Technetium (99mTc) Tilmanocept
Technetium (99mTc) Tilmanocept Uses, Dosage, Side Effects, Food Interaction and all others data.
Technetium (99mTc) Tilmanocept is a radiopharmaceutical diagnostic imaging agent approved by the U.S. Food and Drug Administration (FDA) for the imaging of lymph nodes with or without scintigraphic imaging. It is a macromolecule consisting of multiple units of diethylenetriaminepentaacetic acid (DTPA) and mannose, each covalently attached to a 10 kDa dextran backbone . DTPA serves as a chelating agent for technetium Tc 99m to bind . Technetium (99mTc) Tilmanocept is used in lymphatic mapping and lymph node localization in breast cancer, melanoma, clinically node-negative squamous cell carcinoma of the oral cavity, and other solid tumors . Detecting sentinel lymph node (SLN) is clinically useful in the prognosis and management of the disease, as it is considered as the first lymph node that receives afferent lymphatic drainage from a primary tumor, and may be used to predict tumour staging and metastasis . However, as nodal micrometastasis in breast cancer may not be associated with significant changes in survival, it is also important to identify clinically node-negative patients .
Technetium (99mTc) Tilmanocept is a novel CD206 receptor-targeted molecule that selectively binds to mannose receptors expressed on the surface of reticuloendothelial cells in lymph nodes . Due to its relatively small molecular weight and small molecular diameter of 7 nm , technetium Tc-99m tilmanocept displays more rapid injection site clearance, high sentinel node extraction, and low distal node accumulation compared to other conventional radiocolloids . It achieves high overall accuracy in detecting SLN . Once reconstituted and labelled, technetium Tc99m tilmanocept is intended to be injected in close proximity to the tumor being diagnosed and employed in preoperative gamma detection imaging in combination with various other techniques, including scintigraphy, SPECT, and SPECT/CT . It may be administered via subcutaneous, intradermal, subareolar, or peritumoral injection, depending on the tutor location and planned injection technique . It is marketed under the trade name Lymphoseek. Potential application of technetium Tc-99m tilmanocept to other cancers are being investigated .
Technetium Tc 99m tilmanocept binds to the CD206 receptors on the surface of reticuloendothelial cells, such as macrophages and dendritic cells, which are highly expressed in lymph nodes. In clinical studies, technetium Tc 99m tilmanocept has been shown to be detectable in lymph nodes within 10 minutes and up to 30 hours after injection . Moreover, Phase 1 clinical studies showed approximately 0.5 to 1.8% of a dose accumulating in draining lymph nodes via specific binding after about 30 minutes. Technetium Tc99m tilmanocept bindng appears to be independent of tumor type or severity . It displays rapid injection site clearance, rapid accumulation, long retention in the sentinel node, and low distal node accumulation .
| Trade Name | Technetium (99mTc) Tilmanocept |
| Generic | Technetium Tc-99m tilmanocept |
| Technetium Tc-99m tilmanocept Other Names | Technetium (99mTc) tilmanocept, Technetium Tc 99m Tilmanocept, Technetium Tc99 tilmanocept |
| Type | |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Technetium (99mTc) Tilmanocept is a radiopharmaceutical diagnostic imaging agent indicated with or without scintigraphic imaging for lymphatic mapping and guiding sentinel lymph node biopsy.
Indicated with or without scintigraphic imaging for lymphatic mapping using a handheld gamma counter to locate lymph nodes draining a primary tumor site in patients with solid tumors for which this procedure is a component of intraoperative management .
Indicated with or without scintigraphic imaging for guiding sentinel lymph node biopsy using a handheld gamma counter in patients with clinically node negative squamous cell carcinoma of the oral cavity, breast cancer or melanoma .
Technetium (99mTc) Tilmanocept is also used to associated treatment for these conditions: Squamous Cell Carcinoma (SCC), Squamous Cell Carcinoma of the Oral Cavity, Tumors, Solid
How Technetium (99mTc) Tilmanocept works
The mannose of the molecule acts as a ligand and guides the molecule to selectively bind to human mannose binding receptors (CD206) located on the surface of reticuloendothelial cells residing within lymph nodes, such as macrophages and dendritic cells . According to in vitro studies, technetium Tc 99m tilmanocept demonstrates selective binding to CD206 with a primary binding site affinity of Kd = 2.76 x 10^-11 M.
Toxicity
Tilmanocept was not mutagenic in vitro in the Ames bacterial mutation assay and in the in vitro mouse lymphoma test, and was negative in the in vivo micronucleus test in mice. Studies assessing the carcinogenic potential or effects on reproductive fertility have not been conducted .
Food Interaction
No interactions found.Elimination Route
In clinical studies, technetium Tc 99m tilmanocept was detectable in lymph nodes within 10 minutes and up to 30 hours after injection. The maximum amount of the accumulated radioactive dose in the liver, kidney, and bladder was reached at 1 hour post-injection and was approximately 1-2% of the total, injected dose in each tissue .
Half Life
Technetium Tc99m tilmanocept decays by isomeric transition with a physical half-life of approximately 6 hours. The half-life at the injection site of 1.8 to 3.1 hours .
Clearance
In dose-ranging clinical studies, injection site clearance rates were similar across doses ranging from 4 to 200 mcg with a mean elimination rate constant in the range of 0.222 to 0.396/hr .
Elimination Route
It is believed that technetium Tc 99m tilmanocept is eliminated primarily through the kidneys as primary metabolites. Technetium Tc 99m tilmanocept may undergo hepatic elimination and biliary elimination [L1557]
Innovators Monograph
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