Lupartumab amadotin

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NCI: An antibody-drug conjugate (ADC) composed of an antibody against a structural homolog of the urokinase-type plasminogen activator receptor (uPAR) and tumor-associated antigen, C4.4a, and conjugated with a cytotoxic agent, with potential antineoplastic activity. Upon intravenous administration, anti-C4.4a antibody-drug conjugate BAY1129980 targets and binds to C4.4a-expressing tumor cells. Upon binding and cell entry, the cytotoxic agent kills the tumor cell. C4.4a, a glycolipid-anchored membrane protein and a member of the Ly-6 family, is overexpressed by a variety of cancer cell types whereas it is minimally expressed on healthy cells.

Inn NameLupartumab amadotin
Lab CodesBAY-1129980
Chemical NameImmunoglobulin G1-lambda1, anti-[Homo sapiens LYPD3 (Ly6/PLAUR domain containing 3, GPI-anchored cellsurface protein C4.4a, C4.4A)], Homo sapiens monoclonal antibody conjugated to an auristatin W derivative; gamma1 heavy chain (1-446) [Homo sapiens VH (IGHV3- 48*03 (92.90%) -(IGHD) -IGHJ4*01) [8.8.10](1-117) - IGHG1*01, Gm17,1 (CH1 (118-215), hinge (216-230), CH2 (231-340), CH3 (341-445), CHS K>del (446)) (118-446)], (220-216')-disulfide with lambda1 light chain (1'-217') [Homo sapiens V-LAMBDA (IGLV1-47*01 (87.90%) - IGLJ2*01) [9.3.11] (1'-111') -IGLC2*01 (112'-217')]; dimer (226-226'':229-229'')-bisdisulfide; S-substituted on an average of 4 reduced cysteinyl by reaction with N-demethyl-N-[4-(6-maleimidohexanohydrazido)-4-oxobutyl]auristatin W amide
Alternate NameAnti-C4.4a ADC BAY1129980
SequenceHeavy chain
EVQLLESGGG LVQPGGSLRL SCAASGFTFS NAWMSWVRQA PGKGLEWVSY 50
ISSSGSTIYY ADSVKGRFTI SRDNSKNTLY LQMNSLRAED TAVYYCAREG 100
LWAFDYWGQG TLVTVSSAST KGPSVFPLAP SSKSTSGGTA ALGCLVKDYF 150
PEPVTVSWNS GALTSGVHTF PAVLQSSGLY SLSSVVTVPS SSLGTQTYIC 200
NVNHKPSNTK VDKKVEPKSC DKTHTCPPCP APELLGGPSV FLFPPKPKDT 250
LMISRTPEVT CVVVDVSHED PEVKFNWYVD GVEVHNAKTK PREEQYNSTY 300
RVVSVLTVLH QDWLNGKEYK CKVSNKALPA PIEKTISKAK GQPREPQVYT 350
LPPSRDELTK NQVSLTCLVK GFYPSDIAVE WESNGQPENN YKTTPPVLDS 400
DGSFFLYSKL TVDKSRWQQG NVFSCSVMHE ALHNHYTQKS LSLSPG 446

Light chain
ESVLTQPPSV SGAPGQRVTI SCTGSSSNIG AGYVVHWYQQ LPGTAPKLLI 50
YDNNKRPSGV PDRFSGSKSG TSASLAISGL RSEDEADYYC AAWDDRLNGP 100
VFGGGTKLTV LGQPKAAPSV TLFPPSSEEL QANKATLVCL ISDFYPGAVT 150
VAWKADSSPV KAGVETTTPS KQSNNKYAAS SYLSLTPEQW KSHRSYSCQV 200
THEGSTVEKT VAPTECS 217

Disulfide bridges location
Intra-H (C23-C104) 22-96 144-200 261-321 367-425
22''-96'' 144''-200'' 261''-321'' 367''-425''
Intra-L (C23-C104) 22'-90' 139'-198'
22'''-90''' 139'''-198'''
Inter-H-L (h 5-CL 126)* 220-216' 220''-216'''
Inter-H-H (h 11, h 14)* 226-226' 229-229''

*Two or three of the inter-chain disulfide bridges are not present, an average of 4 cysteinyl being conjugated each via a thioether bond to a drug linker.

N-glycosylation sites
H CH2 N84.4:
297, 297''
Fucosylated complex bi-antennary CHO-type glycans
Potential modified residues
Chemical StructureLupartumab amadotin.png
Cas Registry Number1640972-00-4
New Molecular EntityYes
OriginatorBayer HealthCare
Mechanism Of Action Ly6/PLAUR domain-containing protein 3 (LYPD3; C4.4a) inhibitor, tubulin inhibitor
Who Atc CodesL01 (Antineoplastic Agents)
Ephmra CodesL1 (Antineoplastics)
IndicationNeoplasms

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