Peringatan Keamanan

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 FDA Label.

Technetium Tc-99m tilmanocept

DB09266

small molecule approved investigational

Deskripsi

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 FDA Label. DTPA serves as a chelating agent for technetium Tc 99m to bind FDA 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 A32169, A32170. 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 A32170. 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 A32170.

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 A32168. Due to its relatively small molecular weight and small molecular diameter of 7 nm A32168, technetium Tc-99m tilmanocept displays more rapid injection site clearance, high sentinel node extraction, and low distal node accumulation compared to other conventional radiocolloids A32170. It achieves high overall accuracy in detecting SLN A32169. 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 FDA Label. It is marketed under the trade name Lymphoseek. Potential application of technetium Tc-99m tilmanocept to other cancers are being investigated A32170.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (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 [FDA Label].
Volume Distribusi -
Klirens (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 [FDA Label].

Absorpsi

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 FDA Label.

Metabolisme

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.

Rute Eliminasi

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.

Interaksi Obat

29 Data
Lidocaine Lidocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Ropivacaine Ropivacaine 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.
Cinchocaine Cinchocaine 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.
Procaine Procaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Prilocaine Prilocaine 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.
Mepivacaine Mepivacaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Levobupivacaine Levobupivacaine 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.
Benzocaine Benzocaine 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.
Phenol Phenol may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Tetrodotoxin Tetrodotoxin 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.
Capsaicin Capsaicin may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Etidocaine Etidocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Articaine Articaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Tetracaine Tetracaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Propoxycaine Propoxycaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Pramocaine Pramocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Oxetacaine Oxetacaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Butanilicaine Butanilicaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Metabutethamine Metabutethamine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Quinisocaine Quinisocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Oxybuprocaine Oxybuprocaine may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Meloxicam Meloxicam may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.
Ambroxol Ambroxol may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.

Target Protein

Macrophage mannose receptor 1 MRC1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 23504141
    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)tctilmanocept 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.
  • PMID: 25670018
    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)TcTilmanocept 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.
  • PMID: 25956693
    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.

Contoh Produk & Brand

Produk: 4 • International brands: 0
Produk
  • Kit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept)
    Kit • 250 ug/1 • Intradermal; Subcutaneous • US • Approved
  • Kit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept)
    Kit • 250 ug/1 • Intradermal; Subcutaneous • US • Approved
  • Kit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept)
    Injection, powder, lyophilized, for solution; Kit • 250 ug/1 • Intradermal; Subcutaneous • US • Approved
  • Kit for the preparation of Lymphoseek (technetium Tc 99m tilmanocept)
    Injection, powder, lyophilized, for solution; Kit • 250 ug/1 • Intradermal; Subcutaneous • US • Approved

Sekuens Gen/Protein (FASTA)

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