Radiopharmaceuticals, or medicinal radiocompounds, are a group of pharmaceutical drugs containing radioactive isotopes. Radiopharmaceuticals can be used as diagnostic and therapeutic agents. Radiopharmaceuticals emit radiation themselves, which is different from contrast media which absorb or alter external electromagnetism or ultrasound. Radiopharmacology is the branch of pharmacology that specializes in these agents.
The main group of these compounds are the radiotracers used to diagnose dysfunction in body tissues. While not all medical isotopes are radioactive, radiopharmaceuticals are the oldest and remain the most common of such drugs.
Drug nomenclature
As with other pharmaceutical drugs, there is standardization of the drug nomenclature for radiopharmaceuticals, although various standards coexist. The International Nonproprietary Names (INNs), United States Pharmacopeia (USP) names, and IUPAC names for these agents are usually similar other than trivial style differences.
Specific radiopharmaceuticals
A list of nuclear medicine radiopharmaceuticals follows. Some radioisotopes are used in ionic or inert form without attachment to a pharmaceutical; these are also included. There is a section for each radioisotope with a table of radiopharmaceuticals using that radioisotope. The sections are ordered by atomic number of the radioisotope. Sections for the same element are then ordered by atomic mass number.
Hydrogen-3 3H or tritium is a beta emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingH3-waterTotal body waterOral or IVIn-vitro Non-imaging
Carbon-11 11C is a positron emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingC11-L-methyl-methionineBrain tumour imaging Parathyroid imagingIVIn-vivoImaging
Carbon-14 14C is a beta emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingC14-Glycocholic acidBreath test for small intestine bacterial overgrowthOralIn-vitroNon-imagingC14-PABA (para-amino benzoic acid)Pancreatic studiesOralIn-vitroNon-imagingC14-UreaBreath test to detect Helicobacter pyloriOralIn-vitroNon-imagingC14-d-xyloseBreath test for small intestine bacterial overgrowthOralIn-vitroNon-imaging
Nitrogen-13 13N is a positron emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingN13-AmmoniaMyocardial blood flow imagingIVIn-vivo Imaging
Oxygen-15 15O is a positron emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingO15-WaterCerebral blood flow imaging Myocardial blood flow imagingIV bolusIn-vivo Imaging
Fluorine-18
18F is a positron emitter with a half-life of 109 minutes. It is produced in medical cyclotrons, usually from oxygen-18, and then chemically attached to a pharmaceutical formulation.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingF18-FDG (Fluorodeoxyglucose)Tumor imaging Myocardial imagingIVIn-vivo ImagingF18-Sodium FluorideBone imagingIVIn-vivo ImagingF18-FluorocholineProstate tumor imagingIVIn-vivoImagingF18-DesmethoxyfallyprideDopamine receptor imagingIVIn-vivoImaging
Sodium-22 22Na is a positron and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingNa22-Na+Electrolyte studiesOral or IVIn-vitro Non-imaging
Sodium-24 24Na is a beta and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingNa24-Na+Electrolyte studiesOral or IVIn-vitro Non-imaging
Phosphorus-32 32P is a beta emitter.
