# Predevelopment of VV2003, a Novel CRAC Channel Inhibitor, to Improve Outcomes Associated with Checkpoint Inhibitor Immunotherapy

> **NIH NIH R44** · VIVREON BIOSCIENCES, LLC · 2020 · $249,806

## Abstract

Vivreon Biosciences, LLC NCI Phase 2 SBIR Submission 1R43CA224454-02
Project Summary
Vivreon Biosciences is pleased to apply for NCI’s Phase 2 SBIR. Vivreon Biosciences is an
innovative life sciences company that is developing a novel small molecule, Ca2+ channel inhibitor,
VV2003, to improve outcomes in persons undergoing checkpoint inhibitor immunotherapy.
Checkpoint inhibitors have improved overall survival in numerous cancers, but enterocolitis has
emerged as the most frequent dose-limiting toxicity associated with these therapies. Checkpoint
inhibitor induced colitis is currently treated with immunosuppressive therapy, which blunts the
tumor-killing potential of the checkpoint inhibitor immunotherapy. VV2003 is an oral candidate
therapeutic designed to selectively and safely block checkpoint inhibitor-induced enterocolitis
without systemic immunosuppression side effects.
Vivreon seeks NCI funding to bridge the gap between discovery and development. This grant
aims to further validate VV2003 as a safe and effective candidate therapeutic by answering key
questions regarding VV2003 pharmacokinetics and efficacy prior to advancing VV2003 into full
Investigational New Drug (IND)-enabling studies and into first in human clinical evaluation. Upon
successful completion of the program, our preclinical candidate will be the first to specifically
inhibit Ca2+ release-activated Ca2+ (CRAC) channels for immunosuppression targeted specifically
to sites of enterocolitis. Leukocyte CRAC channels facilitate Ca2+ influx, a process that is
upstream of numerous enterocolitis disease-causing processes including leukocyte proliferation
and inflammatory cytokine secretion. VV2003 has low systemic bioavailability and remains in the
gut lumen following oral administration. This permits VV2003 to achieve colon-restricted
immunosuppression, avoiding unwanted systemic side effects. We have developed several
strategies to confirm that VV2003 can be used in combination with multiple checkpoint inhibitor
immunotherapies, including in vitro and in vivo checkpoint inhibitor immunotherapy efficacy
assays. The final aim for this proposal is characterization and testing of the first CRAC channel
inhibitor to address enterocolitis associated with checkpoint immunotherapy.

## Key facts

- **NIH application ID:** 10242974
- **Project number:** 3R44CA224454-02S2
- **Recipient organization:** VIVREON BIOSCIENCES, LLC
- **Principal Investigator:** Milton L Greenberg
- **Activity code:** R44 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $249,806
- **Award type:** 3
- **Project period:** 2018-03-02 → 2021-01-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10242974

## Citation

> US National Institutes of Health, RePORTER application 10242974, Predevelopment of VV2003, a Novel CRAC Channel Inhibitor, to Improve Outcomes Associated with Checkpoint Inhibitor Immunotherapy (3R44CA224454-02S2). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10242974. Licensed CC0.

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