Is Natalizumab an integrin inhibitor?

Natalizumab, the first α4-integrin antagonist in the class of selective adhesion molecule inhibitors, is in development for the treatment of multiple sclerosis and Crohn's disease. Natalizumab can be studied as a monotherapy and in combination with intramuscular interferon-β-1a in the treatment of patients with relapsing-remitting multiple sclerosis, and may be an important addition to the treatment of multiple sclerosis.

Natalizumab has an elimination half-life of 6 to 9 days after a 300 mg intravenous infusion, but alpha4-integrin receptors expressed on the surface of peripheral blood leukocytes are more than 80% saturated approximately 1 month after infusion. Therefore, natalizumab is administered at a monthly dose of 300 mg. Preliminary efficacy results show that patients with relapsing-remitting or secondary progressive multiple sclerosis who received natalizumab experienced a significant reduction (approximately 90%) in the formation of new gadolinium-enhancing lesions over six months and a 50% reduction in the number of patients who relapsed compared to patients who received placebo. In clinical studies, natalizumab showed a good safety profile.

Targetingα4-integrin prevents the development of demyelinating lesions in a mouse model of multiple sclerosis, elucidating the therapeutic potential of this drug. Natalizumab inhibits the interaction of α4β1 with VCAM-1 and α4β7 with MAdCAM-1. VCAM-1 and MAdCAM-1 are present on endothelial cells and interact with α4β1 and α4β7 on leukocytes, causing leukocytes to firmly adhere to endothelial cells. This is a necessary step for their extravasation into inflamed tissue.

Natalizumab's original patent drug is not marketed in the country and cannot be included in medical insurance. Currently, the generic drug natalizumab on the market overseas may cost more than 8,000 US dollars per box (the price may fluctuate due to exchange rates), which is very expensive. For more drug information and specific prices, please consult Yaode Medical Consultant.