Axumin

In the U.S.

• Axumin

Available Dosage Forms:

• Solution

Therapeutic Class: Diagnostic Agent, Radiopharmaceutical Imaging

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur:

• Cough
• difficulty with swallowing
• dizziness
• fast heartbeat
• hives, itching, or skin rash
• puffiness or swelling of the eyelids or around the eyes, face, lips, throat, or tongue
• tightness in the chest
• trouble breathing
• unusual tiredness or weakness

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Change in taste
• loss of taste
• redness or pain at the injection site

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Axumin is indicated for positron emission tomography (PET) in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment.

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The clinical trial database for Axumin includes data from 877 subjects including 797 males diagnosed with prostate cancer. Most patients received a single administration of Axumin, a small number of subjects (n = 50) received up to five administrations of the drug. The mean administered activity was 370 MBq (range, 163 to 485 MBq).

Adverse reactions were reported in ≤1% of subjects during clinical studies with Axumin. The most common adverse reactions were injection site pain, injection site erythema and dysgeusia.

Pregnancy

Risk Summary

Axumin is not indicated for use in females and there is no information on the risk of adverse development outcomes in pregnant women or animals with the use of fluciclovine F 18.

Lactation

Risk Summary

Axumin is not indicated for use in females and there is no information of the presence of fluciclovine F 18 in human milk.

Pediatric Use

Safety and effectiveness have not been established in pediatric patients.

Geriatric Use

Of the total number of patients in clinical studies of Axumin, the average age was 66 years with a range of 21 to 90 years. No overall differences in safety or effectiveness were observed between older subjects and younger subjects.

Mechanism of action

Fluciclovine F 18 is a synthetic amino acid transported across mammalian cell membranes by amino acid transporters, such as LAT-1 and ASCT2, which are upregulated in prostate cancer cells. Fluciclovine F 18 is taken up to a greater extent in prostate cancer cells compared with surrounding normal tissues.

Pharmacodynamics

Following intravenous administration, the tumor-to-normal tissue contrast is highest between 4 and 10 minutes after injection, with a 61% reduction in mean tumor uptake at 90 minutes after injection.

Pharmacokinetics

Distribution

Following intravenous administration, fluciclovine F 18 distributes to the liver (14% of administered activity), pancreas (3%), lung (7%), red bone marrow (12%) and myocardium (4%). With increasing time, fluciclovine F 18 distributes to skeletal muscle.

Excretion

Across the first four hours post-injection, 3% of administered radioactivity was excreted in the urine. Across the first 24 hours post-injection, 5% of administered radioactivity was excreted in the urine.

• Instruct patients to avoid significant exercise for at least a day before the PET scan.
• Instruct patients not to eat or drink for at least 4 hours before the PET scan (other than small amounts of water for taking medications).

Marketed by Blue Earth Diagnostics Ltd. Oxford, UK OX4 4GA
Axumin™ is a trademark of Blue Earth Diagnostics Ltd.
© 2016 Blue Earth Diagnostics Ltd – all rights reserved.

Sterile

Axumin™

Non-pyrogenic

(fluciclovine F 18) injection
9 - 221 mCi/mL at End of Synthesis (EOS)
Diagnostic - For Intravenous Use Only
Expires 10 hours after EOS

Batch #: ________________________________

EOS Date: __________ EOS Time: __________

Activity @ EOS: ___________________ mCi

Concentration: ___________________ mCi/mL

Volume: ___________________ mL

Exp. Date: __________ Exp. Time: __________

Applies to fluciclovine F 18: intravenous solution

Along with its needed effects, fluciclovine F 18 (the active ingredient contained in Axumin) may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur while taking fluciclovine F 18:

• Cough
• difficulty with swallowing
• dizziness
• fast heartbeat
• hives, itching, or skin rash
• puffiness or swelling of the eyelids or around the eyes, face, lips, throat, or tongue
• tightness in the chest
• trouble breathing
• unusual tiredness or weakness

Some side effects of fluciclovine F 18 may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Change in taste
• loss of taste
• redness or pain at the injection site

This drug is not indicated for use in female patients. Risk Summary: There is no information on the risk of adverse development outcomes in pregnant women or animals.