Oral bioavailability and disposition of [14C]omapatrilat in healthy subjects

Journal of Clinical Pharmacology

Volumn 41, Issue 8, 2001, Pages 833-841

  Malhotra, B K ^a   Iyer, R A ^a   Soucek, K M ^a   Behr, D ^a   Liao, W C ^a   Mitroka, J G ^a   Kaul, S ^a   Cohen, M B ^a   Knupp, C A ^a  

^a BRISTOL MYERS SQUIBB PHARMACEUTICAL RESEARCH INSTITUTE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

OMAPATRILAT;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISPOSITION; DRUG ELIMINATION; DRUG EXCRETION; DRUG METABOLISM; DRUG URINE LEVEL; FIRST PASS EFFECT; HUMAN; HUMAN EXPERIMENT; MALE; RANDOMIZED CONTROLLED TRIAL; STEADY STATE; TOTAL BODY WATER; URINARY EXCRETION;

ABSORPTION; ADMINISTRATION, ORAL; ADULT; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CARBON RADIOISOTOPES; CROSS-OVER STUDIES; HUMANS; MALE; PYRIDINES; THIAZEPINES; TISSUE DISTRIBUTION;

EID: 0034928304     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/00912700122010726     Document Type: Article

References (34)

1. Dual inhibitors of angiotensin converting enzyme and neutral endopeptidase: Design and therapeutic rationale
2. Recent advances in the design and development of vasopeptidase inhibitors
3. Vasopeptidase inhibitors: A new class of cardiovascular agents
4. Vasopeptidase inhibition with omapatrilat improves cardiac geometry and survival in cardiomyopathic hamsters more than does ACE inhibition with captopril
5. Cardiovascular effects of the novel dual inhibitor of neutral endopeptidase and angiotensin converting enzyme BMS-182657 in experimental hypertension and heart failure
6. Effects of omapatrilat in low, normal, and high renin experimental hypertension
7. Dual metalloprotease inhibitors: Mercaptoacetyl-based fused heterocyclic dipeptide mimetics as inhibitors of angiotensin-converting enzyme and neutral endopeptidase
8. Design of orally active dual inhibitors of angiotensin converting enzyme and neutral endopeptidase
9. Dose-related antihypertensive efficacy of omapatrilat, a vasopeptidase inhibitor, in models of normal and low renin hypertension
10. Quantitative determination of BMS186716, a thiol compound, in dog plasma by high-performance liquid chromatography-positive ion electrospray mass spectrometry after formation of the methyl acrylate adduct
11. High performance liquid chromatography/ionspray mass spectrometry of N-ethylmaleimide and acrylic acid ester derivatives for bioanalysis of thiol compounds
12. Noncompartmental analysis based on statistical moments theory
13. 14C]BMS-186716 to male beagle dogs
14. 14C]omapatrilat
15. Isolation and identification of human urinary metabolites of omapatrilat
16. Isolation and identification of human urinary metabolites of omapatrilat, a sulfhydryl-containing vasopeptidase inhibitor
17. Physiological parameters in laboratory animals and humans
18. Apparent volume of distribution
19. Elimination
20. Methylation of captopril in human liver, kidney and intestine
21. S-methylation of captopril: Demonstration of captopril thiol methyltransferase activity in human erythrocytes and enzyme distribution in rat tissues
22. Metabolism of captopril-L-cysteine, a captopril metabolite, in rats and dogs
23. Captopril disulfide: Conjugates may act as prodrugs; disposition of the disulfide dimer of captopril in the rat
24. Thiol-disulfide exchange equilibria and disulfide bond stability
25. Biotransformation of the disulfide of captopril in subcellular fractions of rat tissue
26. Suitability of various noninfinity area under the plasma concentration vs. time curve (AUC) estimates for use in bioequivalence determinations: Relationship to AUC from zero to infinity (AUC(0-INF))
27. The application of partial areas in assessment of rate and extent of absorption in bioequivalence studies of conventional release products: Experimental evidence
28. Truncated area under the curve as a measure of relative extent of bioavailability: Evaluation using experimental data and Monte Carlo simulations
29. Multiple-dose regimens
30. Effective half-life in clinical pharmacology
31. Omapatrilat pharmacokinetics in hepatic cirrhosis
32. Steady-state PK of omapatrilat in healthy subjects
33. Disposition and safety of omapatrilat in subjects with renal impairment