Drug intelligence / Profile preview

cytarabine + 6-thioguanine

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral, Intrathecal, Subcutaneous
01

Overview

Cytarabine + 6-thioguanine is a combination chemotherapy regimen consisting of two antimetabolite agents used primarily in the treatment of acute myeloid leukemia (AML) and other hematologic malignancies. Cytarabine (also known as Ara-C or cytosine arabinoside) is a pyrimidine nucleoside analog that inhibits DNA synthesis by incorporation into DNA and inhibition of DNA polymerase, leading to cell cycle arrest in the S-phase. 6-Thioguanine is a purine analog that interferes with de novo purine synthesis and incorporates into DNA and RNA, resulting in cytotoxicity through disruption of nucleic acid function. The combination exploits synergistic effects on rapidly dividing leukemic cells. This regimen has been used for induction, consolidation, and maintenance therapy in AML[1][2][4][5].

Other names
cytosine arabinoside + 6-thioguanineara-C + TGcytarabine + thioguanine
02

Targets

DNAIMPDH (Inosine-5'-monophosphate dehydrogenase 1)HPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)PPAT (Amidophosphoribosyltransferase)

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