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Margetuximab

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Also known as Margetuximab cmkbMargetuximab-cmkbMGAH-22MGAH22Margenza

Summary

Margetuximab (CHEMBL2364649) is an approved antibody (ATC L01FD06) targeting ERBB2; indicated across 2 conditions including breast neoplasm and neoplasm; with CIViC clinical evidence for 1 variant-indication association (e.g. ERBB2 Amplification in breast cancer).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Antibody
  • ATC class: L01FD06
  • Targets: 1 (ERBB2)
  • Indications: 2 conditions
  • Clinical trials: 11
  • Precision-oncology evidence (CIViC): 1 variant–indication association

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL2364649
NameMargetuximab
TypeAntibody
Max phase4
ATCL01FD06

Also known as: Margetuximab, Margetuximab cmkb, Margetuximab-cmkb, MGAH-22, MGAH22, Margenza, MARGETUXIMAB

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
ERBB2erb-b2 receptor tyrosine kinase 2Binding17.7%P04626

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 1 target gene(s): ERBB2.

Top Reactome pathways

33 total, by targets touching each:

PathwayTargetsGenes
Signaling by ERBB21ERBB2
SHC1 events in ERBB2 signaling1ERBB2
PLCG1 events in ERBB2 signaling1ERBB2
PIP3 activates AKT signaling1ERBB2
GRB7 events in ERBB2 signaling1ERBB2
Downregulation of ERBB2:ERBB3 signaling1ERBB2
GRB2 events in ERBB2 signaling1ERBB2
PI3K events in ERBB2 signaling1ERBB2
Constitutive Signaling by Aberrant PI3K in Cancer1ERBB2
Sema4D induced cell migration and growth-cone collapse1ERBB2
RAF/MAP kinase cascade1ERBB2
ERBB2 Regulates Cell Motility1ERBB2
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling1ERBB2
ERBB2 Activates PTK6 Signaling1ERBB2
Downregulation of ERBB2 signaling1ERBB2
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors1ERBB2
Constitutive Signaling by Overexpressed ERBB21ERBB2
Drug-mediated inhibition of ERBB2 signaling1ERBB2
Signaling by ERBB2 KD Mutants1ERBB2
Resistance of ERBB2 KD mutants to trastuzumab1ERBB2
Resistance of ERBB2 KD mutants to sapitinib1ERBB2
Resistance of ERBB2 KD mutants to tesevatinib1ERBB2
Resistance of ERBB2 KD mutants to neratinib1ERBB2
Resistance of ERBB2 KD mutants to osimertinib1ERBB2
Resistance of ERBB2 KD mutants to afatinib1ERBB2
Resistance of ERBB2 KD mutants to AEE7881ERBB2
Resistance of ERBB2 KD mutants to lapatinib1ERBB2
Signaling by ERBB2 ECD mutants1ERBB2
Signaling by ERBB2 TMD/JMD mutants1ERBB2
Drug resistance in ERBB2 TMD/JMD mutants1ERBB2
Developmental Lineage of Mammary Gland Luminal Epithelial Cells1ERBB2
Developmental Lineage of Mammary Gland Myoepithelial Cells1ERBB2
Developmental Lineage of Mammary Stem Cells1ERBB2

Dominant GO biological processes

GO termTargets
protein phosphorylation1
signal transduction1
cell surface receptor signaling pathway1
enzyme-linked receptor protein signaling pathway1
cell surface receptor protein tyrosine kinase signaling pathway1
epidermal growth factor receptor signaling pathway1
heart development1
neuromuscular junction development1
motor neuron axon guidance1
cell population proliferation1
Schwann cell development1
peptidyl-tyrosine phosphorylation1
neuron differentiation1
positive regulation of cell growth1
regulation of microtubule-based process1

Indications & clinical

Indications

2 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
breast neoplasm4MONDO:0021100MONDO:0007254
neoplasm4MONDO:0005070EFO:0000616

Clinical trials

Total trials: 11.

