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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.
AuthorsP A Levin, L Jovanovic, S A Chalew, L Martin, D K Pitarra, F Kim, A A Kowarski
JournalClinical pharmacology and therapeutics (Clin Pharmacol Ther) Vol. 42 Issue 5 Pg. 498-503 (Nov 1987) ISSN: 0009-9236 [Print] United States
PMID3315390 (Publication Type: Clinical Trial, Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Blood Glucose
  • C-Peptide
  • Hypoglycemic Agents
  • Insulin
  • Pyrrolidines
  • linogliride
Topics
  • Administration, Oral
  • Blood Glucose (analysis)
  • C-Peptide (urine)
  • Clinical Trials as Topic
  • Diabetes Mellitus, Type 2 (drug therapy, metabolism)
  • Dose-Response Relationship, Drug
  • Fasting
  • Humans
  • Hypoglycemic Agents (therapeutic use)
  • Insulin (blood)
  • Pyrrolidines (therapeutic use)
  • Random Allocation
  • Time Factors

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