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LUTETIUM LU 177 VIPIVOTIDE TETRAXETAN

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PLUVICTO LUTETIUM LU 177 VIPIVOTIDE TETRAXETAN
NOVARTIS PHARMACEUTICALS CORPORATION FDA Rx Only

PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) is a radioligand therapeutic agent. Lutetium Lu 177 vipivotide tetraxetan is a PSMA-binding ligand bound to a DOTA chelator radiolabeled with lutetium-177. The chemical name is 2-[4-[2-[[4-[[(2S)-1-[[(5S)-5-carboxy-5-[[(1S)-1,3-dicarboxy propyl]carbamoylamino]pentyl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamoyl]cyclohexyl]methylamino]-2-oxoethyl]-4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate; lutetium-177(3+). The molecular mass is 1216.06 g/mol and the molecular formula is C 49 H 68 177 LuN 9 O 16 . The chemical structure for lutetium Lu 177 vipivotide tetraxetan is shown below: PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) 1,000 MBq/mL (27 mCi/mL) Injection is supplied as a sterile, clear, colorless to slightly yellow solution for intravenous use. Each single-dose vial contains acetic acid (0.30 mg/mL), sodium acetate (0.41 mg/mL), gentisic acid (0.39 mg/mL), sodium ascorbate (50.0 mg/mL), pentetic acid (0.10 mg/mL), and water for injection (q.s. to 1 mL). The pH range of the solution is 4.5 to 7.0. Chemical Structure of lutetium 11.1 Physical Characteristics Lutetium-177 decays to a stable hafnium-177 with a physical half-life of 6.647 days by emitting beta-minus radiation with a maximum energy of 498 keV (79%) and photonic radiation (γ) of 208 keV (11%) and 113 keV (6.4%). The main radiations of lutetium-177 are detailed in Table 7. Table 7: Lutetium-177 Main Radiations Radiation Energy (keV) Iβ - % Iγ% β - 176.5 12.2 β - 248.1 0.05 β - 384.9 9.1 β - 497.8 78.6 γ 71.6 0.15 γ 112.9 6.40 γ 136.7 0.05 γ 208.4 11.0 γ 249.7 0.21 γ 321.3 0.22 11.2 External Radiation Table 8 summarizes the radioactive decay properties of lutetium-177. Table 8: Physical Decay Chart: Lutetium-177 Physical Half-life = 6.647 days Hours Fraction remaining 0 1.000 1 0.996 2 0.991 5 0.979 10 0.958 24 (1 day) 0.901 48 (2 days) 0.812 72 (3 days) 0.731 120 (5 days) 0.594 168 (7 days) 0.482 336 (14 days) 0.232 720 (30 days) 0.044 1080 (45 days) 0.009

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PLUVICTO LUTETIUM LU 177 VIPIVOTIDE TETRAXETAN
NOVARTIS PHARMACEUTICALS CORPORATION FDA Rx Only

PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) is a radioligand therapeutic agent. Lutetium Lu 177 vipivotide tetraxetan is a PSMA-binding ligand bound to a DOTA chelator radiolabeled with lutetium-177. The chemical name is 2-[4-[2-[[4-[[(2S)-1-[[(5S)-5-carboxy-5-[[(1S)-1,3-dicarboxy propyl]carbamoylamino]pentyl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamoyl]cyclohexyl]methylamino]-2-oxoethyl]-4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate; lutetium-177(3+). The molecular mass is 1216.06 g/mol and the molecular formula is C 49 H 68 177 LuN 9 O 16 . The chemical structure for lutetium Lu 177 vipivotide tetraxetan is shown below: PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) 1,000 MBq/mL (27 mCi/mL) Injection is supplied as a sterile, clear, colorless to slightly yellow solution for intravenous use. Each single-dose vial contains acetic acid (0.30 mg/mL), sodium acetate (0.41 mg/mL), gentisic acid (0.39 mg/mL), sodium ascorbate (50.0 mg/mL), pentetic acid (0.10 mg/mL), and water for injection (q.s. to 1 mL). The pH range of the solution is 4.5 to 7.0. Chemical Structure of lutetium 11.1 Physical Characteristics Lutetium-177 decays to a stable hafnium-177 with a physical half-life of 6.647 days by emitting beta-minus radiation with a maximum energy of 498 keV (79%) and photonic radiation (γ) of 208 keV (11%) and 113 keV (6.4%). The main radiations of lutetium-177 are detailed in Table 7. Table 7: Lutetium-177 Main Radiations Radiation Energy (keV) Iβ - % Iγ% β - 176.5 12.2 β - 248.1 0.05 β - 384.9 9.1 β - 497.8 78.6 γ 71.6 0.15 γ 112.9 6.40 γ 136.7 0.05 γ 208.4 11.0 γ 249.7 0.21 γ 321.3 0.22 11.2 External Radiation Table 8 summarizes the radioactive decay properties of lutetium-177. Table 8: Physical Decay Chart: Lutetium-177 Physical Half-life = 6.647 days Hours Fraction remaining 0 1.000 1 0.996 2 0.991 5 0.979 10 0.958 24 (1 day) 0.901 48 (2 days) 0.812 72 (3 days) 0.731 120 (5 days) 0.594 168 (7 days) 0.482 336 (14 days) 0.232 720 (30 days) 0.044 1080 (45 days) 0.009

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PLUVICTO LUTETIUM LU 177 VIPIVOTIDE TETRAXETAN
NOVARTIS PHARMACEUTICALS CORPORATION FDA Rx Only

PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) is a radioligand therapeutic agent. Lutetium Lu 177 vipivotide tetraxetan is a PSMA-binding ligand bound to a DOTA chelator radiolabeled with lutetium-177. The chemical name is 2-[4-[2-[[4-[[(2S)-1-[[(5S)-5-carboxy-5-[[(1S)-1,3-dicarboxy propyl]carbamoylamino]pentyl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamoyl]cyclohexyl]methylamino]-2-oxoethyl]-4,7,10-tris(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate; lutetium-177(3+). The molecular mass is 1216.06 g/mol and the molecular formula is C 49 H 68 177 LuN 9 O 16 . The chemical structure for lutetium Lu 177 vipivotide tetraxetan is shown below: PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) 1,000 MBq/mL (27 mCi/mL) Injection is supplied as a sterile, clear, colorless to slightly yellow solution for intravenous use. Each single-dose vial contains acetic acid (0.30 mg/mL), sodium acetate (0.41 mg/mL), gentisic acid (0.39 mg/mL), sodium ascorbate (50.0 mg/mL), pentetic acid (0.10 mg/mL), and water for injection (q.s. to 1 mL). The pH range of the solution is 4.5 to 7.0. Chemical Structure of lutetium 11.1 Physical Characteristics Lutetium-177 decays to a stable hafnium-177 with a physical half-life of 6.647 days by emitting beta-minus radiation with a maximum energy of 498 keV (79%) and photonic radiation (γ) of 208 keV (11%) and 113 keV (6.4%). The main radiations of lutetium-177 are detailed in Table 7. Table 7: Lutetium-177 Main Radiations Radiation Energy (keV) Iβ - % Iγ% β - 176.5 12.2 β - 248.1 0.05 β - 384.9 9.1 β - 497.8 78.6 γ 71.6 0.15 γ 112.9 6.40 γ 136.7 0.05 γ 208.4 11.0 γ 249.7 0.21 γ 321.3 0.22 11.2 External Radiation Table 8 summarizes the radioactive decay properties of lutetium-177. Table 8: Physical Decay Chart: Lutetium-177 Physical Half-life = 6.647 days Hours Fraction remaining 0 1.000 1 0.996 2 0.991 5 0.979 10 0.958 24 (1 day) 0.901 48 (2 days) 0.812 72 (3 days) 0.731 120 (5 days) 0.594 168 (7 days) 0.482 336 (14 days) 0.232 720 (30 days) 0.044 1080 (45 days) 0.009

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