Porphyrin-based compounds for tumor imaging and photodynamic therapy

A technology of compound and porphyrin, which is applied in the field of porphyrin-based compounds for tumor imaging and photodynamic therapy, can solve the problems of deep malignant lesions, impractical PDT, and inaccessibility of singlet oxygen product light, and achieve high The effect of tumor uptake

Active Publication Date: 2006-10-04
HEALTH RES INC +1
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Problems solved by technology

Superficially visible lesions or those endoscopically detectable, such as endobronchial or esophageal tumors, are easily treatable, but most malignant lesions are too deep for the wavelengths required to elicit singlet oxygen production in the current generation of photosensitizers the light does not reach
Although technology has long been developed to deliver therapeutic light to deep lesions via optical fibers "capped" by terminal diffusers, deep lesions are certainly invisible from the skin surface, making PDT of deep tumors highly impractical

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  • Porphyrin-based compounds for tumor imaging and photodynamic therapy
  • Porphyrin-based compounds for tumor imaging and photodynamic therapy
  • Porphyrin-based compounds for tumor imaging and photodynamic therapy

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Embodiment Construction

[0034] Based on the research on a series of alkyl ether analogues of pyropheophorbide-a, the inventors developed a photosensitizer that absorbs relatively long wavelengths, 3-(1-hexyl oxy)ethyl-derivatives (HPPH). The compound is tumor-avid and is currently in Phase I / II human clinical trials at the Roswell Park Cancer Institute. The inventors have studied this compound and single-or bis-diaminoethanethiol (N 2 S 2 Ligand) in conjunction with use as a "vehicle". Results obtained from in vivo biodistribution assays indicated that tumor / non-tumor uptake rates of drugs depended on time and tumor size. The clearance of HPPH-based compounds from tumors was found to be slower in time than from most non-tumor tissues. However, found 99m The short 6-hour half-life of Tc does not match the 24-hour imaging time, suggesting that the use of longer-lived isotopes could provide useful scanning agents. Another approach to the development of improved tumor imaging agents could be to rep...

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Abstract

This invention describes a first report on the synthesis of certain 124 I-labelled photosensitizers related to chlorines and bacteriochlorins with long wavelength absorption in the range of 660-800 nm. In preliminary studies, these compounds show a great potential for tumor detection by positrom emission tomography (PET) and treatment by photodynamic therapy (PDT). The development of tumor imaging or improved photodynamic therapy agent(s) itself represent an important step, but a dual function agent (PET imaging and PDT) provides the potential for diagnostic body scan followed by targeted therapy.

Description

[0001] Statement Regarding Federally Sponsored Research [0002] This invention was made with funding from the National Institutes of Health grant numbers NIH (1R21 CA109914-01 and CA 55792). The United States Government may have certain rights in this invention. Background of the invention [0003] The application of radiometal-labeled complexes and biomolecules as diagnostic agents is a relatively new field of medicinal chemistry. right 99m The study of Tc radiopharmaceuticals is the beginning of coordination chemistry research as it relates to diagnostic imaging. Since then, the development of novel radiopharmaceuticals for early diagnosis has been an active area of ​​functional imaging. Imaging modalities widely used in nuclear medicine in recent years include gamma scintigraphy and positron emission tomography (PET). Gamma scintigraphy requires radiopharmaceuticals containing gamma-ray-emitting nuclides, and a gamma camera or SPECT (single photon emission tomography) ...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/22A61K49/00
CPCC07H17/02C07D487/22A61K51/0485A61P35/00A61P43/00B32B21/04B32B3/266B32B2305/38
Inventor 拉温德拉·K·潘迪穆纳瓦尔·萨贾德苏雷什·潘迪艾米·格里舒克艾伦·奥塞罗夫哈尼·A·纳比
Owner HEALTH RES INC
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