Sarilumab

Specification

• Cat#: THA-0074
• Product Name: Sarilumab
• Description: Sarilumab is a monoclonal antibody used to treat moderate to severe rheumatoid arthritis who have responded poorly or are intolerant of other DMARDs.
• Sequences: Heavy chain: EVQLVESGGGLVQPGRSLRLSCAASRFTFDDYAMHWVRQAPGKGLEWVSGISWNSGRIGYADSVKGRFTISRDNAENSLFLQMNGLRAEDTALYYCAKGRDSFDIWGQGTMVTVSSASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK Light chain: DIQMTQSPSSVSASVGDRVTITCRASQGISSWLAWYQQKPGKAPKLLIYGASSLESGVPSRFSGSGSGTDFTLTISSLQPEDFASYYCQQANSFPYTFGQGTKLEIKRTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC
• Molecular Weight: 150000.0 Da (143900 Da in absence of N-glycosylation in heavy chains (Asn296))
• Introduction: Sarilumab is a fully human anti-interleukin 6 (IL-6) receptor monoclonal IgG1 antibody that binds to both membrane-bound and soluble IL-6 receptor forms, thus blocking the cis- and trans-inflammatory signalling cascades of IL-6. Sarilumab was developed by Sanofi and Regeneron Pharmaceuticals, Inc; it was US FDA-approved in May 2017 and followed by EU approval in June 2017 for the treatment of moderate to severe rheumatoid arthritis (RA) in combination with methotrexate. RA is a chronic inflammatory disease characterized by polyarthritis, and its treatment has been challenged by the different responses in every patient. Subcutaneous administration of sarilumab has been shown to decrease acute-phase reactant levels and improve clinical RA symptoms.
• Purity: >99% by SDS-Page and HPLC analysis
• Formula: C6388H9918N1718O1998S44
• Appearance: Solid
• Endotoxin Level: < 0.001 EU/μg of the protein by the LAL method

Pharmaceutical Information

• Pharmacodynamics: Single-dose subcutaneous administration of sarilumab produced a rapid reduction of CRP levels, leading to normal levels after two weeks of treatment. Peak reduction in the absolute neutrophile count was observed after 3 to 4 days of treatment, followed by a recovery to baseline levels. A decrease in fibrinogen and serum amyloid A and an increase in hemoglobin and serum albumin were also detected.
• Targets: Interleukin-6 receptor subunit alpha High affinity immunoglobulin gamma Fc receptor I Low affinity immunoglobulin gamma Fc region receptor II-a Low affinity immunoglobulin gamma Fc region receptor II-b Low affinity immunoglobulin gamma Fc region receptor III-A Low affinity immunoglobulin gamma Fc region receptor III-B