Drug intelligence / Profile preview

tocilizumab + methotrexate + folic acid

Development stage
Unknown
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Subcutaneous, Oral
01

Overview

This is a **combination therapy** consisting of **tocilizumab**, **methotrexate**, and **folic acid**, most commonly used in the management of **rheumatoid arthritis (RA)** and sometimes juvenile idiopathic arthritis (JIA). - **Tocilizumab** is a recombinant humanized monoclonal antibody that targets and inhibits the **interleukin-6 receptor (IL-6R)**, blocking IL-6-mediated pro-inflammatory signaling. - **Methotrexate** is a folate analog classified as a disease-modifying antirheumatic drug (DMARD), primarily inhibiting **dihydrofolate reductase** and thus DNA synthesis, leading to immunosuppressive and anti-inflammatory effects. - **Folic acid** is included to mitigate the adverse effects of methotrexate-induced folate deficiency, such as mouth ulcers and hematological toxicity. This combination is used particularly when methotrexate alone does not adequately control RA symptoms. Multiple randomized controlled trials and meta-analyses have shown that the addition of tocilizumab to methotrexate improves clinical response rates compared to methotrexate alone, although the combination is associated with increased risk of transaminase elevations and certain adverse events. Folic acid does not contribute to disease-modifying efficacy but is recommended to improve treatment tolerability[1][3][4][5][6].

02

Targets

ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)IL-6R (Interleukin-6 receptor subunit alpha)DHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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