Futuximab

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The Sym004 product is a mixture of two synergistic full-length anti-EGFR antibodies "(Modotuximab (lab code: 1024-DS) + Futuximab (lab code: 992-DS)", which bind to two separate non-overlapping epitopes on EGFR. The combination has a unique mechanism of action, which leads to sustained growth inhibition of cancer cells. Sym004 has proven to be superior to available monoclonal antibodies in several established animal models and has shown promising results in early human clinical trials. Sym004 is not only designed to block ligand binding, receptor activation and downstream signaling but also elicits effective removal of the EGFR receptors from the cancer cell surface by inducing EGFR internalization and degradation. Both Sym004 antibodies, called 992 and 1024, are mandatory in order to cross-link EGFR receptors on the cell surface, which leads to very effective receptor elimination and induction of secondary effector functions. Such extensive crosslinking of the receptors cannot be achieved with a single monoclonal antibody.

Inn NameFutuximab
Usan NameFutuximab
Lab Codes992DS, Sym-004, (Sym-004 = Modotuximab + Futuximab)
Chemical NameImmunoglobulin G1-kappa, anti-[Homo sapiens EGFR (epidermal growth factor receptor, ERBB1, HER1) domain III], chimeric monoclonal antibody; gamma1 heavy chain (1-452) [Mus musculus VH (IGHV1S5*01 - (IGHD)-IGHJ4*01) [8.8.16] (1-123) -Homo sapiens IGHG1*03 CHSK2>del (124-452)], (226-214')-disulfide with kappa light chain (1'-214') [Mus musculus V-KAPPA (IGKV10-96*01 -IGKJ1*02) [6.3.9](1'-107') -Homo sapiens IGKC*01 (108'-214')]; (232-232'':235-235'')-
bisdisulfide dimer
Alternate NameImmunoglobulin G1, anti-(human epidermal growth factor receptor extracellular domain III) (human-Mus musculus monoclonal 992 DS heavy chain), disulfide with human-Mus musculus monoclonal 992 DS light chain, dimer

Immunoglobulin G1-kappa, anti-(human EGFR (epidermal growth factor receptor, ERBB1, HER1) domain III), human-mouse chimeric monoclonal 992 DS gamma1 heavy chain (226-214')-disulfide with human-mouse chimeric kappa light chain (1'-214'), dimer (232-232'':235-235'')-bisdisulfide
SequenceHeavy chain
EVQLQQPGSE LVRPGASVKL SCKASGYTFT SYWMHWVKQR PGQGLEWIGN 50
IYPGSRSTNY DEKFKSKATL TVDTSSSTAY MQLSSLTSED SAVYYCTRNG 100
DYYVSSGDAM DYWGQGTSVT VSSASTKGPS VFPLAPSSKS TSGGTAALGC 150
LVKDYFPEPV TVSWNSGALT SGVHTFPAVL QSSGLYSLSS VVTVPSSSLG 200
TQTYICNVNH KPSNTKVDKR VEPKSCDKTH TCPPCPAPEL LGGPSVFLFP 250
PKPKDTLMIS RTPEVTCVVV DVSHEDPEVK FNWYVDGVEV HNAKTKPREE 300
QYNSTYRVVS VLTVLHQDWL NGKEYKCKVS NKALPAPIEK TISKAKGQPR 350
EPQVYTLPPS REEMTKNQVS LTCLVKGFYP SDIAVEWESN GQPENNYKTT 400
PPVLDSDGSF FLYSKLTVDK SRWQQGNVFS CSVMHEALHN HYTQKSLSLS 450
PG 452

Light chain
DIQMTQTTSS LSASLGDRVT ISCRTSQDIG NYLNWYQQKP DGTVKLLIYY 50
TSRLHSGVPS RFSGSGSGTD FSLTINNVEQ EDVATYFCQH YNTVPPTFGG 100
GTKLEIKRTV AAPSVFIFPP SDEQLKSGTA SVVCLLNNFY PREAKVQWKV 150
DNALQSGNSQ ESVTEQDSKD STYSLSSTLT LSKADYEKHK VYACEVTHQG 200
LSSPVTKSFN RGEC 214

Disulfide bridges location
Intra-H 22-96 150-206 267-327 373-431
22''-96'' 150''-206'' 267''-327'' 373''-431''
Intra-L 23'-88' 134'-194'
23'''-88''' 134'''-194'''
Inter-H-L 226-214' 226''-214'''
Inter-H-H 232-232'' 235-235''

N-glycosylation sites
H CH2 84.4:
303, 303''
Chemical StructureFutuximab.png
Cas Registry Number1310460-85-5
New Molecular EntityYes
OriginatorSymphogen A/S
Mechanism Of ActionEpidermal growth factor receptor antagonist
Who Atc CodesL01X-C (Monoclonal antibodies)
Ephmra CodesL1G (Monoclonal Antibody Antineoplastics)
IndicationSquamous Non-Small Cell Lung Cancer, Metastatic Colorectal Cancer, Malignant Glioma

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