Other substances

Methotrexate

An antimetabolite dihydrofolate reductase inhibitor.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

Supporting references

Contradictory references

AI-suggested references

Clinical trials

General information

Methotrexate is an antimetabolite dihydrofolate reductase inhibitor (therefore a purine biosynthesis inhibitor). It is used as an immunosuppressor and a antineoplastic agent (NCIt).

Methotrexate on DrugBank
Methotrexate on PubChem
Methotrexate on Wikipedia

Synonyms

4‐amino‐10‐methyl folic acid; MTX

Marketed as

ABITREXATE; ALLTREX; ARTRAIT; ATREXEL; BENDATREXAT; CARDITREX; DERMOTREX; EBETREX; EMTEXATE; LEDERTREXATE; MAXTREX; MEISUSHENG; MEXATE; METOJECT; NORDIMET; OTREXUP; RASUVO; REDITREX; RHEUMATREX; TREXALL; TREXAN; ZEXATE

CN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)O)C(=O)O

Supporting references

Link	Tested on	Impact factor	Notes	Publication date
Reversal of Infected Host Gene Expression Identifies Repurposed Drug Candidates for COVID-19 Preprint	VERO E6 cell cultures			Apr/09/2020
Methotrexate inhibits SARS‐CoV‐2 virus replication “in vitro” Small molecule In vitro	Vero E6 cells, SARS-CoV-2 strain with EBI n. PRJEB38101	2.02	Inhibits SARS-CoV-2 at post-entry stage in vitro in concentration used for established human therapies (in a dose-dependent manner).	Sep/14/2020
Methotrexate inhibits SARS‐CoV‐2 virus replication “in vitro” Small molecule In vitro	Vero E6 cells, SARS-CoV-2 strain with EBI n. PRJEB38101	2.02	Inhibits SARS-CoV-2 at post-entry stage in vitro in concentration used for established human therapies (in a dose-dependent manner).	Sep/14/2020

AI-suggested references

Link	Publication date
Two-week methotrexate discontinuation in patients with rheumatoid arthritis vaccinated with inactivated SARS-CoV-2 vaccine: a randomised clinical trial.	Feb/22/2022
Increment of immunogenicity after third dose of a homologous inactivated SARS-CoV-2 vaccine in a large population of patients with autoimmune rheumatic diseases.	Jan/27/2022
Accelerated waning of immunity to SARS-CoV-2 mRNA vaccines in patients with immune mediated inflammatory diseases.	May/07/2020
Pausing methotrexate improves immunogenicity of COVID-19 vaccination in elderly patients with rheumatic diseases.	Jan/04/2023
Antibody response to BNT162b2 SARS-CoV-2 mRNA vaccine in adult patients with systemic sclerosis.	Jun/08/2020
Methotrexate significantly reduces the humoral vaccination response against SARS-CoV-2 in older but not younger patients with rheumatoid arthritis	Mar/02/2021
A prospective multicenter study assessing humoral immunogenicity and safety of the mRNA SARS-CoV-2 vaccines in Greek patients with systemic autoimmune and autoinflammatory rheumatic diseases.	Oct/28/2021
BNT162b2 vaccine-induced humoral and cellular responses against SARS-CoV-2 variants in systemic lupus erythematosus	May/18/2020
Effectiveness of SARS-CoV-2 vaccination in patients with rheumatoid arthritis (RA) on DMARDs: as determined by antibody and T cell responses	Mar/04/2022
Mitoxantrone dihydrochloride, an FDA approved drug, binds with SARS-CoV-2 NSP1 C-terminal.	Feb/16/2022
Repurposing Methotrexate in Dampening SARS-CoV2-S1-Mediated IL6 Expression: Lessons Learnt from Lung Cancer	Sep/03/2021
The folate antagonist methotrexate diminishes replication of the coronavirus SARS-CoV-2 and enhances the antiviral efficacy of remdesivir in cell culture models	Apr/19/2021
JAK Inhibition as a New Treatment Strategy for Patients with COVID-19	Aug/04/2021
Comparative Anti-Inflammatory Effects of Salix Cortex Extracts and Acetylsalicylic Acid in SARS-CoV-2 Peptide and LPS-Activated Human In Vitro Systems	Jun/23/2021
Immunogenicity of BNT162b2 mRNA SARS-CoV-2 vaccine in patients with psoriatic arthritis on TNF inhibitors	Jul/01/2022

Clinical trials

ID	Title	Status	Phase	Start date	Completion date
NCT04352465	Efficacy and Safety of MTX-loaded Nanoparticles to Treat Severe COVID-19 Patients	Not yet recruiting	Phase 1\|Phase 2	May/01/2020	Nov/30/2020
Alternative id - LDE-MTX_COVID19 Interventions - Drug: Methotrexate Study type - Interventional Study results - No Results Available Locations - Prevent Senior Private Operadora de Saúde LTDA., São Paulo, Brazil Study designs - Allocation: Non-Randomized\|Intervention Model: Sequential Assignment\|Masking: None (Open Label)\|Primary Purpose: Treatment Enrollment - 42 Age - 18 Years and older (Adult, Older Adult) Outcome measures - Change in clinical conditions\|Change of Clinical symptoms - respiratory rate\|Hypoxia\|Changes of blood oxygen\|Inflammatory parameters\|Evolution of Acute Respiratory Syndrome\|Hospital discharge\|ICU discharge\|Rate of mortality

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