Bold Therapeutics Potential to Fight COVID-19.

The global COVID-19 pandemic has highlighted the need for novel antiviral strategies, and the extreme urgency of situation suggests that repurposing existing therapeutics (particularly those with an established safety profile and a scalable manufacturing processes) is the most efficient development strategy. Bold Therapeutics’ lead asset, BOLD-100, is a novel antiviral strategy for COVID-19 that is optimally placed for rapid clinical deployment.


Bold Therapeutics’ BOLD-100 is a first-in-class anti-resistance small molecule therapeutic currently in clinical development for some of the most difficult-to-treat cancer indications. BOLD-100 is currently in clinical trials for the treatment of gastrointestinal cancers.

BOLD-100 targets GRP78, an important protein that is utilized by viruses, including coronaviruses, to enter host cells and replicate. The literature supports that BOLD-100 will have potent antiviral activity, including against COVID-19.

Bold Therapeutics is currently working with a leading group of COVID-19 experts and collaborators to develop BOLD-100. We are currently seeking development partners and/or institutional investors interested in rapidly moving this unique solution into clinical trials.

Antiviral Development Rationale

  • GRP78 is used by viruses, including coronaviruses, to both enter cells and for viral replication.
    • Recent modeling work suggests that COVID-19 can bind to GRP78.
  • Consequently, therapies that downregulate GRP78 should have antiviral utility.
    • Example 1: Blocking antibodies against GRP78 have shown efficacy in reducing viral loads in both Japanese Encephalitis Virus and Dengue Virus.
    • Example 2: Inhibiting GRP78 expression with either epigallocatechin gallate (EGCG) or siRNA decreased viral transcript production in models of Ebola.
  • Bold Therapeutics’ own preclinical work has repeatedly shown that BOLD-100 selectively decreases GRP78 expression in stressed cells.
  • Collectively, these data support exploring BOLD-100 as a novel therapy for COVID-19.


  • International consortium of COVID-19 experts from 6 different universities currently investigating BOLD-100 as an antiviral treatment for COVID-19.
  • Clinical-stage product with an established safety profile.
    • Successfully completed a Phase 1 monotherapy dose-escalation study in 41 patients with advanced cancer with a tolerable safety profile (minimal neurological or hematological effects).
  • Already acceptable to regulators.
    • Open IND in the U.S.
    • Recent (Dec 2019) approval by Health Canada for additional combination studies.
  • Ample cGMP drug product.
    • Packaged for clinical use and available for immediate shipment.
  • Intellectual property filed.
  • The above characteristics enable potentially rapid clinical progression.

Immediate COVID-19 Partnership and/or Targeted Investment

Robust worldwide patent protection

Extensive worldwide patent protection including composition of matter, method of use (including antiviral), and manufacturing process through mid to late 2030s.

Confidential data room already set up for due diligence

Including preclinical antiviral results, COVID-19 scientific rationale/plan, and phase I oncology results.

Potential for near-term Breakthrough Therapy Designation (BTD)

COVID-19 is a life-threatening condition with limited approved therapies.

BOLD-100 is a unique antiviral approach for COVID-19.

Flexible on deal economics and structure.


Investors/Business Development

E. Russell McAllister
President and Chief Executive Officer
[email protected]

Clinical Development

Jim Pankovich
Executive Vice President, Clinical Development
[email protected]


Ha DP, Van Krieken R, Carlos AJ, Lee AS. The stress-inducible molecular chaperone GRP78 as potential therapeutic target for coronavirus infection. J Infect. 2020;S0163-4453(20)30398-4. doi:10.1016/j.jinf.2020.06.017

Ibrahim IM, Abdelmalek DH, Elshahat ME, Elfiky AA. COVID-19 spike-host cell receptor GRP78 binding site prediction [published online ahead of print, 2020 Mar 10]. J Infect. 2020;S0163-4453(20)30107-9. doi:10.1016/j.jinf.2020.02.026

Chu H, Chan CM, Zhang X, et al. Middle East respiratory syndrome coronavirus and bat coronavirus HKU9 both can utilize GRP78 for attachment onto host cells. J Biol Chem. 2018;293(30):11709–11726. doi:10.1074/jbc.RA118.001897

Ibrahim IM, Abdelmalek DH, Elfiky AA. GRP78: A cell's response to stress. Life Sci. 2019;226:156–163. doi:10.1016/j.lfs.2019.04.022

Reid SP, Shurtleff AC, Costantino JA, et al. HSPA5 is an essential host factor for Ebola virus infection. Antiviral Res. 2014;109:171–174. doi:10.1016/j.antiviral.2014.07.004

Siu KL, Chan CP, Kok KH, Woo PC, Jin DY. Comparative analysis of the activation of unfolded protein response by spike proteins of severe acute respiratory syndrome coronavirus and human coronavirus HKU1. Cell Biosci. 2014;4(1):3. Published 2014 Jan 13. doi:10.1186/2045-3701-4-3

Minakshi R, Padhan K, Rani M, Khan N, Ahmad F, Jameel S. The SARS Coronavirus 3a protein causes endoplasmic reticulum stress and induces ligand-independent downregulation of the type 1 interferon receptor. PLoS One. 2009;4(12):e8342. Published 2009 Dec