title: Prospective randomized trial of emtricitabine versus lamivudine short-term monotherapy in human immunodeficiency virus-infected patients.
abstract: We conducted a randomized, open-label, 10-day study that compared the antiretroviral activity of emtricitabine (FTC) 25, 100, and 200 mg once daily and lamivudine (3TC) 150 mg 2 times/day in 82 human immunodeficiency virus (HIV)-infected patients with virus loads >5000 and <100,000 copies/mL who were naive for 3TC and abacavir. All FTC doses demonstrated potent antiretroviral activity. Significantly greater virus suppression was seen at the 200 mg/day dose of FTC than with the lower FTC doses and/or 3TC (P=.02, P=.04, and P=.04, respectively). At the 200 mg/day dose, FTC produced a 1.7-log10 mean reduction in virus load. Trough FTC levels at the 200 mg/day dose exceeded the in vitro 90% inhibitory concentration dose for FTC by 5-fold. The long plasma half-life and the superior antiviral activity versus 3TC of the 200 mg/day FTC dose confirmed the results of other studies and led to the selection of this dose for subsequent therapeutic trials.
authors.affiliation: Triangle Pharmaceuticals, Durham, North Carolina 27717, USA. Frank.rousseau@Gilead.com.
authors.forename: Franck S
authors.initials: FS
authors.lastname: Rousseau
authors.forename: Charles
authors.initials: C
authors.lastname: Wakeford
authors.forename: Herve
authors.initials: H
authors.lastname: Mommeja-Marin
authors.forename: Ian
authors.initials: I
authors.lastname: Sanne
authors.forename: Cary
authors.initials: C
authors.lastname: Moxham
authors.forename: Jeanette
authors.initials: J
authors.lastname: Harris
authors.forename: Laura
authors.initials: L
authors.lastname: Hulett
authors.forename: Laurene H
authors.initials: LH
authors.lastname: Wang
authors.forename: Joseph B
authors.initials: JB
authors.lastname: Quinn
authors.forename: David W
authors.initials: DW
authors.lastname: Barry
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D019380:Anti-HIV Agents / Q000627:therapeutic use*; D003841:Deoxycytidine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000097:blood / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D000068679:Emtricitabine; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D019259:Lamivudine / Q000009:adverse effects / Q000097:blood / Q000627:therapeutic use*; D008875:Middle Aged; D011446:Prospective Studies
chemical_list: D019380:Anti-HIV Agents; D003841:Deoxycytidine; D019259:Lamivudine; D000068679:Emtricitabine