CLINICAL-PHARMACOLOGY OF THE HYPOCHOLESTEROLEMIC AGENT K 12.148 (LIFIBROL) IN HEALTHY-VOLUNTEERS

被引:15
作者
HASIBEDER, H
STAAB, HJ
SEIBEL, K
HEIBEL, B
SCHMIDLE, G
MARZ, W
机构
[1] UNIV FRANKFURT,DEPT BIOL CHEM,W-6000 FRANKFURT 1,GERMANY
[2] KLINGE PHARMA GMBH,DEPT CLIN RES,W-8000 MUNICH 80,GERMANY
[3] INST KLIN PHARMAKOL,GRUNSTADT,GERMANY
关键词
HYPOCHOLESTEROLEMIC AGENT; LIPID-LOWERING DRUG; CLINICAL PHARMACOLOGY; THERAPEUTIC USE;
D O I
10.1007/BF01409417
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
K 12.148 (INN:lifibrol), a new cholesterol synthesis inhibitor, was studied in healthy volunteers to evaluate tolerance/safety, the effects on lipids, and pharmacokinetics. In a sequential block design the doses of 150, 300, 600, or 900 mg, given once daily in the morning for 14 consecutive days, were examined in 40 healthy young males (8 active drug and 2 placebo per group, randomized) under well-controlled conditions. Total and LDL cholesterol serum levels decreased significantly in the 300, 600, and 900 mg groups (-13.4%, -23.8%, -25.6%, and -14.7%, -33.3%, -34.8% respectively), whereas no significant change was seen with placebo and 150 mg. The antiatherogenic index Apo A-I/B increased in a dose-dependent manner between 300 and 900 mg. Changes in HDL cholesterol and triglycerides were not statistically significant. The study compound was tolerated well, and safety laboratory parameters did not show any relevant alterations. K 12.148 might be a very effective drug for the treatment of hypercholesterolemia.
引用
收藏
页码:S91 / S94
页数:4
相关论文
共 13 条
[1]   LOVASTATIN - A PRELIMINARY REVIEW OF ITS PHARMACODYNAMIC PROPERTIES AND THERAPEUTIC USE IN HYPERLIPEMIA [J].
HENWOOD, JM ;
HEEL, RC .
DRUGS, 1988, 36 (04) :429-454
[3]   AN OVERVIEW OF LIPID-LOWERING DRUGS [J].
ILLINGWORTH, DR .
DRUGS, 1988, 36 :63-71
[4]   SERUM CHOLESTEROL, LIPOPROTEINS, AND RISK OF CORONARY HEART DISEASE - FRAMINGHAM STUDY [J].
KANNEL, WB ;
CASTELLI, WP ;
GORDON, T ;
MCNAMARA, PM .
ANNALS OF INTERNAL MEDICINE, 1971, 74 (01) :1-+
[5]  
KULIG W, 1987, 1987 INT S CHOL CONT
[6]   ANALYSIS OF PLASMA-LIPOPROTEINS BY ULTRACENTRIFUGATION IN A NEW FIXED ANGLE ROTOR - EVALUATION OF A PHOSPHOTUNGSTIC ACID/MGCL2 PRECIPITATION AND A QUANTITATIVE LIPOPROTEIN ELECTROPHORESIS ASSAY [J].
MARZ, W ;
GROSS, W .
CLINICA CHIMICA ACTA, 1986, 160 (01) :1-18
[7]   THE EFFECT OF CS-514, AN INHIBITOR OF HMG-COA REDUCTASE, ON SERUM-LIPIDS IN HEALTHY-VOLUNTEERS [J].
NAKAYA, N ;
HOMMA, Y ;
TAMACHI, H ;
GOTO, Y .
ATHEROSCLEROSIS, 1986, 61 (02) :125-128
[8]  
PAN HY, 1987, 1987 INT S CHOL CONT
[9]  
SCHLIACK M, 1989, ARTERY, V16, P90
[10]  
SCHLIACK M, 1986, 9TH INT S DRUGS AFF