UG3DA061645
Cooperative Agreement
Overview
Grant Description
Advancing a non-addictive, peripherally acting opioid analgesic as a medication strategy to prevent opioid use disorder in patients undergoing treatment for pain - in 2021, ~52 million U.S. adults experienced chronic pain.
Opioids, commonly prescribed for chronic pain, can lead to opioid use disorder (OUD), with about 25% of patients using prescription opioids becoming addicted and transitioning to more dangerous substances like heroin and synthetic opioids such as fentanyl.
In response, opioid prescriptions have been limited to prevent OUD, but this has often led to inadequate pain relief and a surge in illicit drug use.
The optimum strategy for preventing OUD involves the development of an effective analgesic that treats chronic pain usually managed by conventional opioids without the risk of addiction.
Thus, a molecule that can reduce pain by acting on peripheral opioid receptors while avoiding central nervous system (CNS) opioid receptor involvement, including addiction, is critically needed.
Dimerx, Inc. has developed DMX-101 (CAS NO: 1820753-68-1), an innovative non-addictive analgesic exclusively targeting peripheral opioid receptors while sparing CNS involvement.
DMX-101 is synthesized by the covalent cross-linking of two dihydrogenated buprenorphine molecules to form a dimer.
DMX-101 acts on peripheral opioid receptors and does not affect the CNS because it does not cross the blood-brain barrier.
Therefore, DMX-101 can deliver the strong pain management effects of opioids while avoiding the negative side effects.
Previous clinical trials of DMX-101 treatment of diarrhea-prominent irritable bowel syndrome, which involves visceral pain, showed beneficial effects of the drug without signs or symptoms of CNS opioid engagement, addiction, or withdrawal effects.
We hypothesize that DMX-101 will ameliorate chronic pain without the inadvertent effects of opioid analgesia, including addiction and hyperalgesia.
This UG3/UH3 project aims to rigorously evaluate DMX-101's safety and efficacy through various phases.
The UG3 phase encompasses three aims that also meet FDA requirements: (1) assess the abuse liability potential of DMX-101 in rats, (2) demonstrate that DMX-101 does not bind to CNS opioid receptors in rats, and (3) evaluate toxicity in dogs.
Successful completion of these aims, including no signs of abuse potential, no CNS receptor occupancy, and confirmation of safety and tolerability, will transition the project to the UH3 phase.
This phase includes conducting two Phase 1 studies on the safety, pharmacokinetics, and pharmacodynamics of twice-daily dosing of DMX-101 in healthy adults and DMX-101's abuse liability in otherwise healthy, non-dependent, recreational opioid users to show the drug's safety profile, dosage parameters, and non-addictive nature.
Successful completion of this project will support future large-scale Phase 2 clinical studies of the effectiveness of DMX-101 in individuals with chronic pain.
The company will also support the program through private financing.
The successful development and clinical approval of DMX-101 would have a profound impact on public health, offering a viable solution to manage chronic pain without contributing to the escalating opioid crisis.
Opioids, commonly prescribed for chronic pain, can lead to opioid use disorder (OUD), with about 25% of patients using prescription opioids becoming addicted and transitioning to more dangerous substances like heroin and synthetic opioids such as fentanyl.
In response, opioid prescriptions have been limited to prevent OUD, but this has often led to inadequate pain relief and a surge in illicit drug use.
The optimum strategy for preventing OUD involves the development of an effective analgesic that treats chronic pain usually managed by conventional opioids without the risk of addiction.
Thus, a molecule that can reduce pain by acting on peripheral opioid receptors while avoiding central nervous system (CNS) opioid receptor involvement, including addiction, is critically needed.
Dimerx, Inc. has developed DMX-101 (CAS NO: 1820753-68-1), an innovative non-addictive analgesic exclusively targeting peripheral opioid receptors while sparing CNS involvement.
DMX-101 is synthesized by the covalent cross-linking of two dihydrogenated buprenorphine molecules to form a dimer.
DMX-101 acts on peripheral opioid receptors and does not affect the CNS because it does not cross the blood-brain barrier.
Therefore, DMX-101 can deliver the strong pain management effects of opioids while avoiding the negative side effects.
Previous clinical trials of DMX-101 treatment of diarrhea-prominent irritable bowel syndrome, which involves visceral pain, showed beneficial effects of the drug without signs or symptoms of CNS opioid engagement, addiction, or withdrawal effects.
We hypothesize that DMX-101 will ameliorate chronic pain without the inadvertent effects of opioid analgesia, including addiction and hyperalgesia.
This UG3/UH3 project aims to rigorously evaluate DMX-101's safety and efficacy through various phases.
The UG3 phase encompasses three aims that also meet FDA requirements: (1) assess the abuse liability potential of DMX-101 in rats, (2) demonstrate that DMX-101 does not bind to CNS opioid receptors in rats, and (3) evaluate toxicity in dogs.
Successful completion of these aims, including no signs of abuse potential, no CNS receptor occupancy, and confirmation of safety and tolerability, will transition the project to the UH3 phase.
This phase includes conducting two Phase 1 studies on the safety, pharmacokinetics, and pharmacodynamics of twice-daily dosing of DMX-101 in healthy adults and DMX-101's abuse liability in otherwise healthy, non-dependent, recreational opioid users to show the drug's safety profile, dosage parameters, and non-addictive nature.
Successful completion of this project will support future large-scale Phase 2 clinical studies of the effectiveness of DMX-101 in individuals with chronic pain.
The company will also support the program through private financing.
The successful development and clinical approval of DMX-101 would have a profound impact on public health, offering a viable solution to manage chronic pain without contributing to the escalating opioid crisis.
Awardee
Funding Goals
NOT APPLICABLE
Grant Program (CFDA)
Awarding / Funding Agency
Place of Performance
Mill Valley,
California
949413719
United States
Geographic Scope
Single Zip Code
Related Opportunity
Analysis Notes
Amendment Since initial award the total obligations have increased 110% from $1,593,126 to $3,349,522.
Dimerx was awarded
Non-Addictive Opioid Analgesic for Chronic Pain Management
Cooperative Agreement UG3DA061645
worth $3,349,522
from National Institute on Drug Abuse in July 2025 with work to be completed primarily in Mill Valley California United States.
The grant
has a duration of 2 years and
was awarded through assistance program 93.279 Drug Abuse and Addiction Research Programs.
The Cooperative Agreement was awarded through grant opportunity Development of Medications to Prevent and Treat Opioid and/or Stimulant Use Disorders and Overdose (UG3/UH3 - Clinical Trial Optional).
Status
(Ongoing)
Last Modified 6/5/26
Period of Performance
7/1/25
Start Date
6/30/27
End Date
Funding Split
$3.3M
Federal Obligation
$0.0
Non-Federal Obligation
$3.3M
Total Obligated
Activity Timeline
Transaction History
Modifications to UG3DA061645
Additional Detail
Award ID FAIN
UG3DA061645
SAI Number
UG3DA061645-7057040
Award ID URI
SAI UNAVAILABLE
Awardee Classifications
Small Business
Awarding Office
75N600 NIH National Insitute on Drug Abuse
Funding Office
75N600 NIH National Insitute on Drug Abuse
Awardee UEI
HPE8WDLFMG25
Awardee CAGE
None
Performance District
CA-02
Senators
Dianne Feinstein
Alejandro Padilla
Alejandro Padilla
Modified: 6/5/26