A Phase 2 Trial of Leflunomide for the Treatment of COVID‐19 in Patients with Solid Tumors and Hematologic Malignancies

NIH RePORTER · NIH · P30 · $440,000 · view on reporter.nih.gov ↗

Abstract

Novel interventions are urgently needed to address the COVID-19 pandemic, especially for highrisk populations. Leflunomide is a dihydroorotate dehydrogenase (DHODH) inhibitor, impacting pyrimidine synthesis for DNA and RNA production, and has been in use for over 20 years for treatment of autoimmune diseases such as rheumatoid arthritis and lupus with an excellent safety profile [1, 2]. It has known anti-viral activity and has been applied against cytomegalovirus (CMV) and polyoma BK virus infections in immunocompromised hosts [3, 4]. Leflunomide is orally available and exhibits hepatic clearance and a long elimination half-life. In vitro and in vivo experiments conducted in Wuhan, China demonstrated DHODH inhibitors have activity against COVID-19, including teriflunomide, the active metabolite of leflunomide [5]. Moreover, our preliminary data at City of Hope also suggest that leflunomide significantly arrests viral RNA replication in cancer cells infected with a naturally-occurring RNA virus (reovirus) and impairs ex vivo IL-6 expression in virally infected peripheral blood mononuclear cells (PBMCs).

Key facts

NIH application ID
10160080
Project number
3P30CA033572-37S2
Recipient
BECKMAN RESEARCH INSTITUTE/CITY OF HOPE
Principal Investigator
STEVEN Terry ROSEN
Activity code
P30
Funding institute
NIH
Fiscal year
2020
Award amount
$440,000
Award type
3
Project period
1997-08-01 → 2022-11-30