Mechanism of Action & Dosing

Mechanism of Action

Strength of Balance from JYSELECA, a JAK1 preferential inhibitor1

JYSELECA regulates the JAK-STAT pathway by modulating the activity of JAK1-containing pairs1

In in vitro studies, JYSELECA preferentially inhibited JAK1 activity and demonstrated >5‑fold greater potency for JAK1-dependent signalling over JAK2, JAK3 and TYK21

In human cellular assays, JYSELECA preferentially inhibited JAK1/3, JAK1/2 and JAK1/TYK2‑mediated signalling, with functional selectivity over cytokine receptors that signal via pairs of JAK2 or JAK2/TYK21

The first generation JAK inhibitors are relatively non-selective.1-4 JYSELECA is a second generation JAK1 preferential inhibitor.1-6

The relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not currently known.

One tablet, once daily1

200 mg once daily1

Taken with MTX or as monotherapy1

100 mg dose available and recommended for:
  • patients with moderate or severe renal impairment (creatinine clearance 15 to <60 mL/min)1
  • as a starting dose for patients aged ≥75 years1
Please consult the Summary of Product Characteristics for full dosing particulars.

Please consult the Summary of Product Characteristics for full dosing particulars.

Considerations for initiation and monitoring of

patients on JYSELECA1


Additional considerations:

JYSELECA is contraindicated in patients1
  •   with hypersensitivity to the active substance or any of its excipients
  •   who have active tuberculosis or other active serious infections
  •   who are pregnant or trying to become pregnant
Women of childbearing potential should use effective contraception during and for at least 1 week after treatment with JYSELECA1
JYSELECA should not be used by women who are breast-feeding1
It is recommended that immunisations, including prophylactic zoster vaccinations, be updated in agreement with current immunisation guidelines prior to initiating JYSELECA treatment1
Galapagos has developed a Prescribing Guide to support healthcare professionals when
initiating and monitoring patients on JYSELECA. Contents include:
 
  • guide to initiation and monitoring
  • information for nurse specialists
  • details of patient support pack

Related Content


JYSELECA is indicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease modifying anti-rheumatic drugs (DMARDs).1 JYSELECA may be used as monotherapy or in combination with methotrexate (MTX).1

References: 1. JYSELECA SPC. Available at: www.medicines.org.uk / www.medicines.ie. Last accessed: November 2022. 2. Banerjee S, et al. Drugs 2017;77:521–546. 3. O’Shea JJ, et al. Nat Rev Rheumatol 2013;9(3):173–182. 4. Angelini J, et al. Biomolecules 2020;10(7):E1002. doi: 10.3390/biom10071002. 5. Traves  PG, et al. Ann Rheum Dis 2021;doi:10.1136/annrheumdis-2020-219012. 6. McInnes IB, et al. Arthr Res Ther 2019;doi.org/10.1186/s13075-019-1964-1.

UK-RA-JY-202203-00021  | Date of preparation December 2022