This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Tengonermin
DrugBank Accession Number
DB16689
Background

Tengonermin, also known as NGR-hTNF, is a vascular-targeting drug.1 It is a recombinant protein and peptide-targeted agent consisting of the human Tumour Necrosis Factor-α (TNF-α) conjugated with the CNGRCG peptide.3 This drug works by modifying the tumor microenvironment and increasing intratumoral chemotherapy penetration and T-cell infiltration.1

NGR-hTNF specifically targets angiogenic tumor blood vessels using the NGR motif.2 Literature demonstrates that NGR-peptides bind to a CD13 isoform, of which expression is restricted to tumor vasculature cells.2 A study also demonstrated that binding of the NGR-motif to CD13 determined both the homing of NGR-hTNF to tumor vessels and the increase in its antiangiogenic activity.2

Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Peptides
Protein Chemical Formula
Not Available
Protein Average Weight
Not Available
Sequences
Not Available
Synonyms
  • NGR-hTNF
  • Tengonermin

Pharmacology

Indication

Not Available

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Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action

Tengonermin has highly selective homing to tumor blood vessels due to the NGR peptide portion binding specifically to a CD13 isoform (expressed selectively by endothelial cells of human tumor vessels during neoangiogenesis) which allows it to spare tumor-unrelated human tissues.3 This drug also increases apoptosis of angiogenic endothelial cells in vivo. 3 The aforementioned effects significantly contribute to controlling the growth of tumors.3 Once the drug targets the tumor vasculature, multiple downstream effects occur, mediated by the interaction of both components of the molecule.3

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

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
Chemical TaxonomyProvided by Classyfire
Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
2YQ0811D7K
CAS number
1960461-99-7

References

General References
  1. Gregorc V, Gaafar RM, Favaretto A, Grossi F, Jassem J, Polychronis A, Bidoli P, Tiseo M, Shah R, Taylor P, Novello S, Muzio A, Bearz A, Greillier L, Fontana F, Salini G, Lambiase A, O'Brien M: NGR-hTNF in combination with best investigator choice in previously treated malignant pleural mesothelioma (NGR015): a randomised, double-blind, placebo-controlled phase 3 trial. Lancet Oncol. 2018 Jun;19(6):799-811. doi: 10.1016/S1470-2045(18)30193-1. Epub 2018 May 9. [Article]
  2. Valentinis B, Porcellini S, Asperti C, Cota M, Zhou D, Di Matteo P, Garau G, Zucchelli C, Avanzi NR, Rizzardi GP, Degano M, Musco G, Traversari C: Mechanism of Action of the Tumor Vessel Targeting Agent NGR-hTNF: Role of Both NGR Peptide and hTNF in Cell Binding and Signaling. Int J Mol Sci. 2019 Sep 12;20(18). pii: ijms20184511. doi: 10.3390/ijms20184511. [Article]
  3. European Medicines Agency (EMA): Zafiride [Link]
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3CompletedTreatmentMalignant Pleural Mesothelioma (MPM)1
2CompletedTreatmentColon Cancer1
2CompletedTreatmentColorectal Cancer1
2CompletedTreatmentDiffuse Large B-Cell Lymphoma (DLBCL)1
2CompletedTreatmentHepatocellular Carcinoma1
2CompletedTreatmentMalignant Pleural Mesothelioma (MPM)1
2CompletedTreatmentMetastatic Adult Soft Tissue Sarcoma1
2CompletedTreatmentNon-Small Cell Lung Cancer (NSCLC)1
2CompletedTreatmentOvarian Cancer2
2CompletedTreatmentOvarian Cancer Metastatic Recurrent1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available

Drug created at April 08, 2021 18:50 / Updated at April 16, 2021 04:48