Pegaspargases

Products

Pegaspargase is commercially available as an injectable (Oncaspar). The drug was approved in the United States in 2006, in the EU in 2016, and in many countries in 2017.

Structure and properties

Pegaspargase (PEG-L-asparaginase) is the pegylated enzyme L-asparaginase. The PEG units are covalently attached to the enzyme.

Effects

Pegaspargase (ATC L01XX24) has antileukemic and cytotoxic properties. The effects are based on the cleavage of the amino acid asparagine into aspartic acid and ammonia. This inhibits protein synthesis, DNA synthesis and RNA synthesis, especially in leukemia cells, leading to cell death. This is because these cells are unable to produce asparagine themselves because they lack the enzyme asparagine synthetase. This in contrast to normal cells.

Indications

For combination therapy of acute lymphoblastic leukemia (ALL).

Dosage

According to the SmPC. The drug is administered as an intramuscular injection or intravenous infusion.

Contraindications

For complete precautions, see the drug label.

Adverse effects

The most common possible adverse effects include hypersensitivity reactions, anaphylaxis, febrile neutropenia, anemia, hyperglycemia, decreased platelet count, decreased neutrophil count, and hyperbilirubinemia.