Title: Pharmacokinetics of the anti-HIV bicyclam SID791 (JM3100) in rabbits, as determined by both analytical and bioassay methods
Authors: Witvrouw, Myriam ×
Seifert, J-M
Henson, GW
Martellucci, SA
Desmyter, J
De Clercq, Erik #
Issue Date: 1996
Series Title: Antivir Chem Chemoth vol:7 pages:27-30
Abstract: The serum levels of the bicyclam derivative 1,1'-[1,4-phenylenebis(methylene)]-bis-1,4,8,11-etraazacyclotetradecane octahydrochloride dihydrate [SID791 (JM3100)], a potent inhibitor of HIV replication (De Clercq ef al., 1994) were determined in rabbits using two different methods, A method based on the UV-absorption of the Cu-complex of SID791 was used to analyse by HPLC the serum drug concentrations, and an antiviral activity bio-assay was performed to investigate whether the drug in the rabbit serum was in an available active form, After subcutaneous (sc) administration of SID791 to rabbits at 25 mg/kg of body weight, the compound was cleared from the serum in a bi-exponential manner (β1-half-lives: 67 and 69 min; β2-half-lives: 320 and 245 min; distribution volumes: 0.40 and 0.37 l; total body clearance: 0.30 and 0.29 l/h; and AUG: 83.3 and 86.2 h µg/ml, as determined by HPLC and bio-assay, respectively), Thus, very similar kinetic parameters were noted if serum drug concentrations were determined by HPLC analysis or bio-assay, suggesting that in the rabbit serum the drug is present as an antiviral active agent.
ISSN: 0956-3202
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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