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Chlorotoxin conjugates and methods of use thereof

A compound and alkylene technology, applied in the field of chlorotoxin conjugates and its use, can solve the problems of dependence, inaccurate intraoperative identification, and limitation of the degree of surgical resection

Pending Publication Date: 2016-07-27
BLAZE BIOSCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Unfortunately, intraoperative identification of tumor margins or small foci of cancerous cells remains imprecise or relies on surgical judgment
Therefore, the extent of surgical resection is limited by the need to avoid harming vital structures

Method used

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  • Chlorotoxin conjugates and methods of use thereof
  • Chlorotoxin conjugates and methods of use thereof
  • Chlorotoxin conjugates and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

example

[0839] The invention is further illustrated by the following non-limiting examples.

example 1

[0841] Stability of compound 16 with ammonium acetate salt

[0842]

[0843] A = MCMPCFTTDHQMARRCDDCCGGRGRGKCYGPQCLCR (K-27 is the attachment point)

[0844] This example demonstrates the production and stability of compound 16 over time under storage conditions at different pH and temperature.

[0845] The peptide portion of compound 16 is a targeting peptide (modified chlorotoxin) conjugated to a fluorescent dye. The targeting peptide selectively binds to cancerous cells and the dye moiety facilitates detection by imaging. The peptide is a modified chlorotoxin of 36 amino acids (with H-Met-Cys-Met-Pro-Cys-Phe-Thr-Thr-Asp-His-Gln-Met-Ala-Arg-Arg-Cys-Asp-Asp - the sequence of Cys-Cys-Gly-Gly-Arg-Gly-Arg-Gly-Lys-Cys-Tyr-Gly-Pro-Gln-Cys-Leu-Cys-Arg-OH) wherein three lysines in the natural chlorotoxin Two of the acidic amino acids were replaced by arginines (K15R and K23R) to facilitate subsequent conjugation of the fluorophore to a single residual lysine (K27) residue, thu...

example 2

[0872] Evaluation of the stability of compound 16 in different buffers and at different pH

[0873]

[0874] A = MCMPCFTTDHQMARRCDDCCGGRGRGKCYGPQCLCR (K-27 is the attachment point)

[0875] This example shows the stability of compound 16 with respect to pH and provides an evaluation using alternative buffers and different excipients and formulations.

[0876] This example further shows that different types of excipients protect compound 16 from heat, light, oxidation and freeze / thaw stress.

[0877] In some cases, the formulations were stored in microcentrifuge tubes in an air atmosphere and after 2d and 5d at 40°C in the dark, in the dark (dk) or at room temperature (rt) in ambient light (lt) Assays were performed after 3 d, and after 3X freeze-thaw (F / T) between -20°C and room temperature in the dark. By visual inspection, centrifugation, RP-HPLC, A 786 Formulations were evaluated by concentration, pH and SDS-PAGE.

[0878] In some cases, the time points were 4, 7, an...

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Abstract

Compositions, formulations and kits comprising chlorotoxin conjugate compounds are provided, including native and modified variants of chlorotoxin peptide conjugated to reporter molecules including fluorescent dyes. Methods of detecting and treating cancers and tumors with chlorotoxin conjugate compounds are also provided, including methods of imaging tumor tissues and cells. Dosing and pharmacokinetic profiles for therapeutic and diagnostic applications using chlorotoxin conjugate compounds are also provided.

Description

[0001] cross reference [0002] This application claims U.S. Provisional Application No. 61 / 879,096, filed September 17, 2013, U.S. Provisional Application No. 61 / 990,101, filed May 7, 2014, and U.S. Provisional Application No. 61 / 879,108, filed September 17, 2013 rights, which are hereby incorporated by reference in their entirety for all purposes. [0003] Statement of Federally Funded Research [0004] This invention was made with United States Government support under contract number HHSN261201200054C awarded by the National Cancer Institute, National Institutes of Health, Department of Health and Human Services. background of the invention [0005] For many types of cancer, the precision of surgical resection directly affects patient prognosis. Unfortunately, intraoperative identification of tumor margins or small foci of cancerous cells remains imprecise or dependent on surgical judgment. Thus, the extent of surgical resection is limited by the need to avoid harming v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/02A61K38/07C12N9/96
CPCC12N9/96A61K38/00G01N33/5743A61K49/0032A61K49/0056A61K9/0019A61K47/26A61K9/19A61K47/6415C07K14/43522A61P35/00A61K45/06
Inventor 克劳迪亚·约赫汉姆丹尼斯·M·米勒娜塔莉·奈恩马克·斯特劳德凯丽·伯恩斯-布莱克S·J·汉森J·E·诺瓦克V·R·维斯
Owner BLAZE BIOSCI
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