Ioflupane

The active drug substance in Ioflupane I 123 Injection is N-ω-fluoropropyl-2β-carbomethoxy-3β-(4-[ 123 I]iodophenyl)nortropane or ioflupane I-123. In vitro , ioflupane binds reversibly to the human dopamine transporter (DaT) (Ki = 0.62 nM; IC 50 = 0.71 nM).

• Ioflupane I 123 Injection is indicated as an adjunct to other diagnostic evaluations for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging in adult patients with: ● suspected Parkinsonian syndromes (PS) or ● suspected dementia with Lewy bodies (DLB). Ioflupane I 123 Injection is a radioactive diagnostic agent indicated as an adjunct to other diagnostic evaluations for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging in adult patients with: suspected Parkinsonian syndromes (PS) or suspected dementia with Lewy bodies (DLB).

• Ioflupane I 123 Injection is contraindicated in patients with known serious hypersensitivity to ioflupane I-123 [see Warnings and Precautions ( 5.1 )] .contraindicated

Administer a thyroid-blocking agent at least one hour before the dose of Ioflupane I 123 Injection. ( 2.2 ) The recommended dose of Ioflupane I 123 Injection in adult patients is 111 MBq to 185 MBq (3 mCi to 5 mCi) administered intravenously over at least 20 seconds. ( 2.3 ) Measure patient dose using a dose calibrator immediately prior to administration. ( 2.4 ) Begin SPECT imaging between 3 hours and 6 hours post-injection. ( 2.6 ) Figure 1,2,3,4 2.1 Radiation Safety Ioflupane I 123 Injection emits radiation and must be handled with safety measures to minimize radiation exposure to healthcare providers and patients [ see Warnings and Precautions ( 5.3 ) ]. Radiopharmaceuticals should be used by or under the control of healthcare providers who are qualified by specific training and experienced in the safe use and handling of radionuclides, and whose experience and training have been approved by the appropriate government agency authorized to license the use of radionuclides. To minimize radiation exposure, encourage hydration prior to and following Ioflupane I 123 Injection administration in order to permit frequent voiding. Encourage the patient to void frequently for the first 48 hours following Ioflupane I 123 Injection administration [ see Dosage and Administration ( 2.5 ) ].

Hypersensitivity Reactions: Hypersensitivity reactions including dyspnea, edema, rash, erythema, and pruritus have been reported. Have treatment measures available prior to Ioflupane I 123 Injection administration. ( 5.1 ) Thyroid Accumulation of Iodine-123: Thyroid uptake of iodine-123 may result in an increased long-term risk for thyroid neoplasia. ( 2.2 , 5.2 ) Radiation Risk: Ensure safe handling to minimize radiation exposure to the patient and healthcare providers. Advise patients to hydrate before and after administration and to void frequently after administration. ( 2.1 , 5.3 ) 5. 1 Hypersensitivity Reactions Hypersensitivity reactions, including dyspnea, edema, rash, erythema, and pruritus, have been reported following Ioflupane I 123 Injection administration [ see Adverse Reactions ( 6.2 ) ]. The reactions have generally occurred within minutes of Ioflupane I 123 Injection administration and have either resolved spontaneously or following the administration of corticosteroids and antihistamines. Ioflupane I 123 Injection is contraindicated in patients with known serious hypersensitivity to ioflupane I-123 [ see Contraindications ( 4 ) ]. Have treatment measures available and monitor patients for symptoms or signs of a hypersensitivity reaction. 5.2 Thyroid Accumulation of Iodine-123 Ioflupane I 123 Injection may contain up to 6% of free iodide (iodine-123). Thyroid uptake of iodine-123 may result in an increased long-term risk for thyroid neoplasia.

The following clinically significant adverse reaction is described elsewhere in the labeling: • Hypersensitivity Reactions [ see Warnings and Precautions ( 5.1 ) ] The following adverse reactions were reported at ≤1%: headache, nausea, vertigo, dry mouth and dizziness. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact CURIUM US LLC at 1-866-789-2211 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of Ioflupane I 123 Injection cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The data from clinical trials reflect exposure to Ioflupane I 123 Injection in 942 subjects with a mean age of 66 years (range 25 years to 90 years). Among these subjects, 42% were female and 99% White. Subjects received 88 MBq to 287 MBq (2 mCi to 8 mCi) [median 173 MBq (4.7 mCi)] intravenously as a single dose. The recommended dose of Ioflupane I 123 Injection is 111 MBq to 185 MBq (3 mCi to 5 mCi) [ see Dosage and Administration ( 2.3 ) ]. The following adverse reactions were reported at a rate of 1% or less: headache, nausea, vertigo, dry mouth, and dizziness. 6.2 Postmarketing Experience The following adverse reactions have been identified during postapproval use of Ioflupane I 123 Injection.

Pregnancy: May cause fetal harm. ( 8.1 ) Lactation: Advise a lactating woman to interrupt breastfeeding and pump and discard breastmilk for at least 6 days after Ioflupane I 123 Injection administration. ( 8.2 ) 8. 1 Pregnancy Risk Summary Radioactive iodine products cross the placenta and can permanently impair fetal thyroid function. Administration of an appropriate thyroid blocking agent is recommended before use of Ioflupane I 123 Injection in a pregnant woman to protect the woman and fetus from accumulation of iodine-123 [ see Dosage and Administration ( 2.2 ) ]. There are no available data on Ioflupane I 123 Injection use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Animal reproduction studies have not been conducted with ioflupane I-123. All radiopharmaceuticals have the potential to cause fetal harm depending on the fetal stage of development and the magnitude of the radiation dose. Administration of Ioflupane I 123 Injection at a dose of 185 MBq (5 mCi) results in an absorbed radiation dose to the uterus of 0.3 rad (3.0 mGy). Radiation doses greater than 15 rad (150 mGy) have been associated with congenital anomalies but doses under 5 rad (50 mGy) generally have not.

