Exploratory Evaluation of [11C]-NOP46

Exploratory Evaluation of [11C]-NOP46 Pharmacokinetics With Positron Emission Tomography (PET)

This is an open-label, single center design. In the first stage, five (5) healthy individuals will receive a microdose (10µg) of [11C]-NOP46, immediately followed by whole body positron emission tomography (PET)/computed tomography (CT) to determine dosimetry and perform an initial safety evaluation of the radiotracer. If no toxicities develop, then the investigation will move to the second stage, in which thirty (30) patients with chronic pain will receive a microdose of [11C]-NOP46 followed by PET/CT of region of interests.

Study Overview

• Status: Completed
• Conditions: Chronic Pain
• Intervention / Treatment: Drug: [11C]-NOP46; Radiation: PET/CT scan

Detailed Description

Pain is a natural response to injury. Pain lets us know there may be damage to our bodies. Pain is the way our body tells us that we must take care of ourselves. Chronic pain is different. Chronic pain is pain that lasts for a long time. Chronic pain can last for weeks, months, and even years. In some cases chronic pain remains without any sign of body damage. Today, there is no way for a doctor to measure someone's chronic pain or accurately determine many details about chronic pain. The investigators at Columbia University are interested in new imaging test that could help doctors look at chronic pain and help patients with chronic pain. The new imaging test uses a new drug called [11C]-NOP46. [11C]-NOP46 is a radioactive drug and is experimental. It is not approved by the Food and Drug Administration (FDA). The investigators believe that, when given to patients, this new drug can go to the exact places of chronic pain within the body. Once the drug goes to the places of chronic pain, a special camera, called a Positron Emission Tomography (PET) camera, can be used to take pictures of the drug. In this study, the investigators will give [11C]-NOP46 to up to 35 subjects.

• Study Type: Interventional
• Enrollment (Actual): 10
• Phase: Early Phase 1

Contacts and Locations

Study Locations

• United States
  • New York
    • New York, New York, United States, 10032
      • Columbia University Irving Medical Center

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 90 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• All subjects must be 18 years of age or older, able to read, understand, and voluntarily sign an informed consent document.

For Healthy Volunteers:

• Volunteers must have no current medical history of sustained pain from a focal injury.
• Negative pregnancy test if female of childbearing potential.
• Women of child-bearing potential and men must agree to use adequate contraception (hormonal or barrier method of birth control; abstinence) prior to study entry and for the duration of study participation.

Patients with Focal Pain:

• Subjects must have current pain from a focal injury for which they are under a physician's care.
• Subjects must have moderate to severe pain, defined as >4 on the Visual Analogue Scale
• Subjects must have a negative pregnancy test if female of childbearing potential.
• Women of child-bearing potential and men must agree to use adequate contraception (hormonal or barrier method of birth control; abstinence) prior to study entry and for the duration of study participation.

Exclusion Criteria:

• Participants with evidence of diffuse pain at the time of enrollment up to agent administration are to be excluded from this study.
• Inability to discontinue pain medication(s) for 48 hours prior to agent administration.(Enrolled participants who have taken pain medication within 48 hours of agent administration may be either withdrawn from the study or rescheduled at the PI's discretion).
• Concomitant medication use (including suspected illicit drugs use) that, in the judgment of the investigator, would make the participant inappropriate for enrollment.
• Severe concurrent disease, infection, or medical co-morbidity that, in the judgment of the investigator, would make the participant inappropriate for enrollment.
• Participants who are receiving any other investigational agents.
• Women who are pregnant or breastfeeding.
• Subjects who are unable to tolerate PET/CT imaging.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: Non-Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Healthy Volunteers; In Stage 1, five healthy volunteers will receive a microdose of [11C]-NOP46 and undergo serial whole body PET/CT scans for up to 240 minutes post-administration. These image sets will be used to evaluate [11C]-NOP46 biodistribution and derive dosimetry estimates.	Drug: [11C]-NOP46; Subjects will receive a microdose (≤10 µg) of [11C]-NOP46.; Radiation: PET/CT scan; After subjects receive a microdose of [11C]-NOP46, whole body PET/CT scan(s) will be performed to determine dosimetry and perform an initial safety evaluation of the radiotracer in Stage 1 and region of interests in Stage 2.
Experimental: Individuals with Focal Pain; In Stage 2, up to 30 subjects with focal pain will receive a microdose of [11C]-NOP46 and undergo PET/CT scans for up to 60 minutes in length. The results of Stage 1 will inform the scanning parameters (uptake period, scan length, reconstruction parameters, etc.) for Stage 2.	Drug: [11C]-NOP46; Subjects will receive a microdose (≤10 µg) of [11C]-NOP46.; Radiation: PET/CT scan; After subjects receive a microdose of [11C]-NOP46, whole body PET/CT scan(s) will be performed to determine dosimetry and perform an initial safety evaluation of the radiotracer in Stage 1 and region of interests in Stage 2.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Uptake ratio for site with pain is >1	The uptake ratio for the site with pain to the site without pain is greater than 1 in the focal pain subjects	48 hours post-scan

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Occurrence of Physiologic Effects of Single Micro-dose of [11C]-NOP46	Total number of physiologic effects associated with a single micro-dose administration of [11C]-NOP46	48 hours post-scan

Collaborators and Investigators

• Sponsor: Columbia University
• Investigators: Principal Investigator: Akiva Mintz, MD, PhD, Columbia University

Publications and helpful links

General Publications

• Centers for Disease Control and Prevention (CDC). Vital signs: overdoses of prescription opioid pain relievers---United States, 1999--2008. MMWR Morb Mortal Wkly Rep. 2011 Nov 4;60(43):1487-92.
• Voscopoulos C, Lema M. When does acute pain become chronic? Br J Anaesth. 2010 Dec;105 Suppl 1:i69-85. doi: 10.1093/bja/aeq323.
• Jamison RN, Serraillier J, Michna E. Assessment and treatment of abuse risk in opioid prescribing for chronic pain. Pain Res Treat. 2011;2011:941808. doi: 10.1155/2011/941808. Epub 2011 Oct 11.
• Pike VW. PET radiotracers: crossing the blood-brain barrier and surviving metabolism. Trends Pharmacol Sci. 2009 Aug;30(8):431-40. doi: 10.1016/j.tips.2009.05.005. Epub 2009 Jul 16.

Helpful Links

• Centers for Disease Control and Prevention (2011). Prescription painkiller overdoses in the U.S.

Study record dates

Study Major Dates

• Study Start (Actual): March 25, 2019
• Primary Completion (Actual): October 30, 2023
• Study Completion (Actual): October 30, 2023

Study Registration Dates

• First Submitted: October 10, 2018
• First Submitted That Met QC Criteria: October 10, 2018
• First Posted (Actual): October 15, 2018

Study Record Updates

• Last Update Posted (Actual): April 13, 2025
• Last Update Submitted That Met QC Criteria: April 9, 2025
• Last Verified: April 1, 2025

More Information

Terms related to this study

• Keywords: [11C]-NOP46
• Additional Relevant MeSH Terms: Pain; Neurologic Manifestations; Chronic Pain
• Other Study ID Numbers: AAAQ8138

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO
• IPD Plan Description: Final data analysis and conclusion will be submitted to scientific journals and made available for publication.

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No