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Details for Patent: 5,714,579

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Details for Patent: 5,714,579

Title: Technetium-99M labeled peptides for imaging inflammation
Abstract:This invention relates to compositions that are radiolabeled scintigraphic imaging agents, comprising a polybasic compound covalently linked to a radiolabel binding moiety and the composition further comprising a polysulfated glycan. The invention also provides methods for producing and using such compositions. Specifically, the invention relates to compositions comprised of technetium-99m (Tc-99m) labeled scintigraphic imaging agents comprising a polybasic compound having at least 5 chemical functionalities that are basic at physiological pH and a radiolabel-binding moiety, the composition further comprising a polysulfated glycan, the composition being capable of specifically binding to inflammatory sites in vivo. Methods and kits for making such compositions, and methods for using such compositions to image sites of infection and inflammation in a mammalian body, are also provided.
Inventor(s): Dean; Richard T. (Bedford, NH), Moyer; Brian R. (Bedford, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jun 05, 1995
Application Number:08/462,784
Claims:1. A method for imaging a site of intimation within a mammalian body comprising mixing whole blood with an amount from about 1 microgram to 100 milligrams of a polysulfated glycan to form a mixture, and further adding to the mixture an amount from about 1 microgram to 100 milligrams of a technetium-99m radiolabeled reagent which comprises a polybasic compound having a molecular weight Of about 500 daltons to about 15,000 daltons and having at least 5 chemical functionalities that are basic at physiological pH, covalently linked to a technetium-99m binding moiety, and further comprising a polysulfated glycan having a molecular weight of about 1,000 daltons to about 60,000 daltons, to form a radiolabeled mixture, administering said radiolabeled mixture to an animal having a site of inflammation in vivo, and detecting a radioactive signal from the Tc-99m localized at the site of inflammation.

2. The method of claim 1 wherein the polysulfated glycan is heparin, heparan sulfate, dextran sulfate, chondroitin sulfate, dermitan sulfate or derivatives thereof.

3. A method for imaging a site of inflammation within a mammalian body comprising mixing whole blood with an amount from about 1 microgram to 100 milligrams of a polysulfated glycan to form a mixture, and further adding to the mixture an amount from about 1 microgram to 100 milligrams of a technetium-99m radiolabeled reagent comprised of a polybasic compound having a molecular weight of about 500 daltons to about 15,000 daltons and having at least 5 chemical functionalities that are basic at physiological pH, covalently linked to a technetium-99m binding moiety, and further comprising a polysulfated glycan having a molecular weight of about 1,000 daltons to about 60,000 daltons, to form a radiolabeled mixture, administering said radiolabeled mixture to an animal having a site of inflammation in vivo, and detecting a radioactive signal from the Tc-99m localized at the site of inflammation, wherein the polybasic compound comprising the technetium-99m radiolabeled reagent is a peptide of 5 to 100 amino acids that is platelet factor 4 or a fragment thereof.

4. The method of claim 3 wherein the polybasic compound comprising the technetium-99m radiolabeled reagent is a peptide having an amino acid sequence comprising the sequence acetyl-KKC.sub.Acm GC.sub.Acm GGPLYKKIIKKLLES (SEQ ID NO:7) or acetyl-KKKC.sub.Acm GC.sub.Acm GGPLYKKIIKKLLES (SEQ ID NO:8.

5. The method of claim 3 wherein the technetium-99m radiolabeled reagent is selected from the group consisting of compounds having the formula:

acetyl-KC.sub.Acm GC.sub.Acm QAPLYKKIIKKLLES (SEQ ID NO:1)

acetyl-KKC.sub.Acm GC.sub.Acm QAPLYKKIIKKLLES (SEQ ID NO:2)

acetyl-KKKC.sub.Acm GC.sub.Acm QAPLYKKIIKKLLES (SEQ ID NO:3)

acetyl-KKKKC.sub.Acm GC.sub.Acm QAPLYKKIIKKLLES (SEQ ID NO:4)

acetyl-KKKKKC.sub.Acm GC.sub.Acm QAPLYKKIIKKLLES (SEQ ID NO:5)

acetyl-KC.sub.Acm GC.sub.Acm GGPLYKKIIKKLLES (SEQ ID NO:6)

acetyl-KKC.sub.Acm GC.sub.Acm GGPLYKKIIKKLLES (SEQ ID NO:7)

acetyl-KKKC.sub.Acm GC.sub.Acm GGPLYKKIIKKLLES (SEQ ID NO:8)

acetyl-KKKKC.sub.Acm GC.sub.Acm GGPLYKKIIKKLLES (SEQ ID NO:9)

and

acetyl-KKKKKC.sub.Acm GC.sub.Acm GGPLYKKIIKKLLES (SEQ ID NO:10),

radiolabeled with technetium-99m.

6. The method of claim 3 wherein the polysulfated glycan is heparin, heparan sulfate, dextran sulfate, chondroitin sulfate, dermitan sulfate or derivatives thereof.
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