Pegaspargase is a modified form of L-asparagine amidohydrolase used to treat acute lymphoblastic leukemia, which is dependent on an external source of asparagine. Pegaspargase is a conjugate of monomethoxypolyethylene glycol (mPEG) and L-asparaginase (L-asparagine amidohydrolase), an asparagine-specific enzyme that converts L-asparagine into aspartic acid and ammonia.
- Mechanism
- Curator reviewed · 4 references
Pegaspargase is a pegylated L-asparaginase that catalyzes the conversion of the amino acid L-asparagine into aspartic acid and ammonia. Asparagine is an amino acid that is vital for DNA and RNA synthesis and cell division. It is not an essential amino acid in humans since most normal human tissues can produce asparagine via the enzyme asparagine synthetase. However, leukemia cells have low levels of this enzyme and are unable to synthesize asparagine, making them dependent on exogenous sources. It has been suggested that pegaspargase kills leukemic cells by depleting plasma asparagine. Both Escherichia coli-derived L-asparaginase and pegaspargase follow the same mechanism of action; however, Escherichia coli-derived L-asparaginase requires frequent administration, presents a high incidence of hypersensitivity reactions, and can be neutralized without any signs of hypersensitivity. By pegylating L-asparaginase, the circulation time of L-asparaginase can be extended, and immunogenicity is reduced.
- Primary indication
- Pegaspargase is indicated as a component of a multi-agent chemotherapeutic regimen for the treatment of pediatric and adult patients with 1) first-line acute lymphoblastic leukemia or 2) acute lymphoblastic leukemia and hypersensitivity to asparaginase.Curator reviewed · 2 structured indications
- Formula / weight
- C1377H2208N382O442S17 · 31731.9 Da
- First approval
- Canada, 2000 · United States, 1994 · European Union, 2016
- Also known as
- PEG-ASP · Peg-asparaginase · PEG-aspargase · PEG-L-Asparaginase · Peg/L-asparaginase
- Brand names
Resolves to
What you can answer from here — as of July 17, 2026
Which other approved drugs treat the same conditions as Pegaspargase, and which companies have late-stage candidates in those indications?
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