[177Lu]Lu-PSMA I&T Composition Stability

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Solution Overview

Problem

There is a clinical need for an effective treatment method for metastatic castration-resistant prostate cancer (mCRPC) that minimizes undesired cumulative absorbed doses of radiation to healthy organ tissue.

Innovation Solution

The development of an improved [177Lu]Lu-PSMA I&T composition that maintains radiochemical purity of ≥95% for extended periods, allowing for administration more than 48 hours after formulation, with a molar ratio of PSMA I&T to 177Lu ranging from 3.0:1.0 to 8.0:1.0, and a PSMA I&T to [177Lu]Lu3+ ratio of 0.20 to 0.60 μg:mCi, thereby reducing radiation absorbed by healthy organs.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If small molecule inhibitors targeting PSMA with 177Lu are used to treat prostate cancer, then treatment efficacy is improved, but undesired absorbed doses of radiation to healthy organs increase

Engineering Contradiction:

Improvetreatment efficacyVSAvoidradiation dose to healthy organs

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the molar ratio of PSMA I&T to 177Lu (3.0:1.0 to 8.0:1.0) and controls the PSMA I&T to [177Lu]Lu3+ ratio (0.20 to 0.60 μg:mCi) to achieve stable radiochemical purity while minimizing radiation dose to healthy organs. This parameter optimization allows effective cancer treatment with reduced toxicity to healthy tissue.

Inventive Principle:

Principle #35Parameter changes

2Duration of action of moving object

If the composition is formulated for stable radiochemical purity over extended periods, then administration flexibility is improved, but formulation complexity increases

Engineering Contradiction:

Improveradiochemical purity durationVSAvoidformulation complexity

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent specifies precise formulation parameters including pH range (3.0 to 6.0), ascorbic acid concentration (25-40 mg/ml), and chelating agent concentration (0.075-0.15 mg/ml) to achieve stable radiochemical purity of ≥95% for more than 48 hours. These optimized parameters enable extended administration flexibility without requiring complex formulation systems.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20250121103A1[177lu] lutetium-PSMA i&t composition and dosimetry, kit, method of making, and method of using thereof

Publication Date: 2025.04.17 CURIUM US LLC

AI summary

The present disclosure relates to a radiopharmaceutical compositions, methods, and kits comprising 177Lu-PSMA I&T. The compositions, methods, and kits may have a molar ratio of the PSMA I&T to 177Lu from greater than 8.0:1.0 to 11.0:1.0. The composition may be formulated as a solution for injection and the solution is suitable for administration at least 72 hours after formulation. The composition(s) have a radiochemical purity (RCP) of 95% or greater, 95.5% or greater, 96% or greater, 96.5% or greater, 97% or greater, 97.5% or greater, 98.0% or greater, 98.5% or greater, 99% or greater, or 99.5% or greater at administration.