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troxacitabine
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- 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
01
Overview
Troxacitabine is a synthetic beta-L-nucleoside analog and a novel L-deoxycytidine analogue with potent antineoplastic activity. It acts as an antimetabolite, being activated by cellular kinases and incorporated into DNA, where its unnatural L-configuration causes chain termination during DNA replication. This results in inhibition of tumor cell proliferation. Unlike other cytosine nucleoside analogs, troxacitabine is resistant to inactivation by cytidine deaminase. It has shown preclinical efficacy in human xenograft tumor models and demonstrated antileukemic responses in patients with relapsed myeloid leukemia and refractory lymphoproliferative conditions[1][2][4][5].
- Brand names
- Troxatyl
- Other names
- troxacitabinatroxacitabinum
02
Targets
DNA polymerase familyDCK (Deoxycytidine kinase)
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