Drug intelligence / Profile preview

thioguanine + cytarabine + daunorubicin

Development stage
Phase 3
Lead developer
Cancer and Leukemia Group B
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Thioguanine + cytarabine + daunorubicin is a multi-agent chemotherapy regimen, commonly abbreviated as TAD, used primarily for induction and consolidation treatment of acute myeloid leukemia (AML) in adults and in some pediatric protocols. Thioguanine is a thiopurine antimetabolite that is converted intracellularly to thioguanine nucleotides, which incorporate into DNA and RNA and inhibit de novo purine synthesis, leading to impaired DNA/RNA replication and cytotoxicity. Cytarabine is a pyrimidine antimetabolite that is phosphorylated to its active triphosphate form and inhibits DNA polymerase, blocking DNA synthesis during S phase and triggering apoptosis in rapidly dividing leukemic blasts. Daunorubicin is an anthracycline that intercalates into DNA, inhibits topoisomerase II, and generates free radicals, resulting in DNA strand breaks and inhibition of cell division. Together, these agents provide complementary antineoplastic mechanisms that intensify cytotoxic effects on AML cells and have been used in regimens such as TAD-HAM-TAD with or without maintenance or additional high-dose cytarabine-based consolidation.[1][11][9][3]

Other names
TAD6-thioguanine + cytarabine + daunorubicin
02

Targets

DNADNA polymerase familyTOP2A (DNA topoisomerase II)

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