The purpose of this study is to test a novel diagnostic Positron Emission Tomography (PET) imaging agent for safety and biodistribution. The agent binds Prostate Specific Membrane Antigen (PSMA) and is designed to detect prostate tumors.
The sponsor has developed a PET imaging agent, CTT1057, labeled with 18F, that is based on a small molecule core and targets an extracellular region of PSMA with high affinity. Although comparable to other inhibitors in terms of affinity for PSMA, this unique class of phosphoramidate agents are the only known irreversible PSMA inhibitors. Due to its irreversible binding to PSMA and rapid uptake by PSMA-expressing prostate cancer cells, accumulation at the cancer target is expected to be rapid, specific and sensitive. Twenty patients will be enrolled in parallel in two cohorts: * (Cohort A) Patients with prostate cancer prior to radical prostatectomy (N = 5). * (Cohort B) Patients with evidence of metastatic castration-resistant prostate cancer (N = 15) Participants receive a single intravenous (IV) dose (370 MBq, or 10 mCi) of CTT1057 in this first-in-human trial. Combined PET/MR imaging (prostate + whole body) will be performed following tracer injection. The 5 patients in the pre-prostatectomy cohort will comprise the dosimetry/pharmacokinetic (PK) cohort to establish organ dosimetry and PK profile. Patients in cohort A will undergo planned radical prostatectomy (plus lymph node dissection) within 12 weeks following CTT1057 PET/MR. Patients in cohort B (metastatic prostate cancer) will have the option for metastatic tumor biopsy following CTT1057 PET imaging. The one-time nominal injected dose will be 370 MBq (10 mCi). Estimated mass dose is 20 µg of CTT1057. Dose will be in a volume of 3 - 5 mL, and will be injected intravenously as a bolus injection. Vital signs, adverse event assessment, and 12 lead ECGs will be performed on day 1 before and after dosing.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
DIAGNOSTIC
Masking
NONE
Enrollment
20
Single IV dose (370 MBq, or 10 mCi) of CTT1057 followed by combined PET/MR imaging (prostate + whole body).
Radical prostatectomy with lymph node dissection
University of California San Francisco
San Francisco, California, United States
Adverse event frequency as graded by Common Toxicity Criteria version 4.03
Time frame: 7 days from time of injection
Organ dosimetry/tissue uptake of CTT1057 as measured by PET/MR imaging of prostate cancer
Time frame: Up to six hours from time of injection
Pharmacokinetic profile of CTT1057 as measured by radiotracer detection in blood samples
Time frame: Up to four hours from time of injection
Level of CTT1057 uptake on PET/MR imaging of localized prostate cancer with PSMA protein expression by immunohistochemistry from subsequent radical prostatectomy specimens
Time frame: 12 weeks
Optimal Standardized Uptake Value (SUV) ratio threshold on CTT1057 PET/MR for discriminating tumor pathology from primary prostate cancer tissue
Time frame: 4 hours
Sensitivity and specificity of CTT1057 PET imaging on a lesion-by-lesion basis as compared with standard imaging in metastatic prostate cancer
Time frame: 4 hours
Number of positive lesions on CTT1057 PET/MR in subjects with equivocal or negative conventional imaging scans
Time frame: 4 hours
Location of positive lesions on CTT1057 PET/MR in subjects with equivocal or negative conventional imaging scans
Time frame: 4 hours
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