Drug intelligence / Profile preview

gemcitabine + cisplatin + dexamethasone + pegaspargase + methotrexate

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Therapeutic Enzymes → Recombinant Proteins and Enzymes
Administration
Intravenous, Intramuscular, Oral, Intrathecal
01

Overview

This is a multi-agent chemotherapy regimen composed of five drugs: - **Gemcitabine** (a nucleoside analog antimetabolite that inhibits DNA synthesis) - **Cisplatin** (a platinum-based alkylating agent that causes DNA crosslinking and apoptosis) - **Dexamethasone** (a synthetic glucocorticoid with anti-inflammatory and immunosuppressive effects, also used to reduce chemotherapy side effects) - **Pegaspargase** (pegylated L-asparaginase, an enzyme that depletes asparagine, inhibiting protein synthesis in certain cancer cells) - **Methotrexate** (an antimetabolite and antifolate agent that inhibits dihydrofolate reductase, blocking DNA synthesis) This combination brings together agents with different mechanisms of action to maximize cytotoxicity against rapidly dividing malignant cells. Such regimens are typically used for aggressive hematologic malignancies or rare solid tumors where multi-drug synergy is required. Each component has established use in oncology—gemcitabine plus cisplatin is standard for several solid tumors[1][2][4], while pegaspargase, methotrexate, and dexamethasone are commonly combined in protocols for acute lymphoblastic leukemia or lymphoma[6][8]. The addition of all five agents may be considered in clinical trials or highly refractory cases.

02

Targets

RNR (Ribonucleotide reductase)DHFR (Dihydrofolate reductase)DNA polymerase familyDNAGR (Glucocorticoid receptor)

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