Locametz

kit for the preparation of gallium Ga 68 gozetotide · Injection, Powder, Lyophilized, For Solution · Intravenous

Prescription (Rx)

Uses

1 INDICATIONS AND USAGE LOCAMETZ, after radiolabeling with gallium-68, 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. for selection of patients who are indicated for PSMA-directed therapy as described in the prescribing information of the therapeutic products. LOCAMETZ, after radiolabeling with gallium-68, 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 for selection of patients who are indicated for PSMA-directed therapy as described in the prescribing information of the therapeutic products. ( 1 )

Dosage and administration

Use appropriate radiation safety measures and aseptic precautions while handling and administering gallium Ga 68 gozetotide injection. ( 2.1 ) The recommended amount of radioactivity is 111 MBq to 259 MBq (3 mCi to 7 mCi). Administered as slow intravenous injection. ( 2.2 ) Advise patients to be well hydrated prior to the administration and to void immediately prior to and frequently after image acquisition. ( 2.3 ) A diuretic expected to act within the uptake time period may be administered at the time of radiotracer injection. ( 2.6 ) Acquire PET whole body images 50 minutes to 100 minutes after administration. ( 2.7 ) See the full prescribing information for detailed instructions on preparation, administration, imaging, and radiation dosimetry. ( 2 ) 2.1 Radiation Safety – Drug Handling After reconstitution and radiolabeling of LOCAMETZ, the vial contains gallium Ga 68 gozetotide injection. Handle the gallium Ga 68 gozetotide injection with appropriate safety measures to minimize radiation exposure [see Warnings and Precautions (5.2)] . Use waterproof gloves, effective radiation shielding, and other appropriate safety measures when preparing and handling gallium Ga 68 gozetotide injection. Radiopharmaceuticals should be used by or under the control of health care providers 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 governmental agency authorized to license the use of radionuclides. 2.2 Recommended Dosage In adults, the recommended amount of radioactivity to be administered for PET is 111 MBq to 259 MBq (3 mCi to 7 mCi) by slow intravenous injection. 2.3 Patient Preparation Advise patients to be well hydrated prior to gallium Ga 68 gozetotide injection administration and to void immediately prior to and frequently during the first hours after image acquisition to reduce radiation exposure [see Warnings and Precautions (5.2)] . 2.4 Drug Preparation LOCAMETZ allows the direct preparation of gallium Ga 68 gozetotide injection with the eluate from one of the following generators (see below for specific instruction for use with each generator): Eckert & Ziegler GalliaPharm germanium-68/gallium-68 ( 68 Ge/ 68 Ga) generator IRE ELiT Galli Eo germanium-68/gallium-68 ( 68 Ge/ 68 Ga) generator The instructions for use provided by the germanium-68/gallium-68 generator manufacturer should also be followed. Prepare gallium Ga 68 gozetotide injection according to the following aseptic procedure: a. Use suitable shielding to reduce radiation exposure. b. Wear waterproof gloves. c. Flip the cap off the LOCAMETZ vial and swab the septum with an appropriate antiseptic, then allow the septum to dry. d. Pierce the LOCAMETZ vial septum with a sterile needle connected to a 0.2-micron sterile air venting filter to maintain atmospheric pressure within the vial during the reconstitution process. e. Place the LOCAMETZ vial in a lead shield container. f. Follow the generator specific procedures below. Schematic diagrams are provided in Figures 1 and 2. Preparation with Eckert & Ziegler GalliaPharm Generator 1) Connect the male luer of the outlet line of the generator to a sterile elution needle (size 21G to 23G). 2) Connect the LOCAMETZ vial directly to the outlet line of the generator by pushing the elution needle through the rubber septum. 3) Elute directly from the generator into the LOCAMETZ vial. 4) Perform the elution manually or by means of a pump according to the generator instructions for use. 5) Reconstitute the lyophilized powder with 5 mL of eluate. 6) At the end of the elution, disconnect the LOCAMETZ vial from the generator by removing the elution needle and the vent needle with the 0.2-micron sterile air venting filter from the rubber septum. Then, invert LOCAMETZ vial once and place it upright. 7) Incubate the LOCAMETZ vial upright between 20°C to 30°C (68°F to 86°F) for at least 5 minutes without agitation or stirring. 8) After 5 minutes, assay the vial containing the gallium Ga 68 gozetotide injection for total radioactivity using a dose calibrator, calculate the radioactivity concentration and record the result. 9) After radiolabeling, gallium Ga 68 gozetotide injection may be diluted with Sterile Water for Injection, USP or 0.9% Sodium Chloride Injection, USP up to a final volume of 10 mL. 10) Perform quality controls according to the recommended methods in order to check compliance with the specifications [see Dosage and Administration (2.5)] . 11) Store the LOCAMETZ vial containing the gallium Ga 68 gozetotide injection upright in a lead shield container below 30°C (86°F) until use. 12) After addition of gallium-68 chloride to the LOCAMETZ vial, use gallium Ga 68 gozetotide injection within 6 hours. Preparation with IRE ELiT Galli Eo Generator 1) Connect the male luer of the outlet line of the generator to a sterile elution needle (size 21G to 23G). 2) Connect the LOCAMETZ vial directly to the outlet line of the generator by pushing the elution needle through the rubber septum. 3) Connect the LOCAMETZ vial through the vent needle with 0.2-micron sterile air venting filter to a vacuum vial (25 mL minimum volume) by means of a sterile needle (size 21G to 23G) or to a vacuum pump to start the elution. 4) Elute directly from the generator into the LOCAMETZ vial. 5) Reconstitute the lyophilized powder with 1.1 mL of eluate. 6) At the end of the elution, first withdraw the sterile needle from the vacuum vial or disconnect the vacuum pump in order to establish atmospheric pressure into the LOCAMETZ vial, then disconnect the vial from the generator by removing both the elution needle and the vent needle with the 0.2-micron sterile air venting filter needle from the rubber septum. Inversion of the LOCAMETZ vial is not needed. 7) Incubate the LOCAMETZ vial upright between 20°C to 30°C (68°F to 86°F) for at least 5 minutes without agitation or stirring.

