Therapeutic Radiopharmaceuticals

Subgroup III: Pharmaceutical and Radiopharmaceutical Agents

I-131 half-life

8 days

I-131 energy

364 keV

I-131 production

nuclear reactor, uranium fission byproduct

I-131 sodium iodide mechanism of localization

active transport, trapped and organified

I-131 therapy indications

treatment of hyperthyroidism, treatment of thyroid carcinomas that take up iodine

I-131 therapy contraindications

vomiting and diarrhea, in treatment of thyroid malignancies shown to have no iodide uptake, pregnancy

I-131 therapy administration

oral capsule

Lu-177 half-life

6.65 days

Lu-177 energy

495, 208, 113 keV

Lu-177 production

nuclear reactor, direct or indirect method

Lu-177 dotatate (Lutathera) method of localization

receptor binding, somatostatin receptors

Lu-177 dotatate (Lutathera) indications

treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs)

Lu-177 dotatate (Lutathera) contraindications

none

Lu-177 dotatate (Lutathera) administration

IV infusion

Lu-177 vipivotide tetraxetan (Pluvicto) method of localization

receptor binding, prostate-specific membrane antigen (PSMA)

Lu-177 vipivotide tetraxetan (Pluvicto) indications

treatment of patients with prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer who have been treated with androgen receptor (AR) pathway inhibition and taxane-based chemotherapy

Lu-177 vipivotide tetraxetan (Pluvicto) contraindications

none

Lu-177 vipivotide tetraxetan (Pluvicto) administration

IV injection or infusion

Ra-223 half-life

11.4 days

Ra-223 energy

28.2 MeV (α)

Ra-223 production

nuclear reactor

Ra-223 radium dichloride (Xofigo) method of localization

chemisorption, calcium analog

Ra-223 radium dichloride (Xofigo) indications

treatment and palliation of pain for patients with castration-resistant prostate cancer, symptomatic bone metastases and no known visceral metastatic disease

Ra-223 radium dichloride (Xofigo) contraindications

pregnancy

Ra-223 radium dichloride (Xofigo) administration

IV injection

Sr-89 half-life

50.5 days

Sr-89 energy

1.46 MeV (β)

Sr-89 production

nuclear reactor

Sr-89 chloride (Metastron) method of localization

chemisorption, calcium analog

Sr-89 chloride (Metastron) indications

palliation of pain in patients with painful skeletal metastases

Sr-89 chloride (Metastron) contraindications

none

Sr-89 chloride (Metastron) administration

IV injection

Y-90 half-life

64 hours

Y-90 energy

0.93 MeV (β)

Y-90 production

nuclear reactor

Y-90 microspheres (SIR-Spheres, TheraSpheres) method of localization

capillary blockade

Y-90 microspheres (SIR-Spheres, TheraSpheres) indications

treatment for patients with unresectable hepatocellular carcinoma who can have placement of appropriately positioned hepatic arterial catheters

Y-90 microspheres (SIR-Spheres, TheraSpheres) contraindications

• Tc99m MAA hepatic arterial perfusion scintigraphy shows any deposition to the GI tract

• ““ shows shunting of blood to lungs which could result in delivery of more than 16.5 mCi of Y90 to the lungs

• hepatic artery catheterization is contraindicated

• severe liver dysfunction

• severe pulmonary insufficiency

Y-90 microspheres (SIR-Spheres, TheraSpheres) administration

injected via hepatic arterial catheter (by physician)

Y-90 ibritumomab tiuxetan method of localization

receptor binding, CD20 antigen

Y-90 ibritumomab tiuxetan indications

treatment of patients with relapsed or refractory, low-grade or follicular B-cell non-Hodgkin’s lymphoma; treatment of previously untreated follicular NHL who achieve a partial or complete response to first-line chemotherapy

Y-90 ibritumomab tiuxetan contraindications

none

Y-90 ibritumomab tiuxetan administration

IV infusion