Only CKD and Jeil have high-dose Xeljanz generics approved

in Korea

Higher dosage formulations have lower performance, concerns over safety are also an issue…most companies focus on developing low-dose generics

May release the generic versions after after patent expiry in November 2025

Pfizer

Jeil Pharm received approval for its ‘Topazan Tab 10mg,’ a high-dose generic version of the rheumatoid arthritis treatment ‘Xeljanz (tofacitinib citrate).’ With the Ministry of Food and Drug Safety’s approval of Topazan Tab 10mg on November 11 in addition to the Topazan Tab 5mg that was approved on November 27, Jeil Pharm now owns both low- and high-dose generic versions of Xeljanz.

 

Following Boryung, which received approval for ‘Boryung Tofacitinib TAb 5mg (tofacitinib aspartate) as the first Xeljanz generic in August 2020, 58 generics have been approved to date, but Chong Kun Dang is the only company that received approval for both the 5mg and 10mg doses.

 

Reasons include safety concerns and reduced indications associated with the higher dosage formulation, and even the outpatient prescription amount of the original shows this clear difference in demand between the low and high doses.

 

The low dose is approved for five indications including rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, polyarticular juvenile idiopathic arthritis (pJIA), and juvenile psoriatic arthritis, whereas the indication for the high dose formulation is limited to ulcerative colitis.

 

In addition, post-marketing surveillance studies of Xeljanz have shown that the drug is associated with an increased risk of blood clots in ulcerative colitis.

 

The MFDS also added a warning to the drug’s label in 2020, cautioning healthcare providers to evaluate the risk of thrombosis in patients with ulcerative colitis and to cautiously use Xeljanz 10mg in patients with risk factors for thrombosis.

 

With persisting safety concerns over the higher dose, according to the market research institution IQIVA, out of the KRW 15.9 billion sales of Xeljanz in 2021, the 5mg dose accounted for about KRW 13 billion, while the 10mg dose accounted for only a mere KRW 2.1 billion.

 

Meanwhile, Xeljanz owns a substance patent that expires in November 2025 and a crystalline patent that expires in November 2027.

 

20 companies, led by Chong Kun Dang, have tried to overcome it by filing an invalidation trial, and 16 companies including Boryung Pharmaceutical, have tried to avoid the patents by filing a passive scope of patent rights trial.

 

As a result, generic companies succeeded in avoiding Xeljanz’s patent in January 2018, and then won the invalidation trial in November 2019, thereby removing the crystalline patent from the green list in March 2020.

 

As a result, Xeljanz generics that are being granted marketing authorization will be launched after November 2025, when the substance patent expires.