Phase distribution

PhaseTrials
PHASE24
PHASE13
PHASE31
PHASE2/PHASE31
PHASE1/PHASE21
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT02492711PHASE3COMPLETEDMargetuximab Plus Chemotherapy vs Trastuzumab Plus Chemotherapy in the Treatment of HER2+ Metastatic Breast Cancer
NCT04082364PHASE2/PHASE3COMPLETEDCombination Margetuximab, Retifanlimab, Tebotelimab, and Chemotherapy Phase 2/3 Trial in HER2+ Gastric/GEJ Cancer
NCT04425018PHASE2ACTIVE_NOT_RECRUITINGMARGetuximab Or Trastuzumab (MARGOT)
NCT01828021PHASE2COMPLETEDPhase 2 Study of the Monoclonal Antibody MGAH22 (Margetuximab) in Patients With Relapsed or Refractory Advanced Breast Cancer
NCT02689284PHASE1/PHASE2COMPLETEDCombination Margetuximab and Pembrolizumab for Advanced, Metastatic HER2(+) Gastric or Gastroesophageal Junction Cancer
NCT04262804PHASE2UNKNOWNA Study to Evaluate the Efficacy and Safety of Margetuximab Plus Chemotherapy in the Treatment of Chinese Patients With HER2+ MBC
NCT05227131PHASE2WITHDRAWNMargetuximab Plus Tucatinib and Capecitabine in HER2-positive Metastatic Breast Cancer
NCT01148849PHASE1COMPLETEDSafety Study of MGAH22 in HER2-positive Carcinomas
NCT03219268PHASE1COMPLETEDA Study of MGD013 in Patients With Unresectable or Metastatic Neoplasms
NCT04398108PHASE1COMPLETEDA Study to Evaluate the Pharmacokinetics of Margetuximab in Chinese Patients With HER2+ MBC
NCT03133988Not specifiedAPPROVED_FOR_MARKETINGMargetuximab Expanded Access Program

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
ERBB2 AmplificationBreast CancerSensitivity/ResponseMargetuximabCIViC AEID11249

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

86 molecules share ≥1 primary target. Top 86 by shared-target count:

