Topotecan

Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity^[1]. IC50 & Target:Topoisomerase I^[1] In Vitro: Topotecan obviously inhibits proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner^[1].
Topotecan (0-40 μM) obviously inhibits the cell viability compared with the control groups, in a dose-dependent manner^[1].
Topotecan shows anti-proliferation activity against U251, U87, GSCs-U251 and GSCs-U87 cells, with IC₅₀ values of 2.73±0.25, 2.95±0.23, 5.46±0.41, and 5.95±0.24 μM, respectively^[1]. In Vivo: NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days treatment. Compared with the control, Low dose metronomic (LDM) Topotecan (TP) and TP+Pazopanib (PZ) liver weights are significantly lower in TP+PZ-treated animals, compared with PZ. Microscopic tumors are visible in the livers of mice belonging to all the groups except TP+PZ confirming the ability of TP+PZ to control liver metastasis^[2].
Topotecan (0.5, 1.0, and 1.5 mg/kg; Orally, daily) causes greater reduction in microvascular density in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan show decreased food intake, and a lesser antitumor effect^[2].