Home › Drugs › Flotufolastat F-18

Flotufolastat F-18

FDA Drug Information • Also known as: Posluma

Brand Names
Posluma
Drug Class
Radioactive Diagnostic Agent [EPC]
Route
INTRAVENOUS
Dosage Form
INJECTION
Product Type
HUMAN PRESCRIPTION DRUG

Description

11 DESCRIPTION 11.1 Chemical Characteristics POSLUMA (flotufolastat F 18) injection is a radioactive diagnostic agent for intravenous use. The active ingredient of POSLUMA is flotufolastat F 18 gallium, of which the molecular structure includes a DOTAGA complex with nonradioactive gallium. Radioactive fluorine-18 is covalently bound to silicon. Chemically, flotufolastat F 18 gallium is gallate(6-), [(4 S ,8 S ,13 R ,27 R ,30 R ,35 S )-35-[4,10-bis[(carboxy-k O )methyl]-7-(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl-k N 1 ,k N 4 ,k N 7 ,k N 10 ]-30-[[[4-[bis(1,1-dimethylethyl)fluoro- 18 F -silyl]benzoyl]amino]methyl]-1,36-dihydroxy-1,6,11,18,21,29,32,36-octaoxo-5,7,12,17,22,28,31-heptaazahexatriacontane-4,8,13,27-tetracarboxylato(9-)]-, hydrogen (1:6). The molecular weight is 1537.3 g/mol and the structural formula is: POSLUMA is a sterile, non-pyrogenic, clear, colorless, and isotonic solution. Each mL contains up to 20 mcg of flotufolastat gallium, up to 5,846 MBq (158 mCi) as flotufolastat F 18 gallium at end of synthesis, and the following inactive ingredients: 6.3% (v/v) alcohol, 1.9 mg anhydrous citric acid, 7.2 mg sodium chloride, and 0.75 mg sodium hydroxide to adjust pH between 4 and 6. POSLUMA contains no preservative. Structural Formula 11.2 Physical Characteristics POSLUMA contains fluorine-18 (F 18) which is a cyclotron produced radionuclide that decays by positron emission (β+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen-18 with a physical half-life of 109.8 minutes ( Table 3 ). The principal photons useful for diagnostic imaging are the coincident pair of 511 keV gamma photons, resulting from the interaction of the emitted positron with an electron ( Table 4 ). Table 3: Physical Decay Chart for Fluorine-18 Minutes Fraction Remaining 0 1 15 0.909 30 0.826 60 0.683 110 0.5 220 0.25 Table 4: Principal Radiation Produced from Decay of Fluorine-18 Energy (keV) Abundance (%) Positron 249.8 96.7 Gamma 511 193.5 11.3 External...

What Is Flotufolastat F-18 Used For?

1 INDICATIONS AND USAGE POSLUMA is indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy. with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. POSLUMA is a radioactive diagnostic agent indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer: with suspected metastasis who are candidates for initial definitive therapy with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. ( 1 )

