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Tenofovir exalidex

產(chǎn)品活性：Tenofovir exalidex (CMX157) 是一種非環(huán)核苷酸類似物 Tenofovir 的脂質(zhì)結(jié)合物，對(duì)野生型和抗逆轉(zhuǎn)錄病毒耐藥的 HIV 毒株，包括多藥核苷/核苷酸類似物耐藥病毒，都有活性。Tenofovir exalidex 對(duì)人外周血單個(gè)核細(xì)胞中所有主要的HIV-1和HIV-2亞型以及單核細(xì)胞來源的巨噬細(xì)胞中所有 HIV-1 菌株具有活性，EC₅₀ 范圍在 0.2 和 7.2 nM 之間。Tenofovir exalidex 具有口服活性，無明顯毒性。Tenofovir exalidex 對(duì) HBV 也有活性。

研究領(lǐng)域：Anti-infection  |  Cell Cycle/DNA Damage

作用靶點(diǎn)：HIV  |  HBV  |  Nucleoside Antimetabolite/Analog

In Vitro: Tenofovir exalidex is consistently >300-fold more active than Tenofovir against multiple viruses in several different cell systems. Tenofovir exalidex will be effective against MNR mutants, including those that are unresponsive to all currently available NRTIs. Notably, the average EC₅₀ in PBMCs for CMX157 against a panel of 27 wild-type HIV-1 isolates representing group M subtypes A to G and group O was 2.6 nM (range, 0.2 to 7.2 nM).
Tenofovir exalidex exerts its therapeutic actions by inhibiting HBV polymerase-mediated HBV DNA elongation, but there is no known binding of cyclophilins to HBV polymerase nor participation of cyclophilins in DNA elongation. The combinational effect of CRV431 (host-targeting) and Tenofovir exalidex (direct-acting) on HBV DNA production is more consistent with the two compounds acting on distinct steps of the HBV life cycle.

In Vivo: Tenofovir exalidex (Sprague-Dawley rats) is orally available and has no apparent toxicity when given orally to rats for 7 days at doses of 10, 30, or 100 mg/kg/day.Tenofovir exalidex (5-10 mg/kg; oral gavage; daily for a period of 16 days) decreases liver HBV DNA levels dose-dependently.

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