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Ximelagatran, an Oral Direct Thrombin Inhibitor, Has a Low Potential for Cytochrome P450-Mediated Drug-Drug Interactions
TLDR
In vitro and in vivo studies indicate that metabolic drug-drug interactions involving the major human CYP enzymes should not be expected with ximelagatran. Expand
Influence of Severe Renal Impairment on the Pharmacokinetics and Pharmacodynamics of Oral Ximelagatran and Subcutaneous Melagatran
TLDR
Subjects with severe renal impairment had significantly higher melagatran exposure and longer half-life because of lower CLr of melag atran compared with the control group with normal renal function, suggesting that a decrease in dose and/or an increase in the administration interval in patients with severe kidneys impairment would be appropriate. Expand
Effect of Tenapanor on Serum Phosphate in Patients Receiving Hemodialysis.
TLDR
Tenapanor treatment resulted in statistically significant, dose-dependent reductions in serum phosphate concentrations in patients with hyperphosphatemia receiving hemodialysis, and diarrhea was the most common adverse event. Expand
Pharmacokinetic Evaluations of the Co-Administrations of Vandetanib and Metformin, Digoxin, Midazolam, Omeprazole or Ranitidine
TLDR
Vandetanib with CYP3A4 substrates or omeprazole/ranitidine is unlikely to result in clinically relevant drug–drug interactions, but may require additional monitoring of metformin/digoxin, with dose adjustments where necessary. Expand
Combined in vitro-in vivo approach to assess the hepatobiliary disposition of a novel oral thrombin inhibitor.
TLDR
In conclusion, the hepatobiliary transport pathways of AZD0837 and its metabolites were identified in vitro and in vivo and Ketoconazole was shown to inhibit all of these three transporters; in particular, inhibition of P-gp and MATE1 occurred in a clinically relevant concentration range. Expand
Effects of Tenapanor on Cytochrome P450‐Mediated Drug‐Drug Interactions
TLDR
It is suggested that tenapanor can be coadministered with CYP3A4‐metabolized drugs without affecting their exposure and found findings were similar for metabolites of midazolam. Expand
Tenapanor administration and the activity of the H+‐coupled transporter PepT1 in healthy volunteers
TLDR
It is suggested that tenapanor 15 mg twice daily does not have a clinically relevant impact on the activity of the H+‐coupled transporter PepT1 in humans, and this may guide future research on drug–drug interactions involving NHE3 inhibitors. Expand
The Pharmacokinetics and Pharmacodynamics of Ximelagatran, an Oral Direct Thrombin Inhibitor, Are Unaffected by a Single Dose of Alcohol
TLDR
Alcohol did not alter the melagatran‐induced prolongation of the activated partial thromboplastin time or the good tolerability/safety profile of ximelag atran, and the pharmacokinetics, pharmacodynamics, and tolerability / safety of oral ximelsgatran were not affected by alcohol. Expand
Managing the Risk of CYP3A Induction in Drug Development: A Strategic Approach
TLDR
This model, the AstraZeneca induction strategy integrates in vitro assays and in vivo studies to make a comprehensive assessment of the induction potential of new chemical entities, and includes the sensitive CYP3A biomarker 4β-hydroxycholesterol. Expand
A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers
TLDR
Tenapanor treatment reduced absorption of intestinal sodium and phosphate from the gut in Japanese adults and had minimal systemic exposure and was well tolerated. Expand
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