Dosage forms and strengths

3 DOSAGE FORMS AND STRENGTHS LOCAMETZ is a kit for the preparation of gallium Ga 68 gozetotide injection supplied in a multiple-dose vial containing 25 micrograms of gozetotide as a white lyophilized powder. Gallium-68 is obtained from one of the following generators: Eckert & Ziegler GalliaPharm (Ge 68/Ga 68) generator IRE ELiT Galli Eo (Ge 68/Ga 68) generator After radiolabeling with gallium-68, each vial contains a sterile, clear, colorless solution free from particulate matter of gallium Ga 68 gozetotide at an activity of up to 2,590 MBq (70 mCi) in up to 10 mL at calibration date and time. Kit for the preparation of gallium Ga 68 gozetotide injection supplied in a multiple-dose vial containing 25 mcg of gozetotide as a white lyophilized powder. After radiolabeling with gallium-68, the vial contains a sterile solution of gallium Ga 68 gozetotide at a strength up to 2,590 MBq (70 mCi) in up to 10 mL at calibration date and time. ( 3 )

Contraindications

None. None. ( 4 )

Warnings and precautions

Risk for Misinterpretation: Gallium Ga 68 gozetotide uptake may occur in other tumor types and in non-malignant processes. Interpretation of LOCAMETZ PET imaging with histopathology and/or other diagnostic procedures is recommended. ( 5.1 ) Radiation Risk: Gallium Ga 68 gozetotide contributes to a patient’s overall long-term cumulative radiation exposure. Ensure safe handling and preparation procedures to protect patients and health care workers from unintentional radiation exposure. ( 5.2 ) 5.1 Risk for Misinterpretation Image interpretation errors can occur with LOCAMETZ PET. Negative imaging does not rule out the presence of prostate cancer and positive imaging does not confirm the presence of prostate cancer. Gallium Ga 68 gozetotide uptake is not specific for prostate cancer and may occur with other types of cancer as well as non-malignant processes, such as Paget’s disease, fibrous dysplasia, and osteophytosis. Clinical correlation, which may include histopathological evaluation of the suspected prostate cancer site, is recommended. The performance of LOCAMETZ for imaging of biochemically recurrent prostate cancer seems to be affected by serum PSA levels and by site of disease. The performance of LOCAMETZ for imaging of metastatic pelvic lymph nodes prior to initial definitive therapy seems to be affected by Gleason score [see Clinical Studies (14.1, 14.2)] . 5.2 Radiation Risk Gallium Ga 68 gozetotide contributes to the patient’s overall long-term cumulative radiation exposure. Long-term cumulative radiation exposure is associated with an increased risk of cancer. Ensure safe handling to minimize radiation exposure to the patient and health care workers. Advise patients to be well hydrated prior to gallium Ga 68 gozetotide injection administration and to void immediately prior to and frequently during the first hours after image acquisition to reduce radiation exposure [see Dosage and Administration (2.1, 2.3)] .

