Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
  • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
  • A61K51/04—Organic compounds
  • A61K51/06—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules
  • A61K51/065—Macromolecular compounds, carriers being organic macromolecular compounds, i.e. organic oligomeric, polymeric, dendrimeric molecules conjugates with carriers being macromolecules
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K49/00—Preparations for testing in vivo
  • A61K49/0002—General or multifunctional contrast agents, e.g. chelated agents
• • 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
  • A61K49/0013—Luminescence
  • A61K49/0017—Fluorescence in vivo
  • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
  • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
  • A61K49/0032—Methine dyes, e.g. cyanine dyes
• • 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
  • A61K49/0013—Luminescence
  • A61K49/0017—Fluorescence in vivo
  • A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
  • A61K49/0054—Macromolecular compounds, i.e. oligomers, polymers, dendrimers

Definitions

• a composition as described herein can have a high affinity for CD206 on TAMs.
• High affinity binding of CD206 and its ligands can rely on multivalent interactions between sugars displayed on the ligands and multiple CBDs on CD206.
• the term "subject” can be a vertebrate, such as a mammal, a fish, a bird, a reptile, or an amphibian.
• the subject of the herein disclosed methods can be a human, non- human primate, horse, pig, rabbit, dog, sheep, goat, cow, cat, guinea pig or rodent.
• the term does not denote a particular age or sex. Thus, adult and newborn subjects, as well as fetuses, whether male or female, are intended to be covered.
• the subject is a mammal.
• a patient refers to a subject afflicted with a disease or disorder.
• patient includes human and veterinary subjects.
• the effective daily dose can be divided into multiple doses for purposes of administration. Consequently, single dose compositions can contain such amounts or submultiples thereof to make up the daily dose.
• the dosage can be adjusted by the individual physician in the event of any contraindications. Dosage can vary, and can be administered in one or more dose administrations daily, for one or several days. Guidance can be found in the literature for appropriate dosages for given classes of pharmaceutical products.
• Preferred carbocyclic groups include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, and cycloheptyl. More preferred carbocyclic groups include cyclopropyl and cyclobutyl. The most preferred carbocyclic group is cyclopropyl.
• Certain materials, compounds, compositions, and components disclosed herein can be obtained commercially or readily synthesized using techniques generally known to those of skill in the art.
• the starting materials and reagents used in preparing the disclosed compounds and compositions are either available from commercial suppliers such as Aldrich Chemical Co., (Milwaukee, Wis.), Acros Organics (Morris Plains, N.J.), Fisher Scientific (Pittsburgh, Pa.), or Sigma (St.
• suitable diagnostic moieties include, but are not limited to: -contrast agents suitable for magnetic resonance imaging (MRI), such as gadolinium (Gd 3+ ), paramagnetic and superparamagnetic materials such as superparamagnetic iron oxide;
• MRI magnetic resonance imaging
• gadolinium (Gd 3+ ) paramagnetic and superparamagnetic materials
• superparamagnetic iron oxide superparamagnetic iron oxide
• the linker may be a straight chain or branched.
• bifunctional linkers include:
• a backbone comprised of dextran
• the imaging of a subject can be done using planar gamma imaging wherein an image comprises visual indications of uptake of said compound in one or more tumors in the subject.
• the method is for imaging tumors that are not a result of breast cancer.
• the composition further comprises a therapeutic agent.
• Certain embodiments described herein comprise a composition for detecting one or more metastasized tumors, comprising: 99m Tc-tilmanocept, wherein said composition is used for detecting one or more metastasized tumors. Certain embodiments can comprise a composition used for quantifying the size of a tumor, including estimating its mass and size.
• Certain embodiments can comprise a composition comprising a dextran backbone having one or more CD206 targeting moieties and one or more therapeutic moieties attached thereto.
• Certain methods can comprise the steps of administering a composition comprising a dextran backbone having one or more CD206 targeting moieties and one or more diagnostic moieties to a subject; imaging the subject using SPECT/CT; and determining the presence of tumor-associated macrophages.
• Certain embodiments may further comprise the step of quantifying the number of tumor- associated macrophages.
• Certain embodiments comprise the step of identifying the presence of tumors.
• Certain embodiments comprise the step of identifying metastases of previously-existing tumors.
• Certain embodiments comprise the step of administering a composition as described herein comprising a therapeutic agent for
• Mannosylated constructs such as the ones discussed herein, including 99m Tc tilmanocept, and FDG are both molecular markers relevant to tumor biology and progressions.
• the results shown in Fig. 6 show that 99m Tc tilmanocept binding may detect TAMS surrounding liver metastases.
• the diagnostic, prognostic, and therapeutic implications of TAM imaging in metastasized liver CRC remains to be determined, but mannosylated-based agents may serve to aid in targeting TAMs with a therapeutic payload, where response may be directly monitored through mannosylated-construct imaging.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Animal Behavior & Ethology (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Epidemiology (AREA)
• Biomedical Technology (AREA)
• Engineering & Computer Science (AREA)
• Pharmacology & Pharmacy (AREA)
• Physics & Mathematics (AREA)
• Optics & Photonics (AREA)
• Proteomics, Peptides & Aminoacids (AREA)
• Medicinal Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)
• Measuring And Recording Apparatus For Diagnosis (AREA)

Priority Applications (5)

Applications Claiming Priority (2)

Publications (1)

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Cited By (1)

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Citations (4)

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• 2018
  • 2018-07-20 WO PCT/US2018/043176 patent/WO2019018815A1/en not_active Ceased
  • 2018-07-20 JP JP2020502669A patent/JP2020528059A/ja active Pending
  • 2018-07-20 US US16/041,673 patent/US20190022259A1/en not_active Abandoned
  • 2018-07-20 CA CA3070494A patent/CA3070494A1/en active Pending
  • 2018-07-20 CN CN201880061342.0A patent/CN111447955A/zh active Pending
  • 2018-07-20 EP EP18834762.9A patent/EP3655107A4/en not_active Withdrawn
• 2020
  • 2020-01-19 IL IL272123A patent/IL272123A/en unknown

Patent Citations (4)

Non-Patent Citations (3)

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