Drug intelligence / Profile preview

pegaspargase + gemcitabine

Development stage
Unknown
Lead developer
Servier
Modality
Replacement Enzymes → Therapeutic Enzymes → Recombinant Proteins and Enzymes, Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Pegaspargase + gemcitabine is a combination of two chemotherapeutic agents used in oncology, particularly for hematologic malignancies and lymphomas. Pegaspargase is a pegylated form of L-asparaginase, an enzyme that catalyzes the hydrolysis of asparagine to aspartic acid and ammonia. This depletes circulating asparagine, an amino acid essential for leukemic cell survival due to their low levels of asparagine synthetase, leading to selective cytotoxicity in malignant cells[2][3][8]. Gemcitabine is a nucleoside analog (deoxycytidine analog) that undergoes intracellular phosphorylation to active metabolites which inhibit DNA synthesis by incorporation into DNA and inhibition of ribonucleotide reductase. This results in masked chain termination during DNA replication and ultimately leads to apoptosis[1][6]. The combination has been studied for use in aggressive lymphomas such as extranodal natural killer/T-cell lymphoma (ENKTL), where it has demonstrated efficacy with manageable toxicity profiles[5].

Other names
pegylated L-asparaginasedFdC
02

Targets

RRM2TS (Thymidylate synthase)RRM1CMPK1 (Deoxycytidylate kinase)

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