Imaging probes, methods of making imaging probes, and methods of imaging

• US 8,753,605 B2
• Filed: 08/30/2011
• Issued: 06/17/2014
• Est. Priority Date: 08/31/2010
• Status: Active Grant

• Current Assignee: Board of Trustees of the Leland Stanford Junior University (Stanford Management Co.)
• Original Assignee: Board of Trustees of the Leland Stanford Junior University (Stanford Management Co.)
• Inventors: Cheng, Zhen, Gambhir, Sanjiv Sam, Miao, Zheng, Liu, Hongguang, Ren, Gang
• Primary Examiner(s): Jones, D L
• Application Number:
  US13/199,428
• Publication Number:
  US 20120052009A1
• Time in Patent Office: 1,022 Days
• Field of Search: 424/1.11, 424/1.65, 424/1.69, 424/1.81, 424/1.85, 424/1.89, 424/9.1, 424/9.2, 424/9.3, 424/9.4, 424/9.5, 424/9.6, 424/9.7, 424/9.8, 514/1, 514/1.1, 530/300, 530/317, 530/324, 530/333, 530/338
• US Class Current: 424/1.89
• CPC Class Codes: A61K 38/16 Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof enzyme inhibitors A61K38/005
• CPC Class Codes: A61K 49/0004 Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
• CPC Class Codes: A61K 49/0008 Screening agents using (non-human) animal models or transgenic animal models or chimeric hosts, e.g. Alzheimer disease animal model, transgenic model for heart failure
• CPC Class Codes: A61K 49/14 Peptides, e.g. proteins
• CPC Class Codes: A61K 51/08 Peptides, e.g. proteins , carriers being peptides, polyamino acids, proteins
• CPC Class Codes: A61K 51/088 conjugates with carriers being peptides, polyamino acids or proteins antibodies A61K51/10
• CPC Class Codes: G01N 2333/71 for growth factors; for growth regulators
• CPC Class Codes: G01N 33/574 for cancer
• CPC Class Codes: G01N 33/74 involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors

Abstract

In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein, embodiments of the present disclosure, in one aspect, relate to methods of detecting the over-expression of epidermal growth factor receptor (EGFR) in a subject or sample, methods of diagnosing the presence of one or more angiogenesis related diseases or related biological events in a subject or sample, method of monitoring the progress of one or more angiogenesis related diseases or related biological events in a subject or sample, a ¹⁸F-FBEM-CYS-Z_EGFR:1907 probe, compositions including a ¹⁸F-FBEM-CYS-Z_EGFR:1907 probe, and pharmaceutical compositions including a ¹⁸F-FBEM-CYS-Z_EGFR:1907 probe and the like.

Claims

1. A method of detecting the over-expression of epidermal growth factor receptor (EGFR) in a subject, comprising:

administering to the subject a ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z<sub>EGFR;

1907</sub> is SEQ ID NO;

1, and CYS is cysteine;

imaging at least a portion of the subject; and

detecting the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein the location of the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe corresponds to the over-expression of the EGFR.

2. A method of diagnosing the presence of a cancer or tumor in a subject comprising:

administering to the subject a ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z_EGFR;

1907 is SEQ ID NO;

1, and CYS is cysteine;

imaging at least a portion of the subject; and

detecting the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein the location of the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe corresponds to the over-expression of the EGFR, wherein over-expression of EGFR corresponds to a cancer or tumor.

3. A method of diagnosing the presence of a cancer or tumor in a sample comprising:

contacting or administering to the sample a ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z_EGFR;

1907 is SEQ ID NO;

1, and CYS is cysteine;

imaging at least a portion of the sample; and

detecting the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein the location of the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe corresponds to the over-expression of the EGFR, wherein over-expression of EGFR corresponds to a cancer or tumor.

4. A method of monitoring the progress of a cancer or tumor in a subject comprising:

contacting or administering to the subject a ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z<sub>EGFR;

1907</sub> is SEQ ID NO;

1, and CYS is cysteine;

imaging at least a portion of the subject; and

detecting the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein the location of the 18F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe corresponds to the over-expression of the EGFR, wherein over-expression of EGFR corresponds to a cancer or tumor, wherein the size of the location is monitored over time.

5. A method of monitoring the progress of a cancer or tumor in a sample comprising:

contacting or administering to the sample a ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z<sub>EGFR;

1907</sub> is SEQ ID NO;

1, and CYS is cysteine;

imaging at least a portion of the sample; and

detecting the ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein the location of the 18F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe corresponds to the over-expression of the EGFR, wherein over-expression of EGFR corresponds to a cancer or tumor, wherein the size of the location is monitored over time.

6. A probe, comprising:

a ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z<sub>EGFR;

1907</sub> is SEQ ID NO;

1, and CYS is cysteine.

7. A composition, comprising:

a ¹⁸F-FBEM-CYS-Z_EGFR-1907 probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z<sub>EGFR;

1907</sub> is SEQ ID NO;

1, and CYS is cysteine.

8. A pharmaceutical composition, comprising:

a pharmaceutical carrier and an effective dose of a ¹⁸F-FBEM-CYS-Z<sub>EGFR;

1907</sub> probe, wherein ¹⁸F-FBEM is N-2-(4-¹⁸F-fluorobenzamido)ethyl-maleimide), wherein Z<sub>EGFR;

1907</sub> is SEQ ID NO;

1, and CYS is cysteine.