Approval Date

Feb. 13, 2009


Release Date

Mid-March 2009



TakedaPharmaceuticals North America, Inc.



A xanthineoxidase inhibitor



Once-daily,oral medication for the treatment of hyperuricemia associated with gout.


Active Ingredient



Agency Roster



Marketing Strategy/Execution

Experts recognize that managingserum uric acid (sUA) to a target level of less than 6.0 mg/dL is the key tomanaging hyperuricemia in patients with gout. ULORIC is the first new treatmentoption for patients with hyperuricemia and gout in more than 40 years. Thefocus at launch will be to increase awareness of this disease, including theimportance of managing sUA to less than 6.0 mg/dL. Physician educationmaterials will illustrate that ULORIC lowered sUA to the target level betterthan existing therapies, and it also has an established safety profilerequiring no dose adjustments in patients with mild-to-moderate renal orhepatic impairment. Educational resources and adherence programs will beavailable to support patients seeking information on gout, hyperuricemia andULORIC.


Physician Outlook

Uloric(febuxostat) is entering a relatively crowded marketplace for the chronicmanagement of hyperuricemia.  Yet,physicians will likely welcome Uloric given its new mechanism of action and norequired dose adjustment in renal (or hepatic) impairment.   Impaired renal function is a seriousco-morbidity for some gout patients and allopurinol, a lead product in thechronic gout market, has risks for this patient population.     


– GeoffPenney, Vice President, GfK Healthcare


Also in the Pipeline (courtesy ofAdis R&D Insight)

Nocompetitor compounds in phase III or pre-registration, US.


Recent MM&M Coverage

Product news

Peoplenews from the 01/16/07 news brief



Gout is achronic condition characterized by attacks, or “flares,” that are marked byintense pain, redness, swelling and heat in the affected joint. These symptomsare caused by the buildup of uric acid which crystallizes and deposits underthe skin and in joints. Gout is the most common inflammatory arthritispresented in men over 40 years of age.


Febuxostatexerts its therapeutic effect by blocking the enzyme xanthine oxidase. Xanthineoxidase is responsible for the breakdown of the purine base, hypoxanthine, toxanthine and subsequently to uric acid. By blocking this enzyme, febuxostathelps to prevent the production of uric acid, thereby reducing the elevatedlevels of serum uric acid.


Clinical Trials

Threerandomized, double-blind, controlled clinical studies evaluated the efficacy ofdaily treatment with febuxostat compared to that of allopurinol 300mg daily, orplacebo in 3402 patients with hyperuricemia and gout. Hyperuricemia was definedas a baseline serum uric acid level =8mg/dL. In all 3 studies, patients alsoreceived naproxen 250mg twice daily or colchicine 0.6mg once or twice daily forgout flare prophylaxis.


The primaryefficacy endpoint was the proportion of patients with a serum uric acid level<6mg/dL at the final visit. Febuxostat 40mg demonstrated comparable efficacyto allopurinol in lowering serum uric acid to <6mg/dL at the final visit;whereas febuxostat 80mg demonstrated superior efficacy. Of the patients treatedwith febuxostat 80mg, 76% achieved a serum uric acid level <6mg/dL by week 2and 83% of these patients maintained average serum uric acid levels of<6mg/dL throughout the treatment period.


Adverse Reactions

Liverfunction abnormalities, nausea, arthralgia, rash, gout flares.



=18yrs:initially 40mg once daily; if serum uric acid is not <6mg/dL after 2 weeks,may increase to 80mg once daily. Gout flare prophylaxis, with an NSAID orcolchicine, upon initiation of therapy and for up to 6 months, is recommended.



<18yrs:not recommended.



Concomitantazathioprine, mercaptopurine, theophylline.



Notrecommended for treating asymptomatic hyperuricemia. Cardiovascular events:monitor for signs and symptoms of MI and stroke. Severe renal impairment orESRD on dialysis. Severe hepatic impairment. Monitor liver function at 2 and 4months after initiation and periodically thereafter. Obtain target serum uricacid levels <6mg/dL after 2 weeks of initiating therapy. Secondaryhyperuricemia (eg, Lesch-Nyhan syndrome, malignant disease, or in organtransplant recipients): not recommended. Pregnancy (Cat.C). Nursing mothers.



SeeContraindications. Potentiates xanthine oxidase substrate drugs.