NameTreatment ofRoute of administrationP32-PhosphatePolycythemia and related disordersIV or Oral
Calcium-47 47Ca is a beta and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingCa-47-Ca2+Bone metabolismIVIn-vitro Non-imaging
Chromium-51 51Cr is a gamma emitter. NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingCr51-[heart scan/blood volumeRed cell volume heart scan; sites of sequestration; gastrointestinal blood lossIVIn-vitro Non-imagingCr51-Cr3+Gastrointestinal protein lossIVIn-vitro Non-imagingCr51-EDTA (ethylenediaminetetraacetic acid)Glomerular filtration rate measurementIVIn-vitro Non-imaging
Iron-59 59Fe is a beta and gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingFe59-Fe2+ or Fe3+Iron metabolismIVIn-vitro Non-imaging
Cobalt-57 57Co is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingCo57-Cyanocobalamin (vitamin B12)Gastrointestinal absorptionOralIn-vitro Non-imaging
Cobalt-58 58Co is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingCo58-Cyanocobalamin (vitamin B12)Gastrointestinal absorptionOralIn-vitro Non-imaging
Gallium-67
67Ga is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingGa67-Ga3+Tumor imagingIVIn-vivo ImagingGa67-Ga3+Infection/inflammation imagingIVIn-vivo Imaging
Gallium-68 68Ga is a positron emitter, with a 68-minute half-life, produced by elution from germanium-68 in a gallium-68 generator or by proton irradiation of zinc-68.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingGa68-Dotatoc or DotatateNeuroendocrine tumor imagingIVIn-vivo ImagingGa68-PSMAProstate cancer imagingIVIn-vivoImaging
Selenium-75 75Se is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingSe75-SelenorcholesterolAdrenal gland imagingIVIn-vivo ImagingSe75-SeHCAT (23-Seleno-25-homo-tauro-cholate)Bile salt absorptionOralIn-vivo Imaging
Krypton-81m 81Krm is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imaging the radioactive substanceKr81m-GasLung ventilation imagingInhalationIn-vivo ImagingKr-81m-Aqueous solutionLung perfusion imagingIVIn-vivo Imaging
Rubidium-82 82Rb is a positron and gamma emitter.
NameInvestigation ofRoute of administrationRb-82 chlorideMyocardial ImagingIV
Strontium-89 89Sr is a beta emitter.
NameTreatment ofRoute of administrationSr89-ChlorideBone metastasesIV
Yttrium-90 90Y is a beta emitter.
NameTreatment ofRoute of administrationY90-SilicateArthritic conditionsIntra-articularY90-SilicateMalignant diseaseIntracavitary
Technetium-99m Technetium-99m is a gamma emitter. It is obtained on-site at the imaging center as the soluble pertechnetate which is eluted from a technetium-99m generator, and then either used directly as this soluble salt, or else used to synthesize a number of technetium-99m-based radiopharmaceuticals.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingTc99m-pertechnetateThyroid uptake and thyroid imaging Stomach and salivary gland imaging Meckel's diverticulum imaging Brain imaging Micturating cystogram First pass blood flow imaging First pass peripheral vascular imagingIVIn-vivo ImagingTc99m-pertechnetateLacrimal imagingEye dropsIn-vivo ImagingTc99m-Human albuminCardiac blood pool imagingIVIn-vivo ImagingTc99m-Human albuminPeripheral vascular imagingIVIn-vivo ImagingTc99m-Human albumin macroaggregates or microspheresLung perfusion imagingIVIn-vivo ImagingTc99m-Human albumin macroaggregates or microspheresLung perfusion imaging with venographyIVIn-vivo ImagingTc99m-Phosphonates and phosphates (MDP/HDP)Bone imagingIVIn-vivo ImagingTc99m-Phosphonates and phosphatesMyocardial imagingIVIn-vivo ImagingTc99m-DTPA (diethylenetriaminepenta-acetic acid)Renal imagingFirst pass blood flow studiesBrain imagingIVIn-vivo ImagingTc99m-DTPA (diethylenetriaminepenta-acetic acid)Lung ventilation imagingAerosol inhalationIn-vivo ImagingTc99m-DMSA(V) (dimercaptosuccinic acid)Tumor imagingIVIn-vivo ImagingTc99m-DMSA(III) (dimercaptosuccinic acid)Renal imagingIVIn-vivo ImagingTc99m-ColloidBone marrow imaging GI BleedingIVIn-vivo