Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats

@article{Kim2015PharmacokineticsOE,
  title={Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats},
  author={Tae-Heon Kim and Jong-woo Jeong and Ji-Hye Song and Kyeong-Ryoon Lee and Sunjoo Ahn and Sung-hoon Ahn and Sungsub Kim and Tae-Sung Koo},
  journal={Archives of Pharmacal Research},
  year={2015},
  volume={38},
  pages={2076-2082}
}
Abstract We characterized the pharmacokinetics of enzalutamide, a novel anti-prostate cancer drug, in rats after intravenous and oral administration in the dose range 0.5–5 mg/kg. Tissue distribution, liver microsomal stability, and plasma protein binding were also examined. After intravenous injection, systemic clearance, volumes of distribution at steady state (Vss), and half-life (T½) remained unaltered as a function of dose, with values in the ranges of 80.4–86.3 mL/h/kg, 1020–1250 mL/kg… Expand
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References

SHOWING 1-10 OF 22 REFERENCES
Pharmacokinetics of lurasidone, a novel atypical anti-psychotic drug, in rats
TLDR
To characterise the pharmacokinetics of lurasidone, a new atypical anti-psychotic drug, in rats after intravenous and oral administration at dose range 0.5–2.5 and 2.5-10 mg/kg, lurasidsone showed dose-independent Pharmacokinetics and appeared to be primarily eliminated by its metabolism. Expand
Pharmacokinetics, brain distribution, and plasma protein binding of the antiepileptic drug lacosamide in rats
TLDR
After intravenous injection, terminal half-life, systemic clearance, and steady state volumes of distribution remained unaltered as a function of dose with values in the range 3.01–3.53 h, 221–241 mL/h/kg and 702–732 mL/kg, respectively. Expand
Increased survival with enzalutamide in prostate cancer after chemotherapy.
TLDR
Enzalutamide significantly prolonged the survival of men with metastatic castration-resistant prostate cancer after chemotherapy, and was shown with respect to all secondary end points. Expand
Quantitative determination of enzalutamide, an anti-prostate cancer drug, in rat plasma using liquid chromatography-tandem mass spectrometry, and its application to a pharmacokinetic study.
TLDR
This analytical method could be successfully applied to the pharmacokinetic study of enzalutamide in rats and demonstrated a linear standard curve over a concentration range of 0.001-1 µg/mL and an intra- and inter-assay precision of 2.7 and 5.1%. Expand
Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1–2 study
TLDR
The results of this phase 1-2 trial validate in man preclinical studies implicating sustained androgen-receptor signalling as a driver in this disease. Expand
Enzalutamide as a second generation antiandrogen for treatment of advanced prostate cancer
TLDR
Enzalutamide is a novel second generation antiandrogen that has been demonstrated to significantly improve survival in men with metastatic CRPC in several clinical trials and its limitations for treatment of CRPC are discussed. Expand
A controlled trial of leuprolide with and without flutamide in prostatic carcinoma.
TLDR
Treatment with le uprolide and flutamide is superior to treatment with leuprolide alone in patients with advanced prostate cancer, and Symptomatic improvement was greatest during the first 12 weeks of the combined androgen blockade. Expand
Development of a Second-Generation Antiandrogen for Treatment of Advanced Prostate Cancer
TLDR
The diarylthiohydantoins RD162 and MDV3100 are characterized, two compounds optimized from a screen for nonsteroidal antiandrogens that retain activity in the setting of increased androgen receptor expression that appear to be promising candidates for treatment of advanced prostate cancer. Expand
Hepatic clearance of drugs. I. Theoretical considerations of a “well-stirred” model and a “parallel tube” model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance
  • K. Pang, M. Rowland
  • Chemistry, Medicine
  • Journal of Pharmacokinetics and Biopharmaceutics
  • 2005
TLDR
Although both models predict similar hepatic drug clearances under a variety of conditions, marked differences between them become apparent in their predictions of the influence of changes in the determinants of drug clearance on various pharmacokinetic parameters. Expand
Flutamide and cyproterone acetate exert agonist effects: induction of androgen receptor-dependent neuroprotection.
TLDR
It is observed that, although flutamide and cyproterone acetate blocked androgen-induced gene expression, they failed to inhibit DHT protection against apoptotic insults in cultured hippocampal neurons, suggesting a role for AR in the agonist effects of antiandrogens. Expand
...
1
2
3
...