DFP-14927

DFP-14927 is a novel PEGylated (polyethylene glycol-conjugated) deoxycytidine analog and a polymeric derivative of the nucleoside analog DFP-10917. It is designed to improve pharmacokinetic properties and antitumor efficacy by enabling long-circulating drug delivery. Upon intravenous administration, DFP-14927 is selectively activated in the tumor microenvironment by proteases such as amidase or matrix metalloproteinases (MMPs), releasing the active anticancer substance. The released agent incorporates into DNA of rapidly proliferating cells, directly inhibiting DNA-dependent DNA polymerase activity, which leads to inhibition of DNA replication, cell cycle arrest at G2/M phase, DNA fragmentation, and ultimately tumor cell death. Preclinical studies have shown antitumor effects in pancreatic cancer models comparable to standard therapies like gemcitabine. The drug is being developed primarily for solid tumors (including gastroesophageal cancer, pancreatic cancer, cholangiocarcinoma, colorectal cancer), refractory/relapsed acute myeloid leukemia (AML), and myeloblastic syndrome.

Other names

pegylated deoxycytidine analogue DFP-14927