WO2018081262A1 - Detectable molecules that target and bind to malignant tumors and not benign tumors - Google Patents

Detectable molecules that target and bind to malignant tumors and not benign tumors Download PDF

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Publication number
WO2018081262A1
WO2018081262A1 PCT/US2017/058276 US2017058276W WO2018081262A1 WO 2018081262 A1 WO2018081262 A1 WO 2018081262A1 US 2017058276 W US2017058276 W US 2017058276W WO 2018081262 A1 WO2018081262 A1 WO 2018081262A1
Authority
WO
WIPO (PCT)
Prior art keywords
bind
tumors
malignant
benign
target
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2017/058276
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English (en)
French (fr)
Inventor
Steven D. Jensen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Cao Group Inc
Original Assignee
Cao Group Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Cao Group Inc filed Critical Cao Group Inc
Priority to CN201780071462.4A priority Critical patent/CN109982721A/zh
Priority to JP2019523046A priority patent/JP2019536015A/ja
Priority to US16/345,073 priority patent/US20190255195A1/en
Publication of WO2018081262A1 publication Critical patent/WO2018081262A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/006—Biological staining of tissues in vivo, e.g. methylene blue or toluidine blue O administered in the buccal area to detect epithelial cancer cells, dyes used for delineating tissues during surgery
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61B—DIAGNOSIS; SURGERY; IDENTIFICATION
    • A61B5/00—Measuring for diagnostic purposes; Identification of persons
    • A61B5/0059—Measuring for diagnostic purposes; Identification of persons using light, e.g. diagnosis by transillumination, diascopy, fluorescence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/70—Mechanisms involved in disease identification
    • G01N2800/7023—(Hyper)proliferation
    • G01N2800/7028—Cancer

Definitions

  • the present invention discloses detectable molecules that target and bind to malignant tumors and not benign tumors, and related methods.
  • Embodiments of the present invention provide detectable molecules that target and bind to malignant tumors and not benign tumors, and related methods.
  • the contemporary means to determine if a tumor is malignant or benign is usually a biopsy followed by a histological examination.
  • a biopsy of a malignant tumor is a high-risk surgical operation as it cuts into the tumor and dislodges cancerous cells that can be circulated throughout the body via the blood stream (metastasize).
  • a biopsy of a malignant tumor is a means to increase the spread of cancer throughout the body.
  • the present invention utilizes targeting molecules that when circulated within the bloodstream tend to bind to malignant cells and minimize attachment to healthy tissue cells and benign tumor cells.
  • the targeting molecule is designed to be detectable such that it can be identified by various means such as an MRI, X-ray, ultrasound, chromatically visible to the eye, and any other useful means of detection.
  • a medical professional by practice of the present invention would introduce the targeting molecule into the bloodstream of the patient and allow the molecule to circulate and bind or not to bind to the tumor(s) in question. After a prescribed interval, the practitioner would examine the tumor site with respect to the detection properties of the targeting molecule; this is done by various means such as an MRI, X-ray, ultrasound, chromatically visible to the eye, and any other useful means of detection. For example, if the targeting molecule was radiopaque, then an X-ray radiograph would be utilized to determine if the targeting molecule accumulated within the tumor in question or not. The detection of a malignant tumor would be determined if the tumor was radiographic ally anomalous.
  • the present invention utilizes peptides, polypeptides, polymers, proteins, biopolymers and phospholipids as targeting molecules that are known to collect and bind within cancer cells.
  • An embodiment of the present invention prefers targeting molecules that bind to fibrin and fibrinogen.
  • Another embodiment of the present invention prefers targeting molecules that have an affinity to bind to pleomorphic cells.
  • Another embodiment of the present invention prefers targeting molecules that have an affinity to bind to neoplastic cells.
  • Another embodiment of the present invention prefers targeting molecules that bind to both malignant and benign tumors, yet takes advantage of the differences in cell densities within these tumors such that there is a measurable difference between malignant and benign tumors that can be quantified and measured.
  • Another embodiment of the present invention prefers targeting molecules that bind to DNA.
  • Another embodiment of the present invention prefers targeting molecules that bind to the nucleus.
  • a list of peptides, polypeptides, polymers, biopolymers and proteins that have an affinity to bind fibrinogen and fibrin are found in United States Patent No. 8,513,380 and is hereby incorporated in its entirety by reference. United States Patent No. 8,513,380 also disclose the means of manufacture and the means to discover additional peptides when applied in practice.
  • Phospholipids that have an affinity to bind to cancer cells are found in United States Patent No. 4,935,520 and is hereby incorporated in its entirety by reference. United States Patent No. 4,935,520 also disclose the means of manufacture and the means to discover additional peptides when applied in practice.
  • the present invention is designed to target the inherent differences between malignant and benign cells within a tumor such as: cell density, cellular and nuclear pleomorphism, the nuclear to cytoplasmic ratio, DNA density, nuclear density, and any other useful differentiation between cells and tumors alike.
  • An embodiment of the present invention selects targeting molecules that have a greater affinity to bind to malignant tumors and at the same time minimizes binding to benign tumors and healthy tissue; to these are added chemical moieties that allow them to be detected by various means such as an MRI, X-ray, ultrasound, chromatically visible to the eye, and any other useful means of detection.
  • a radio-opaque targeting molecule is created by adding a radio-opaque moiety onto a peptide, polypeptides, polymers, proteins, biopolymers and
  • the present invention utilizes heavy elements as a source of radio- opaque substances such as: iodine, bromine, calcium, barium, strontium, bismuth, tungsten, zirconium, iron, copper, nickel, zinc, silver, tin, gallium, antimony, palladium, rhodium, yttrium, molybdenum, cobalt, chromium, titanium, vanadium, magnesium, gold, platinum, and iridium and any other radiographically visible substance.
  • radio-opaque substances can be used in their elemental form, as a salt, bound in chelated form, or as an organometallic compound. Any radio-opaque moiety that can be attached to a targeting molecule that does not inhibit the resultant compound' s ability to collect and bind to cancer cells is within the scope of this patent.
  • a MRI detectable targeting molecule is created by adding a MRI contrasting moiety onto a peptide, polypeptides, polymers, proteins, biopolymers and phospholipids.
  • the present invention utilizes gadolinium, iron oxides, iron platinum, manganese, and any other MRI contrastable agent as MRI contrasting moieties.
  • These MRI contrasting moieties can be used in their elemental form, as a salt, bound in chelated form, or as an organometallic compound. Any MRI contrasting moiety that can be attached to a targeting molecule that does not inhibit the resultant compound' s ability to collect and bind to cancer cells is within the scope of this patent.
  • a chromatic targeting molecule is created by adding a chromatic moiety onto a peptide, polypeptides, polymers, proteins, biopolymers and phospholipids.
  • the present invention utilizes: conjugated organic compounds, organometallic compounds and any other useful compounds of color. Any chromatic moiety that can be attached to a targeting molecule that does not inhibit the resultant compound' s ability to collect and bind to cancer cells is within the scope of this patent.
  • a targeting molecule that is detectable by ultrasound is created by adding a hollow nano-sphere moiety onto a peptide, polypeptides, polymers, proteins, biopolymers and phospholipids.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Surgery (AREA)
  • Molecular Biology (AREA)
  • Medical Informatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pathology (AREA)
  • Biodiversity & Conservation Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Optics & Photonics (AREA)
  • Biophysics (AREA)
  • Magnetic Resonance Imaging Apparatus (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
PCT/US2017/058276 2016-10-26 2017-10-25 Detectable molecules that target and bind to malignant tumors and not benign tumors Ceased WO2018081262A1 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CN201780071462.4A CN109982721A (zh) 2016-10-26 2017-10-25 靶向并结合恶性肿瘤而非良性肿瘤的可检测分子
JP2019523046A JP2019536015A (ja) 2016-10-26 2017-10-25 良性腫瘍ではなく悪性腫瘍を標的とし、かつ結合する検出可能な分子
US16/345,073 US20190255195A1 (en) 2016-10-26 2017-10-25 Detectable molecules that target and bind to malignant tumors and not to benign tumors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662412948P 2016-10-26 2016-10-26
US62/412,948 2016-10-26

