Qilu Pharmaceutical Submits China's First Application for Tofacitinib Citrate Extended-Release Tablets

Text | Jia Yi

On August 27, the CDE website showed that Qilu Pharmaceutical’s Class 3 generic drug “Tofacitinib Citrate Extended-Release Tablets” had its marketing application accepted (Acceptance Number: CYHS2000583), marking the first domestic filing for this dosage form.

Source: CDE Official Website

Tofacitinib Citrate is a prescription oral Janus kinase (JAK) inhibitor originally developed by Pfizer (brand name Xeljanz). It selectively inhibits JAK kinases, blocks the JAK/STAT pathway, and thereby suppresses cell signal transduction as well as related gene expression and activation. It is used to treat various immune-mediated diseases, including rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis.

The drug is available in three formulations: immediate-release tablets, extended-release tablets, and oral solution. The immediate-release tablet was first approved by the FDA for marketing in 2012, while the extended-release formulation received FDA approval in February 2016, becoming the first once-daily oral JAK inhibitor for the treatment of rheumatoid arthritis. In December 2019, the extended-release formulation gained approval for an additional indication: moderate to severe active ulcerative colitis (UC). Furthermore, Phase 3 clinical trials for plaque psoriasis have been completed, and six additional Phase 3 trials are currently underway, covering various indications such as active psoriatic arthritis and juvenile idiopathic arthritis. The long-acting nature of the extended-release tablets, requiring only once-daily dosing, facilitates better disease management for patients.

Since its market launch, its sales have grown year on year, reaching US$2.242 billion in 2019. In China, the tablet formulation was approved for marketing in March 2017 and was included in Category B of the National Reimbursement Drug List through price negotiations in 2019, with the latest successful bid price at RMB 26.79. However, due to the high technical barriers associated with extended-release formulations, this dosage form has not yet been marketed in China.

Source: Insight Database

According to the Insight database, in addition to the originator product, five generic versions of tofacitinib tablets from Chia Tai Tianqing, Qilu Pharmaceutical, Kelun Pharmaceutical, Yangtze River Pharmaceutical, and Nanjing Chia Tai Tianqing have been approved for marketing in China. However, for the extended-release tablet formulation, only the originator, Pfizer, submitted a marketing application on May 26. Qilu Pharmaceutical was the first domestic company to submit a marketing application for this formulation. Additionally, CSPC Ouyi is currently conducting bioequivalence (BE) trials.

JAK kinases play a crucial role in inflammation, and their inhibitors have demonstrated efficacy in treating certain inflammatory and autoimmune diseases. To date, seven JAK inhibitors have been approved globally, including LEO Pharma’s delgocitinib, Celgene’s fedratinib, AbbVie’s upadacitinib, Astellas’ peficitinib, Eli Lilly’s baricitinib, and Novartis’ ruxolitinib. However, among the aforementioned drugs, only tofacitinib, baricitinib, and ruxolitinib have been approved in China. We look forward to the early approval of Qilu Pharmaceutical’s “Tofacitinib Citrate Extended-Release Tablets” to benefit more patients.