Glembatumumab vedotin

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

Identification

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Name
Glembatumumab vedotin
Accession Number
DB05996
Type
Biotech
Groups
Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
Description

A conjugate of an anti-glycoprotein non-metastatic melanoma protein B mAb and monomethyl auristatin E for the treatment of melanoma and breast cancer.

Protein chemical formula
Not Available
Protein average weight
Not Available
Sequences
>Heavy chain
QVQLQESGPGLVKPSQTLSLTCTVSGGSISSFNYYWSWIRHHPGKGLEWIGYIYYSGSTY
SNPSLKSRVTISVDTSKNQFSLTLSSVTAADTAVYYCARGYNWNYFDYWGQGTLVTVSSA
STKGPSVFPLAPCSRSTSESTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG
LYSLSSVVTVPSSNFGTQTYTCNVDHKPSNTKVDKTVERKCCVECPPCPAPPVAGPSVFL
FPPKPKDTLMISRTPEVTCVVVDVSHEDPEVQFNWYVDGVEVHNAKTKPREEQFNSTFRV
VSVLTVVHQDWLNGKEYKCKVSNKGLPAPIEKTISKTKGQPREPQVYTLPPSREEMTKNQ
VSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPMLDSDGSFFLYSKLTVDKSRWQQGNV
FSCSVMHEALHNHYTQKSLSLSPGK
>Light Chain
EIVMTQSPATLSVSPGERATLSCRASQSVDNNLVWYQQKPGQAPRLLIYGASTRATGIPA
RFSGSGSGTEFTLTISSLQSEDFAVYYCQQYNNWPPWTFGQGTKVEIKRTVAAPSVFIFP
PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL
TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
Download FASTA Format
Synonyms
Not Available
External IDs
CDX 011 / CDX-011 / CR-011-VCMMAE / CR011-VCMMAE
Categories
UNII
1568H6A58U
CAS number
1182215-65-1

Pharmacology

Indication

Investigated for use/treatment in melanoma.

Pharmacodynamics
Not Available
Mechanism of action

CR011 is a fully-human monoclonal antibody which utilizes antibody-drug conjugation (ADC) technology licensed from Seattle Genetics. The ADC technology links vcMMAE, a potent chemotherapeutic, to the CR011 antibody resulting in the antibody-drug conjugate CR011-vcMMAE. CR011-vcMMAE targets GPNMB, a protein located specifically on the surface of melanoma cells. After CR011-vcMMAE binds to GPNMB, it is transported inside the cancer cell where the chemotherapy payload, Auristatin E, is cleaved from the antibody and activated.

TargetActionsOrganism
UTransmembrane glycoprotein NMB
binder
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
Toxicity
Not Available
Affected organisms
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.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Glembatumumab vedotin.
AbituzumabThe risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Abituzumab.
AbrilumabThe risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Abrilumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Glembatumumab vedotin.
AdecatumumabThe risk or severity of adverse effects can be increased when Adecatumumab is combined with Glembatumumab vedotin.
AducanumabThe risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Aducanumab.
AfelimomabThe risk or severity of adverse effects can be increased when Afelimomab is combined with Glembatumumab vedotin.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Glembatumumab vedotin.
AlirocumabThe risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Alirocumab.
AmatuximabThe risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Amatuximab.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
Not Available

References

General References
Not Available
External Links
ChEMBL
CHEMBL1743028
Wikipedia
Glembatumumab_vedotin

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0WithdrawnTreatmentTriple Negative Breast Cancer (TNBC)1
1, 2CompletedTreatmentBreast Cancer1
1, 2CompletedTreatmentUnresectable Stage III or Stage IV Melanoma1
1, 2TerminatedTreatmentSquamous Cell Carcinoma of the Lung1
1, 2WithdrawnTreatmentAdvanced Malignant Solid Neoplasm / Estrogen Receptor Negative / GPNMB Positive / HER2/Neu Negative / Metastatic Malignant Solid Neoplasm / Metastatic Melanoma / Progesterone Receptor Negative / Stage III Breast Cancer AJCC V7 / Stage III Cutaneous Melanoma AJCC v7 / Stage III Uveal Melanoma / Stage III Uveal Melanoma AJCC v7 / Stage IIIA Cutaneous Melanoma AJCC v7 / Stage IIIB Cutaneous Melanoma AJCC v7 / Stage IIIC Cutaneous Melanoma AJCC v7 / Stage IV Breast Cancer AJCC v6 and v7 / Stage IV Cutaneous Melanoma AJCC v6 and v7 / Stage IV Uveal Melanoma / Stage IV Uveal Melanoma AJCC v7 / Triple-Negative Breast Carcinoma / Unresectable Solid Neoplasm1
2CompletedTreatmentBreast Cancer1
2CompletedTreatmentMetastatic gpNMB Over-expressing Triple Negative Breast Cancer1
2CompletedTreatmentRecurrent Osteosarcoma1
2CompletedTreatmentRecurrent Uveal Melanoma / Stage IV Uveal Melanoma / Stage IV Uveal Melanoma AJCC v71
2TerminatedTreatmentMelanoma1
Not AvailableNo Longer AvailableNot AvailableMetastatic gpNMB Expressing Triple Negative Breast Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

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

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Heparin binding
Specific Function
Could be a melanogenic enzyme.
Gene Name
GPNMB
Uniprot ID
Q14956
Uniprot Name
Transmembrane glycoprotein NMB
Molecular Weight
63922.065 Da
References
  1. Tse KF, Jeffers M, Pollack VA, McCabe DA, Shadish ML, Khramtsov NV, Hackett CS, Shenoy SG, Kuang B, Boldog FL, MacDougall JR, Rastelli L, Herrmann J, Gallo M, Gazit-Bornstein G, Senter PD, Meyer DL, Lichenstein HS, LaRochelle WJ: CR011, a fully human monoclonal antibody-auristatin E conjugate, for the treatment of melanoma. Clin Cancer Res. 2006 Feb 15;12(4):1373-82. doi: 10.1158/1078-0432.CCR-05-2018. [PubMed:16489096]
  2. Rose AA, Grosset AA, Dong Z, Russo C, Macdonald PA, Bertos NR, St-Pierre Y, Simantov R, Hallett M, Park M, Gaboury L, Siegel PM: Glycoprotein nonmetastatic B is an independent prognostic indicator of recurrence and a novel therapeutic target in breast cancer. Clin Cancer Res. 2010 Apr 1;16(7):2147-56. doi: 10.1158/1078-0432.CCR-09-1611. Epub 2010 Mar 9. [PubMed:20215530]

Drug created on November 18, 2007 11:29 / Updated on December 02, 2019 07:17