# Development of CP-analogs as novel treatments for opioid use disorder.

> **NIH NIH R44** · SPARIAN BIOSCIENCES, INC. · 2021 · $319,223

## Abstract

ABSTRACT
Opioid use disorder (OUD) is a chronic disorder characterized by the repeated, compulsive use
of opioid drugs with a detrimental impact to one's physical, social, and psychological wellbeing.
The use of prescription opiates is often necessary to control moderate to severe levels of pain.
However, about 10% of patients prescribed an opiate for a medical condition are at risk for
developing OUD. Opiate Use Disorder is a global problem but is at crisis levels in the U.S with
significant mortality. It is estimated in this country that about ~11M misuse opioids, ~2M people
have OUD and close to 50K died from opioid related overdoses. At Sparian, we have
assembled a comprehensive team of accomplished scientists, key clinical opinion leaders, and
pharmaceutical industry experts across critical disciplines including translational research,
medicinal chemistry, CMC, toxicology and clinical trials in an effort to develop an oral, potent,
and selective small molecules for the treatment of OUD. Mitragyna speciosa, a plant
commonly known as Kratom, is commonly used in the US as a self-remidy to treat opiate
withdrawal and OUD. We have identified and synthesized a distinct new chemical entity based
on Kratom named 9-methoxy corynantheidine pseudoindoxyl (9CP). 9CP has a different
receptor binding profile and different pharmacology than mitragynine. 9CP is both a potent a
MOR agonist and delta antagonist. In acute dosing studies it attenuates precipitated
withdrawal, it is not rewarding, does not cause physical dependence, and has limited respiratory
depression and tolerance. Our Fast Tract proposal aims to take an innovative pharmacological
approach to develop orally active, highly potent and selective 9CP analogs, devoid of unwanted
side effects, for the treatment of OUD with a better pharmacotherapeutic profile than either
methadone or buprenorphine. It is organized into two coordinated phases that employ a
succinct experimental plan and a focused drug development approach. In phase 1, we will use
an in vitro and in vivo screening paradigm to select one lead molecule and 5-8 backup
molecules with suitable drug-like properties. In phase 2, we will progress the selected lead and
confirm our choice though exploratory safety and toxicology studies, while also characterizing
our backup compounds to better understand our template mitigating risk. In summary, we
propose a novel strategy to develop a new class of agents with potential to provide better
therapy for OUD.

## Key facts

- **NIH application ID:** 10255890
- **Project number:** 1R44DA053846-01
- **Recipient organization:** SPARIAN BIOSCIENCES, INC.
- **Principal Investigator:** Jeffrey Reich
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $319,223
- **Award type:** 1
- **Project period:** 2021-08-01 → 2022-09-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10255890

## Citation

> US National Institutes of Health, RePORTER application 10255890, Development of CP-analogs as novel treatments for opioid use disorder. (1R44DA053846-01). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10255890. Licensed CC0.

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