ArticleCancers2022
Upregulation of PSMA Expression by Enzalutamide in Patients with Advanced mCRPC.
Article in Cancers, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 32 citations in OpenAlex.
- 131I-LNTH-1095 Radioligand Therapy plus Enzalutamide versus Enzalutamide Alone in Men with PSMA-Avid Metastatic Castration-Resistant Prostate Cancer: A Phase II Study.Clinical cancer research : an official journal of the American Association for Cancer Research · 2026Trial
- Efficacy and outcomes of [European journal of nuclear medicine and molecular imaging · 2026Article
- Effects of androgen receptor signaling inhibitors on absorbed doses in mCRPC patients undergoing [European journal of nuclear medicine and molecular imaging · 2026Article
- Article
- Drug interactions involving therapeutic radiopharmaceuticals: a systematic review.EJNMMI radiopharmacy and chemistry · 2026Review
- Advancing CAR-T therapy in prostate cancer: overcoming the tumor microenvironment and enhancing efficacy.Frontiers in oncology · 2026Review
- PSMA expression assessed by [Cancer imaging : the official publication of the International Cancer Imaging Society · 2025Article
- α-Therapy and Combination Strategies to Overcome Resistance and Enhance Clinical Outcomes in Prostate Cancer.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2025Article
- Review
- Enhancing outcomes in mCRPC: the impact of androgen receptor inhibitor sequencing before 177Lu-PSMA-617 therapy.The oncologist · 2025Article
- [Theranostics · 2024Article
- Alpha Particle-Emitting Radiopharmaceuticals as Cancer Therapy: Biological Basis, Current Status, and Future Outlook for Therapeutics Discovery.Molecular imaging and biology · 2023Review
- Towards Improving the Efficacy of PSMA-Targeting Radionuclide Therapy for Late-Stage Prostate Cancer-Combination Strategies.Current oncology reports · 2023Review
- Pharmacological Optimization of PSMA-Based Radioligand Therapy.Biomedicines · 2022Review
- Addition of Standard Enzalutamide Medication Shows Synergistic Effects on Response to [Cancers · 2022Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In this study, we investigated upregulation of prostate-specific membrane antigen (PSMA) by enzalutamide in a cohort (n = 30) of patients with advanced metastatic castration-resistant prostate cancer (mCRPC). Patients were examined by [68Ga]Ga-PSMA-11 PET/CT pre- and post-enzalutamide medication (mean 13 ± 7 days). Imaging results were compared based on quantification of whole-body PSMA tumor burden: total lesion PSMA (TLP) and normalized TLP values to liver (TLP-LR) and to parotid gland (TLP-PR). In addition, lesion-based analyses were performed. The median (mean) increases in TLP, TLP-LR and TLP-PR after enzalutamide medication were 10.1% (20.2%), 29.5% (34.8%) and 27.6% (24.4%), respectively. These increases were statistically significant (p = 0.002, p < 0.001, and p < 0.001), while prostate-specific antigen (PSA) serum values did not change significantly (p = 0.483). The increase was independent of prior patient exposure to enzalutamide. SUVmax increased substantially (>10%) in 49.6% of target lesions. The relative change was significantly higher in the subgroup of lesions with SUVmax < 10 (p < 0.001). In conclusion, short-term enzalutamide medication significantly increases PSMA expression in patients with mCRPC, irrespective of prior enzalutamide exposure. The relative PSMA upregulation effect seems to be more pronounced in lesions with only moderate baseline PSMA expression. Enzalutamide may provide a potential enhancer medication for PSMA-targeted radioligand therapy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.