# Development of a Commercial-Ready Kit for CTT1403, a Novel PSMA-Targeted Radiotherapy

> **NIH NIH R44** · CANCER TARGETED TECHNOLOGY, LLC · 2022 · $999,998

## Abstract

PROJECT ABSTRACT
Prostate-Specific Membrane Antigen (PSMA) is an ideal tumor biomarker with specific expression on >90% of
all prostate cancers that increases with disease progression. Cancer Targeted Technology (CTT) has developed
an innovative phosphoramidate-based peptidomimetic that binds irreversibly to PSMA, leading to >90%
internalization and selective accumulation in tumor cells. With previous SBIR grant support, CTT developed and
evaluated an 18F-labeled PET diagnostic imaging agent, CTT1057. In a Phase 1 clinical trial, CTT1057
demonstrated significant uptake in PSMA-avid bone and visceral lesions in prostate cancer (PCa) patients with
far greater accuracy than standard of care scans. CTT1057 was subsequently licensed to Advanced Accelerator
Applications/Novartis. CTT then modified the novel scaffold to develop a specific and potent companion
therapeutic, CTT1403, radiolabeled with 177Lu. CTT1403, unlike other PSMA-targeting agents in development,
not only binds irreversibly to PSMA but also incorporates an albumin-binding motif to dramatically slow blood
clearance, resulting in unprecedented tumor uptake of >80% that translates to a significant survival advantage
in animal models. Manually radiomanufactured CTT1403 is currently in a 40-patient Phase 1 trial in men with
castration resistant PCa and to date has demonstrated an excellent safety profile, extended blood circulation
time, extended tumor exposure and low uptake in kidney and other dose limiting normal organs. With excellent
drug characteristics and a high likelihood of efficacy, the development of a reliable, robust and efficient CTT1403
manufacturing and distribution strategy is critical for subsequent clinical trials with very large patient cohorts.
Automated, kit-based radiomanufacture has proven rapid, robust, and reproducible for benchmark agents like
18F-FDG. Development of a novel CTT1403 manufacturing process that facilitates automation will expand access
to CTT1403 for radiopharmacies across the United States, increasing availability for pivotal clinical trials and
potential for subsequent market and commercialization success. In this SBIR Direct to Phase II grant, we will
develop a novel, simplified method for CTT1403 synthesis by developing a new drug precursor, CTT2001, for
direct (1-step) 177Lu radiolabeling to be converted to a kit format for use in an automated synthesizer. This
process and automation will reduce cost of goods, manufacturing time, and increase distribution efficiency. AIM
1: Demonstrate feasibility of a PSMA-targeted 1-step radiolabeling process. CTT will manufacture the
CTT2001 precursor, develop a simple and efficient CTT1403 radiolabeling process, and assess whether the
PSMA-targeting function remains intact. AIM 2: Develop an automated kit formulation for CTT1403
synthesis, on the Trasis synthesizer, will include a custom designed, disposable cassette and a custom kit of
pre-measured reagents for simple and robust 177Lu labeling. CTT1403 re...

## Key facts

- **NIH application ID:** 10491276
- **Project number:** 5R44CA257799-02
- **Recipient organization:** CANCER TARGETED TECHNOLOGY, LLC
- **Principal Investigator:** Hunter Nicole Bomba
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $999,998
- **Award type:** 5
- **Project period:** 2021-09-20 → 2024-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10491276

## Citation

> US National Institutes of Health, RePORTER application 10491276, Development of a Commercial-Ready Kit for CTT1403, a Novel PSMA-Targeted Radiotherapy (5R44CA257799-02). Retrieved via AI Analytics 2026-06-14 from https://api.ai-analytics.org/grant/nih/10491276. Licensed CC0.

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