Drug intelligence / Profile preview

pegaspargase + doxorubicin liposomal + dexamethasone

Development stage
Unknown
Lead developer
Servier
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Liposomes → Lipid-based Nanoparticles → Nanoparticles → Drug Delivery Systems, Therapeutic Enzymes → Recombinant Proteins and Enzymes
Administration
Intravenous, Intramuscular, Oral
01

Overview

This is a combination chemotherapy regimen consisting of three agents: - **Pegaspargase** is a pegylated form of L-asparaginase, an enzyme that depletes asparagine, an amino acid essential for the survival of certain leukemic cells. By breaking down asparagine, pegaspargase inhibits protein synthesis in cancer cells, leading to cell death. - **Doxorubicin liposomal** (also known as pegylated liposomal doxorubicin) is an anthracycline antibiotic encapsulated in liposomes with polyethylene glycol (PEG), which enhances its circulation time and reduces cardiotoxicity compared to conventional doxorubicin. It acts primarily by intercalating DNA and inhibiting topoisomerase II, resulting in DNA damage and apoptosis. - **Dexamethasone** is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive properties. In oncology regimens, it induces apoptosis in certain lymphoid malignancies. This combination leverages multiple mechanisms—enzyme depletion of amino acids critical for tumor growth (pegaspargase), direct cytotoxicity via DNA damage (doxorubicin liposomal), and steroid-induced apoptosis/anti-inflammatory effects (dexamethasone). The regimen has been explored particularly for hematologic malignancies such as acute lymphoblastic leukemia and lymphoma[9][7].

02

Targets

GR (Glucocorticoid receptor)TOP2A (DNA topoisomerase II)

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