Pfizer's Once-Daily Extended-Release JAK Inhibitor Tofacitinib Approved in China for Rheumatoid Arthritis

By | Pharma Observer

On September 13, Pfizer announced that China’s National Medical Products Administration (NMPA) has officially approved the marketing application for its oral JAK inhibitor, tofacitinib citrate extended-release tablets, for adult patients with moderately to severely active rheumatoid arthritis (RA) who have had an inadequate response to or are intolerant of methotrexate, to be used in combination with methotrexate or other non-biologic disease-modifying antirheumatic drugs (DMARDs).

Tofacitinib is an oral JAK inhibitor that acts on the JAK pathway to block intracellular signaling associated with inflammation in moderate to severe active rheumatoid arthritis. Pfizer introduced tofacitinib to China in 2017 (brand name: Xeljanz). The approved recommended dosage for its immediate-release formulation is 5 mg twice daily.

Bioequivalence studies comparing the extended-release (XR) and immediate-release (IR) formulations of tofacitinib demonstrate that the area under the curve (AUC) and peak plasma concentration (Cmax) of tofacitinib XR 11 mg once daily are comparable to those of tofacitinib IR 5 mg twice daily. When administered with a high-fat meal, the AUC remains unchanged, indicating that clinical efficacy is not affected by food intake. Additionally, real-world data show significantly improved medication adherence with the tofacitinib XR formulation compared to the IR formulation.

Furthermore, data from the US CORRONA registry demonstrate no significant difference in the primary endpoint of achieving the minimal clinically important difference (MCID) in Clinical Disease Activity Index (CDAI) improvement between the extended-release and immediate-release formulations of tofacitinib. The extended-release formulation of tofacitinib (11 mg orally once daily) offers convenient dosing, reduces dosing frequency, improves patient adherence, and effectively improves disease activity.

Rheumatoid arthritis is a chronic inflammatory autoimmune disease that can cause a range of symptoms, including joint pain and swelling, particularly in the hands, feet, and knee joints. When patients fail to adhere to regular follow-up schedules, it may readily lead to treatment interruption, disease relapse, or exacerbation, thereby significantly impacting the long-term prognosis of the disease.

The approval of Pfizer’s 11 mg extended-release tofacitinib formulation provides a new treatment option for patients with rheumatoid arthritis. Its once-daily oral dosing regimen is expected to improve medication convenience and patient adherence.

References:

[1] Pfizer's Innovative Rheumatoid Arthritis Drug Tofacitinib Citrate Extended-Release Tablets Approved in China. Retrieved July 12, 2021, from https://mp.weixin.qq.com/s/gGI3LnZj5M2dx7sJ1ldQeQ

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