The pharmacodynamics, safety and pharmacokinetics of single doses of the motilin agonist, camicinal, in type 1 diabetes mellitus with slow gastric emptying

Br J Pharmacol. 2016 Jun;173(11):1768-77. doi: 10.1111/bph.13475. Epub 2016 Apr 13.

Abstract

Background and purpose: Here we have investigated the pharmacokinetics, pharmacodynamics and safety of single doses of camicinal in type 1 diabetes mellitus (T1DM) patients with a history of slow gastric emptying with symptoms consistent with gastroparesis.

Experimental approach: In a randomized, double-blind, placebo-controlled, incomplete block, three-period, two-centre crossover study, patients received oral administration of placebo and two of the three possible doses of camicinal (25, 50 or 125 mg). Gastric emptying ((13) C-octanoic acid breath test), pharmacokinetics and safety were primary outcomes.

Key results: Nine of the 10 patients enrolled completed the study. Gastric half-emptying time decreased by -95 min (95% CI: -156.8, -34.2) after a single dose of camicinal 125 mg compared with placebo (52 vs. 147 min, P < 0.05), representing a 65% improvement. A decrease of the gastric half-emptying time compared with placebo (approximately 39 min) was observed with camicinal 25 and 50 mg, representing a 27% reduction for both doses (not statistically significant). A positive exposure-response relationship was demonstrated across all doses. The effects of camicinal on gastric half-emptying time were not influenced by fasting glucose levels. Single doses up to 125 mg were well tolerated. Camicinal was well absorbed, exhibiting linear and approximately dose-proportional pharmacokinetic characteristics and a clear exposure-response relationship with gastric emptying.

Conclusions and implications: Camicinal significantly accelerated gastric emptying of solids in T1DM patients following administration of a single oral dose. Camicinal was well tolerated and exhibited similar pharmacokinetic characteristics in diabetic patients to those previously reported in healthy volunteers.

Trial registration: ClinicalTrials.gov NCT00861809.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Diabetes Mellitus, Type 1 / drug therapy*
  • Diabetes Mellitus, Type 1 / metabolism
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Gastric Emptying / drug effects*
  • Gastrointestinal Agents / administration & dosage
  • Gastrointestinal Agents / adverse effects*
  • Gastrointestinal Agents / pharmacokinetics*
  • Humans
  • Middle Aged
  • Motilin / agonists*
  • Motilin / metabolism
  • Piperazines / administration & dosage
  • Piperazines / adverse effects*
  • Piperazines / pharmacokinetics*
  • Piperidines / administration & dosage
  • Piperidines / adverse effects*
  • Piperidines / pharmacokinetics*
  • Young Adult

Substances

  • Gastrointestinal Agents
  • N-(3-fluorophenyl)-1-((4-(((3S)-3-methyl-1-piperazinyl)methyl)phenyl)acetyl)-4-piperidinamine
  • Piperazines
  • Piperidines
  • Motilin

Associated data

  • ClinicalTrials.gov/NCT00861809