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)ERBB2
DACOMITINIBChEMBL + PubChemPhase 4 (approved)ERBB2
GEFITINIBChEMBL + PubChemPhase 4 (approved)ERBB2
LAPATINIB DITOSYLATEChEMBL + PubChemPhase 4 (approved)ERBB2
LAZERTINIBChEMBL + PubChemPhase 4 (approved)ERBB2
MOBOCERTINIBChEMBL + PubChemPhase 4 (approved)ERBB2
ACALABRUTINIBChEMBLPhase 4 (approved)ERBB2
AFATINIB DIMALEATEChEMBLPhase 4 (approved)ERBB2
AMIODARONEChEMBLPhase 4 (approved)ERBB2
ASTEMIZOLEChEMBLPhase 4 (approved)ERBB2
BITHIONOLChEMBLPhase 4 (approved)ERBB2
BOSUTINIBChEMBLPhase 4 (approved)ERBB2
BRIGATINIBChEMBLPhase 4 (approved)ERBB2
CABOZANTINIBChEMBLPhase 4 (approved)ERBB2
CHLORPROMAZINEChEMBLPhase 4 (approved)ERBB2
CLOTRIMAZOLEChEMBLPhase 4 (approved)ERBB2
COLISTINChEMBLPhase 4 (approved)ERBB2
DASATINIBChEMBLPhase 4 (approved)ERBB2
DOXORUBICINChEMBLPhase 4 (approved)ERBB2
EBASTINEChEMBLPhase 4 (approved)ERBB2
ECONAZOLEChEMBLPhase 4 (approved)ERBB2
ERLOTINIBChEMBLPhase 4 (approved)ERBB2
FLUPHENAZINEChEMBLPhase 4 (approved)ERBB2
HEXACHLOROPHENEChEMBLPhase 4 (approved)ERBB2
IBRUTINIBChEMBLPhase 4 (approved)ERBB2
IMATINIBChEMBLPhase 4 (approved)ERBB2
LAPATINIBChEMBLPhase 4 (approved)ERBB2
MICONAZOLEChEMBLPhase 4 (approved)ERBB2
MITOXANTRONEChEMBLPhase 4 (approved)ERBB2
NERATINIBChEMBLPhase 4 (approved)ERBB2
OSIMERTINIBChEMBLPhase 4 (approved)ERBB2
PACLITAXELChEMBLPhase 4 (approved)ERBB2
PONATINIBChEMBLPhase 4 (approved)ERBB2
SORAFENIBChEMBLPhase 4 (approved)ERBB2
TAMOXIFENChEMBLPhase 4 (approved)ERBB2
TIRABRUTINIBChEMBLPhase 4 (approved)ERBB2
TRIBROMSALANChEMBLPhase 4 (approved)ERBB2
TUCATINIBChEMBLPhase 4 (approved)ERBB2
VANDETANIBChEMBLPhase 4 (approved)ERBB2
ZANUBRUTINIBChEMBLPhase 4 (approved)ERBB2
ALISERTIBChEMBLPhase 3ERBB2
ALVOCIDIBChEMBLPhase 3ERBB2
CANDESARTANChEMBLPhase 3ERBB2
CANERTINIBChEMBLPhase 3ERBB2
CEDIRANIBChEMBLPhase 3ERBB2
ENCLOMIPHENEChEMBLPhase 3ERBB2
MASITINIBChEMBLPhase 3ERBB2
POZIOTINIBChEMBLPhase 3ERBB2
PYROTINIBChEMBLPhase 3ERBB2
REMIBRUTINIBChEMBLPhase 3ERBB2
TANESPIMYCINChEMBLPhase 3ERBB2
ZONGERTINIBChEMBLPhase 3ERBB2
AEE-788ChEMBLPhase 2ERBB2
ALLITINIBChEMBLPhase 2ERBB2
ATUZABRUTINIBChEMBLPhase 2ERBB2
BENZETHONIUM CHLORIDEChEMBLPhase 2ERBB2
CENISERTIBChEMBLPhase 2ERBB2
CLOSANTELChEMBLPhase 2ERBB2
CP-724714ChEMBLPhase 2ERBB2
DEFOSBARASERTIBChEMBLPhase 2ERBB2
ELLAGIC ACIDChEMBLPhase 2ERBB2
FALNIDAMOLChEMBLPhase 2ERBB2
FORETINIBChEMBLPhase 2ERBB2
ILORASERTIBChEMBLPhase 2ERBB2
IODOQUINOLChEMBLPhase 2ERBB2
MUBRITINIBChEMBLPhase 2ERBB2
PELITINIBChEMBLPhase 2ERBB2
PU-H71ChEMBLPhase 2ERBB2
R-406ChEMBLPhase 2ERBB2
SAPITINIBChEMBLPhase 2ERBB2
SOTRASTAURINChEMBLPhase 2ERBB2
SPH-5030ChEMBLPhase 2ERBB2
TG100-115ChEMBLPhase 2ERBB2
VARLITINIBChEMBLPhase 2ERBB2
ApremilastPubChemApprovedERBB2
belumosudilPubChemApprovedERBB2
BinimetinibPubChemApprovedERBB2
chenodiolPubChemApprovedERBB2
CrizotinibPubChemApprovedERBB2
ErythromycinPubChemApprovedERBB2
IdelalisibPubChemApprovedERBB2
ImipenemPubChemApprovedERBB2
OlodaterolPubChemApprovedERBB2
PazopanibPubChemApprovedERBB2
RitlecitinibPubChemApprovedERBB2
SelumetinibPubChemApprovedERBB2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot