Safety Study of Intravenous 6β-Naltrexol (AIKO-150) in Opioid-Dependent Subjects

A Phase-I, Two-Stage, Double-Blind, Placebo-Controlled, Pharmacokinetic and Pharmacodynamic Trial of Low Doses of Intravenous 6β-Naltrexol (AIKO-150) in Opioid-Dependent Subjects.

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT00829777

Acronym

AIKO-150

Enrollment

Registered

2009-01-27

Start date

2009-03-31

Completion date

2009-09-30

Last updated

2009-09-16

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Opiate Addiction

Keywords

Naloxone, 6β-Naltrexol, Opioid-dependent, Pharmacokinetics, peripheral effects of withdrawal, central effects of withdrawal

Brief summary

The purpose of this study is to evaluate the safety and efficacy of intravenous 6β-Naltrexol administered to opiate dependent subjects

Interventions

DRUG6β-Naltrexol escalating doses from 0.05-0.5 mg IV

Drug: Naloxone 0.1 mg IV/5 minutes to all subjects to determine tolerability to precipitated withdrawal during screening. Those that tolerate withdrawal proceed to Stage 1: Drug: Lactulose 10 gm orally plus 3 IV infusions 30 minutes apart of Naloxone 0.1 mg IV and 2 placebo given randomly to all subjects. If tolerated, proceed to 5 additional medication dosing sessions with all subjects receiving oral Lactulose 10 GM plus IV escalating 6β-Naltrexol 0.05 mg, 0.15 mg, 0.5 mg with a randomized placebo.

Study design

Allocation

RANDOMIZED

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Masking

DOUBLE (Subject, Caregiver)

Eligibility

Sex/Gender

ALL

Age

21 Years to 45 Years

Healthy volunteers

Inclusion criteria

* Opiate dependent males and females age 21-45 on stable doses of methadone * Fluent English speaker * Willing and able to give written consent

Exclusion criteria

* Pregnancy or lactation FOR MORE DETAILS CONTACT THE RESEARCH CLINIC.

Design outcomes

Primary

Measure	Time frame
- 6β-Naltrexol will have 13 hr half-life. Plasma collected	-0-24 hrs post dose
- 6β-Naltrexol pharmacokinetic profile in opioid-dependent population will be similar in non-opioid-dependent population. Plasma levels collected	0-8 hrs post dose

Secondary

Measure	Time frame
-6β-Naltrexol will have a lower potency in precipitating withdrawal and be better tolerated than Naloxone assessed by vital signs, objective/subjective ate Withdrawal Scales, Visual Analog Scales, Pupil Size and GI Motility measures	0-8 hrs post dose
6β-Naltrexol dose-dependent increases to reverse methadone-induced bowel dysfunction. Plasma levels and Hydrogen Breath Tests	0-8 hrs post dose

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026