Technetium Tc-99m nofetumomab merpentan
Identification
- Generic Name
- Technetium Tc-99m nofetumomab merpentan
- DrugBank Accession Number
- DB09336
- Background
Technetium Tc-99m nofetumomab merpentan (Tc-99m nm) consists of a Fab fragment of an IgG2b of the pancarcinoma murine antibody NR-LU-10.1 The NR-LU-10 antibody is directed against a 40 kDa glycoprotein antigen expressed in a variety of cancers and some normal tissues.Label Tc-99m nm was developed by Boehringer Ingelheim Pharma KG and FDA approved on September 14, 1992. It was after discontinued on August 13, 2013, but in the 2018 FDA submission list, it can be found as a substance type II (Drug substance) with an active status.8,9
- Type
- Small Molecule
- Groups
- Approved, Withdrawn
- Synonyms
- Nofetumomab
- Technetium (99mTc) nofetumomab merpentan
- Technetium Tc 99m nofetumomab merpentan
Pharmacology
- Indication
Tc-99m nm is one of the technetium-labeled antibodies and it is indicated for the detection of small-cell lung cancer.3 The small cell lung cancer is a syndrome characterized by the abnormal and uncontrolled cell growth and it is characterized by a shorter doubling time, higher growth fraction and earlier development of metastases.4
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- Pharmacodynamics
Studies have shown that the Fab fragment presents high immunoreactivity in small cell lung cancer tumors. The adenocarcinomas of the kidney and pancreas are not detected. This lack of diagnostic detection can be explained because some radioactivity gets accumulated in the excretion pathway, in nonspecific vascular locations and in non-tumor areas with traces of inflammation, increased vascular pool or recent surgical. Therefore, the detection rate may be reduced in those areas and its adjacent zones.Label
- Mechanism of action
The mechanism of action in Tc-99m nm is ruled by the presence of nofetumomab, which can recognize the pancarcinoma antigen EpCAM and/or CD20/MS4A1,2 and merpentan, that acts as a linker for the binding of technetium.6
Target Actions Organism AEpithelial cell adhesion molecule binderHumans AB-lymphocyte antigen CD20 binderHumans - Absorption
After intravenous administration, Tc-99m nm presents a rapid distribution phase.Label
- Volume of distribution
Not Available
- Protein binding
There are no reports of binding of Tc-99m nm to binding proteins.Label
- Metabolism
- Not Available
- Route of elimination
The primary route of elimination is renal and accounts for the 64% of the administered dose. After renal clearance, the main route is hepatobiliary. All the different elimination pathways lead to accumulation of radioactivity on the kidney, urinary bladder, gall bladder and intestines.7
- Half-life
The radioactive half-life of the Tc-99m nm is of 6 hours. It is important to consider this short half-life as the use of this agent should be done within the active time.5 Tc-99m nm presents a serum half-life of 1.5 hours and an elimination phase half-life of 10.5 hours.7
- Clearance
Not Available
- Adverse Effects
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- Toxicity
Long-term preclinical studies to determine the carcinogenic, mutagenic or fertility effect have not been studied.Label
- 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.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 9UFH75HT7S
- CAS number
- 165942-79-0
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Breitz HB, Tyler A, Bjorn MJ, Lesley T, Weiden PL: Clinical experience with Tc-99m nofetumomab merpentan (Verluma) radioimmunoscintigraphy. Clin Nucl Med. 1997 Sep;22(9):615-20. [Article]
- Honjo T., Alt F. and Neuberger M. (2004). Molecular biology of B cells. Elsevier .
- Technetium radiopharmaceutical chemistry [Link]
- Cancer [Link]
- Pharmacopeia [Link]
- Pharmacological science [Link]
- National Public library [Link]
- FDA CDER list [Link]
- FDA Submission [Link]
- External Links
- PubChem Substance
- 347910442
- FDA label
- Download (1.32 MB)
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source Radioactivity (mCi/mL) 30 FDA label - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Protein complex binding
- Specific Function
- May act as a physical homophilic interaction molecule between intestinal epithelial cells (IECs) and intraepithelial lymphocytes (IELs) at the mucosal epithelium for providing immunological barrier...
- Gene Name
- EPCAM
- Uniprot ID
- P16422
- Uniprot Name
- Epithelial cell adhesion molecule
- Molecular Weight
- 34932.005 Da
References
- Honjo T., Alt F. and Neuberger M. (2004). Molecular biology of B cells. Elsevier .
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Mhc class ii protein complex binding
- Specific Function
- This protein may be involved in the regulation of B-cell activation and proliferation.
- Gene Name
- MS4A1
- Uniprot ID
- P11836
- Uniprot Name
- B-lymphocyte antigen CD20
- Molecular Weight
- 33076.99 Da
References
- Honjo T., Alt F. and Neuberger M. (2004). Molecular biology of B cells. Elsevier .
Drug created at November 27, 2015 00:09 / Updated at June 12, 2020 16:52