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Synonyms: AN100226 | anti-alpha4 integrin | anti-VLA4 | Tysabri®
natalizumab is an approved drug (FDA (2004), EMA (2006))
Compound class:
Antibody
Comment: Natalizumab was the first migration-inhibitory biological drug to be approved for inflammatory diseases. It targets α4β1 integrin (VLA-4) on leukocytes to block interaction with vascular cell adhesion molecule 1 (VCAM-1) on inflamed endothelium, thus inhibiting leukocyte extravasation into sites of inflammation. It is active in peripheral tissues and the central vervous system.
Targeting cell migration-related molecules in immune conditions (and cancer) is regarded as a valid approach for the development of novel anti-inflammatory therapeutics [3]. The design and synthesis of this antibody was originally described in a 1997 publication [2]. Biosimilars: The first natalizumab biosimilar was approved by the FDA in August 2023. Like the originator/reference agent, Tyruko® (natalizumab-sztn; Sandoz Inc.) is indicated for relapsing forms of multiple sclerosis and moderate-severe active Crohn's disease (when conventional therapies, including TNF-α inhibitors, are inadequate or not tolerated). 
View more information in the IUPHAR Pharmacology Education Project: natalizumab |
| Immunopharmacology Comments |
| Natalizumab targets α4-containing intergrins, including the α4β1 lymphocyte homing receptor. |
| Immunopharmacology Disease | |||
| Disease | X-Refs | Comment | References |
| Crohn's disease |
Disease Ontology:
DOID:8778 OMIM: 266600 Orphanet: ORPHA206 |
Approved drug for CD. | |
| Multiple sclerosis |
Disease Ontology:
DOID:2377 OMIM: 126200 Orphanet: ORPHA802 |
Approved for the treatment of relapsing forms of multiple sclerosis. | |
