Hospital Pharmacy - November 2017 - 668

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Hospital Pharmacy 52(10)

Table 1. Janus Kinase Inhibitors.
Generic name

Sponsor

JAK inhibition

Tofacitinib

Pfizer Inc

JAK 1, 2, 3
inhibitor

Baricitinib

Eli Lily and Company;
Incyte Corporation

JAK 1, 2 inhibitor

Filgotinib

Galapagos NV;
Gilead Sciences

JAK 1 inhibitor

Upadacitinib

AbbVie Inc

JAK 1 inhibitor

Comments
Approved for use in rheumatoid arthritis. In the Phase III Oral-Sync trial,
tofacitinib demonstrated improvements in PtGA, Pain, HAQ DI, all 8 SF36 domains, FACIT-F, and MOS Sleep at 3 months.4
An NDA was submitted in January 2016, but review has been delayed
pending submission of additional clinical data on safety and dosing.
Baricitinib is approved in Europe for RA. In a trial of 684 rheumatoid
arthritis patients who had had an inadequate response to methotrexate,
62% of patients treated with baricitinib achieved ACR20 response at
week 52 compared with 39%, with placebo.5
In the 12-week, 594 rheumatoid arthritis patient, dose ranging, Phase
II DARWIN-1 trial, 69-74% of filgotinib treated patients achieved an
ACR20 response compared with 44%, with placebo.6
Topline results were announced for SELECT-NEXT, a 662 patient, Phase
III trial in patients with moderate-to-severe RA. Upadacitinib doses
demonstrated ACR20 response rates of 64%, and 66% in the 15 mg and
30 mg compared with 36% in the placebo group at 12 weeks.

Source. Information adapted from the Prescribe Right Pharmaceutical Pipeline Tracker database.7
Note. JAK = Janus kinase; ORAL-Sync = Oral Rheumatoid Arthritis Phase 3 TriaLs-Syncronized; PtGA = Patient Global Assessment; HAQ DI = Health
Assessment Questionnaire-Disability Index; SF-36 = Short Form Health Survey; FACIT-F = Functional Assessment of Chronic Illness Therapy-Fatigue; MOS
= Medical Outcome Study; NDA = New Drug Application; RA = rheumatoid arthritis; ACR20 = American College of Rheumatology 20% response rate.

as traditional DMARDs. In addition, Phase III trials using filgotinib and upadacitinib, specific JAK 1 inhibitors, are currently underway. JAK inhibitors are novel therapies for RA,
but further studies are needed to determine their risk-benefit
ratio and selection of the most appropriate patients for such
therapy.4 The cost of JAK inhibitors per year average around
the same price as a TNFi. Drug administration time and convenience are greatly saved with JAK inhibitors because of the
oral administration. Due to the promising findings of JAK
Inhibitors, they are expected to represent the next generation
compounds for treating RA.

References
1.

Authors' Note
Information is summarized from selected materials; additional
information may be available from other sources. Due to the preapproval nature of the information, non-peer-reviewed data may be
utilized. The information provided is meant to provide a way to
assess the development status of a new drug and should not be used
in making patient care decisions.

Declaration of Conflicts of Interest

The author(s) declared no potential conflicts of interest with respect
to the research, authorship, and/or publication of this article.

Funding
The author(s) received no financial support for the research, authorship, and/or publication of this article.

Singh JA, Saag KG, Bridges SL, et al. 2015 American College
of Rheumatology guideline for the treatment of rheumatoid
arthritis. Arthritis Care Res. 2015;68(1):1-25. doi:10.1002/
acr.22783.
Rheumatoid Arthritis Support Network. Rheumatoid arthritis
treatment costs. https://www.rheumatoidarthritis.org/treatment/costs/. Accessed June 10, 17.
Nakayamada S, Kubo S, Iwata S, et al. Recent progress in JAK
inhibitors for the treatment of rheumatoid arthritis. BioDrugs.
2016;30(5):407-419.
Strand V, Kremer JM, Gruben D, et al. Tofacitinib in combination with conventional disease-modifying antirheumatic drugs
in patients with active rheumatoid arthritis: patient-reported
outcomes from a phase III randomized controlled trial. Arthritis
Care Res. 2017;69(4):592-598. doi:10.1002/acr.23004
Dougados M, Van HD, Chen YC, et al. Baricitinib in patients
with inadequate response or intolerance to conventional synthetic DMARDs: results from the RA-BUILD study. Ann Rheum
Dis. 2017;76(1):88-95. doi:10.1136/annrheumdis-2016-210094.
Vanhoutte F, Mazur M, Voloshyn O,et al. Filgotinib (GLPG0634/
GS-6034), an oral JAK1 selective inhibitor, is effective in combination with methotrexate (MTX) in patients with active rheumatoid arthritis and insufficient response to MTX: results from
a randomised, dose-finding study (DARWIN 1). Annals of the
Rheumatic Diseases. 2017;76:998-1008.
Prescribe Right. Pharmaceutical Pipeline Tracker. 2017. http://
www.prescriberight.com/pharmaceutical-pipeline-tracker.
html. Accessed July 28, 2017.

https://www.rheumatoidarthritis.org/treatment/costs/ https://www.rheumatoidarthritis.org/treatment/costs/ http://www.prescriberight.com/pharmaceutical-pipeline-tracker.html http://www.prescriberight.com/pharmaceutical-pipeline-tracker.html http://www.prescriberight.com/pharmaceutical-pipeline-tracker.html

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