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Calaspargase pegol is an asparagine specific enzyme used to treat acute lymphoblastic leukemia. Asparagine is incorporated into most proteins, and the synthesis of proteins is stopped when asparagine is absent, which inhibits RNA and DNA synthesis, resulting in a halt in cellular proliferation.
- Mechanism
- Curator reviewed · 5 references
L-asparaginase (the main component of this drug) is an enzyme that catalyzes the conversion of the amino acid L-asparagine into both aspartic acid and ammonia. This process depletes malignant cells of their required asparagine. The depletion of asparagine then blocks protein synthesis and tumor cell proliferation, especially in the G1 phase of the cell cycle. As a result, tumor cell death occurs. Asparagine is important in protein synthesis in acute lymphoblastic leukemia (ALL) cells which, unlike normal cells, cannot produce this amino acid due to lack of the enzyme asparagine synthase.
Pegylation decreases enzyme antigenicity and increases its half-life. Succinimidyl carbamate (SC) is used as a PEG linker to facilitate attachment to asparaginase and enhances the stability of the formulation. SC-PEG urethane linkages formed with lysine groups are more hydrolytically stable.
- Primary indication
- This drug is is an asparagine specific enzyme indicated as a component of a multi-agent chemotherapeutic regimen for the treatment of acute lymphoblastic leukemia in pediatric and young adult patients age 1 month to 21...Curator reviewed · 1 structured indication
- First approval
- Canada, 2023 · United States, 2019
- Also known as
- calaspargase pegol-mknl
- Code names
- EZN-2285
- Brand names
- Asparlas
Resolves to
What you can answer from here — as of March 06, 2025
Which drugs share a target with Calaspargase pegol, and which of those have an active Phase 3 trial?