"目录号: HY-13672
LY2334737是口服活性的gemcitabine原药。
Nucleoside Antimetabolite/Analog
相关产品
5-Fluorouracil-Gemcitabine-5-Azacytidine-Cytarabine-Capecitabine-5-BrdU-Forodesine hydrochloride-Triciribine-Trifluorothymidine-Merimepodib-Raltitrexed-Floxuridine-Nelarabine-Tipiracil hydrochloride-6-Mercaptopurine-
生物活性
Description
LY2334737 is an orally available prodrug of gemcitabine which is a nucleoside analog used as chemotherapy.IC50 Value:Target: Nucleoside analogin vitro: Five cell lines that express CES2 responded to LY2334737treatment. LY2334737 was less cytotoxic to a SK-OV-3 CES2 knockdown than parental cells. The drug response of CES2-transfected HCT-116 cells correlated with CES2 expression level. Bystander studies showed statistically greater PC-3-GFP growth inhibition by LY2334737 when cells were cocultured with CES2 and not mock transfectants [1].in vivo: Oral treatment of xenograft models with 3.2 mg/kg LY2334737 once a day for 21 days showed greater tumor growth inhibition of CES2 transfectant than the mock transfectant (P ≤ 0.001) [1]. The MTD was 40 mg LY2334737. Fatigue was the most frequent DLT for LY2334737monotherapy (4 patients) followed by elevated transaminase levels (2 patients), both observed at the 40- to 50-mg dose levels. Among the 10 patients in the combination arm, 2 had DLTs at the 40-mg dose level. These were fatigue and elevated liver enzyme levels [2]. Metronomic LY2334737 administration caused increased blood flow in luciferase-tagged LM2-4 tumor xenografts, and this effect, readily measured using contrast micro-ultrasound, coincided with a relative increase in tumor bioluminescence [3].
Clinical Trial
Eli Lilly and Company
Malignant Solid Tumor-Solid Tumor-Metastatic Tumor
September 2008
Phase 1
View MoreCollapse
References
