Aprutumab ixadotin

View Clinical trials for Aprutumab ixadotin Get Aprutumab ixadotin Patent Info for Free

NCI: An antibody-drug conjugate (ADC) directed against the fibroblast growth factor receptor type 2 (FGFR2) and conjugated to an as of yet unidentified toxin, with potential antineoplastic activity. Upon intravenous administration, the anti-FGFR2 ADC BAY1187982 binds to FGFR2. Upon binding, the toxin selectively induces cell death, through an as of yet undisclosed mechanism of action, in FGFR2-expressing tumor cells. FGFR2, a receptor tyrosine kinase upregulated in many tumor cell types, plays an essential role in tumor cell proliferation, differentiation and survival.

Inn NameAprutumab ixadotin
Lab CodesBAY-1187982
Chemical NameImmunoglobulin G1-lambda1, anti-[Homo sapiens FGFR2 (fibroblast growth factor receptor 2, keratinocyte growth factor receptor, KGFR, CD332)], Homo sapiens monoclonal antibody conjugated to an auristatin W derivative; gamma1 heavy chain (1-451) [Homo sapiens VH (IGHV3-23*01 (98.00%) -(IGHD) -IGHJ5*02) [8.8.15](1-122) -IGHG1*01, Gm17,1 (CH1 (123-220), hinge (221-235), CH2 (236-345), CH3 (346-450),CHS K>del (451)) (123-451)], (225-215')-disulfide with lambda1 light chain (1'-216') [Homo sapiens V-LAMBDA (IGLV1-47*01 (90.70%) - IGLJ3*02) [8.3.11] (1'-110') -IGLC2*01 (111'-216')]; dimer (231-231'':234-234'')-bisdisulfide; conjugated, on an average of 4 lysyl, to N-(5-carboxypentyl)-N-demethylauristatin W (AW) C1.5-(1,2-oxazinan-2-yl) derivative
SequenceHeavy chain
EVQLLESGGG LVQPGGSLRL SCAASGFTFS SYAMSWVRQA PGKGLEWVSA 50
ISGSGTSTYY ADSVKGRFTI SRDNSKNTLY LQMNSLRAED TAVYYCARVR 100
YNWNHGDWFD PWGQGTLVTV SSASTKGPSV FPLAPSSKST SGGTAALGCL 150
VKDYFPEPVT VSWNSGALTS GVHTFPAVLQ SSGLYSLSSV VTVPSSSLGT 200
QTYICNVNHK PSNTKVDKKV EPKSCDKTHT CPPCPAPELL GGPSVFLFPP 250
KPKDTLMISR TPEVTCVVVD VSHEDPEVKF NWYVDGVEVH NAKTKPREEQ 300
YNSTYRVVSV LTVLHQDWLN GKEYKCKVSN KALPAPIEKT ISKAKGQPRE 350
PQVYTLPPSR DELTKNQVSL TCLVKGFYPS DIAVEWESNG QPENNYKTTP 400
PVLDSDGSFF LYSKLTVDKS RWQQGNVFSC SVMHEALHNH YTQKSLSLSP 450
G 451

Light chain
QSVLTQPPSA SGTPGQRVTI SCSGSSSNIG NNYVSWYQQL PGTAPKLLIY 50
ENYNRPAGVP DRFSGSKSGT SASLAISGLR SEDEADYYCS SWDDSLNYWV 100
FGGGTKLTVL GQPKAAPSVT LFPPSSEELQ ANKATLVCLI SDFYPGAVTV 150
AWKADSSPVK AGVETTTPSK QSNNKYAASS YLSLTPEQWK SHRSYSCQVT 200
HEGSTVEKTV APTECS 216

Disulfide bridges location
Intra-H (C23-C104) 22-96 149-205 266-326 372-430
22''-96'' 149''-205'' 266''-326'' 372''-430''
Intra-L (C23-C104) 22'-89' 138'-197'
22'''-89''' 138'''-197'''
Inter-H-L (h 5-CL 126) 225-215' 225''-215'''
Inter-H-H (h 11, h 14) 231-231' 234-234''

N-glycosylation sites
H CH2 N84.4:
302, 302''
Fucosylated complex bi-antennary CHO-type glycans

Potential modified residues
An average of 4 lysyl are substituted
Chemical StructureAprutumab ixadotin.png
Cas Registry Number1708947-48-1
New Molecular EntityYes
Mechanism Of ActionType-2 fibroblast growth factor receptor antagonist, keratinocyte growth factor (KGF) receptor antagonist
Who Atc CodesL01 (Antineoplastic Agents)
Ephmra CodesL1 (Antineoplastics)

Free counters!