Chiral switch, a successful way to drug development: Example esomeprazole

被引:11
作者
Creutzfeldt, W [1 ]
机构
[1] Univ Gottingen, Zentrum Innere Med, D-37075 Gottingen, Germany
来源
ZEITSCHRIFT FUR GASTROENTEROLOGIE | 2000年 / 38卷 / 11期
关键词
chirality; chiral switch; enantiomer; isomeric protonpump inhibitor; esomeprazole; omeprazole;
D O I
10.1055/s-2000-10301
中图分类号
R57 [消化系及腹部疾病];
学科分类号
摘要
About 25% of common drugs are racemates, i.e. mixtures of their optical or spatial isomers (stereoisomers or enantiomers). Frequently the enantiomers differ in their pharmacokinetics, pharmacodynamics, drug interactions and side effects. Therefore, the pharmaceutical industry, pharmacologists and clinicians are increasingly interested in the development of enantiomers as drugs. Since advances in synthetic and analytical chemistry have provided the tools to produce stereoisomeric drugs, also the authorities recommend and support chiral switch. As example for the therapeutic gain the recent studies with esomeprazole, the first isomeric protonpump inhibitor (iPPI) are summarized and discussed.
引用
收藏
页码:893 / 897
页数:7
相关论文
共 27 条
[1]   Intellectual property and chirality of drugs [J].
Agranat, I ;
Caner, H .
DRUG DISCOVERY TODAY, 1999, 4 (07) :313-321
[2]  
ANDERSSON T, 2000, GASTROENTEROLOGY S2, V118, P1210
[3]   IS THERE AN OPTIMAL DEGREE OF ACID SUPPRESSION FOR HEALING OF DUODENAL-ULCERS - A MODEL OF THE RELATIONSHIP BETWEEN ULCER HEALING AND ACID SUPPRESSION [J].
BURGET, DW ;
CHIVERTON, SG ;
HUNT, RH .
GASTROENTEROLOGY, 1990, 99 (02) :345-351
[4]  
*COMM PROP MED PRO, 1993, III350191 COMM PROP
[5]  
CREUTZFELDT W, 1995, Z GASTROENTEROL S1, V33, P12
[6]   ROLES OF GASTRIC-ACID AND PH IN THE PATHOGENESIS OF GASTROESOPHAGEAL REFLUX DISEASE [J].
DENT, J .
SCANDINAVIAN JOURNAL OF GASTROENTEROLOGY, 1994, 29 :55-61
[7]   Safety of long-term treatment with a new PPI, esomeprazole in GERD patients. [J].
Genta, RM ;
Magner, DJ ;
D'Amico, D ;
Levine, DS .
GASTROENTEROLOGY, 2000, 118 (04) :A16-A16
[8]   Drug chirality and its clinical significance [J].
Hutt, AJ ;
Tan, SC .
DRUGS, 1996, 52 :1-12
[9]   Efficacy and safety of esomeprazole as maintenance therapy in GERD patients with healed erosive esophagitis [J].
Johnson, DA ;
Benjamin, SB ;
Whipple, J ;
D'Amico, D ;
Hamelin, B .
GASTROENTEROLOGY, 2000, 118 (04) :A17-A17
[10]   Comparison of esomeprazole, a novel PPI, vs omeprazole in GERD patients with erosive esophagitis (EE). [J].
Kahrilas, PJ ;
Falk, G ;
Whipple, J ;
D'Amico, D ;
Joelsson, B .
GASTROENTEROLOGY, 2000, 118 (04) :A193-A193