Natalizumab: α4-integrin antagonist selective adhesion molecule inhibitors for MS
作者： Richard A Rudick , Alfred Sandrock
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摘要: Natalizumab (Antegren, Elan Corp. plc.; Biogen Idec.) is the first alpha4-integrin antagonist in class of selective adhesion molecule inhibitors and Phase III clinical trials for treatment multiple sclerosis. After a 300 mg intravenous infusion, natalizumab has an elimination half-life 6 to 9 days, but receptors expressed on surface peripheral blood leukocytes are more than 80% saturated approximately 1 month postinfusion. Therefore, given as dose administered monthly. Preliminary efficacy results showed marked reduction (approximately 90%) formation new gadolinium-enhancing lesions reduced number patients with relapse by 50% relapsing-remitting or secondary progressive sclerosis receiving versus those placebo over 6-month period. In studies, demonstrated favorable safety profile. Pivotal studies monotherapy combination intramuscular interferon-beta-1a underway may be important addition therapeutic armamentarium
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