Pfizer's first-in-class JAK inhibitor pricey for rheumatoid arthritis market

  title={Pfizer's first-in-class JAK inhibitor pricey for rheumatoid arthritis market},
  author={Ken Garber},
  journal={Nature Biotechnology},
  • K. Garber
  • Published 9 January 2013
  • Medicine
  • Nature Biotechnology
On November 6, two weeks ahead of deadline, the US Food and Drug Administration (FDA) approved the first Janus kinase (JAK) inhibitor for rheumatoid arthritis. With the approval, New York based Pfizer’s smallmolecule Xeljanz (tofacitinib) is poised to test the multibillion dollar rheumatoid arthritis market, currently dominated by tumor necrosis factor alpha (TNF) inhibitors. In clinical trials, Xeljanz showed similar efficacy to TNF inhibitors and a comparable safety profile. As a pill, it has… 

JAK Inhibitors in Rheumatoid Arthritis: An Evidence-Based Review on the Emerging Clinical Data

This narrative review article aims to synthesise and distil the key available trial data on JAK inhibitor efficacy and safety, along with their place in the ACR and European League Against Rheumatism guidelines for RA, to determine which is most efficacious and which has the most favourable safety profile.

Clinical utility of the oral JAK inhibitor tofacitinib in the treatment of rheumatoid arthritis

Tofacitinib is an oral JAK inhibitor that is now available and effective in RA treatment, as shown in multiple Phase II and Phase III clinical trials, however, long-term safety data and comparisons with other disease-modifying antirheumatic drugs and small molecule inhibitors are necessary to better determine the role of tofacitinIB in RA.

Setback for JAK2 inhibitors

The first results of an in-house program to try and elucidate the mechanism of why fedratinib was causing Wernicke’s encephalopathy indicate that it is not a class effect of JAK inhibitors, and Incyte expects to submit the results of its structural analysis of different JAK inhibitor for publication in the next month or two.

Selective Tyk2 inhibitors as potential therapeutic agents: a patent review (2015–2018)

This review sought to give an overview of patents related to small molecule selective Tyk2 inhibitors published from 2015 to 2018 to prove valid, interesting, and promising within the therapeutic paradigm.

EULAR recommendations for the management of rheumatoid arthritis with synthetic and biological disease-modifying antirheumatic drugs: 2013 update

The 2010 European League against Rheumatism recommendations for the management of rheumatoid arthritis (RA) with synthetic and biological disease-modifying antirheumatic drugs (sDMARDs and b DMARDs, respectively) have been updated and are intended to improve outcome in patients with RA.

Advances in treating psoriasis in the elderly with small molecule inhibitors

Apremilast, ruxolitinib, and peficitinib are effective agents with favorable side effect profiles; however, physicians should exercise caution when prescribing tofacitinib or baricitinIB in elderly populations due to adverse events.

Covalent Janus Kinase 3 Inhibitors

Current research efforts culminated in the development of PF-06651600, a phase II clinical candidate from Pfizer under investigation for the treatment of rheumatoid arthritis, inflammatory bowel disease, and alopecia areata, and paved the way for the in-depth examination of JAK3-dependent signaling in cells and in vivo.

New pathogenic insights into rheumatoid arthritis

Recent discoveries, particularly those which have attempted to integrate genome-wide association studies (GWAS) with biological pathways and cell types known to play a role in disease pathology, are reviewed in order to expand current understanding of the pathogenesis of RA.

From Science to Success? Targeting Tyrosine Kinase 2 in Spondyloarthritis and Related Chronic Inflammatory Diseases

Seminal studies uncovering the basic science of TYK2 have provided sound foundations for targeting it in SpA and related inflammatory diseases, and novel selectiveTYK2 inhibitors may well be the next blockbuster therapeutic for SpA.

Generation of a chemical genetic model for JAK3

It is reported here that mutating this cysteine to serine does not prevent JAK3 catalytic activity but does greatly increase the IC50 for covalent JAK2 inhibitors, and provides a chemical-genetic model to study Jak3 function.



Pfizer's JAK inhibitor sails through phase 3 in rheumatoid arthritis

  • K. Garber
  • Biology, Medicine
    Nature Biotechnology
  • 2011
467 JAK inhibitors like tofacitinib tread a fine line between therapeutic down-modulation of autoimmunity and outright immunosuppression. (Tofacitinib was first conceived as an immunosuppressant for

Tofacitinib or adalimumab versus placebo in rheumatoid arthritis.

In patients with rheumatoid arthritis receiving background methotrexate, tofacitinib was significantly superior to placebo and was numerically similar to adalimumab in efficacy.