# Arylepoxamides: A new class of potent, safer analgesics

> **NIH NIH UG3** · SLOAN-KETTERING INST CAN RESEARCH · 2021 · $329,534

## Abstract

Project Summary:
This supplemental funding application proposes to address unforeseen, yet solvable issues which
arose in the development of SBS-1000 which is being funded by the parent grant DA048379-01 entitled
“Arylepoxamides: A new class of potent, safer analgesics.” The parent UG3 grant provides funding for
CMC development and IND-enabling toxicology studies for SBS-1000 and the UH3 funds phase 1
clinical trials. SBS-1000 is a novel analgesic acting through a newly discovered target – the AEAr. In
preclinical studies, SBS-1000 has demonstrated potent analgesia across nociceptive, neuropathic, and
inflammatory pain models and has not demonstrated respiratory depression, abuse liability, or physical
dependence.
The initial scale up API synthesis, purification and formulation development proved challenging for
Patheon/Thermo Fisher and resulted in unrecognized process impurities and a formulation that
required a strong buffer and low pH. The combination of the impurities, acidic formulation, and an
aggressive dosing paradigm at Charles River Labs lead to spurious results in the 7-day non-GLP rat
toxicology study. These results were inconsistent with the MTD rat and dog studies, the 7-day non-
GLP dog study, and 8 years of prior data accumulated from academic and industry sponsored research.
Re-examination of the API and formulation indicate that the toxicity was a result of the vehicle and
experimental design rather than the drug itself. This application proposes to specifically address these
unforeseen events and develop a new purification method, optimize the formulation, and repeat the 7-
day non-GLP rat toxicology study. We are confident that these aims are achievable given that we have
already made progress in a purification method, have generated preliminary data on a new formulation,
and have decided on a different dosing paradigm for the rat tox study. The supplemental funding we
are requesting is critical to complete this work and address the unforeseen CMC and tox issues. The
remaining funding in the parent grant is all allocated for the GMP manufacturing and GLP studies which
will be required to meet the UG3 milestone and for IND submission. Beyond the complications outlined
in this application there have been no drug-related issues to preclude the successful development of
SBS-1000 from either the exploratory tox work, MTD studies, the 7-day non- GLP dog study, or any of
the in vitro assays.
NOTE: MP1000 = SBS-1000
 - MP1000 was laboratory name used in original grant application. SBS-1000 the new name from Sparian Biosciences

## Key facts

- **NIH application ID:** 10291187
- **Project number:** 3UG3DA048379-02S1
- **Recipient organization:** SLOAN-KETTERING INST CAN RESEARCH
- **Principal Investigator:** YING-XIAN PAN
- **Activity code:** UG3 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $329,534
- **Award type:** 3
- **Project period:** 2020-12-15 → 2021-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10291187

## Citation

> US National Institutes of Health, RePORTER application 10291187, Arylepoxamides: A new class of potent, safer analgesics (3UG3DA048379-02S1). Retrieved via AI Analytics 2026-05-25 from https://api.ai-analytics.org/grant/nih/10291187. Licensed CC0.

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