Topotecan 是一种拓扑异构酶 I 抑制剂，通过抑制 DNA 拓扑异构酶起抗肿瘤作用，可用于治疗卵巢癌。

Topotecan is a Topoisomerase I inhibitor,and is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.

Topoisomerase I inhibitors, ?topotecan, inhibited growth and induced apoptosis of GSCs as well as glioma cells, which suggested that they might be the potential anticancer agents targeting gliomas to provide a novel therapeutic strategy[1].

Topotecan-hydrogels can deliver sustained concentrations of active drug into the vitreous with excellent biocompatibility in vivo and pronounced cytotoxic activity in retinoblastoma cells and may become an additional strategy for intraocular retinoblastoma treatment[2].

After isolated and identified the GSCs from glioma cells successfully, U251, U87, GSCs-U251 and GSCs-U87 cells were administrated with various concentrations of shikonin or topotecan at different time points to seek for the optimal administration concentration and time point.?The cell viability, cell cycle and apoptosis were detected using cell counting kit-8 and flow cytometer to observe the inhibitory effects on glioma cells and GSCs[1].

Hydrogel cytotoxicity was evaluated in retinoblastoma cells as a surrogate for efficacy and Topotecan vitreous pharmacokinetics and systemic as well as ocular toxicity were evaluated in rabbits. The pseudoplastic behavior of the hydrogels makes them suitable for intraocular administration. In vitro release profiles showed a sustained release of Topotecan from PCL-PEG-PCL up to 7days and drug loading did not affect the release pattern. Blank hydrogels did not affect retinoblastoma cell viability but 0.4% (w/w) Topotecan-loaded hydrogel was highly cytotoxic for at least 7days. After intravitreal injection, Topotecan vitreous concentrations were sustained above the pharmacologically active concentration. One month after injection, animals with blank or Topotecan-loaded hydrogels showed no systemic toxicity or retinal impairment on fundus examination, electroretinographic, and histopathological assessments[2].

123948-87-8

C23H23N3O5

421.453

SKF 104864A;NSC 609669;拓扑替康

DMSO:84 mg/mL (199.31 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years