Brentuximab Vedotin

Products

Brentuximab vedotin is commercially available as a powder for the preparation of an infusion solution (Adcetris). It has been approved in many countries since 2013.

Structure and properties

Brentuximab vedotin is an anti-CD30 antibody-drug conjugate, a recombinant chimeric lgG1 antibody conjugated to the cytotoxic agent monomethylauristatin E (MMAE, C39H67N5O7, Mr = 718.0 g/mol). It consists of three moieties:

  • CAC10 antibody to CD30
  • Monomethylauristatin E (MMAE, cytostatic).
  • Linker between cAC10 and MMAE

Effects

Brentuximab vedotin (ATC L01XC12) has antitumor and cytotoxic properties. The complex binds to CD30 and is taken up into the cell. Cleavage of the linker in lysosomes releases the active drug MMAE. This binds to tubulin, inducing apoptosis of CD30-expressing tumor cells.

Indications

  • Relapsed or refractory CD30+ Hodgkin lymphoma.
  • Relapsed or refractory systemic anaplastic large cell lymphoma.

Dosage

According to the professional information. The drug is administered as an intravenous infusion.

Contraindications

Brentuximab vedotin is contraindicated in the presence of hypersensitivity and concomitant use of bleomycin. For complete precautions, see the drug label.

Interactions

MMAE is metabolized by CYP3A. Drug-drug interactions have been described with potent CYP3A4 and P-gp inhibitors.

Adverse effects

The most common potential adverse effects include peripheral sensory neuropathy, fatigue, nausea, diarrhea, neutropenia, vomiting, fever, and upper respiratory tract infection. Brentuximab vedotin may weaken the immune system and promote the occurrence of infectious diseases.