Dosage and Administration

2 DOSAGE AND ADMINISTRATION Recommended amount of radioactivity of POSLUMA is 296 MBq (8 mCi) administered as an intravenous bolus injection. ( 2.2 ) Initiate imaging approximately 60 minutes after administration. Scanning should start from mid-thigh and proceed to base of skull. ( 2.4 ) See full prescribing information for additional preparation, handling, administration, imaging, and radiation dosimetry information. ( 2.3 , 2.4 ) 2.1 Radiation Safety - Drug Handling Handle POSLUMA with safety measures to minimize radiation exposure [ see Warnings and Precautions ( 5.2 )] . Use waterproof gloves, effective radiation shielding, including syringe shields, and other appropriate safety measures when handling and administering POSLUMA. Radiopharmaceuticals should be used by or under the control of physicians who are qualified by specific training and experience in the safe use and handling of radionuclides, and whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radionuclides. 2.2 Recommended Dose and Administration Instructions Recommended Dose The recommended amount of radioactivity to be administered in adults is 296 MBq (8 mCi) as an intravenous bolus injection. Preparation and Administration Instructions Inspect POSLUMA visually for particulate matter and discoloration before administration. Do not use the drug if the solution contains particulate matter or is discolored. Use aseptic technique and radiation shielding when withdrawing and administering POSLUMA. Calculate the necessary volume to administer based on calibration time and required dose. The recommended maximum volume of undiluted POSLUMA is 5 mL. POSLUMA may be diluted with 0.9% Sodium Chloride Injection, USP. Assay the dose in a dose calibrator before administration. Post Administration Instructions After the POSLUMA injection, administer an intravenous flush of sterile 0.9% Sodium Chloride Injection, USP to ensure full delivery of the dose. Dispose of any unused drug in a safe manner in compliance with applicable regulations. 2.3 Patient Preparation Instruct patients to drink water prior to administration of POSLUMA to ensure adequate hydration and to continue drinking and voiding frequently for the first few hours following administration to reduce radiation exposure. 2.4 Image Acquisition Patients should void immediately prior to imaging. Position the patient supine with arms above the head. Begin image acquisition approximately 60 minutes after POSLUMA injection. Image acquisition should start from mid-thigh and proceed to the base of the skull. Scan duration is approximately 20 minutes depending on the number of bed positions and acquisition time per bed position (typically 3 minutes). Adapt imaging technique according to the equipment used and patient characteristics in order to obtain the best image quality possible. 2.5 Image Display and Interpretation POSLUMA binds to PSMA. PET images obtained using...

Side Effects (Adverse Reactions)

6 ADVERSE REACTIONS The most common adverse reactions (≥0.4%) are diarrhea, blood pressure increase, and injection site pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Blue Earth Diagnostics Ltd at 1-844-POSLUMA (1-844-767-5862) 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 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 safety of POSLUMA was evaluated in 747 patients with prostate cancer [see Clinical Studies ( 14.1 , 14.2 )] . All patients received a single administration of POSLUMA with an administered radioactivity (mean ± SD) of 307 ± 23 MBq (8.3 ± 0.6 mCi). The mean age of patients was 67 years (range: 43 to 86 years); distribution by race was 78% White, 12% Black or African American, 2% other, and 7% unreported; and distribution by ethnicity was 5% Hispanic/Latino, 87% non-Hispanic/Latino, and 8% unreported. The adverse reactions reported in ≥ 0.4% of patients are shown in Table 2 . Table 2: Adverse Reactions in ≥ 0.4% of Patients with Prostate Cancer Receiving POSLUMA Adverse Reaction POSLUMA N = 747 n (%) Diarrhea 5 (0.7%) Blood pressure increase 4 (0.5%) Injection site pain 3 (0.4%)

Drug Interactions

7 DRUG INTERACTIONS Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway, such as androgen receptor antagonists, can result in changes in uptake of flotufolastat F 18 in prostate cancer. The effect of these therapies on performance of POSLUMA PET has not been established.

Contraindications

4 CONTRAINDICATIONS None. None. ( 4 )

Pregnancy and Breastfeeding

8.1 Pregnancy Risk Summary POSLUMA is not indicated for use in females. There are no available data on the use of POSLUMA 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 flotufolastat F 18. Radioactive drugs, including POSLUMA, have the potential to cause fetal harm depending on the fetal stage of development and the magnitude of the radiation dose.

Overdosage

10 OVERDOSAGE In the event of an overdose of POSLUMA, maintain hydration of the patient and frequent voiding to minimize radiation exposure. A diuretic might also be considered. If possible, an estimate of the radiation effective dose administered to the patient should be made.

How Supplied

16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied POSLUMA injection is supplied as a clear, colorless solution in a multiple-dose glass vial (NDC 69932-002-50) containing 296 MBq/mL to 5,846 MBq/mL (8 mCi/mL to 158 mCi/mL) as flotufolastat F 18 gallium in approximately 25 mL at end of synthesis. Storage and Handling Store POSLUMA at 20°C to 25°C (68°F to 77°F) [see USP Controlled Room Temperature]. Store POSLUMA in the original container in radiation shielding. The expiration date and time are provided on the container label. Use POSLUMA within 10 hours from end of synthesis. Dispose of unused POSLUMA in compliance with applicable regulations. This preparation is approved for use by persons under license by the Nuclear Regulatory Commission or the relevant regulatory authority of an Agreement State.

About This Information

This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.

What are side effects?

Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.

What are drug interactions?

Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.