Brentuximab vedotin
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Chimeric (mouse/human) |
| Target | CD30 |
| Clinical data | |
| Trade names | Adcetris |
| License data |
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| Pregnancy category |
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| Routes of administration |
Intravenous |
| ATC code | |
| Legal status | |
| Legal status |
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| Identifiers | |
| Synonyms | SGN-35, previously cAC10-vcMMAE |
| CAS Number | |
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| Chemical and physical data | |
| Formula | C6476H9930N1690O2030S40 (C68H105N11O15)3–5 |
| Molar mass | 149.2–151.8 kg/mol |
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Brentuximab vedotin (INN, trade name Adcetris) is an antibody-drug conjugate (ADC) directed to the protein CD30, which is expressed in classical Hodgkin lymphoma (HL) and systemic anaplastic large cell lymphoma (sALCL).
On 28 February 2011 Seattle Genetics submitted a Biologics License Application or BLA to the U.S. Food and Drug Administration (FDA) for the use of brentuximab vedotin in relapsed or refractory Hodgkin's lymphoma and relapsed or refractory systemic anaplastic large cell lymphoma.
The drug was granted accelerated approval by the FDA on August 19, 2011 for relapsed HL and relapsed sALCL and conditional Marketing authorization from the European Medicines Agency in October 2012 for relapsed or refractory HL and relapsed or refractory sALCL.
Brentuximab vedotin consists of the chimeric monoclonal antibody brentuximab (cAC10, which targets the cell-membrane protein CD30) linked to cathepsin cleavable linker (valine-citrulline), para-aminobenzylcarbamate spacer three to five units of the antimitotic agent monomethyl auristatin E (MMAE, reflected by the 'vedotin' in the drug's name). The peptide-based linker bonds the antibody to the cytotoxic compound in a stable manner so the drug is not easily released from the antibody under physiologic conditions to help prevent toxicity to healthy cells and ensure dosage efficiency. The peptide antibody-drug bond facilitates rapid and efficient drug cleavage inside target tumor cell. The antibody cAC10 part of the drug binds to CD30 which often occurs on diseased cells but rarely on normal tissues.The antibody portion of the drug attaches to CD30 on the surface of malignant cells, delivering MMAE which is responsible for the anti-tumour activity. Once bound brentuximab vedotin is internalised by endocytosis and thus selectively taken up by targeted cells. The vesicle containing the drug is fused with lysosomes and lysosomal cysteine proteases, particularly cathepsin B start to break down valine-citrulline linker and MMAE is no longer bound to the antibody and is released directly into the tumor environment.
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