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MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
First-in-human Evaluation of a Prostate-specific Membrane Antigen-targeted Near-infrared Fluorescent Small Molecule
Hao G Nguyen1, Nynke S van den Berg2, Alexander L Antaris2
1Department of Urology, Helen Diller Family Comprehensive Cancer Center, University of California, San Francisco, CA, USA.
Background:
Men with high-risk prostate cancer undergoing surgery likely recur due to failure to completely excise regional and/or local disease.
Objective:
The first-in-human evaluation of safety, pharmacokinetics, and exploratory efficacy of IS-002, a novel near-infrared prostate-specific membrane antigen (PSMA)-targeted fluorescence imaging agent, designed for intraoperative prostate cancer visualization.
Design, Setting, And Participants:
A phase 1, single-center, dose-escalation study was conducted in 24 men with high-risk prostate cancer scheduled for robotic-assisted radical prostatectomy with (extended) pelvic lymph node dissection using the da Vinci surgical system.
Outcome Measurements And Statistical Analysis:
Adverse events (AEs), vital signs, complete blood count, complete metabolic panel, urinalysis, and electrocardiogram were assessed over a 14-d period and compared with baseline. The pharmacokinetic profile of IS-002 was determined. Diagnostic accuracy was assessed for exploratory efficacy.
Results And Limitations:
AEs predominantly included discoloration of urine (n = 22/24; expected, related, grade 1). There were no grade ≥2 AEs. IS-002 Cmax and area under the curve increased with increasing dose. Plasma concentrations declined rapidly in a biphasic manner, with the median terminal half-lives ranging from 5.0 to 7.6 h, independent of dose and renal function. At 25 μg/kg, the exploratory efficacy readouts for the negative and positive predictive values were, 97% and 45% for lymph nodes, and 100% and 80% for residual/locoregional disease detection, respectively.
Conclusions:
IS-002 is safe and well tolerated, and has the potential to enable intraoperative tumor detection that could not be identified using standard imaging.
Patient Summary:
IS-002 is a new imaging agent that specifically targets the prostate-specific membrane antigen receptor. In this study, we tested IS-002 for the first time in men with high-risk prostate cancer undergoing surgery and found that IS-002 is safe, is cleared from the body quickly, and potentially allows identification of prostate cancer in areas that would not be identified by conventional white light imaging.
Insights
This study shows IS-002, a new imaging agent for prostate cancer, is safe and well-tolerated. It has the potential to improve intraoperative tumor detection during surgery for high-risk prostate cancer.
Area of Science:
- Oncology
- Surgical Imaging
- Pharmacokinetics
Background:
- High-risk prostate cancer surgery recurrence is often due to incomplete excision of regional/local disease.
- Novel imaging agents are needed for intraoperative visualization to improve surgical outcomes.
Purpose of the Study:
- To evaluate the safety, pharmacokinetics, and exploratory efficacy of IS-002, a novel near-infrared PSMA-targeted fluorescence imaging agent.
- To assess IS-002's potential for intraoperative prostate cancer visualization during surgery.
Main Methods:
- Phase 1, single-center, dose-escalation study in 24 men with high-risk prostate cancer undergoing robotic-assisted radical prostatectomy.
- Safety assessments included adverse events, vital signs, and laboratory tests over 14 days.
- Pharmacokinetics and diagnostic accuracy for tumor detection were evaluated.
Main Results:
- IS-002 was safe and well-tolerated, with predominantly grade 1 urine discoloration as the main adverse event.
- Pharmacokinetic analysis showed rapid plasma clearance with median terminal half-lives of 5.0-7.6 hours.
- Exploratory efficacy at 25 μg/kg demonstrated high negative predictive values (97% for lymph nodes, 100% for residual disease).
Conclusions:
- IS-002 is a safe and well-tolerated imaging agent for high-risk prostate cancer.
- The agent's rapid clearance and favorable pharmacokinetic profile support its potential clinical utility.
- IS-002 may enable intraoperative detection of tumors not visible with standard imaging techniques.
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