REGISTRY: https://classic.
CLINICALTRIALS: gov/ct2/show/NCT05603559 .
Full text links
Related Resources
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app
All material on this website is protected by copyright, Copyright © 1994-2024 by WebMD LLC.
This website also contains material copyrighted by 3rd parties.
By using this service, you agree to our terms of use and privacy policy.
Your Privacy Choices 
You can now claim free CME credits for this literature searchClaim now
Get seemless 1-tap access through your institution/university
For the best experience, use the Read mobile app