Pharmacokinetic disposition of the novel atypical anxiolytic CGS 9896 in the cynomolgus monkey

1988 ◽  
Vol 94 (3) ◽  
Author(s):  
GregoryM. Kochak ◽  
Ashok Rakhit ◽  
Frank Honc ◽  
C.James Mahoney
Keyword(s):  
Cynomolgus Monkey ◽  
The Novel ◽  
Cgs 9896

scholarly journals Pharmacokinetics of the Novel Echinocandin CD101 in Multiple Animal Species

2017 ◽  
Vol 61 (4) ◽  
Author(s):  
Voon Ong ◽  
Kenneth D. James ◽  
Steven Smith ◽  
B. Radha Krishnan
Keyword(s):  
Cynomolgus Monkey ◽  
Half Life ◽  
Fungal Infections ◽  
Volume Of Distribution ◽  
The Novel ◽  
Time Curve ◽  
Content Type ◽  
Treatment And Prevention ◽  
The Mean ◽  
Rat Tissue

ABSTRACT CD101 is a novel semisynthetic echinocandin with antifungal activity against Candida and Aspergillus spp. The pharmacokinetics (PK) of CD101 administered intravenously to mice, rats, dogs, cynomolgus monkeys, and chimpanzees are presented. CD101 consistently exhibited very low clearance, a modest volume of distribution at steady state (V ss), and a long half-life (t 1/2) across all species tested. In mouse, rat, dog, cynomolgus monkey, and chimpanzee, CD101 clearance was 0.10, 0.47, 0.30, 0.41, and 0.06 ml/min/kg, respectively; V ss was 206, 1,390, not determined, 597, and 400 ml/kg, respectively; and t 1/2 was 25, 39, 53, 40, and 81 h, respectively. CD101 demonstrated a lower clearance and correspondingly longer half-life than those of anidulafungin, with more pronounced differences in higher species (anidulafungin t 1/2, 8 h in cynomolgus monkey and 30 h in chimpanzee). In the rat, tissue/plasma area under the concentration-time curve (AUC) ratios, in descending order, were 4.62 (kidney), 4.33 (lung), 4.14 (liver), 3.87 (spleen), 1.09 (heart), and 0.609 (brain), indicating that CD101 exposure relative to plasma levels was comparable for major organs (approximately 4-fold higher in tissue than in plasma), with the exception of the heart and brain. Biliary elimination of intact CD101 was the predominant route of excretion; the mean cumulative amount of CD101 excreted into the bile and feces over the course of 5 days accounted for 22.6% and 27.7% of the total dose administered, respectively. There were no sex differences in the pharmacokinetics of CD101. Given its low clearance, long half-life, and wide tissue distribution, CD101 once weekly is expected to provide appropriate systemic levels for treatment and prevention of invasive fungal infections.

The novel steroidal glycoside from the dried bulb of Allium Macrostemon Bunge inhibits platelet activation

2010 ◽  
Vol 34 (8) ◽  
pp. S33-S33
Author(s):  
Wenchao Ou ◽  
Haifeng Chen ◽  
Yun Zhong ◽  
Benrong Liu ◽  
Keji Chen
Keyword(s):  
Platelet Activation ◽  
The Novel ◽  
Steroidal Glycoside ◽  
Allium Macrostemon
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