ImagingTc99m-ColloidLymph node imagingInterstitialIn-vivo ImagingTc99m-ColloidEsophageal transit and reflux imaging Gastric emptying imagingOralIn-vivo ImagingTc99m-ColloidLacrimal imagingEye dropsIn-vivo ImagingTc99m-HIDA (Hepatic iminodiacetic acid)Functional biliary system imagingIVIn-vivo ImagingTc99m-Denatured (heat damaged) red blood cellsRed cell volume Spleen imagingIVIn-vitro Non-imagingTc99m-Whole red blood cellsGI bleeding Cardiac blood pool imaging Peripheral vascular imagingIVIn-vivo ImagingTc99m-MAG3 (mercaptoacetyltriglycine)Renal imaging First pass blood flow imagingIVIn-vivo ImagingTc99m-Exametazime (HMPAO)Cerebral blood flow imagingIVIn-vivo ImagingTc99m-Exametazime labelled leucocytesInfection/inflammation imagingIVIn-vivo ImagingTc99m-Sestamibi (MIBI - methoxy isobutyl isonitrile)Parathyroid imaging Non-specific tumor imaging Thyroid tumor imaging Breast imaging Myocardial imagingIVIn-vivo ImagingTc99m-Sulesomab (IMMU-MN3 murine Fab'-SH antigranulocyte monoclonal antibody fragments)Infection/inflammation imagingIVIn-vivo ImagingTc99m-TechnegasLung ventilation imagingInhalationIn-vivo ImagingTc99m-Human immunoglobulinInfection/inflammation imagingIVIn-vivo ImagingTc99m-TetrofosminParathyroid imaging Myocardial imagingIVIn-vivo ImagingTc99m-ECD (ethyl cysteinate dimer)Brain imaging-----IVIn-vivo Imaging
Indium-111 111In is a gamma emitter.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingIn111-DTPA (diethylenetriaminepenta-acetic acid)Ventriculo-peritoneal shunt (LaVeen Shunt)intraperitoneal injectionIn-vivo Imaging the radioactive substance In111-DTPA (diethylenetriaminepenta-acetic acid)CisternographyIntra-cisternalIn-vivo ImagingIn111-LeukocytesInfection/inflammation imagingIVIn-vivo ImagingIn111-PlateletsThrombus imagingIVIn-vivo ImagingIn111-PentetreotideSomatostatin receptor imagingIVIn-vivo ImagingIn111-OctreotideSomatostatin receptor imaging (Octreoscan)IVIn-vivo Imaging
Iodine-123 Iodine-123 (I-123) is a gamma emitter. It is used only diagnostically, as its radiation is penetrating and short-lived.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingI123-IodideThyroid uptakeOral or IVIn-vivo Non-imagingI123-IodideThyroid imaging Thyroid metastases imagingOral or IVIn-vivo ImagingI123-o-IodohippurateRenal imagingIVIn-vivo ImagingI123-MIBG (m-iodobenzylguanidine)Neuroectodermal tumour imagingIVIn-vivo ImagingI123-FP-CITSPECT imaging of Parkinson's DiseaseIVIn-vivoImaging
Iodine-125 125I is a gamma emitter with a long half-life of 59.4 days (the longest of all radioiodines used in medicine). Iodine-123 is preferred for imaging, so I-125 is used diagnostically only when the test requires a longer period to prepare the radiopharmaceutical and trace it, such as a fibrinogen scan to diagnose clotting. I-125's gamma radiation is of medium penetration, making it more useful as a therapeutic isotope for brachytherapy implant of radioisotope capsules for local treatment of cancers.
NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingI125-fibrinogenClot imagingIVIn-vivo Imaging
Iodine-131 131I is a beta and gamma emitter. It is used both to destroy thyroid and thyroid cancer tissues (via beta radiation, which is short-range), and also other neuroendocrine tissues when used in MIBG. It can also be seen by a gamma camera, and can serve as a diagnostic imaging tracer, when treatment is also being attempted at the same time. However iodine-123 is usually preferred when only imaging is desired.
Diagnostic NameInvestigationRoute of administrationIn-vitro / in-vivoImaging / non-imagingI131-IodideThyroid uptakeOralIn-vivo Non-imagingI131-IodideThyroid metastases imagingOral or IVIn-vivo ImagingI131-MIBG (m-iodobenzylguanidine)Neuroectodermal tumor imagingIVIn-vivo Imaging
Therapeutic NameTreatment ofRoute of administrationI131-IodideThyrotoxicosisIV or OralI131-IodideNon-toxic goiterIV or OralI131-IodideThyroid carcinomaIV or OralI131-MIBG (m-iodobenzylguanidine)Malignant diseaseIV
Xenon-133