Side effects

The adverse reactions (incidence ≥ 0.5%) are fatigue, nausea, constipation, and vomiting. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Novartis Pharmaceuticals Corporation at 1-888-669-6682 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 LOCAMETZ has been established based on three prospective studies of gallium Ga 68 gozetotide in patients with prostate cancer (i.e., Studies 1, 2, and 3). Adverse reactions from these studies are reported below. In Studies 1 and 2 using another formulation of gallium Ga 68 gozetotide injection, 960 patients received one dose of gallium Ga 68 gozetotide intravenously with the amount (mean ± SD) of radioactivity 188.7 ± 40.7 MBq (5.1 ± 1.1 mCi) [see Clinical Studies (14.1, 14.2)] . The most commonly reported adverse reactions were nausea, diarrhea and dizziness, occurring at a rate of < 1%. In a randomized, multicenter, open-label clinical study (NCT03511664, referred to as Study 3) in which gallium Ga 68 gozetotide was used to identify PSMA-positive patients on PET imaging to determine eligibility for PSMA-directed therapy, 1,003 patients with progressive metastatic castration-resistant prostate cancer (mCRPC) received one dose of gallium Ga 68 gozetotide intravenously with the amount of radioactivity 167.1 ± 23.1 MBq (4.52 ± 0.62 mCi). Patients were males with median age of 70 years (range, 40 to 94 years), were White (87%), Black or African American (7%), or Asian (2.4%), and had median baseline PSA levels of 74 ng/mL (range, 0 to 8995 ng/mL). Adverse reactions occurring at ≥ 0.5% in patients with metastatic prostate cancer who received gallium Ga 68 gozetotide injection in Study 3 are presented in Table 3. Table 3. Adverse Reactions (≥ 0.5%) in Patients with Metastatic Prostate Cancer Who Received Gallium Ga 68 Gozetotide Injection in Study 3 Adverse reactions Gallium Ga 68 Gozetotide Injection N = 1003 n (%) General disorders Fatigue 12 (1.2) Gastrointestinal disorders Nausea 8 (0.8) Constipation 5 (0.5) Vomiting 5 (0.5) Adverse reactions occurring at a rate of < 0.5% in the study were diarrhea, dry mouth, injection site reactions including injection site hematoma and injection site warmth, and chills.

Drug interactions

Androgen Deprivation Therapy and Other Therapies Targeting the Androgen Pathway Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway, such as androgen receptor antagonists, can result in changes in uptake of gallium Ga 68 gozetotide in prostate cancer. The effect of these therapies on performance of LOCAMETZ PET has not been established.

Use in specific populations

8.1 Pregnancy Risk Summary LOCAMETZ is not indicated for use in females. There are no available data with gallium Ga 68 gozetotide use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. All radiopharmaceuticals, including LOCAMETZ, have the potential to cause fetal harm depending on the fetal stage of development and the magnitude of radiation dose. Animal reproduction studies have not been conducted with gallium Ga 68 gozetotide. 8.2 Lactation Risk Summary LOCAMETZ is not indicated for use in females. There are no data on the presence of gallium Ga 68 gozetotide in human milk, the effect on the breastfed infant, or the effect on milk production. 8.4 Pediatric Use The safety and effectiveness of gallium Ga 68 gozetotide in pediatric patients have not been established. 8.5 Geriatric Use The efficacy of LOCAMETZ in geriatric patients with prostate cancer is based on data from three prospective studies. Of the total number of patients in Studies 1 and 2 [see Clinical Studies (14.1, 14.2)] , 691 of 960 (72%) were 65 years of age and older while 195 (20%) were 75 years of age and older. Of the total number of patients in Study 3 [see Adverse Reactions (6.1)] , 752 of 1,003 (75%) were 65 years of age and older while 284 (28%) were 75 years of age and older. The efficacy and safety profiles of gallium Ga 68 gozetotide appeared similar in younger adult and geriatric patients with prostate cancer and other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Pregnancy

Pediatric use

8.4 Pediatric Use The safety and effectiveness of gallium Ga 68 gozetotide in pediatric patients have not been established.

Geriatric use

8.5 Geriatric Use The efficacy of LOCAMETZ in geriatric patients with prostate cancer is based on data from three prospective studies. Of the total number of patients in Studies 1 and 2 [see Clinical Studies (14.1, 14.2)] , 691 of 960 (72%) were 65 years of age and older while 195 (20%) were 75 years of age and older. Of the total number of patients in Study 3 [see Adverse Reactions (6.1)] , 752 of 1,003 (75%) were 65 years of age and older while 284 (28%) were 75 years of age and older. The efficacy and safety profiles of gallium Ga 68 gozetotide appeared similar in younger adult and geriatric patients with prostate cancer and other reported clinical experience has not identified differences in responses between the elderly and younger patients.

Overdosage

In the event of an overdose of gallium Ga 68 gozetotide, reduce the radiation absorbed dose to the patient where possible by increasing the elimination of the radioactivity from the body by hydration and frequent bladder voiding. A diuretic might also be considered. If possible, an estimate of the effective radiation dose exposure to the patient should be made.

