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Vedolizumab is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease. | [Clinical Use]
Monoclonal antibody:
Treatment of ulcerative colitis and Crohn’s disease | [in vivo]
Blockade of α4β7 receptors on T-lymphocytes has been shown to occur for several weeks after a single dose of vedolizumab. The drug concentration following the infusion has been shown to be dose related with a mean maximum concentration of 12.5 μg/mL in those receiving 0.5 mg/kg of vedolizumab and 52.0 μg/mL in those receiving 2 mg/kg. The serum half-life of these two doses is 9-12 days respectively and saturation of α4β7 receptors on T-lymphocytes is >90% at both 4-6 weeks following infusion. In a dose ranging study, the serum drug concentrations increase with increasing dose and when regular induction infusions are used (on day 1, 15, 29 and 85), the serum half-life is between 15 and 22 days across all groups[1]. | [Drug interactions]
Potentially hazardous interactions with other drugs
Live vaccines: risk of generalised infections - avoid. | [Metabolism]
The expected consequence of metabolism is proteolytic degradation to small peptides and individual amino acids, and receptor-mediated clearance. The exact elimination route of vedolizumab is unknown although renal clearance is expected to be negligible. | [References]
[1] Soler D, et al. The binding specificity and selective antagonism of vedolizumab, an anti-alpha4beta7 integrintherapeutic antibody in development for inflammatory bowel diseases. J Pharmacol Exp Ther. 2009 Sep;330(3):864-75. DOI:10.1124/jpet.109.153973
[2] Singh H, et al. Vedolizumab: A novel anti-integrin drug for treatment of inflammatory bowel disease. J Nat Sci Biol Med. 2016 Jan-Jun;7(1):4-9. DOI:10.4103/0976-9668.175016 |
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