Gemcitabine monophosphate is a novel HDAC inhibitor with broad-spectrum antitumor activity against solid (IC50: 30 to 300 nM) and hematological malignancies. Gemcitabine monophosphate was found to be a potent inhibitor of HDAC1 and -8 (class I) in vitro.
Gemcitabine-O-Si(di-iso)-O-Mc, a drug-linker conjugate for Antibody-Drug Conjugates (ADC), exhibits potent antitumor activity. It incorporates Gemcitabine, a pyrimidine nucleoside analog antimetabolite and antineoplastic agent, connected through the ADC linker[1].
Troxacitabine, a DNA polymerase inhibitor, is potentially used for the treatment of acute myeloid leukemia (AML). In comparison with gemcitabine, troxacitabine was equally active against MiaPaCa and was more efficacious against Panc-01.