TY - JOUR
T1 - Safety and pharmacokinetics of 566C80, a hydroxynaphthoquinone with anti-Pneumocystis carinii activity
T2 - A phase I study in Human Immunodeficiency Virus (HIV)-infected men
AU - Hughes, Walter T.
AU - Kennedy, Wren
AU - Shenep, Jerry L.
AU - Flynn, Patricia M.
AU - Hetherington, Seth V.
AU - Fullen, Glenda
AU - Lancaster, Danny J.
AU - Stein, Daniel S.
AU - Palte, Steven
AU - Rosenbaum, Deborah
AU - Liao, San H.T.
AU - Blum, M. Robert
AU - Rogers, Michael D.
N1 - Funding Information:
Received 15 June 1990; revised 19 November 1990. Financial support: National Institute of Allergy and Infectious Diseases (AI-20673); National Cancer Institute Cancer Support (P30 CA21765); American-Lebanese-Syrian Associated Charities. Reprints or correspondence: Dr. Walter T. Hughes, S1. Jude Children's Research Hospital, 332 N. Lauderdale, Memphis, TN 38101-0318.
PY - 1991/4
Y1 - 1991/4
N2 - A hydroxynaphthoquinone compound (566C80) has been shown to be effective in the prevention and treatment of murine Pneumocystis carinii pneumonitis. In a phase I study, five cohorts of four human immunodeficiency virus-infected men received 100, 250, 750, 1500, and 3000 mg of the compound orally once daily for 12 days. A sixth cohort received 750 mg three times daily for 5 days then twice daily for 16 days. Evaluation included clinical, hematologic, and biochemical studies and the pharmacokinetics of 566C80. The only drug-related adverse effect was a maculopapular rash in one patient that resolved without discontinuation of the drug. With the largest dosage tested (3000 mg) the following pharmacokinetic measures were achieved: maximum plasma concentration, 39 μg/ml; time to maximum plasma concentration, 8.0 h; area under plasma concentration-time curve at steady state, 1088 h·μg/ml; plasma half-life, 51 h; and total plasma clearance, 4.09 l/h. Compound 566C80 offers promise as a new drug class for P. carinii pneumonia.
AB - A hydroxynaphthoquinone compound (566C80) has been shown to be effective in the prevention and treatment of murine Pneumocystis carinii pneumonitis. In a phase I study, five cohorts of four human immunodeficiency virus-infected men received 100, 250, 750, 1500, and 3000 mg of the compound orally once daily for 12 days. A sixth cohort received 750 mg three times daily for 5 days then twice daily for 16 days. Evaluation included clinical, hematologic, and biochemical studies and the pharmacokinetics of 566C80. The only drug-related adverse effect was a maculopapular rash in one patient that resolved without discontinuation of the drug. With the largest dosage tested (3000 mg) the following pharmacokinetic measures were achieved: maximum plasma concentration, 39 μg/ml; time to maximum plasma concentration, 8.0 h; area under plasma concentration-time curve at steady state, 1088 h·μg/ml; plasma half-life, 51 h; and total plasma clearance, 4.09 l/h. Compound 566C80 offers promise as a new drug class for P. carinii pneumonia.
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M3 - Article
C2 - 2010637
AN - SCOPUS:0025804551
SN - 0022-1899
VL - 163
SP - 843
EP - 848
JO - Journal of Infectious Diseases
JF - Journal of Infectious Diseases
IS - 4
ER -