NAV

Depatuxizumab mafodotin

Identification

Generic Name
Depatuxizumab mafodotin
DrugBank Accession Number
DB11731
Background

Depatuxizumab/Denintuzumab mafodotin has been used in trials studying the treatment of Lymphoma, Gliosarcoma, Glioblastoma, Malignant Glioma, Squamous Cell Tumors, and Glioblastoma Multiforme.

Type
Biotech
Groups
Investigational
Synonyms
  • Denintuzumab mafodotin
  • Depatuxizumab mafodotin
External IDs
  • 1399672-02-6
  • ABT-414
  • SGN-19A
  • SGN-CD 19A
  • SGN-CD19A
Poor quality drug data slowing you down?
Unlock 38% more drug discovery time and eliminate decision-making doubts with this one-stop guide to quality drug data.
Download eBook
Poor quality drug data slowing you down?
Download eBook

Pharmacology

Indication

No approved indication.

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Contraindications & Blackbox Warnings
Prevent Adverse Drug Events Today
Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events with our Clinical API
Learn more
Pharmacodynamics

Selectively targets cancer cells expressing mutant epidermal growth factor receptor (EGFR) vIII or over expressing wild type EGFR 1. Depatuxizumab mafodotin acts on these cells to inhibit microtuble polymerization thus disrupting mitosis and vesicular trafficking 2

Mechanism of action

Depatuxizumab is a chimeric monoclonal antibody for EGFR which is linked to monomethyl aurastatin F via a maleimidocaproyl linker (mafodotin) 1. Once delivered to the cancer cell, the mafodotin component is able to bind to tubulin and inhibit the exchange of GDP for GTP necessary for the polymerization of tubulin subunits to form microtubules. The inhibition of microtubule polymerization disrupts mitosis and interferes with vesicle trafficking in the cancer cell 3 2.

TargetActionsOrganism
ATubulin beta chain
nucleotide exchange blocker
Humans
NEpidermal growth factor receptor
antibody
Humans
UB-lymphocyte antigen CD19
regulator
Humans
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
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!
See the data
Improve decision support & research outcomes with our structured adverse effects data.
See a data sample
Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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.
DrugInteraction
Integrate drug-drug
interactions in your software
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Depatuxizumab mafodotin.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Depatuxizumab mafodotin.
AducanumabThe risk or severity of adverse effects can be increased when Depatuxizumab mafodotin is combined with Aducanumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Depatuxizumab mafodotin.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Depatuxizumab mafodotin.
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
F3R7A4P04N
CAS number
1585973-65-4

References

General References
  1. Phillips AC, Boghaert ER, Vaidya KS, Mitten MJ, Norvell S, Falls HD, DeVries PJ, Cheng D, Meulbroek JA, Buchanan FG, McKay LM, Goodwin NC, Reilly EB: ABT-414, an Antibody-Drug Conjugate Targeting a Tumor-Selective EGFR Epitope. Mol Cancer Ther. 2016 Apr;15(4):661-9. doi: 10.1158/1535-7163.MCT-15-0901. Epub 2016 Feb 4. [Article]
  2. Waight AB, Bargsten K, Doronina S, Steinmetz MO, Sussman D, Prota AE: Structural Basis of Microtubule Destabilization by Potent Auristatin Anti-Mitotics. PLoS One. 2016 Aug 12;11(8):e0160890. doi: 10.1371/journal.pone.0160890. eCollection 2016. [Article]
  3. Bai RL, Pettit GR, Hamel E: Binding of dolastatin 10 to tubulin at a distinct site for peptide antimitotic agents near the exchangeable nucleotide and vinca alkaloid sites. J Biol Chem. 1990 Oct 5;265(28):17141-9. [Article]
PubChem Compound
71300933
PubChem Substance
347828090
ChemSpider
57523411
Wikipedia
Depatuxizumab_mafodotin

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
PhaseStatusPurposeConditionsCount
3CompletedTreatmentHigh Grade Glioma: Glioblastoma (GBM) / High Grade Glioma: Gliosarcoma1
3TerminatedTreatmentGlioblastoma Multiforme (GBM)1
2CompletedTreatmentHigh Grade Glioma: Glioblastoma (GBM)1
2TerminatedTreatmentB-Cell Lymphoma / Diffuse Large B-Cell Lymphoma (DLBCL) / Grade 3b Follicular Lymphoma1
2TerminatedTreatmentDiffuse Large B-Cell Lymphoma (DLBCL) / Grade 3b Follicular Lymphoma / Transformed Lymphoma / DLBCL1

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

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Details1. Tubulin beta chain
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Nucleotide exchange blocker
General Function
Ubiquitin protein ligase binding
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
Gene Name
TUBB
Uniprot ID
P07437
Uniprot Name
Tubulin beta chain
Molecular Weight
49670.515 Da
References
  1. Bai RL, Pettit GR, Hamel E: Binding of dolastatin 10 to tubulin at a distinct site for peptide antimitotic agents near the exchangeable nucleotide and vinca alkaloid sites. J Biol Chem. 1990 Oct 5;265(28):17141-9. [Article]
  2. Waight AB, Bargsten K, Doronina S, Steinmetz MO, Sussman D, Prota AE: Structural Basis of Microtubule Destabilization by Potent Auristatin Anti-Mitotics. PLoS One. 2016 Aug 12;11(8):e0160890. doi: 10.1371/journal.pone.0160890. eCollection 2016. [Article]
Details2. Epidermal growth factor receptor
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Antibody
General Function
Ubiquitin protein ligase binding
Specific Function
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TG...
Gene Name
EGFR
Uniprot ID
P00533
Uniprot Name
Epidermal growth factor receptor
Molecular Weight
134276.185 Da
References
  1. Phillips AC, Boghaert ER, Vaidya KS, Mitten MJ, Norvell S, Falls HD, DeVries PJ, Cheng D, Meulbroek JA, Buchanan FG, McKay LM, Goodwin NC, Reilly EB: ABT-414, an Antibody-Drug Conjugate Targeting a Tumor-Selective EGFR Epitope. Mol Cancer Ther. 2016 Apr;15(4):661-9. doi: 10.1158/1535-7163.MCT-15-0901. Epub 2016 Feb 4. [Article]
Details3. B-lymphocyte antigen CD19
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Regulator
General Function
Receptor signaling protein activity
Specific Function
Assembles with the antigen receptor of B-lymphocytes in order to decrease the threshold for antigen receptor-dependent stimulation.
Gene Name
CD19
Uniprot ID
P15391
Uniprot Name
B-lymphocyte antigen CD19
Molecular Weight
61127.985 Da
References
  1. Kyriakidis I, Vasileiou E, Rossig C, Roilides E, Groll AH, Tragiannidis A: Invasive Fungal Diseases in Children with Hematological Malignancies Treated with Therapies That Target Cell Surface Antigens: Monoclonal Antibodies, Immune Checkpoint Inhibitors and CAR T-Cell Therapies. J Fungi (Basel). 2021 Mar 5;7(3). pii: jof7030186. doi: 10.3390/jof7030186. [Article]

Drug created at October 20, 2016 20:43 / Updated at December 08, 2022 21:17