Peficitinib: First Global Approval

  title={Peficitinib: First Global Approval},
  author={Anthony Markham and Susan J. Keam},
Peficitinib [Smyraf® (Astellas Pharma)] is a Janus kinase (JAK)1, JAK2, JAK3 and tyrosine kinase (Tyk)2 (pan-JAK) inhibitor recently approved in Japan for the treatment of rheumatoid arthritis. Inhibition of JAK suppresses the activation of cytokine signalling pathways involved in inflammation and joint destruction in rheumatoid arthritis. Peficitinib has been shown to significantly improve ACR20 and other measures of disease severity and to reduce the mean modified total Sharp score change… 
Peficitinib for the treatment of rheumatoid arthritis: an overview from clinical trials
Peficitinib has proven clinical efficacy in Asian patients (Japan, Korea, and Taiwan) with RA who have an inadequate response to conventional DMARDs, and further studies are necessary to determine its potential use in non-Asian populations.
JAK-Inhibitors for the Treatment of Rheumatoid Arthritis: A Focus on the Present and an Outlook on the Future
Their efficacy and safety profile are comparable or superior to those of biologic agents and JAKi proved to be efficacious when given as monotherapy.
Tyrosine kinase inhibitors for the treatment of rheumatoid arthritis: phase I to Ⅱ clinical trials
The response rates among RA patients to TKIs are diverse; genetic and environmental factors may be involved in the varying responses which are closely related to the pathogenesis of RA.
The rationale for targeting the JAK/STAT pathway in scleroderma-associated interstitial lung disease.
It is likely that the use of oral small molecule JAK-inhibitors, especially if prescribed early, may prevent or slow the progression of SSc-associated ILD, but few clinical studies currently support this hypothesis.
[Janus kinase inhibitors : State of the art in clinical use and future perspectives].
Arelatively new drug group of targeted synthetic disease-modifying antirheumatic drugs (tsDMARD) are JAK inhibitors (JAKi) and are a promising treatment approach for autoimmune diseases.
JAK3 inhibitors for the treatment of inflammatory and autoimmune diseases: a patent review (2016–present)
A comprehensive review of the available patent literature on JAK-family inhibitors published from 2016 to the present found that selective JAK3 inhibitors may offer valid, interesting, and promising therapeutic potential in inflammatory and autoimmune diseases.
Immunosuppressive agents for rheumatoid arthritis: a systematic review of clinical trials and their current development stage
The whole pipeline of immunosuppressive and immunomodulating drugs evaluated in RA is analysed and their mechanisms of action and stage of clinical development are described, with a total of 243 molecules in RA.
A pooled safety analysis of peficitinib (ASP015K) in Asian patients with rheumatoid arthritis treated over a median of 2 years
Peficitinib was well tolerated in Asian patients with RA over a median of 2 years, with no observed dose or temporal dependency for AEs with prolonged administration.


Efficacy and safety of the oral Janus kinase inhibitor peficitinib (ASP015K) monotherapy in patients with moderate to severe rheumatoid arthritis in Japan: a 12-week, randomised, double-blind, placebo-controlled phase IIb study
Treatment with peficitinib as monotherapy for 12 weeks in Japanese patients with moderate to severe RA is efficacious and showed acceptable safety profile, and these findings support further developments of pefindexinib for RA treatment.
AB0363 Coadministration of asp015k, a novel janus kinase inhibitor, with methotrexate demonstrates tolerability and lack of pharmacokinetic interactions in patients with rheumatoid arthritis
Coadministration of ASP015K and MTX was well tolerated in this short-term study, exhibiting no clinically significant effect on the PK profile of either drug.
Peficitinib, a JAK Inhibitor, in Combination With Limited Conventional Synthetic Disease‐Modifying Antirheumatic Drugs in the Treatment of Moderate‐to‐Severe Rheumatoid Arthritis
To evaluate the efficacy and safety of orally administered once‐daily peficitinib in combination with limited conventional synthetic disease‐modifying antirheumatic drugs (csDMARDs) in patients with
Peficitinib, a JAK Inhibitor, in the Treatment of Moderate‐to‐Severe Rheumatoid Arthritis in Patients With an Inadequate Response to Methotrexate
To evaluate the efficacy and safety of orally administered once‐daily peficitinib in combination with methotrexate (MTX) in patients with moderate‐to‐severe rheumatoid arthritis (RA) who had an
Pharmacokinetics, Pharmacodynamics, and Safety of ASP015K (Peficitinib), a New Janus Kinase Inhibitor, in Healthy Subjects
The most common adverse events (AEs) were neutropenia, headache, and abdominal pain; no serious AEs occurred; the safety findings at pharmacologically effective doses of ASP015K support further clinical development.
Drug Interactions Between Peficitinib, an Orally Administered, Once-Daily Janus Kinase Inhibitor, and Rosuvastatin in Healthy Subjects
Once-daily oral administration of peficitinib had no clinically significant effect on the pharmacokinetics of rosuvastatin, a probe substrate for OATP1B1.
The Effect of Verapamil, a P‐Glycoprotein Inhibitor, on the Pharmacokinetics of Peficitinib, an Orally Administered, Once‐Daily JAK Inhibitor
Overall, the most commonly reported adverse event was headache, which occurred in 5 subjects (21%); all reported adverse events were grade 1 severity, with the exception of 1 grade 2 incident of vomiting.
Smyraf® tablets 50 mg and 100 mg: prescribing information. 2019. https :// earch / iyaku Detai l/Resul tData SetPD F/80012
  • 2019
Astellas announces end of license agreement with Janssen to develop and commercialize ASP015K [media release
  • 2014