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发表于 2003-9-4 07:57
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ACH126443 is an L nucleoside analogue which is highly potent against both HIV and hepatitis B. In vitro there is no mitochondrial toxicity. Due to its susceptibility to stomach acid, it must be dosed with an antacid, although an enteric coated preparation is now available. Due to the high levels of drug that may be potentiality achieved, it may be active against Epivir-resistant HBV and HIV.
Early results of a phase I b/ II clinical study are available, although it is important to realize that there are still placebo patients in each of the 3 arms therefore giving potential dilution of efficacy results. Results are available at day 14, and showed a drop in HBV DNA of 0.68, 1.43 and 1.74 log10 copies/mL in those receiving 1, 5 or 10mg, respectively. Clearly this drug does have activity against HBV, although much greater data needs to be made available before the manufacturers claims that this drug is "best in class" for both HIV and hepatitis B can be proven.
Reference
Selected Highlights from Drug Development for Antiretroviral Therapies 2001 (Hep DART 2001) [Abstract 040]
December 16-20, 2001, Maui, Hawaii
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