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Pharmacokinetics of apricitabine, a novel nucleoside reverse transcriptase inhibitor, in healthy volunteers treated with trimethoprim-sulphamethoxazole. 2008

L Shiveley, and C Struthers-Semple, and S Cox, and J Sawyer
Shire Pharmaceutical Development Inc., Wayne, PA, USA.

OBJECTIVE Apricitabine is a novel deoxycytidine analogue reverse transcriptase inhibitor under development for the treatment of human immunodeficiency virus-1 infection. This study was performed to investigate potential pharmacokinetic interactions between apricitabine and trimethoprim-sulphamethoxazole. METHODS Pharmacokinetic parameters were calculated for single and multiple doses of apricitabine (and its metabolite BCH-335) in the presence and absence of steady-state concentrations of trimethoprim-sulphamethoxazole in healthy volunteers. RESULTS Plasma concentrations and areas under the concentration-time curves of apricitabine and BCH-335 metabolite were higher when apricitabine was administered with trimethoprim-sulphamethoxazole than when apricitabine was given alone, both following single doses and during multipledosing. Apricitabine was well tolerated, both when given alone and with trimethoprim-sulphamethoxazole. CONCLUSIONS These results suggest that exposure to apricitabine and its metabolite BCH-335 is moderately increased during co-administration with up to 960 mg q.d.s. trimethoprim-sulphamethoxazole. The size of this interaction does not appear to be influenced by the dose of trimethoprim-sulphamethoxazole and is consistent with that seen with other cytidine analogues. Dose adjustment of apricitabine does not appear to be warranted when the drug is given with trimethoprim-sulphamethoxazole.

UI MeSH Term Description Entries
D008297 Male Males
D003841 Deoxycytidine A nucleoside component of DNA composed of CYTOSINE and DEOXYRIBOSE. Cytosine Deoxyribonucleoside,Cytosine Deoxyriboside,Deoxyribonucleoside, Cytosine,Deoxyriboside, Cytosine
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000890 Anti-Infective Agents Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection. Anti-Infective Agent,Anti-Microbial Agent,Antimicrobial Agent,Microbicide,Microbicides,Anti-Microbial Agents,Antiinfective Agents,Antimicrobial Agents,Agent, Anti-Infective,Agent, Anti-Microbial,Agent, Antimicrobial,Agents, Anti-Infective,Agents, Anti-Microbial,Agents, Antiinfective,Agents, Antimicrobial,Anti Infective Agent,Anti Infective Agents,Anti Microbial Agent,Anti Microbial Agents
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor

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