title: Pharmacokinetics of sifuvirtide in treatment-naive and treatment-experienced HIV-infected patients.
abstract: The pharmacokinetics assessment in two clinical studies of sifuvirtide (a novel HIV fusion inhibitor) was first reported in Chinese HIV patients. Nineteen treatment-naive HIV patients were treated with s.c.(subcutaneous injection) sifuvirtide [10 or 20 mg q.d.(quaque die)] for 28 days in study 1, and eight treatment-experienced HIV patients were treated with s.c. sifuvirtide (20 mg q.d.) in combination with HAART drugs (lamivudine, didanosine, and Kaletra) for 168 days in study 2. In study 1, T1/2 was 17.8 ± 3.7 h for 10 mg group and 39.0 ± 3.5 h for 20 mg group; the mean Cmax of last dose was 498 ± 54 ng/mL for 10 mg group and 897 ± 136 ng/mL for 20 mg group. In study 2, T1/2 was 6.71 ± 2.17 h in treatment-experienced patients. Cmax was 765 ± 288 ng/mL after last 168th dosage. Sifuvirtide showed improved clinical pharmacokinetics characteristics compared with Enfuvirtide, and showed very different pharmacokinetic characteristics between treatment-naive and treatment-experienced patients. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:4038-4047, 2014.
authors.affiliation: School of Life Science, Beijing Institute of Technology, Beijing 100081, People's Republic of China; Lab of Drug Metabolism and Pharmacokineticsm, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, People's Republic of China.
authors.forename: Qingfang
authors.initials: Q
authors.lastname: Meng
authors.affiliation: FusoGen Pharmaceuticals, Inc, Tianjin 300308, People's Republic of China.
authors.forename: Tianhao
authors.initials: T
authors.lastname: Dong
authors.affiliation: FusoGen Pharmaceuticals, Inc, Tianjin 300308, People's Republic of China.
authors.forename: Xin
authors.initials: X
authors.lastname: Chen
authors.affiliation: Lab of Drug Metabolism and Pharmacokineticsm, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, People's Republic of China.
authors.forename: Baohui
authors.initials: B
authors.lastname: Tong
authors.affiliation: School of Life Science, Beijing Institute of Technology, Beijing 100081, People's Republic of China; State Key Laboratory of Proteomics, Beijing Proteome Research Center, Beijing Institute of Radiation Medicine, Beijing 102206, People's Republic of China.
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Qian
authors.affiliation: Lab of Drug Metabolism and Pharmacokineticsm, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, People's Republic of China. Electronic address: selenameng@gmail.com.
authors.forename: Jinjing
authors.initials: J
authors.lastname: Che
authors.affiliation: Lab of Drug Metabolism and Pharmacokineticsm, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, People's Republic of China.
authors.forename: Yuanguo
authors.initials: Y
authors.lastname: Cheng
mesh_terms: D000328:Adult; D019380:Anti-HIV Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D023241:Antiretroviral Therapy, Highly Active / Q000379:methods; D016049:Didanosine / Q000627:therapeutic use; D004311:Double-Blind Method; D004338:Drug Combinations; D000077560:Enfuvirtide; D005260:Female; D015700:HIV Envelope Protein gp41 / Q000627:therapeutic use; D023581:HIV Fusion Inhibitors / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D019259:Lamivudine / Q000627:therapeutic use; D061466:Lopinavir / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged; D010446:Peptide Fragments / Q000627:therapeutic use; D010455:Peptides / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D019438:Ritonavir / Q000627:therapeutic use
chemical_list: D019380:Anti-HIV Agents; D004338:Drug Combinations; D015700:HIV Envelope Protein gp41; D023581:HIV Fusion Inhibitors; D010446:Peptide Fragments; D010455:Peptides; C558899:lopinavir-ritonavir drug combination; D000077560:Enfuvirtide; D061466:Lopinavir; D019259:Lamivudine; C505768:sifuvirtide; D016049:Didanosine; D019438:Ritonavir
keywords: HIV/AIDS; LC-MS; bioanalysis; clinical pharmacokinetics; metabolism; peptides