Metabolism

The pharmacokinetics of ioflupane I-123 were studied by monitoring radioactivity following intravenous injection; only 5% of the administered radioactivity remained in whole blood at 5 minutes post-injection. Uptake in the brain reached approximately 7% of injected radioactivity at 10 minutes post-injection and decreased to 3% after 5 hours; striata to background ratios were relatively constant between 3 hours and 6 hours post-injection.

The risks of overdose relate predominantly to increased radiation exposure, with the long-term risks for neoplasia. In case of overdosage of radioactivity, frequent urination and defecation should be encouraged to minimize radiation exposure to the patient.

• Jan 14, 2011NDANDA022454Ge Hlthcare Inc
• Mar 30, 2022ANDAANDA213792Curium

1. 1No Adverse Event25749%
2. 2Radioisotope Scan Abnormal14527%
3. 3Drug Ineffective12724%
4. 4Injection Site Pain5911%
5. 5Drug Interaction468.7%
6. 6Burning Sensation244.5%
7. 7Parkinsonism244.5%
8. 8False Positive Radioisotope Investigation Result163.0%
9. 9Dopamine Transporter Scintigraphy Abnormal122.3%
10. 10Nausea122.3%
11. 11Product Quality Issue112.1%
12. 12Dizziness101.9%
13. 13Malaise91.7%
14. 14Pain91.7%
15. 15Headache81.5%

The 10 most recently updated of 54 ClinicalTrials.gov registrations naming Ioflupane as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Imaging of Vesicular Acetylcholine and Dopamine Transporters in Dementia With Lewy Bodies
  Completed · Interventional · 34 enrolled · University Hospital, Bordeaux
  NCT00917709updated 2026-05-14
• The Neurobiology of Two Distinct Types of Progressive Apraxia of Speech
  Recruiting · Observational · 47 enrolled · Mayo Clinic
  NCT03313011updated 2026-05-01
• DaTSCAN Imaging in Aging and Neurodegenerative Disease
  Enrolling by invitation · Phase 4 · Interventional · 500 enrolled · Mayo Clinic
  NCT01453127updated 2026-03-10
• Terazosin Effect on Cardiac Changes in Early Parkinson's Disease
  Active not recruiting · Phase 2 · Interventional · 15 enrolled · Cedars-Sinai Medical Center
  NCT04386317updated 2026-03-02
• Cardiac Changes in Early Parkinson's Disease: A Follow up Study
  Active not recruiting · Phase 2 · Interventional · 15 enrolled · Cedars-Sinai Medical Center
  NCT04218968updated 2026-03-02
• Terazosin and Parkinson's Disease Extension Study
  Active not recruiting · Phase 2 · Interventional · 15 enrolled · Cedars-Sinai Medical Center
  NCT05109364updated 2026-03-02
• Markers of Disease Progression and Gait Within the Parkinsonian Population
  Completed · Interventional · 83 enrolled · University Hospital, Lille
  NCT04653688updated 2025-12-04
• [18F] LBT-999 PET Compared to [123I]-FP/CIT SPECT to Distinguish Between Parkinson's Diseases and Essential Tremor
  Completed · Phase 3 · Interventional · 152 enrolled · GE Healthcare
  NCT04265209updated 2025-11-17
• Molecular and Functional Imaging in Monogenic PD.
  Recruiting · Observational · 45 enrolled · University of Exeter
  NCT05518617updated 2025-10-07
• Video-oculography and Parkinson's Disease
  Recruiting · Interventional · 30 enrolled · Association de Recherche Bibliographique pour les Neurosciences
  NCT04731246updated 2025-10-01

Frequently asked questions

How does Ioflupane work?

The active drug substance in Ioflupane I 123 Injection is N-ω-fluoropropyl-2β-carbomethoxy-3β-(4-[ 123 I]iodophenyl)nortropane or ioflupane I-123. In vitro , ioflupane binds reversibly to the human dopamine transporter (DaT) (Ki = 0.62 nM; IC 50 = 0.71 nM).

What is Ioflupane used for?

According to FDA labeling, Ioflupane carries indications including: Ioflupane I 123 Injection is indicated as an adjunct to other diagnostic evaluations for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging in adult patients with: ● suspected Parkinsonian syndromes (PS) or ● suspected dementia with Lewy bodies (DLB). Ioflupane I 123 Injection is a radioactive diagnostic agent indicated as an adjunct to other diagnostic evaluations for striatal dopamine transporter visualization using single photon emission computed tomography (SPECT) brain imaging in adult patients with: suspected Parkinsonian syndromes (PS) or suspected dementia with Lewy bodies (DLB).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ioflupane?

Ioflupane is classified as Radiopharmaceutical Activity.

What are the contraindications for Ioflupane?

Ioflupane labeling lists contraindications including: Ioflupane I 123 Injection is contraindicated in patients with known serious hypersensitivity to ioflupane I-123 [see Warnings and Precautions ( 5.1 )] .. Always consult the full prescribing information and a clinician.