Wisconsin Alumni Research Foundation

Cellectar, Inc.

Cellectar Biosciences, Inc.

Mirus Bio Corporation

Anatoly Pinchuk

Jamey Paul Weichert

Marc Longino

Chorom Pak

William R Clarke

Irawati Kandela

Kevin Kozak

Paul M Sondel

Zachary Scott Morris

Mario Otto

Bryan P Bednarz

Joseph J Grudzinski

Benjamin Titz

Nathan Stehle

Reinier Hernandez

Peter Carlson

Wolfgang A Tome

Karen Neder

Nicholas A A Rossi

Wolfgang Axel Tomé

Laura Juckem

James Ludtke

Jamie Weichert

Theranostic agents incorporating a chelating moiety that can chelate a radioactive metal isotope and a PSMA-targeting moiety are disclosed herein. The theranostic agents, which can be used to treat and/or detect cancers associated with increased PSMA expression, have the formula: and include complexes, anions or salts thereof. Rincludes a chelating moiety; a is 0 or 1; n is an integer from 12 to 21; and Rincludes a prostate specific membrane antigen (PSMA)-targeting moiety. Optionally, the chelating moiety is chelated to a metal atom, where the metal atom is a positron or single photon emitting metal isotope, or an alpha, beta, or Auger emitting metal isotope.

PSMA-targeting ligands with optimal properties for imaging and therapy

A method of treating a malignant solid tumor in a subject is disclosed herein. The method includes the steps of administering to the subject an immunomodulatory dose of a radiohalogenated compound that is differentially taken up by and retained within malignant solid tumor tissue, and performing in situ tumor vaccination in the subject by intratumorally injecting into (or treating via a separate method) at least one of the malignant solid tumors a composition that includes one or more agents capable of stimulating specific immune cells within the tumor microenvironment. In certain exemplary embodiments, the radiohalogenated compound has the formula: wherein Ris a radioactive halogen isotope, n is 18 and Ris —N(CH).

Radiohalogenated agents for in situ immune modulated cancer vaccination

Cationic cyclic amine containing polymers and copolymers as well as novel lipids have been designed and synthesized for efficient delivery of nucleic acids to cells in biological systems, specifically for in vitro cell transfection research.

Cationic cyclic amine and amphipathic transfection reagents

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 metal chelate compound that is differentially retained within malignant solid tumor tissue, and 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 by performing another method of in situ tumor vaccination. In a non-limiting example, the radioactive phospholipid metal chelate compound has the formula: wherein Rcomprises 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. In one such embodiment, a is 1, n is 18, m is 0, b is 1, and Ris &#x2014;N(CH).

Targeted radiotherapy chelates for in situ immune modulated cancer vaccination

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: or a salt therof. Rincludes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is &#x2014;H, &#x2014;OH, &#x2014;COOH, &#x2014;COOX, &#x2014;OCOX, or &#x2014;OX, wherein X is an alkyl or an arylalkyl; Ris &#x2014;NH, &#x2014;NHZ, &#x2014;NHZ, or &#x2014;NZ, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

Long-lived gadolinium based tumor targeted imaging and therapy agents

The present invention is directed to a method of identifying, isolating, and enabling downstream analysis of circulating tumor cells comprising contacting a blood or blood serum sample of a subject with a composition comprising a phospholipid ether analog bound to a luminescent molecule or a magnetic bead and subjecting the blood or blood serum sample of the subject to fluorescent microscopy, flow cytometry or magnetic isolation.

Luminescent phospholipid analogs for the identification and isolation of circulating tumor cells

The present invention is directed to therapeutic compounds capable of targeting cancer cells and cancer stem cells. The present invention is further directed to compositions comprising these therapeutic compounds and methods of treating cancer comprising administering these therapeutic compounds.

Phospholipid ether analogs as cancer-targeting drug vehicles

Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: Rincludes a chelating agent that is chelated to a metal atom, wherein the metal atom is a positron or single photon emitting metal isotope with a half life of greater than or equal to 4 hours, or an alpha, beta or Auger emitting metal isotope with a half life of greater than 6 hours and less than 30 days; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is &#x2014;H, &#x2014;OH, &#x2014;COOH, &#x2014;COOX, &#x2014;OCOX, or &#x2014;OX, wherein X is an alkyl or an arylalkyl; Ris &#x2014;NH, &#x2014;NHZ, &#x2014;NHZ, or &#x2014;NZ, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2.

Radioactive phospholipid metal chelates for cancer imaging and therapy

Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: or a salt thereof. Rincludes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is &#x2014;H, &#x2014;OH, &#x2014;COOH, &#x2014;COOX, &#x2014;OCOX, or &#x2014;OX, wherein X is an alkyl or an arylalkyl; Ris &#x2014;NH, &#x2014;NHZ, &#x2014;NHZ, or &#x2014;NZ, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

Long-lived gadolinium based tumor targeting imaging and therapy agents

A method of treating a malignant solid tumor in a subject is disclosed herein. The method includes the steps of administering to the subject an immunomodulatory dose of a radiohalogenated compound that is differentially taken up by and retained within malignant solid tumor tissue, and performing in situ tumor vaccination in the subject by intratumorally injecting into (or treating via a separate method) at least one of the malignant solid tumors a composition that includes one or more agents capable of stimulating specific immune cells within the tumor microenvironment. In certain exemplary embodiments, the radiohalogenated compound has the formula: wherein Ris a radioactive halogen isotope, n isand Ris &#x2014;N(CH).

Methods and compositions utilizing ether and alkyl phospholipid ether analog compounds for treating cancer and imaging, monitoring, and detecting cancer stem cells in humans.

Growing community of inventors

Madison, WI, United States of America

Anatoly Pinchuk