Article: A randomized placebo-controlled, dose-finding study of oral LB80380 in HBeAg-positive patients with chronic hepatitis B

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TitleA randomized placebo-controlled, dose-finding study of oral LB80380 in HBeAg-positive patients with chronic hepatitis B
AuthorsYuen, MF2
Kim, J1
Kim, CR1
Ngai, V2
Yuen, JCH2
Min, C1
Kang, HM1
Shin, BS3
Yoo, SD3
Lai, CL2
Issue Date2006
PublisherInternational Medical Press. The Journal's web site is located at http://www.intmedpress.com/Journals/AVT/journals_avt_home.cfm
CitationAntiviral Therapy, 2006, v. 11 n. 8, p. 977-983 [How to Cite?]
AbstractBackground: LB80380 is potent antiviral agent against hepatitis B virus (HBV) in vitro and in the woodchuck model. It has an excellent preclinical safety profile including lower potential for renal toxicity than adefovir. It is effective against both wild-type and YMDD mutant HBV. LB80380 is converted to its parent drug, LB80331, after oral absorption, and further metabolized to its active form, LB80317. Aims/Methods: This randomized placebo-controlled Phase I/II clinical study of LB80380 was conducted to assess the safety, antiviral activity and pharmacokinetics of its parent drug LB80331 and its active form LB80317 in 29 Asian adults with chronic hepatitis B positive for hepatitis B e antigen in four escalating dose groups (30, 60, 120 and 240 mg once per day) for 4 weeks with a 12-week follow-up period. Results: The mean maximum HBV DNA reduction was 3.05, 4.20, 3.67 and 3.68 log10 copies/ml for 30, 60, 120 and 240 mg per day, respectively. Viral dynamic analysis suggested a high degree of inhibition of HBV replication at doses of 60 mg or higher per day. LB80380 was well tolerated at all dose groups, and no dose-related clinical or laboratory adverse event was reported. Conclusion: LB80380 is shown to be a potent and safe antiviral agent for HBV. Marked HBV DNA suppression was observed in all dose groups. The HBV DNA suppression was approximately constant at doses of 60 mg and higher over the 28-day dosing period. The dose response of LB80380 will be evaluated further in large clinical studies. © 2006 International Medical Press.
ISSN1359-6535
2011 Impact Factor: 3.161
2011 SCImago Journal Rankings: 0.335
ISI Accession Number IDWOS:000243183100003
ReferencesReferences in Scopus
DC Field
Value
dc.contributor.authorYuen, MF
dc.contributor.authorKim, J
dc.contributor.authorKim, CR
dc.contributor.authorNgai, V
dc.contributor.authorYuen, JCH
dc.contributor.authorMin, C
dc.contributor.authorKang, HM
dc.contributor.authorShin, BS
dc.contributor.authorYoo, SD
dc.contributor.authorLai, CL
dc.date.accessioned2010-09-06T07:31:22Z
dc.date.available2010-09-06T07:31:22Z
dc.date.issued2006
dc.description.abstractBackground: LB80380 is potent antiviral agent against hepatitis B virus (HBV) in vitro and in the woodchuck model. It has an excellent preclinical safety profile including lower potential for renal toxicity than adefovir. It is effective against both wild-type and YMDD mutant HBV. LB80380 is converted to its parent drug, LB80331, after oral absorption, and further metabolized to its active form, LB80317. Aims/Methods: This randomized placebo-controlled Phase I/II clinical study of LB80380 was conducted to assess the safety, antiviral activity and pharmacokinetics of its parent drug LB80331 and its active form LB80317 in 29 Asian adults with chronic hepatitis B positive for hepatitis B e antigen in four escalating dose groups (30, 60, 120 and 240 mg once per day) for 4 weeks with a 12-week follow-up period. Results: The mean maximum HBV DNA reduction was 3.05, 4.20, 3.67 and 3.68 log10 copies/ml for 30, 60, 120 and 240 mg per day, respectively. Viral dynamic analysis suggested a high degree of inhibition of HBV replication at doses of 60 mg or higher per day. LB80380 was well tolerated at all dose groups, and no dose-related clinical or laboratory adverse event was reported. Conclusion: LB80380 is shown to be a potent and safe antiviral agent for HBV. Marked HBV DNA suppression was observed in all dose groups. The HBV DNA suppression was approximately constant at doses of 60 mg and higher over the 28-day dosing period. The dose response of LB80380 will be evaluated further in large clinical studies. © 2006 International Medical Press.
dc.description.natureLink_to_subscribed_fulltext
dc.identifier.citationAntiviral Therapy, 2006, v. 11 n. 8, p. 977-983 [How to Cite?]
dc.identifier.epage983
dc.identifier.hkuros130673
dc.identifier.isiWOS:000243183100003
dc.identifier.issn1359-6535
2011 Impact Factor: 3.161
2011 SCImago Journal Rankings: 0.335
dc.identifier.issue8
dc.identifier.openurl
dc.identifier.pmid17302367
dc.identifier.scopuseid_2-s2.0-33845675035
dc.identifier.spage977
dc.identifier.urihttp://hdl.handle.net/10722/77388
dc.identifier.volume11
dc.languageeng
dc.publisherInternational Medical Press. The Journal's web site is located at http://www.intmedpress.com/Journals/AVT/journals_avt_home.cfm
dc.publisher.placeUnited Kingdom
dc.relation.ispartofAntiviral Therapy
dc.relation.referencesReferences in Scopus
dc.subject.meshAdult
dc.subject.meshAntiviral Agents - administration & dosage - adverse effects - pharmacokinetics - therapeutic use
dc.subject.meshDose-Response Relationship, Drug
dc.subject.meshFemale
dc.subject.meshGuanine - administration & dosage - adverse effects - analogs & derivatives - pharmacokinetics - therapeutic use
dc.subject.meshHepatitis B e Antigens - blood
dc.subject.meshHepatitis B, Chronic - blood - drug therapy
dc.subject.meshHumans
dc.subject.meshMale
dc.subject.meshMiddle Aged
dc.subject.meshMolecular Structure
dc.subject.meshPhosphonic Acids - administration & dosage - adverse effects - pharmacokinetics - therapeutic use
dc.titleA randomized placebo-controlled, dose-finding study of oral LB80380 in HBeAg-positive patients with chronic hepatitis B
dc.typeArticle
Author Affiliations
  1. LG
  2. The University of Hong Kong
  3. Sungkyunkwan University