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The primary objective of this study is: to evaluate the safety of technetium [99mTc]-H7ND injection in patients with gastrointestinal malignancies and in healthy subjects. The secondary objectives of this study are: (1) to examine the pharmacokinetics of technetium [99mTc]-H7ND Injection in healthy subjects. (2) Detect the metabolic stability of technetium [99mTc]-H7ND injection in healthy humans. (3) Detect the biodistribution and estimate the absorbed dose of radiation from internal irradiation of technetium [99mTc]-H7ND injection in patients with malignant tumors of the gastrointestinal tract and in healthy humans.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Patients with malignant tumors of the gastrointestinal tract or healthy subjects | Experimental | Each patient will receive 10 or 20 mCi ± 20% technetium [99mTc]-H7ND injection intravenously |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Technetium [99mTc]-H7ND injection | Drug | Technetium [99mTc]-H7ND injection is a radiolabeled fibroblast activation protein inhibitor |
|
| Measure | Description | Time Frame |
|---|---|---|
| Security Indicators | Evaluation of adverse events and serious adverse events according to the Common Terminology Criteria for the Evaluation of Adverse Events (NCI-CTCAE) version 5.0 | 1-7 days from time of injection |
| Measure | Description | Time Frame |
|---|---|---|
| uptake value ratio | Measure the count ratio of technetium [99mTc]-H7ND tumor area to blood pool, surrounding normal tissue, liver, and muscle in the integrated region of interest. | 3 days after injection |
| biodiversity distribution |
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Inclusion Criteria:
Exclusion Criteria:
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| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Zhongshan Hospital Affiliated to Fudan University | Shanghai | China |
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| ID | Term |
|---|---|
| D013667 | Technetium |
| ID | Term |
|---|---|
| D004603 | Elements, Radioactive |
| D004602 | Elements |
| D007287 | Inorganic Chemicals |
| D019216 | Metals, Heavy |
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SPECT/CT whole-body scans were performed at different time points after drug injection to obtain radioactivity counts (%ID) in each major irradiated organ at each time phase to reflect the biodistribution of the drug in the body
| 3 days after injection |
| internal radiation dose | Plot the "time-activity count" curve for each major organ and calculate the area under the curve. Calculate the retention time of each major exposed organ and apply the software to estimate the absorbed dose of internal radiation for each major exposed organ. | 3 days after injection |
| Concentration of technetium [99mTc] H7ND prototype and its radioactive metabolites | Blood samples were collected at different time points after drug injection, and urine samples were collected at different time intervals for detection of technetium [99mTc] H7ND prototype and its radioactive metabolites using either a radioactive HPLC detector or a radioactive TLC detector. | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | Cmax | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | AUC(0-t) | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | AUC(0-∞) | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | Tmax | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | T1/2 | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | AUC_%Extrap | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | CL | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | Vd | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | MRT | Predose and up to 72 hours postdose |
| Pharmacokinetic parameters | λz | Predose and up to 72 hours postdose |
| D028561 |
| Transition Elements |
| D011868 | Radioisotopes |
| D007554 | Isotopes |
| D008670 | Metals |