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Namespace Prefixes

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Statements

Subject Item
n2:DB08870
rdf:type
n3:Drug
n3:description
Brentuximag vedotin or Adcetris® is an antibody-drug conjugate that combines an anti-CD30 antibody and the drug monomethyl auristatin E (MMAE). It is an anti-neoplastic agent used in the treatment of Hodgkin lymphoma and systemic anaplastic large cell lymphoma. Brentuximag vedotin was approved in 2011, and in January 2012, the drug label was revised to include a boxed warning of progressive multifocal leukoencephalopathy and death following JC virus infection.
n3:dosage
n9:271B599F-363D-11E5-9242-09173F13E4C5 n9:271B59A0-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Francisco JA, Cerveny CG, Meyer DL, Mixan BJ, Klussman K, Chace DF, Rejniak SX, Gordon KA, DeBlanc R, Toki BE, Law CL, Doronina SO, Siegall CB, Senter PD, Wahl AF: cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. Blood. 2003 Aug 15;102(4):1458-65. Epub 2003 Apr 24. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12714494
n3:group
approved
n3:halfLife
The terminal half-life is 4-6 days.
n3:indication
Used in the treatment of Hodgkin lymphoma and systemic anaplastic large cell lymphoma.
owl:sameAs
n7:DB08870
dcterms:title
Brentuximab vedotin
adms:identifier
n11:DB08870 n15:D09587 n16:Brentuximab_vedotin
n3:mechanismOfAction
Brentuximab vedotin is composed of 3 parts: a chimeric human-murine IgG1 that targets CD30, monomethyl auristatin E (MMAE),which is a microtubule disrupting agent, and a protease-susceptible linker that covalently links the antibody and MMAE. The IgG1 antibody enables brentuximab vedotin to target tumor cells expressing CD30 on their cell surface then brentuximab vedotin gets internalized into the cell. Once inside, the linker is cleaved releasing MMAE which binds disrupts the microtuble network.
n3:routeOfElimination
MMAE is eliminated by the feces (with 72% unchanged) and urine.
n3:synonym
cAC10-vcMMAE
n3:toxicity
The most severe toxic reaction seen in patients is progressive multifocal leukoencephalopathy. Other toxicities include bone marrow suppression, infusion reactions, peripheral neuropathy, Stevens-Johnson syndrome, and tumor lysis syndrome.
n3:volumeOfDistribution
The steady state volume of distribution is 6-10 L.
n3:proteinBinding
MMAE has a plasma protein binding range of 68-82%, and highly-protein bound drugs are not likely to displace it.
n3:synthesisReference
Francisco JA, Cerveny CG, Meyer DL, Mixan BJ, Klussman K, Chace DF, Rejniak SX, Gordon KA, DeBlanc R, Toki BE, Law CL, Doronina SO, Siegall CB, Senter PD, Wahl AF: cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. Blood. 2003 Aug 15;102(4):1458-65. Epub 2003 Apr 24
foaf:page
n5:adcetris-drug.htm n8:brentuximab-vedotin.html
n3:Molecular-Formula
n17:271B59A2-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n17:271B59A1-363D-11E5-9242-09173F13E4C5
n12:hasATCCode
n13:L01XC12
n3:absorption
Brentuximab vedotin is administered only as an intravenous infusion so absorption is 100%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
914088-09-8
n3:clearance
MMAE is cleared by the liver but not quantitative studies have been performed.