A phase I/II study of the safety and activity of a microsphere formulation of KNI-272 in patients with HIV-1 infection.
Eighteen patients with symptomatic HIV disease were enrolled into a phase I/II study of a microsphere formulation of the HIV protease inhibitor KNI-272, with doses escalated up to a maximum dose of 60 mg/kg/day. One patient developed reversible elevation in hepatic transaminase. The plasma half-life of the drug was very short, varying between 0.25 and 1.1 h. No consistent effect on plasma HIV RNA levels or CD4(+) lymphocyte counts was seen.
Department of Genitourinary Medicine and Communicable Diseases, Imperial College School of Medicine at St Mary's, Norfolk Place, London W2 1PG, UK.
D R
DR
Churchill
P M
PM
Slade
M
M
Youle
B G
BG
Gazzard
J N
JN
Weber
D000328:Adult; D000410:Alanine Transaminase / Q000187:drug effects / Q000378:metabolism; D019380:Anti-HIV Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D019540:Area Under Curve; D018791:CD4 Lymphocyte Count; D015496:CD4-Positive T-Lymphocytes / Q000166:cytology / Q000187:drug effects; D015331:Cohort Studies; D004305:Dose-Response Relationship, Drug; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics; D006801:Humans; D008297:Male; D008863:Microspheres; D008875:Middle Aged; D009842:Oligopeptides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010352:Patient Dropouts; D012367:RNA, Viral / Q000097:blood / Q000187:drug effects; D016896:Treatment Outcome
D019380:Anti-HIV Agents; D009842:Oligopeptides; D012367:RNA, Viral; D000410:Alanine Transaminase; C077822:kynostatin 272