01 Mar 1998·Zhonghua shi yan he lin chuang bing du xue za zhi = Zhonghua shiyan he linchuang bingduxue zazhi = Chinese journal of experimental and clinical virology

[Preliminary clinic observation on the inhibition of HBV by receptor-targeted drug L-HSA-AraAMP].

Article

Author: Wang, X ; Wang, H ; Zhang, L

To preliminarily observe the antiviral effect of receptor-targeted drug, the Lactosaminated Human Serum Albumin Arabinoside Adenine Monophosphate (L-HSA-Ara-AMP), 10 patients with chronic type B hepatitis (HBsAg, HbeAg/HBV DNA positive) were treated with this drug for 5 days. The daily dose of L-HSA-Ara-AMP was 35 mg/Kg (containing 1.5 mg Ara-AMP), whereas the usual daily dose of free Ara-AMP is 10 mg/Kg. In 10 patients treated, three patients' HBeAg became negative and six patients' HBeAg titer fell. Anti-HBc IgM all became negative in 4 anti-HBc IgM positive patients. In 8 HBV DNA positive patients, four patients' HBV DNA became negative and the other four patients' HBV DNA decreased. HBsAg remained positive in all of the ten patients. No adverse effects were observed. The results showed that L-HSA-Ara-AMP inhibits HBV as effective as free Ara-AMP, but at a daily dose 6.7 times lower than free Ara-AMP.

01 Apr 1996·Hepatology

Adenine arabinoside monophosphate coupled to lactosaminated human albumin administered for 4 weeks in patients with chronic type B hepatitis decreased viremia without producing significant side effects

Article

Author: Bonino, F ; Di Stefano, G ; Busi, C ; Lavezzo, B ; Verme, G ; De Bernardi Venon, W ; Brunetto, M R ; Ponzetto, A ; Gervasi, G B ; Fiume, L ; Torrani Cerenzia, M ; Mattioli, A

A conjugate of adenine arabinoside monophosphate (ara-AMP) with the liver-targeting molecule lactosaminated human serum albumin (L-HSA) was administered by intravenous infusion for 28 days to eight patients with chronic type B hepatitis. The daily dose varied among the patients, ranging from 34 mg/kg to 53 mg/kg (equal to 1.5 and 2.3 mg/kg ara-AMP, respectively). Pharmacokinetic analysis indicated that, at every dose tested, the conjugate was disposed of without accumulation. Viral DNA serum levels fell markedly during treatment; values rose again when treatment was ceased. The L-HSA-ara-AMP conjugate did not cause either the neurotoxic side effects of free ara-AMP or other adverse clinical reactions. It produced a significant increase both in serum alkaline phosphatase activity and platelet number, and a small but significant decrease in erythrocyte number. These laboratory parameters returned to normal levels within 2 months after treatment. The conjugate induced the production of small amounts of antibodies (˜ 20 pmol of conjugate bound by 1 mL of serum) in one patient only. In conclusion, the present results indicate that the L-HSA-ara-AMP conjugate can exert the antiviral activity of ara-AMP in chronic type B hepatitis patients without producing the neurotoxic side effects which hamper a 4-week period of treatment with the free drug.

01 May 1995·The Italian journal of gastroenterology

Liver targeting of adenine arabinoside monophosphate (ara-AMP) by coupling to lactosaminated human serum albumin.

Article

Author: Fiume, L ; Ponzetto, A ; Mattioli, A ; Lavezzo, B ; Bonino, F ; De Bernardi, W ; Busi, C ; Torrani-Cerenzia, M ; Capra, G ; Di Stefano, G

Adenine arabinoside monophosphate (ara-AMP) is a potent antiviral agent against hepadnaviruses but its use in the treatment of chronic hepatitis B is hampered by severe neurotoxic side effects, which are dose dependent. In order to reduce these adverse reactions and to adopt the lysosomotropic approach to antiviral chemotherapy, ara-AMP was coupled to lactosaminated human serum albumin (L-HSA), a neoglycoprotein which specifically penetrates hepatocytes. In mice with Ectromelia virus hepatitis, ara-AMP coupled with L-HSA was selectively delivered to liver cells in which it was released in a pharmacologically active form. Moreover in woodchucks with WHV hepatitis and in patients with chronic HBV infection, coupled ara-AMP inhibited hepadnavirus replication at a dose (1.5 mg/kg/day) 3-6 times lower than the free drug. A clinical study using a 28-day period of treatment with conjugated ara-AMP at 1.5 mg/kg/day has now been started. In the first 6 patients the treatment has been completed. The conjugate inhibited virus growth without producing any side effects. L-HSA-ara-AMP conjugate must be given by intravenous infusion. New hepatotropic conjugates of ara-AMP have been recently prepared which could be administered by bolus intravenous injection or by intramuscular route. These complexes might assure a better compliance in patients with hepatitis B virus infection for a long lasting liver targeted antiviral treatment.

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Indication	Highest Phase	Country/Location	Organization	Date
Hepatitis B	Phase 1	Italy	Laboratori Baldacci SpA	-

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