Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Label indication ULORIC is a xanthine oxidase (XO) inhibitor indicated for the chronic management of hyperuricemia in adult patients with gout who have an inadequate response to a maximally titrated dose of allopurinol, who are intolerant to allopurinol, or for whom treatment with allopurinol is not advisable. FDA label
Also known as Febuxostat XR, TMX-67, Uloric, Tei-6720
Febuxostat · 12 trials · 7 indications
Major adverse cardiovascular events (MACE) were defined as a composite of cardiovascular (CV) death, non-fatal myocardial infarction (MI), nonfatal stroke and unstable angina with urgent coronary revascularization; these events were adjudicated by an independent cardiovascular endpoints committee.
Major adverse cardiovascular events (MACE) were defined as a composite of cardiovascular (CV) death, non-fatal myocardial infarction (MI), nonfatal stroke and unstable angina with urgent coronary revascularization; these events were adjudicated by an independent cardiovascular endpoints committee.
The percentage of subjects whose serum urate level was \<6.0 mg/dL at the Final Visit was summarized. The Final Visit was the last visit at which a serum urate value was collected.
Serum urate values were obtained at the Month 1 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 1 visit was summarized.
Serum urate values were obtained at the Month 12 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 12 visit was summarized.
Serum urate values were obtained at the Month 24 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 24 visit was summarized.
Serum urate values were obtained at the Month 36 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 36 visit was summarized.
The percentage of subjects whose serum urate was \<6.0 mg/dL at the last visit on treatment was summarized. The last visit on treatment was the last visit at which a serum urate value was collected prior to any changes in drug and/or dose from the initial treatment assignment.
Each subject's serum urate at the last 3 visits determined the subject's response for the primary efficacy variable. A subject who prematurely discontinued without least 3 postbaseline serum urate levels was considered a nonresponder; if at least 3 serum urate were obtained postbaseline, those 3 visits were used. The last 3 visits used may have differed for each subject.
Each subject's serum urate at the last 3 visits determined the subject's response for the primary efficacy variable. A subject who prematurely discontinued without least 3 postbaseline serum urate levels was considered a nonresponder; if at least 3 serum urate were obtained postbaseline, those 3 visits were used. The last 3 visits used may have differed for each subject.
The change in 24-hour mean SBP measured at final visit or Week 6 relative to baseline. Ambulatory blood pressure monitoring measures blood pressure at regular intervals throughout the day and night. The 24-hour mean is the average of all measurements recorded for 24 hours after dosing.
Renal function was assessed by measuring the change from Baseline in serum creatinine. Analyses were conducted by the Central Laboratory.
The single affected joint was defined as the joint with the history of the first acute gout flare. Radiographs (X-rays) of this single joint in the hands or feet were evaluated using the modified Sharp/van der Heijde method. Each erosion was assessed using a 4-point scale where 0=no erosions (best) to 3=large erosion passing the mid-line (worst). Individual erosion scores were summed to a maximum erosion score of 5 for joints in the hands and 10 for joints in the feet. Higher scores indicated more joint damage. A negative change from Baseline indicated improvement.
The change from Baseline to Month 6 in 24-hour urine uric acid is expressed as a percentage of the Baseline uUA value.
Serum urate values were obtained at the Month 6 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 6 visit was summarized.
Serum urate values were obtained at the Month 12 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 12 visit was summarized.
Serum urate values were obtained at the Month 18 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 18 visit was summarized.
Serum urate values were obtained at the Month 24 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 24 visit was summarized.
Serum urate values were obtained at the Month 36 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 36 visit was summarized.
Serum urate values were obtained at the Month 48 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 48 visit was summarized.
Serum urate values were obtained at the Month 60 visit. The percentage of subjects whose serum urate was \<6.0 mg/dL at the Month 60 visit was summarized.
The percentage of subjects whose serum urate was \<6.0 mg/dL at the final visit was summarized. The final visit was the last visit at which a serum urate value was collected.
Serum urate values were obtained at the Day 28 visit. The percentage of subjects whose serum urate decreased to \<6.0 mg/dL at the Day 28 visit was summarized.
Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. Participant blood samples were collected pre-dose and following a single oral dose.
Maximum observed plasma concentration (Cmax) is the peak plasma concentration of a drug after administration, obtained directly from the plasma concentration-time curve. Participant blood samples were collected pre-dose and following a single oral dose.
AUCt is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration. Participant blood samples were collected pre-dose and following a single oral dose.
AUCt is a measure of total plasma exposure to the drug from Time 0 to Time of the Last Quantifiable Concentration (AUCt) Participant blood samples were collected pre-dose and following a single oral dose.
