634907-30-5
634907-30-5 结构式
基本信息
BMS 986001
Festinavir
Censavudine
2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine
Thymidine, 2',3'-didehydro-3'-deoxy-4'-ethynyl-
物理化学性质
常见问题列表
|
HIV-2 30-81 nM (EC 50 ) |
HIV-1 450-890 nM (IC 50 ) |
BMS-986001 shows greater activity against HIV-2
ROD9
than against HIV-1
NL4-3
; the mean EC
50
s for BMS-986001 are 74 nM for HIV-2
ROD9
and 890 nM for HIV-1
NL4-3
in the single-cycle assay. HIV-2
ROD9
also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC
50
for HIV-2
ROD9
(EC
50
of 0.14 nM) being 30-fold lower than that for HIV-1
NL4-3
(EC
50
of 4.2 nM).
BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase.
The pharmacokinetic parameters of Censavudine (BMS-986001; 100-750 mg/kg) generated from the dried blood spot (DBS) assay and the plasma assay is compared. The ratios of the AUC (0-24 h) and C max for BMS-986001 in DBS compared to those in plasma are consistent at 0.83-0.91 and 0.81-0.97, respectively, across all dose groups in rats. The T max in rat DBS and plasma are also consistent at about 1 h.