# Arylepoxamides: A new class of potent, safer analgesics

> **NIH NIH UG3** · SLOAN-KETTERING INST CAN RESEARCH · 2020 · $3,182,170

## Abstract

The expansion of opioid prescribing in recent years to better treat pain has markedly increased
their usage and availability and fueled an epidemic of abuse. Estimates of up to 80% of addicts
reported initiating their habit through prescriptions drugs. Decreasing opioid prescriptions would
lower opioid exposure with fewer people receiving the drugs and less drug available for
diversion. We have identified a novel target in brain distinct from any of the traditional opioid
receptors capable of mediating potent analgesia without the reward behavior and side-effects
seen with traditional opioids. We have targeted this site with a series of arylepoxamides and
have identified a clinical candidate (MP1000) and backup compound. MP1000 is a potent
analgesic in a range of thermal, inflammatory and neuropathic analgesic assays. It fails to show
reward behavior and does not produce respiratory depression at doses 5-fold greater than its
analgesic ED50. Chronic administration does not produce physical dependence or withdrawal
when challenged with an antagonist. It shows no cross tolerance to morphine and can be co-
administered to subjects already on opioids for pain to lower their opioid usage (i.e. ‘opioid
sparing), facilitating the eventual discontinuation of the opioid. Preliminary safety and toxicology
studies are encouraging, and, based upon these results we are proposing to carry out IND-
enabling studies and a Phase 1 clinical trial.

## Key facts

- **NIH application ID:** 9833507
- **Project number:** 5UG3DA048379-02
- **Recipient organization:** SLOAN-KETTERING INST CAN RESEARCH
- **Principal Investigator:** YING-XIAN PAN
- **Activity code:** UG3 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $3,182,170
- **Award type:** 5
- **Project period:** 2018-12-15 → 2021-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9833507

## Citation

> US National Institutes of Health, RePORTER application 9833507, Arylepoxamides: A new class of potent, safer analgesics (5UG3DA048379-02). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/9833507. Licensed CC0.

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