Penetration of SCH-39304, a new antifungal triazole into cerebrospinal fluid of primates

T. J. Walsh; C. Lester-McCully; M. G. Rinaldi; J. E. Wallace; F. M. Balis; J. W. Lee; P. A. Pizzo; D. G. Poplack

doi:10.1128/AAC.34.6.1281

Penetration of SCH-39304, a new antifungal triazole into cerebrospinal fluid of primates

T. J. Walsh, C. Lester-McCully, M. G. Rinaldi, J. E. Wallace, F. M. Balis, J. W. Lee, P. A. Pizzo, D. G. Poplack

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Abstract

We characterize the cerebrospinal fluid (CSF) penetration and pharmacokinetics of SCH-39304 in adult rhesus monkeys receiving a single oral dose of SCH-39304 (2.0 mg/kg of body weight). The mean CSF-to-lasma area under the curve ratio was 0.63 (± 0.18, standard error of the mean); maximum concentrations were 1.34 μg/ml (± 0.18) in CSF and 1.96 μg/ml (± 0.43) in plasma. The mean plasma half-life was 45.7 (± 0.3) in plasma and 0.96 μg/ml (± 0.12) in CSF. We conclude that SCH-39304 effectively penetrates into CSF and achieves concentrations considered active against many opportunistic yeast and that these concentrations are sustained in CSF for ≥ 24 h.

Original language	English (US)
Pages (from-to)	1281-1284
Number of pages	4
Journal	Antimicrobial agents and chemotherapy
Volume	34
Issue number	6
DOIs	https://doi.org/10.1128/AAC.34.6.1281
State	Published - 1990
Externally published	Yes

ASJC Scopus subject areas

Pharmacology
Pharmacology (medical)
Infectious Diseases

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title = "Penetration of SCH-39304, a new antifungal triazole into cerebrospinal fluid of primates",

abstract = "We characterize the cerebrospinal fluid (CSF) penetration and pharmacokinetics of SCH-39304 in adult rhesus monkeys receiving a single oral dose of SCH-39304 (2.0 mg/kg of body weight). The mean CSF-to-lasma area under the curve ratio was 0.63 (± 0.18, standard error of the mean); maximum concentrations were 1.34 μg/ml (± 0.18) in CSF and 1.96 μg/ml (± 0.43) in plasma. The mean plasma half-life was 45.7 (± 0.3) in plasma and 0.96 μg/ml (± 0.12) in CSF. We conclude that SCH-39304 effectively penetrates into CSF and achieves concentrations considered active against many opportunistic yeast and that these concentrations are sustained in CSF for ≥ 24 h.",

author = "Walsh, {T. J.} and C. Lester-McCully and Rinaldi, {M. G.} and Wallace, {J. E.} and Balis, {F. M.} and Lee, {J. W.} and Pizzo, {P. A.} and Poplack, {D. G.}",

year = "1990",

doi = "10.1128/AAC.34.6.1281",

language = "English (US)",

volume = "34",

pages = "1281--1284",

journal = "Antimicrobial Agents and Chemotherapy",

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publisher = "American Society for Microbiology",

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T1 - Penetration of SCH-39304, a new antifungal triazole into cerebrospinal fluid of primates

AU - Walsh, T. J.

AU - Lester-McCully, C.

AU - Rinaldi, M. G.

AU - Wallace, J. E.

AU - Balis, F. M.

AU - Lee, J. W.

AU - Pizzo, P. A.

AU - Poplack, D. G.

PY - 1990

Y1 - 1990

N2 - We characterize the cerebrospinal fluid (CSF) penetration and pharmacokinetics of SCH-39304 in adult rhesus monkeys receiving a single oral dose of SCH-39304 (2.0 mg/kg of body weight). The mean CSF-to-lasma area under the curve ratio was 0.63 (± 0.18, standard error of the mean); maximum concentrations were 1.34 μg/ml (± 0.18) in CSF and 1.96 μg/ml (± 0.43) in plasma. The mean plasma half-life was 45.7 (± 0.3) in plasma and 0.96 μg/ml (± 0.12) in CSF. We conclude that SCH-39304 effectively penetrates into CSF and achieves concentrations considered active against many opportunistic yeast and that these concentrations are sustained in CSF for ≥ 24 h.

AB - We characterize the cerebrospinal fluid (CSF) penetration and pharmacokinetics of SCH-39304 in adult rhesus monkeys receiving a single oral dose of SCH-39304 (2.0 mg/kg of body weight). The mean CSF-to-lasma area under the curve ratio was 0.63 (± 0.18, standard error of the mean); maximum concentrations were 1.34 μg/ml (± 0.18) in CSF and 1.96 μg/ml (± 0.43) in plasma. The mean plasma half-life was 45.7 (± 0.3) in plasma and 0.96 μg/ml (± 0.12) in CSF. We conclude that SCH-39304 effectively penetrates into CSF and achieves concentrations considered active against many opportunistic yeast and that these concentrations are sustained in CSF for ≥ 24 h.

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Penetration of SCH-39304, a new antifungal triazole into cerebrospinal fluid of primates

Abstract

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