Rosmantuzumab

View Clinical trials for Rosmantuzumab Get Rosmantuzumab Patent Info for Free

NCI: An immunoglobulin (Ig) G1 humanized monoclonal antibody targeting human R-spondin 3 (RSPO3), with potential immunostimulating and antineoplastic activities. Upon intravenous administration, the anti-RSPO3 monoclonal antibody OMP-131R10 targets and binds to RSPO3 expressed on tumor cells. This prevents the activation of RSPO3, and inhibits both the binding of RSPO3 to leucine-rich repeat-containing G-coupled receptors (LGRs) and the activation of the RSPO-LGR pathway. This may result in an inhibition of both cancer stem cell (CSC) survival and the proliferation of cancer cells in which this pathway is overactivated. The RSPO-LGR pathway is a CSC pathway activated in a variety of cancer cell types.

Inn NameRosmantuzumab
Lab CodesOMP-131R10
Chemical NameImmunoglobulin G1-kappa, anti-[Homo sapiens RSPO3 (Rspondin 3, thrombospondin type I (TSP1) domain containing protein 2, THSD2)], humanized monoclonal antibody; gamma1 heavy chain (1-447) [humanized VH (Homo sapiens IGHV1-46*01 (84.50%) -(IGHD)-IGHJ4*01) [8.8.10] (1-117) -Homo sapiens IGHG1*03, (CH1 (118- 215), hinge (216-230), CH2 (231-340), CH3 (341-445), CHS (446-447)) (118-447)], (220-218')-disulfide with kappa light chain (1’-218’) [humanized V-KAPPA (Homo sapiens IGKV1-39*01 (83.80%) -IGKJ4*01) [10.3.9] (1'-111') - Homo sapiens IGKC*01, Km3 (112'-218')]; dimer (226-226":229-229")-bisdisulfide
Alternate NameImmunoglobulin G1, anti-(human roof plate-specific spondin R-spondin-3) (human-mus musculus monoclonal OMP-131R10 heavy chain), disulfide with human-mus musculus monoclonal OMP-131R10 kappa-chain, dimer
SequenceHeavy chain
QVQLVQSGAE VKKPGASVKV SCKASGYTFT DYSIHWVRQA PGQGLEWIGY 50
IYPSNGDSGY NQKFKNRVTM TRDTSTSTAY MELSRLRSED TAVYYCATYF 100
ANNFDYWGQG TTLTVSSAST KGPSVFPLAP SSKSTSGGTA ALGCLVKDYF 150
PEPVTVSWNS GALTSGVHTF PAVLQSSGLY SLSSVVTVPS SSLGTQTYIC 200
NVNHKPSNTK VDKRVEPKSC DKTHTCPPCP APELLGGPSV FLFPPKPKDT 250
LMISRTPEVT CVVVDVSHED PEVKFNWYVD GVEVHNAKTK PREEQYNSTY 300
RVVSVLTVLH QDWLNGKEYK CKVSNKALPA PIEKTISKAK GQPREPQVYT 350
LPPSREEMTK NQVSLTCLVK GFYPSDIAVE WESNGQPENN YKTTPPVLDS 400
DGSFFLYSKL TVDKSRWQQG NVFSCSVMHE ALHNHYTQKS LSLSPGK 447

Light chain
DIQMTQSPSS LSASVGDRVT ITCKASQSVD YDGDSYMNWY QQKPGKAPKL 50
LIYAASNLES GVPSRFSGSG SGTDFTLTIS PVQAEDFATY YCQQSNEDPL 100
TFGAGTKLEL KRTVAAPSVF IFPPSDEQLK SGTASVVCLL NNFYPREAKV 150
QWKVDNALQS GNSQESVTEQ DSKDSTYSLS STLTLSKADY EKHKVYACEV 200
THQGLSSPVT KSFNRGEC 218

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) 23'-92' 138'-198'
23'''-92''' 138'''-198'''
Inter-H-L (h 5-CL 126) 220-218' 220''-218'''
Inter-H-H (h 11, h 14) 226-226'' 229-229''

N-glycosylation sites
H CH2 N84.4:
297, 297''
Fucosylated complex bi-antennary CHO-type glycans
Other post-translational modifications
H CHS K2 C-terminal lysine clipping:
447, 447''
Chemical StructureRosmantuzumab.png
Cas Registry Number1684393-04-1
OriginatorOncoMed Pharmaceuticals
Mechanism Of ActionRSPO3 protein inhibitor, Anti-RSPO3 antibody
Who Atc CodesL01X-C (Monoclonal antibodies)
Ephmra CodesL1G (Monoclonal Antibody Antineoplastics)
IndicationAdvanced Relapsed Tumor, Refractory Solid Tumors

Free counters!