From the Guidelines
Tofacitinib is a Janus kinase inhibitor, which is a class of drug that interrupts the Janus kinase/signal transduction pathway. This class of medication is used to treat various inflammatory conditions, including rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis, as approved by the FDA 1. The mechanism of action of tofacitinib involves blocking the activity of JAK enzymes, which are involved in signaling pathways that trigger inflammation in the body. Some key points about tofacitinib include:
- It has shown beneficial effects in psoriasis, although it is not currently approved for this indication 1
- It is available in oral formulations, including immediate-release and extended-release tablets, as well as an oral solution
- The dosing regimen varies depending on the condition being treated, with rheumatoid arthritis typically requiring 5 mg twice daily or 11 mg once daily
- JAK inhibitors, including tofacitinib, carry boxed warnings for serious infections, malignancy, major adverse cardiovascular events, and thrombosis, so regular monitoring is essential during treatment 1. Tofacitinib's efficacy and safety have been demonstrated in multiple large phase III clinical trials, including the Oral treatment Psoriasis Trial (OPT) Pivotal 1 and OPT Pivotal 2, which investigated its use in psoriasis 1.
From the FDA Drug Label
Tofacitinib is a Janus kinase (JAK) inhibitor. The class of drug that tofacitinib belongs to is a Janus kinase (JAK) inhibitor 2.
- Key points:
- Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.
- It inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations.
From the Research
Classification of Tofacitinib
- Tofacitinib is classified as a Janus kinase (JAK) inhibitor 3, 4, 5.
- It is a disease-modifying antirheumatic drug (DMARD) that preferentially inhibits Janus kinase (JAK) 1 and JAK3 3.
- Tofacitinib is the first approved drug in a new class of DMARDs, the JAK inhibitors 4.
Mechanism of Action
- Tofacitinib works by selectively inhibiting JAKs, which have a pivotal role in triggering cytokine-induced signal transduction pathways that influence normal and pathological cellular processes of haematopoiesis and immune cell function 4.
- The inhibition of JAKs by tofacitinib potentially modulates inflammatory processes and provides a novel approach for the treatment of rheumatoid arthritis (RA) 4.