Description

11.1 Chemical Characteristics LOCAMETZ (kit for the preparation of gallium Ga 68 gozetotide injection) is a sterile, radioactive diagnostic agent for intravenous administration after radiolabeling. Each vial contains 25 micrograms of gozetotide, 1 mg gentisic acid, 78 mg of sodium acetate trihydrate, and 40 mg sodium chloride. Gozetotide is also known as PSMA-11. After reconstitution and radiolabeling of LOCAMETZ, the vial contains gallium Ga 68 gozetotide injection at a radioactivity of up to 2,590 MBq (70 mCi) in up to 10 mL at calibration date and time. The vial also contains hydrochloric acid derived from the gallium-68 chloride solution. Gallium Ga 68 gozetotide injection has a pH between 3.2 to 6.5. Gallium Ga 68 gozetotide is a urea based peptidomimetic that has a covalently bound chelator (HBED-CC). The peptide has amino acid sequence OH-Glu-CO-Lys(Ahx-CC-HBED)-OH. Gallium Ga 68 gozetotide has a molecular weight of 1011.91 g/mol. The chemical structure is shown in Figure 3. Figure 3. Chemical Structure of Gallium Ga 68 Gozetotide 11.2 Physical Characteristics Gallium-68 decays with a half-life of 68 minutes to stable zinc-68. Table 4 and Table 5 display the principle radiation emission data, and physical decay of gallium-68. Table 4. Principal Radiation Emission Data (> 1%) for Gallium-68 Radiation/Emission % Disintegration Mean energy (MeV) beta+ 88% 0.8360 beta+ 1.1% 0.3526 Gamma 178% 0.5110 Gamma 3% 1.0770 X-ray 2.8% 0.0086 X-ray 1.4% 0.0086 Table 5. Physical Decay Chart for Gallium-68 Minutes Fraction remaining 0 1 15 0.858 30 0.736 60 0.541 90 0.398 120 0.293 180 0.158 240 0.086 360 0.025 11.3 Radiation Attenuation Table 6 displays the radiation attenuation by lead shielding of gallium-68. Table 6. Radiation Attenuation of 511 keV Photons by Lead (Pb) Shielding Shield thickness (Pb) mm Coefficient of attenuation 6 0.5 12 0.25 17 0.1 34 0.01 51 0.001 Figure 3. Chemical Structure of Gallium Ga 68 Gozetotide

Mechanism of action

12.1 Mechanism of Action Gallium Ga 68 gozetotide binds to PSMA. It binds to cells that express PSMA, including malignant prostate cancer cells, which usually overexpress PSMA. Gallium-68 is a β+ emitting radionuclide that allows PET.

How supplied

How Supplied LOCAMETZ is supplied as a kit for the preparation of gallium Ga 68 gozetotide injection in a carton of 1 vial (NDC# 0078-1224-61). Each multiple-dose vial contains 25 micrograms of gozetotide as white lyophilized powder packaged in a 10 mL type I Plus glass vial closed with a rubber stopper and sealed with a flip-off cap. Storage and Handling Before radiolabeling, store at 2°C to 25°C (36°F to 77°F). Do not freeze. After radiolabeling, store upright with an appropriate lead shielding to protect from radiation, below 30°C (86°F). Do not freeze. After radiolabeling, use within 6 hours. This preparation is approved for use by persons under license by the Nuclear Regulatory Commission or the relevant regulatory authority of an Agreement State.

Patient information

Adequate Hydration Advise patients to be well hydrated prior to the administration of gallium Ga 68 gozetotide injection and urge them to urinate immediately prior to image acquisition and frequently during the first hours following administration to reduce radiation exposure [see Dosage and Administration (2.3), Warnings and Precautions (5.2)] . Distributed by: Novartis Pharmaceuticals Corporation East Hanover, NJ 07936 ©2025 Novartis LOCAMETZ ® is a registered trademark of Novartis AG and/or its affiliates. U.S. Patent 11369590 T2025-37

Label text from the FDA structured product label by Novartis Pharmaceuticals Corporation (revised Jan 15, 2026). Long sections are shortened; the complete label is on DailyMed.

Active ingredients

Gozetotide in 1 product

Locametz NDC products (1)

NDC	Strength & form	Labeler	Type
0078-1224	Gozetotide 25 ug/1 Injection, Powder, Lyophilized, For Solution	Novartis Pharmaceuticals Corporation	NDA

Frequently asked questions

What is Locametz used for?

What are the side effects of Locametz?

Who makes Locametz?

Locametz is listed by 1 labeler in the FDA NDC directory, including Novartis Pharmaceuticals Corporation.