Publications (1)

Publication Number Publication Date
WO2018081262A1 true WO2018081262A1 (en) 2018-05-03

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/058276 Ceased WO2018081262A1 (en) 2016-10-26 2017-10-25 Detectable molecules that target and bind to malignant tumors and not benign tumors

Country Status (4)

Country Link
US (1) US20190255195A1 (enExample)
JP (1) JP2019536015A (enExample)
CN (1) CN109982721A (enExample)
WO (1) WO2018081262A1 (enExample)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130059758A1 (en) * 2010-05-23 2013-03-07 Technion Research And Development Foundation Ltd. Detection, Staging and Grading of Benign and Malignant Tumors
US20160017292A1 (en) * 2012-11-08 2016-01-21 Whitehead Institute For Biomedical Research Selective targeting of cancer stem cells

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040047804A1 (en) * 1998-10-29 2004-03-11 The General Hospital Corporation, A Massachusetts Corporation Enhanced radiation therapy
CN102372771A (zh) * 2010-08-26 2012-03-14 杨静雯 一种肿瘤靶向分子及其应用
CN104892820B (zh) * 2015-05-11 2017-08-04 厦门大学 一种受体类分子靶向显像剂及其制备方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130059758A1 (en) * 2010-05-23 2013-03-07 Technion Research And Development Foundation Ltd. Detection, Staging and Grading of Benign and Malignant Tumors
US20160017292A1 (en) * 2012-11-08 2016-01-21 Whitehead Institute For Biomedical Research Selective targeting of cancer stem cells

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DOMANN JR. ET AL.: "Constitutive AP -1 DNA Binding and Transactivating Ability of Malignant but not Benign Mouse Epidermal Cells", MOLECULAR CARCINOGENESIS, vol. 9, February 1994 (1994-02-01), pages 61 - 66 *

Also Published As

Publication number Publication date
CN109982721A (zh) 2019-07-05
US20190255195A1 (en) 2019-08-22
JP2019536015A (ja) 2019-12-12

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