# Theranostic NTSR1-targeting Agents for Complementary Management of PSMA-negative Prostate Cancer

> **NIH NIH R43** · ACCUNOVO BIOTECHNOLOGIES INC · 2022 · $376,447

## Abstract

Project Summary
The long-term goal of this project is to develop a theranostic (for both diagnosis and therapy) agent targeting
neurotensin receptor 1 (NTSR1) for prostate cancer management.
Prostate cancer is the second-leading cause of cancer deaths for men in the United States. Approximately 1 in
9 men will be diagnosed with prostate cancer in their lifetime. Despite recent developments in its diagnosis and
treatments, the advanced stages of prostate cancer still have poor survival rates. In fact, patients with advanced
stage prostate cancer may initially respond to hormone therapy with more than 90% rate, but they could relapse
into the hormone-refractory state and generally die within 3 years. Clearly, this urgent unmet need warrants
further exploration of clinically relevant molecular targets for patient screening, detection of metastatic disease,
and corresponding treatment strategies. Accumulating evidence suggests that neurotensin (NTS) and
neurotensin receptors (NTSRs) play key roles in prostate cancer progression. In our recent histology analysis,
all examined PSMA-negative prostate cancer tissues were found to have positive NTSR1 expression, suggesting
the potential complementary role of NTSR1 targeted imaging/therapy towards PSMA based imaging/therapy. In
another word, NTSR1 targeted therapy could be used when PSMA targeted therapy fails.
In this project, AccuNovo Biotech Inc. will partner with Profs. Zibo Li and Rihe Liu at UNC Chapel Hill to develop
new theranostic agents targeting NTSR1 based on the recent progress on ligand discovery. Recently, we found
that the introduction of crosslinked polyamines into SR142948A (leading to new agent SR-CP-05) could increase
the tumor uptake by 10 times compared with peptide-based agent. This discovery offered us an unprecedented
opportunity to develop NTSR1 targeted theranostic agents. We will focus on imaging agent development in
Phase I. The specific aims of this proposal are: Aim 1: Develop 64Cu labeled NTSR1-targeting PET agents with
high and persistent tumor uptake; Aim 2: Perform side-by-side comparison of lead agents in prostate cancer
mouse models and select the best agent for Phase II efficacy study. The success of this project will not only lead
to an accurate imaging-based method to efficiently detect NTSR1 expression in prostate cancer (for patient
screening and treatment monitoring), but also be further developed into a radionuclide-based agent for prostate
cancer therapy.

## Key facts

- **NIH application ID:** 10484532
- **Project number:** 1R43CA261503-01A1
- **Recipient organization:** ACCUNOVO BIOTECHNOLOGIES INC
- **Principal Investigator:** Xiaomei Li
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $376,447
- **Award type:** 1
- **Project period:** 2022-04-05 → 2024-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10484532

## Citation

> US National Institutes of Health, RePORTER application 10484532, Theranostic NTSR1-targeting Agents for Complementary Management of PSMA-negative Prostate Cancer (1R43CA261503-01A1). Retrieved via AI Analytics 2026-05-25 from https://api.ai-analytics.org/grant/nih/10484532. Licensed CC0.

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