| Identification | Back Directory | [Name]
Immunoglobulin, anti-(human glycoprotein NMB extracellular domain) (human monoclonal CR011 heavy chain), disulfide with human monoclonal CR011 κ-chain, dimer, thioether with N-[[[4-[[N-[6-(3-mercapto-2,5-dioxo-1-pyrrolidinyl)-1-oxohexyl]-L-valyl-N5-(aminocarbonyl)-L-ornithyl]amino]phenyl]methoxy]carbonyl]-N-methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide (1:?) | [CAS]
1182215-65-1 | [Synonyms]
Immunoglobulin, anti-(human glycoprotein NMB extracellular domain) (human monoclonal CR011 heavy chain), disulfide with human monoclonal CR011 κ-chain, dimer, thioether with N-[[[4-[[N-[6-(3-mercapto-2,5-dioxo-1-pyrrolidinyl)-1-oxohexyl]-L-valyl-N5-(aminocarbonyl)-L-ornithyl]amino]phenyl]methoxy]carbonyl]-N-methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide (1:) |
| Hazard Information | Back Directory | [Uses]
Glembatumumab vedotin (CDX-011) is an ADC (antibody-drug conjugates (ADCs)) comprising a fully human IgG2 monoclonal antibody (CR011) directed against glycoprotein NMB (GPNMB) and conjugated to the potent tubulinbinding cytotoxic agent MMAE via a protease-sensitive vc linker. Glembatumumab vedotin has potent anticancer effects[1]. | [in vivo]
Glembatumumab vedotin (CR011-vcMMAE; 1.25-80 mg/kg; i.v.; every 4 days; for 16 days) shows short-term anti-tumor effects (inhibition of tumor growth) and long-term effects (complete regression) in human SK-MEL-2 and SK-MEL-5 melanoma xenografts[2]. | Animal Model: | Athymic mice (6-week-old) injected with human SK-MEL-2 and SK-MEL-5 melanoma cells[2] | | Dosage: | 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 60 mg/kg, 80 mg/kg | | Administration: | i.v.; every 4 days; for 16 days | | Result: | Showed inhibition of tumor growth. |
| [References]
[1] Christopher H Keir, et al. The use of an antibody drug conjugate, glembatumumab vedotin (CDX-011), for the treatment of breast cancer. Expert Opin Biol Ther. 2012 Feb;12(2):259-63. DOI:10.1517/14712598.2012.642357
[2] Vincent A Pollack, et al. Treatment parameters modulating regression of human melanoma xenografts by an antibody-drug conjugate (CR011-vcMMAE) targeting GPNMB. Cancer Chemother Pharmacol. 2007 Aug;60(3):423-35. DOI:10.1007/s00280-007-0490-z
[3] Michael Roth, et al. Targeting Glycoprotein NMB With Antibody-Drug Conjugate, Glembatumumab Vedotin, for the Treatment of Osteosarcoma. Pediatr Blood Cancer. 2016 Jan;63(1):32-8. DOI:10.1002/pbc.25688 |
|
|