●  SK chemicals, introducing the new gout drug, FEBURIC®

SK chemicals(CEO, Chang-Geun Kim) announced on September 26 that it will launch FEBURIC® 80mg(general name: Febuxostat 80mg), a novel drug for treating gout-hyperuricemia developed by Teijin Pharma Limited in Japan, in Korea.
 
FEBURIC® is a highly potent xanthine oxidase inhibitor(XOI) from Teijin Pharma in Japan. This novel drug lowers the level of uric acid, which is associated with the occurrence of gout, by inhibiting xanthine oxidase, an enzyme that generates uric acid from xanthine.

FEBURIC® shows superior affinity and selectivity with xanthine oxidase compared to the conventional gout medicine allopurinol, so it is able to lower the level of uric acid up to the target range and ensure the lowered level affirmatively without influencing the metabolism of **purine compounds. 

Furthermore, FEBURIC® can effectively decrease uric acid level in patients who overproduce or underexcrete uric acid. Unlike conventional therapies, it has attracted academic attention for its unique feature, namely that it can be also administered safely to patients with mild to intermediate renal insufficiency without any need to adjust the dose.

Dr. Song Yeonguk, a professor in Seoul who led the bridging study of FEBURIC® in Korea, said, “In this randomized, controlled confirmative study, conducted in ten university hospitals, involving 182 patients with gout showing a uric acid level of ≥ 8.0mg/dL, the difference in the uric acid level at the end of the study from that of the baseline in the group of administered with 80mg of Febuxostat was 80%, while the difference in the group of administered with 300mg of Allopurinol was 58%. The efficacy endpoints between the two groups were found to be significantly different.”

In terms of safety, the adverse event rate in the 80mg Febuxostat treatment group(19.44%) was similar to that of the placebo treatment group(16.22%), while twice as many patients in the 300mg Allopurinol treatment group(35.14%) experienced adverse events, indicating that the potent anti-gout drug Febuxostat can be used safely.
 
The EMA(European Medicines Agency, the regulatory authority in the EU for pharmaceutical products) approved the marketing authorization of FEBURIC® from Ipsen France in April 2008. Following its first approval in the EU, it was also approved by the FDA(Food and Drug Administration, the regulatory authority in the U.S.A.) and the KFDA(Korea Food and Drug Administration, the regulatory authority in South Korea) in February and June 2009, respectively.

Generally ***allopurinol and ****benzbromarone were used to treat gout and hyperuricemia, which are mainly caused by the overproduction of uric acid or a decrease in the excretion of uric acid through the kidney.

Allopurinol, which was developed 43 years ago, remained the first choice for gout treatment despite its potential for critical adverse events such as allopurinol hypersensitivity syndrome (AHS).

In particular, use of the drug entails dose adjustment for patients with renal impairment, while limitations on the use of a high dosage treatment prevent the intensive treatment of those with an uncontrolled uric acid level. Therefore, quite a large percentage of gout patients have actually had to rely on symptomatic therapy using anti-inflammatory painkillers, including NSAIDs.

Gout is a condition characterized by inflammation resulting from the deposition of uric acid crystals in the joints or surrounding tissue, mainly affecting men aged 40-50. According to Statistics Korea, gout occurs in 3 out of every 100 men aged 40 years old or older, and the rate of incidence is increasing.

Its main symptoms include erythema, swelling, and episodic bouts of severe pain - mainly in the metatarsophalageal joint, ankles, foot pads, elbows and so forth. Gout can be a serious disease, leading to deformation of the affected joints and kidney dysfunction in its later stages.

With a more than 10% annual increase in its rate of incidence due to many Koreans’ increasingly westernized diet and the increase in the elderly population, the market for gout treatments is expected to continue growing.

Mr. Choi Nakjong, head of the marketing team at the Life Science Biz of SK chemicals, said, “Though the number of gout patients in Korea has been increasing steadily, they do not have many options for treating their condition because no new treatment has been made available for a long time. FEBURIC® will offer a new opportunity for effective treatment to the patient and we will lead them to this new treatment actively.”

<Terminology>

*Xanthine Oxidase Inhibitor (XOI)
: XOI refers to drugs which lower the level of uric acid, which is responsible for the patient’s development of gout, by inhibiting xanthine oxidase, a kind of enzyme that generates uric acid from xanthine (a kind of purine base in the human body).

**Purine compounds: Purines including adenine, gunine and so forth are components of DNA, RNA and ATP (the energy source utilized by cells). They can be increased by genetic factors, disease, drugs and so forth, and excreted as uric acid, the final metabolite.

***Allopurinol (Brand name: Zyloric, Sam Il Pharm.)
: Allopurinol is a drug that lowers the level of uric acid in the blood by inhibiting uric acid production. It has long been used as the drug of choice for lowering the level of uric acid in gout patients, but it entails dosage adjustment for those with renal impairment due to the potential risk of serious adverse events, the most typical of which is Allopurinol Hypersensitivity Syndrome (AHS).

 ****Benzbromarone (Hanlim Pharm. Co.): Benzromarone may be selected after Allopurinol as the second drug of choice for patients suffering from AHS or for patients whose level of uric acid cannot be controlled with Allopurinol. It can be administered to patients with mild to intermediate symptoms, but its use is highly limited due to its hepatic toxicity.

*****Allopurinol Hypersensitivity Syndrome (AHS)
: AHS is a very rare hyper skin reaction among patients treated with Allopurinol. The risk is higher in patients with renal impairment, and may be fatal, causing death in as many as 25% of patients who experience AHS.