Imaging and radiotherapeutics agents targeting fibroblast-activation protein-α (FAP-α) and their use in imaging and treating FAP-α related diseases and disorders are disclosed.

This application relates to compounds of Formula (I-a) or Formula (I-b), or is salts or solvates thereof. R.sup.1 is —(CH.sub.2).sub.5CH.sub.3 or comprises 2-4 fused benzene rings. R.sup.2 is I, Br, F, Cl, H, OH, OCH.sub.3, NH.sub.2, NO.sub.2 or CH.sub.3. R.sup.3 is a peptide-bonded glycine, aspartate or glutamate or is glutamate peptide bonded through C.sub.delta. L is —CH.sub.2NH—, —(CH.sub.2).sub.2NH—, —(CH.sub.2).sub.3NH—, or —(CH.sub.2).sub.4NH—. R.sup.4 is a radiometal chelator optionally bound by a radiometal. Variable ‘n’ is 1-3. The compounds may be useful for imaging prostate specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

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The present invention relates to conjugates including a chelating moiety of a metal complex thereof and a therapeutic or targeting moiety, methods for their production, and uses thereof.

Theranostic probes comprising a porphyrin-based photosensitizer, a D-peptide linker, and a urea-based PSMA-targeting ligand and methods of their use for treating and/or imaging PMSA-expressing tumors are disclosed.

The present disclosure relates to a solution comprising a water insoluble carbohydrate and a fluorescent dye, such as a near infrared (NIR) contrast agent, wherein the solution sets under aqueous conditions, such as in vivo, to form e.g. a gel, a glass, a semi-solid, a solid, a crystal or any mixtures thereof. The disclosure further relates to preparation of such solution and use of such solution for in vivo imaging and/or guidance of surgery or interventional therapeutic procedures.

The disclosed method of treating a malignant solid tumor in a subject includes the steps of administering to the subject an immunomodulatory dose of a radioactive phospholipid ether metal chelate, a radiohalogenated phospholipid ether, or other targeted radiotherapy (TRT) agent that is differentially retained within malignant solid tumor tissue, and either (a) performing in situ tumor vaccination in the subject by introducing into at least one of the malignant solid tumors one or more agents capable of stimulating specific immune cells within the tumor microenvironment, or (b) performing immunotherapy in the subject by systemically administering to the subject an immunostimulatory agent, such as an immune checkpoint inhibitor. In a non-limiting example, the radioactive phospholipid ether metal chelate or radiohalogenated phospholipid ether has the formula:

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wherein R.sub.1 comprises a chelating agent that is chelated to a metal atom, wherein the metal atom is an alpha, beta or Auger emitting metal isotope with a half-life of greater than 6 hours and less than 30 days, or wherein R.sub.1 comprises a radioactive halogen isotope. In one such embodiment, a is 1, n is 18, m is 0, b is 1, and R.sub.2 is —N.sup.+(CH.sub.3).sub.3.

Described herein are radiotherapeutics that target tumor cells expressing the melanocortin type 2 receptor (MC2R) and their use in the treatment and/or diagnosis of cancer.

PSMA targeted compounds, pharmaceutical compositions comprising these compounds, and methods for treating and detecting cancers in a subject are described herein.

A compound of the following general formula (I), and isomers, physiologically acceptable salts, and complexes thereof, for use as a contrast agent in diagnostic imaging: ##STR00001##

Embodiments of the invention relate to compositions comprising a corrole and optionally a protein, wherein the composition are characterized by improved water solubility. The corrole may be a hydrophobic corrole, according to formula [I]. The protein may be a plasma protein. The plasma protein may be albumin. The compositions may be in nanoparticulate form.