brentuximab vedotin

Ligand id: 6772

Name: brentuximab vedotin

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Summary of Clinical Use
Brentuximab vedotin is an anti-neoplastic agent used in the treatment of Hodgkin's lymphoma [4] and systemic anaplastic large cell lymphoma. Several clinical trials are evaluating the combination of brentuximab vedotin with immune checkpoint inhibitors, to assess any synergistic effects as a result of dual targeting. Checkpoint inhibitors being investigated in this way include nivolumab and pembrolizumab (both anti-PD-1), and ipilimumab (anti-CTLA4). Brentuximab vedotin + pembrolizumab (NCT02684292) and brentuximab vedotin + nivolumab (NCT03138499) are both Phase 3 studies in patients with relapsed/refractory classical Hodgkin's lymphoma.
Mechanism Of Action and Pharmacodynamic Effects
This drug efficiently delivers a highly cytotoxic drug to a specific set of cells, namely CD30 +ve cancer cells. Upon binding to cell surface antigen the conjugate is rapidly internalised and the cytotoxic portion (MMAE) is cleaved. This then travels to the nucleus where it binds β-tubulin and disrupts microtubule formation, thereby causing cell cycle arrest and subsequent cell death. MMAE seems to only bind to β-tubulin [3], at a similar location to the Vinca domain.
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