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treosulfan + cytarabine
- Development stage
- Unknown
- Lead developer
- medac
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Intrathecal, Subcutaneous
01
Overview
Treosulfan + cytarabine is a combination of two chemotherapeutic agents used primarily in the treatment and conditioning regimens for hematologic malignancies, especially acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Treosulfan is a prodrug of a bifunctional alkylating agent that exerts its effects through DNA alkylation, leading to stem cell depletion, immunosuppression, and broad antineoplastic activity. Cytarabine is an antimetabolite pyrimidine analog that inhibits DNA polymerase after being converted intracellularly to its active triphosphate form; it disrupts DNA synthesis during the S-phase of the cell cycle. The combination aims to enhance anti-leukemic efficacy by leveraging both direct cytotoxicity and immunosuppressive effects[1][6][8]. This regimen may be used as part of preparative conditioning before allogeneic hematopoietic stem cell transplantation.
- Brand names
- Trecondyv
- Other names
- Ara-C (for cytarabine)
02
Targets
DNA polymerase family
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