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Technetium Tc-99m tilmanocept
Identification
- Name
- Technetium Tc-99m tilmanocept
- Accession Number
- DB09266
- Description
Technetium Tc-99m 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 Label. DTPA serves as a chelating agent for technetium Tc 99m to bind Label. Technetium Tc-99m 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 2,3. 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 3. 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 3.
Technetium Tc-99m tilmanocept is a novel CD206 receptor-targeted molecule that selectively binds to mannose receptors expressed on the surface of reticuloendothelial cells in lymph nodes 1. Due to its relatively small molecular weight and small molecular diameter of 7 nm 1, technetium Tc-99m tilmanocept displays more rapid injection site clearance, high sentinel node extraction, and low distal node accumulation compared to other conventional radiocolloids 3. It achieves high overall accuracy in detecting SLN 2. 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 4. It may be administered via subcutaneous, intradermal, subareolar, or peritumoral injection, depending on the tutor location and planned injection technique Label. It is marketed under the trade name Lymphoseek. Potential application of technetium Tc-99m tilmanocept to other cancers are being investigated 3.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Technetium (99mTc) tilmanocept
- Technetium Tc 99m Tilmanocept
- Technetium Tc99 tilmanocept
Pharmacology
- Indication
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 Label.
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 Label.
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
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 Label. 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 4. It displays rapid injection site clearance, rapid accumulation, long retention in the sentinel node, and low distal node accumulation 3.
- Mechanism of action
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 Label. 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.
Target Actions Organism AMacrophage mannose receptor 1 ligandHumans - Absorption
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 Label.
- Volume of distribution
- Not Available
- Protein binding
- Not Available
- Metabolism
Although the metabolism of technetium Tc 99m tilmanocept has not yet been experimentally investigated, tilmanocept may be metabolized in the liver to its main component molecules dextran, mannose and diethylenetriaminepentaacetic acid (DTPA). Subsequently, dextran may be further broken down into glucose. Furthermore, given the predominant role of the liver in the metabolism of technetium Tc 99m tilmanocept, some biliary elimination of the radiopharmaceutical is also expected. [L1557]
- Route of elimination
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]
- 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 Label.
- 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 Label.
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- 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 Label.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataArticaine Articaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Benzocaine Benzocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Benzyl alcohol Benzyl alcohol may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Bupivacaine Bupivacaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Capsaicin Capsaicin may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Chloroprocaine Chloroprocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Cinchocaine Cinchocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Cocaine Cocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Diphenhydramine Diphenhydramine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Dyclonine Dyclonine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- No interactions found.
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataKit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept) Kit 250 ug/1 Intradermal; Subcutaneous Cardinal Health 414, Llc 2017-09-20 Not applicable US 
Kit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept) Kit 250 ug/1 Intradermal; Subcutaneous Navidea Biopharmaceuticals, Inc. 2016-10-20 2019-06-01 US Kit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept) Kit 250 ug/1 Intradermal; Subcutaneous Cardinal Health 414, Llc 2017-09-20 Not applicable US Kit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept) Kit 250 ug/1 Intradermal; Subcutaneous Navidea Biopharmaceuticals, Inc. 2013-03-13 2019-06-01 US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories
- ATC Codes
- V09IA09 — Technetium (99mtc) tilmanocept
- Drug Categories
- Classification
- Not classified
Chemical Identifiers
- UNII
- 8IHI69PQTC
- CAS number
- 1262984-82-6
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Wallace AM, Han LK, Povoski SP, Deck K, Schneebaum S, Hall NC, Hoh CK, Limmer KK, Krontiras H, Frazier TG, Cox C, Avisar E, Faries M, King DW, Christman L, Vera DR: Comparative evaluation of [(99m)tc]tilmanocept for sentinel lymph node mapping in breast cancer patients: results of two phase 3 trials. Ann Surg Oncol. 2013 Aug;20(8):2590-9. doi: 10.1245/s10434-013-2887-8. Epub 2013 Mar 17. [PubMed:23504141]
- Agrawal A, Civantos FJ, Brumund KT, Chepeha DB, Hall NC, Carroll WR, Smith RB, Zitsch RP, Lee WT, Shnayder Y, Cognetti DM, Pitman KT, King DW, Christman LA, Lai SY: [(99m)Tc]Tilmanocept Accurately Detects Sentinel Lymph Nodes and Predicts Node Pathology Status in Patients with Oral Squamous Cell Carcinoma of the Head and Neck: Results of a Phase III Multi-institutional Trial. Ann Surg Oncol. 2015 Oct;22(11):3708-15. doi: 10.1245/s10434-015-4382-x. Epub 2015 Feb 11. [PubMed:25670018]
- Surasi DS, O'Malley J, Bhambhvani P: 99mTc-Tilmanocept: A Novel Molecular Agent for Lymphatic Mapping and Sentinel Lymph Node Localization. J Nucl Med Technol. 2015 Jun;43(2):87-91. doi: 10.2967/jnmt.115.155960. Epub 2015 May 8. [PubMed:25956693]
- Electronic Medicines Compendium: Lymphoseek (technetium TC 99M tilmanocept) Monograph [Link]
- External Links
- FDA label
- Download (281 KB)
- MSDS
- Download (124 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Diagnostic Breast Cancer 1 3 Completed Diagnostic Breast Cancer / Melanoma 1 3 Completed Treatment Breast Cancer / Melanoma 1 2 Not Yet Recruiting Diagnostic Endometrial Cancer 1 1 Terminated Diagnostic Carcinoma, Colorectal / Hepatic Metastases 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit Intradermal; Subcutaneous 250 ug/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS6409990 No 2002-06-25 2020-05-12 US US9439985 No 2016-09-13 2033-09-27 US Additional Data Available- Filed On
Properties
- State
- Solid
- Experimental Properties
Property Value Source boiling point (°C) 100 MSDS - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Ligand
- General Function
- Mediates the endocytosis of glycoproteins by macrophages. Binds both sulfated and non-sulfated polysaccharide chains.
- Specific Function
- Mannose binding
- Gene Name
- MRC1
- Uniprot ID
- P22897
- Uniprot Name
- Macrophage mannose receptor 1
- Molecular Weight
- 166010.315 Da
Drug created on October 27, 2015 17:51 / Updated on June 12, 2020 11:42
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