title: Linogliride fumarate, representing a new class of oral hypoglycemic agent for diabetes.
abstract: This study presents the first multiday therapy trial of linogliride fumarate, a representative of a new class of oral hypoglycemic agents. Linogliride demonstrated a significant hypoglycemic activity in 26 patients with non-insulin-dependent diabetes mellitus receiving 1 week of therapy. In a dose range of 150 to 400 mg b.i.d., fasting glucose levels fell from 237 +/- 52 mg to 199 +/- 59 mg by day 7 (P less than 0.01). Eight-hour glucose AUCs fell from 2121 +/- 617 mg/dl/8 hr baseline to 1781 +/- 631 mg/dl/8 hr on day 7 of treatment (P less than 0.01). This was associated with a significant increase in insulin AUC from 380 +/- 327 to 610 +/- 417 on day 7 (P less than 0.01). Thus its initial action appears to be by an insulin secretagogue mechanism. No patient had any major adverse effect. This initial study indicates that linogliride fumarate is an effective hypoglycemic agent that significantly lowers fasting and postprandial glucose levels with short-term use. Linogliride fumarate represents a new group of hypoglycemic agents that may be shown to have therapeutic utility.
authors.affiliation: Department of Medicine, University of Maryland School of Medicine, Baltimore 21201.
authors.forename: P A
authors.initials: PA
authors.lastname: Levin
authors.forename: L
authors.initials: L
authors.lastname: Jovanovic
authors.forename: S A
authors.initials: SA
authors.lastname: Chalew
authors.forename: L
authors.initials: L
authors.lastname: Martin
authors.forename: D K
authors.initials: DK
authors.lastname: Pitarra
authors.forename: F
authors.initials: F
authors.lastname: Kim
authors.forename: A A
authors.initials: AA
authors.lastname: Kowarski
mesh_terms: D000284:Administration, Oral; D001786:Blood Glucose / Q000032:analysis; D002096:C-Peptide / Q000652:urine; D002986:Clinical Trials as Topic; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005215:Fasting; D006801:Humans; D007004:Hypoglycemic Agents / Q000627:therapeutic use*; D007328:Insulin / Q000097:blood; D011759:Pyrrolidines / Q000627:therapeutic use*; D011897:Random Allocation; D013997:Time Factors
chemical_list: D001786:Blood Glucose; D002096:C-Peptide; D007004:Hypoglycemic Agents; D007328:Insulin; D011759:Pyrrolidines; C044425:linogliride