DRF-1042 is an orally active camptothecin analog that inhibits DNA topoisomerase I (DNA topoisomerase I). DRF-1042 shows promising anticancer activity against a panel of human cancer cell lines, including multidrug resistant (MDR) phenotypes.
in vitro
DRF-1042 demonstrates superior lactone stability and good in vitro anticancer activity against a panel of human cancer cell lines including multi-drug resistance (MDR) phenotype.
in vivo
In clonogenic assay against murine, canine and human bone marrow cells, DRF-1042 treatment shows less mylosupression that supports the possibility of protracted dose schedule in both experimental and clinical studies.