Albumin conjugates and radiopharmaceutical composition thereof

A sterile radiopharmaceutical composition, comprising:

• X-J-MAA,
• wherein X is a diagnostic or therapeutic radioisotope selected from the group consisting of copper-61, copper-64, copper-67, gallium-68, gallium-67, gallium-66, iodine-131, iodine-123, iodine-124, iodine-125, lutetium-177, yttrium-86, yttrium-90, technetium-99m, indium-114, indium-111, scandium-47, scandium-44, scandium-43, terbium-149, zirconium-89, bismuth-213, bismuth-212, actinium-225, astatine-211, lead-212, lead-214, gold-198, gold-199, rhenium-188, rhenium-186, and holmium-166;
• J is an optional chelating agent;
• MAA is macroaggregated albumin particles wherein the average particle size of the macroaggregated albumin particles is 20-35 μm, at least 95% of the macroaggregated albumin particles are between 10 μm to 70 μm, not more than 3% particles are below 10 μm and no particle is larger than 100 μm;
• and
• wherein the reconstituted and/or ready-to-use composition has not more than 5% soluble and dispersed radiochemical impurities;
• and
• wherein the reconstituted and/or ready-to-use composition has a pH of about 3.5 to about 8.5;
• and
• wherein the reconstituted and/or ready-to-use composition has bacterial endotoxin content less than 20 EU/vial;
• and
• wherein the reconstituted and/or ready-to-use composition has a radiochemical purity of at least 95% or more for at least 6 hours;
• wherein the reconstituted and/or ready-to-use composition has a radioactivity of 0.185 MBq to 11100 MBq.

A method of administering a sterile and stable radiopharmaceutical composition, the method comprising injecting a sterile radiopharmaceutical composition into a patient in need thereof, the radiopharmaceutical composition comprising X-J-MAA,

• wherein X is a diagnostic or therapeutic radioisotope selected from the group consisting of copper-61, copper-64, copper-67, gallium-68, gallium-67, gallium-66, iodine-131, iodine-123, iodine-124, iodine-125, lutetium-177, yttrium-86, yttrium-90, technetium-99m, indium-114, indium-111, scandium-47, scandium-44, scandium-43, terbium-149, zirconium-89, bismuth-213, bismuth-212, actinium-225, astatine-211, lead-212, lead-214, gold-198, gold-199, rhenium-188, rhenium-186, and holmium-166;
• J is an optional chelating agent;
• and
• MAA is macroaggregated albumin particles wherein the average particle size of the macroaggregated albumin particles is 20-35 μm, at least 95% of the macroaggregated albumin particles are between 10 μm to 70 μm, not more than 3% particles are below 10 μm and no particle is larger than 100 μm;
• and
• wherein the reconstituted and/or ready-to-use composition has not more than 5% soluble and dispersed radiochemical impurities;
• and
• wherein the reconstituted and/or ready-to-use composition has a pH of about 3.5 to about 8.5;
• and
• wherein the reconstituted and/or ready-to-use composition has bacterial endotoxin content less than 20 EU/vial;
• and
• wherein the reconstituted and/or ready-to-use composition has a radioactivity of 0.185 MBq to 11100 MBq;
• and
• wherein the reconstituted and/or ready-to-use composition has a radiochemical purity of at least 95% or more for at least 6 hours after radiolabeling.