CHICAGO (Reuters) - Drugmakers are working on experimental diabetes drugs using a novel mechanism to help flush excess blood sugar out of the body, according to results of small studies presented at a medical meeting on Sunday.

Bristol-Myers Squibb hopes their drug, known as dapagliflozin, will be the first in a new class that seeks to block the reabsorption of glucose to lower elevated blood sugar levels in diabetics. GlaxoSmithKline Plc is also working on a drug using the same concept.

The drugs, known as SGLT-2, or sodium glucose uptake transporter 2 inhibitors, work by overriding the kidney's normal inclination to reabsorb excess glucose from the body rather than excreting it.

Diabetes is a chronic disease divided into two separate categories that result in similar symptoms. Diabetes type 1 is a genetic disorder, sometimes referred to as juvenile diabetes, in which the pancreas is unable to produce enough of or the hormone insulin, which regulates blood sugar.

Type II diabetes, or "adult-onset" diabetes, is the most common form of the disease that afflicts about 180 million people worldwide, and develops when the body can longer adequately utilize insulin. It is usually precipitated by obesity.

If uncontrolled, serious complications of diabetes include damage to eyesight, the kidneys and limb amputation. About 13,000 doctors and researchers are gathering at the American Diabetes Association's annual meeting in Chicago to discuss treatment options.

Bristol's 47-patient trial found that the drug helped improve fasting glucose values over 14 days. Patients received one of three different doses alone or with the oral generic medication metformin.

Two side effects were of "clinical interest" in the study, according to lead investigator Bernard Komoroski, a researcher at Bristol-Myers.

Two patients had hypoglycemia, or low blood sugar and two patients developed vaginal infections, he said.

"It's just something for us to keep our eye on," he said.

Bristol is developing the drug with British drugmaker AstraZeneca The companies expect to start the final phase of testing before requesting regulatory approval this year.

New data was also presented on GlaxoSmithKline's investigational SGLT-2 inhibitor, called sergliflozin.

The drug was found to decrease glucose concentrations in plasma in two studies of 14 healthy and eight diabetic patients. The most common adverse side effects in healthy patients were headache and sore throat. Among diabetic patients, the most common side effects were headache and stomach ailments.

(Additional reporting by Ransdell Pierson in New York)

看不懂啊

看不懂,就没有什么意思了.

实验糖尿病药物的新策略
芝加哥（路透社）——根据在星期天的医学会议上的一个小型研究的结果表明，制药商正在运用一个稳定的机制研究一个实验阶段的糖尿病药物，这个药帮助人们把多余的血糖排出体外。
Bristol-Myers Squibb公司希望他们的药物Dapagliflozin(葡萄糖钠吸收转运蛋白2(SGLT-2)抑制剂),在新类药中是最先推出的用来组织葡萄糖的重吸收而降低糖尿病人的血糖水平。GlaxoSmithKline公司也在以这个相同的概念研制新药。
Dapagliflozin是葡萄糖钠吸收转运蛋白2(SGLT-2)抑制剂，肾脏正常情况下具有重吸收多余的葡萄糖而不是排出它们，这个药物正是抑制了肾脏的这个特点。
糖尿病是一个慢性疾病，通过不同的症状分为两类；
I型糖尿病是种遗传性失调症，有些时候被称为青少年糖尿病，是因为胰腺不能分泌或分泌足够的调节血糖的胰岛素。
II型糖尿病或称为成人性发作糖尿病，是在全世界范围影响将近1.8亿人的最普通的糖尿病，是身体不能利用足够的胰岛素而引发的，通常伴肥胖。
如果控制不好，一些严重的并发症，如对视力的损害，肾脏及肢端切除可能会发生。大概有一万三千多个医生和研究人员聚在芝加哥的美国糖尿病协会的年会上讨论治疗方案。
Bristol的47例病人的试验发现，这个药物在14天内帮助改善病人的糖耐量（fasting glucose value）。病人在试验中服用Dapagliflozin三种不同剂量中的一种或者同二甲双胍一同服用。
Bristol-Myers公司的总研究员Bernard Komoroski 表示，这个研究中的“临床兴趣”是对两个副反应的研究。有两个病人出现了低血糖，两个病人出现了阴道感染。“这是我们需要注意的。”他说。
Bristol和英国的制药商AstraZeneca共同开发此药。两个药商都希望在今年申请正式的药品生产批准之前开展最后一期试验。
GlaxoSmithKline公司的关于SGL-2阻断剂的新数据也在会议上提出了，他们称这个药为sergliflozin.在14例健康人和8例糖尿病患者身上的实验中，这个药物能够降低血浆血糖浓度。在健康人身上出现的最普遍的副反应是头痛和喉咙痛，而在糖尿病人身上出现的最普遍的副反应则是头痛和胃痛。

Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats

Songping Han, Ph.D.1, Deborah L. Hagan, B.S.1, Joseph R. Taylor, B.S.1, Li Xin, M.D.1, Wei Meng, Ph.D.2, Scott A. Biller, Ph.D.2,,3, John R. Wetterau, Ph.D.1,,4, William N. Washburn, Ph.D.2, and Jean M. Whaley, Sc.D.
1Metabolic Diseases Biology
2Metabolic Diseases Chemistry, Bristol-Myers Squibb Research and Development, Princeton, NJ
3Current Affiliation: Novartis Institute for Biomedical Research, Cambridge, MA
4Cerenis Therapeutics, Ann Arbor, MI

Objective: The inhibition of gut and renal sodium-glucose cotransporters (SGLTs) has been proposed as a novel therapeutic approach to the treatment of diabetes. We have identified dapagliflozin as a potent and selective inhibitor of the renal sodium-glucose cotransporter SGLT2 in vitro and characterized its in vitro and in vivo pharmacology.

Research Design and Methods: Cell based assays measuring glucose analog uptake were used to assess dapagliflozin's ability to inhibit sodium-dependent and facilitative glucose transport activity. Acute and multidose studies in normal and diabetic rats were performed to assess the ability of dapagliflozin to improve fed and fasting plasma glucose levels. A hyperinsulinemic euglycemic clamp study was performed to assess the ability of dapagliflozin to improve glucose utilization following multidose treatment.

Results: Dapagliflozin potently and selectively inhibited human SGLT2 vs. human SGLT1, the major cotransporter of glucose in the gut, and did not significantly inhibit facilitative glucose transport in human adipocytes. In vivo, dapagliflozin acutely induced renal glucose excretion in normal and diabetic rats, improved glucose tolerance in normal rats, and reduced hyperglycemia in Zucker diabetic fatty (ZDF) rats following single oral doses ranging from 0.1–1.0 mg/kg. Once-daily dapagliflozin treatment over two weeks significantly lowered fasting and fed glucose levels at doses ranging from 0.1–1.0 mg/kg, and resulted in a significant increase in glucose utilization rate accompanied by a significant reduction in glucose production.

Conclusions: These data suggest that dapagliflozin has the potential to be an efficacious treatment for type 2 diabetes.

文章出处：http://diabetes.diabetesjournals ... bstract/db07-1472v1

[ 本帖最后由 queque 于 2008-4-15 03:51 PM 编辑 ]

你真的很伟大啊
翻译的这么好

我们这回才看懂了

只是不知道这药什么时候用到临床

已经到二期了。
我去他们公司主页看了看，并没有这个药的详细报道，可惜他们的原文文献我们看不到

你英语这么好啊

我过了四级，和着饭吃回三级

现只认识几个单词