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Updated: May 20, 2026

Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
[Janus kinase inhibitors]
E Ostermeier1, P Roll, H-P Tony
1Med. Klinik und Poliklinik II, Sektion Rheumatologie/Immunologie, Universitätsklinikum Würzburg, Oberdürrbacherstr. 6, 97080, Würzburg, Deutschland. Ostermeier_E@klinik.uni-wuerzburg.de
Abstract:
Janus protein tyrosine kinase (JAK) inhibitors are new therapeutic targets in the treatment of rheumatoid arthritis. Tofacitinib has shown good clinical efficacy in phase II and III studies with American College of Rheumatology (ACR) 20 response rates over 50% for monotherapy and in combination with methotrexate (MTX). Also the safety profile shows similar infection rates as observed with known biologicals. The crude rate of serious infection events was 3/100 patient-years. Often reported adverse events are infections of the upper respiratory tract and urogenital infections.
Insights
Janus kinase (JAK) inhibitors like tofacitinib show over 50% efficacy for rheumatoid arthritis treatment. Safety profiles are comparable to biologics, with common side effects including upper respiratory and urogenital infections.
Area of Science:
- Rheumatology
- Immunology
- Pharmacology
Context:
- Rheumatoid arthritis (RA) is a chronic autoimmune disease.
- Janus kinase (JAK) inhibitors represent a novel therapeutic class for RA.
- Tofacitinib is an oral JAK inhibitor.
Purpose:
- To evaluate the clinical efficacy and safety of tofacitinib in rheumatoid arthritis patients.
- To assess American College of Rheumatology (ACR) 20 response rates.
- To compare the safety profile of tofacitinib with existing biological therapies.
Summary:
- Tofacitinib demonstrated significant clinical efficacy in Phase II and III studies, achieving ACR20 response rates exceeding 50% in both monotherapy and combination with methotrexate (MTX).
- The safety profile of tofacitinib is comparable to established biological treatments for RA.
- The incidence of serious infections was low (3/100 patient-years), with common adverse events including upper respiratory tract and urogenital infections.
Impact:
- Tofacitinib offers a new oral treatment option for rheumatoid arthritis patients.
- The findings support JAK inhibitors as a viable therapeutic strategy for RA management.
- Understanding the safety profile, including common adverse events, is crucial for clinical practice.
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