AUCinf is a measure of total plasma exposure to the drug from time zero extrapolated to infinity. Participant blood samples were collected pre-dose and following a single oral dose.
AUCinf is a measure of total plasma exposure to the drug from time zero extrapolated to infinity. Participant blood samples were collected pre-dose and following a single oral dose.
| Arm | Type | Description |
|---|---|---|
| Febuxostat | EXPERIMENTAL | Febuxostat 40 mg (or 80 mg beginning on week 4 if serum uric acid level was ≥6.0 mg/dL), tablets, orally, once daily for up to approximately 82 months. |
| Allopurinol | ACTIVE_COMPARATOR | Allopurinol 300 mg to 600 mg (increased in 100 mg increments each month until serum uric acid was \<6.0 mg/dL), tablets, orally, once daily for up to approximately 83 months to participants with mildly impaired renal function or normal renal function (estimated creatinine clearance \[eCLcr\] ≥60 mL/min) or allopurinol 200 mg to 400 mg (increased in 100 mg increments each month until serum uric acid was \<6.0 mg/dL), tablets, orally, once daily for up to approximately 83 months to participants with moderately impaired renal function (eCLcr ≥30 but \<60 mL/min). |
| Febuxostat 40 mg QD | EXPERIMENTAL | - |
| Febuxostat 80 mg QD | EXPERIMENTAL | - |
| Allopurinol 200 mg or 300 mg QD | ACTIVE_COMPARATOR | (dependent on renal function) |
| Febuxostat 120 mg QD | EXPERIMENTAL | - |
| Allopurinol QD | ACTIVE_COMPARATOR | - |
| Febuxostat 240 mg QD | EXPERIMENTAL | - |
| Placebo QD | PLACEBO_COMPARATOR | - |
| Allopurinol 300 mg QD | ACTIVE_COMPARATOR | - |
| Placebo | PLACEBO_COMPARATOR | Placebo-matching capsules, orally, twice daily for up to 12 months. |
| Febuxostat 30 mg BID | EXPERIMENTAL | Febuxostat 30 mg, capsules, orally, twice daily (BID) for up to 12 months. |
| Febuxostat 40/80 mg QD | EXPERIMENTAL | Participants initially received febuxostat 40 mg, capsules, once daily (QD) and one placebo-matching capsule QD and remained on this dose for up to 12 months if their serum urate (sUA) was \<6.0 mg/dL at the Day 14 visit. Participants whose sUA was ≥6.0 mg/dL at the Day 14 visit received febuxostat 80 mg, capsule, QD, and one placebo-matching capsule QD at the Month 1 visit, and for the remainder of the study. |
| Febuxostat 40 mg or 80 mg | EXPERIMENTAL | Febuxostat 40 mg or 80 mg (based on serum urate levels at Day 14), capsules, orally, once daily for up to 24 Months. |
| 1 | EXPERIMENTAL | - |
| 2 | EXPERIMENTAL | - |
| 3 | EXPERIMENTAL | - |
| Treatment Sequence ABC | EXPERIMENTAL | Febuxostat extended release (XR) 80 mg, capsules, orally, once on Day 1 of Period 1 after a high-fat meal, followed by a 7-day washout period, followed by febuxostat XR 40 mg, capsules, orally, once on Day 1 of Period 2 after a 10-hour fast, followed by a 7-day washout period, followed by febuxostat XR 80, capsules, orally, once on Day 1 of Period 3 after a 10-hour fast. |
| Treatment Sequence BCA | EXPERIMENTAL | Febuxostat XR 40 mg, capsules, orally, once on Day 1 of Period 1 after a 10-hour fast, followed by a 7-day washout period, followed by febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 2 after a 10-hour fast, followed by a 7-day washout period, followed by Febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 3 after a high-fat meal. |
| Treatment Sequence CAB | EXPERIMENTAL | Febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 1 after a 10-hour fast, followed by a 7-day washout period, followed by febuxostat XR 80 mg, capsules, orally, once on Day 1 of Period 2 after a high-fat meal, followed by a 7-day washout period, followed by febuxostat XR 40 mg, capsules, orally, once on Day 1 of Period 3 after a 10-hour fast. |
| Name | Type | Description |
|---|---|---|
| Febuxostat | DRUG | Febuxostat tablets |
| Allopurinol | DRUG | Allopurinol tablets |
| Placebo | DRUG | Placebo, orally, once daily for up to 28 weeks. |
| Placebo for Febuxostat | DRUG | Febuxostat placebo-matching capsules |
| Febuxostat XR | DRUG | Febuxostat XR capsules |
Inclusion Criteria: 1. The participant or the participant's legally acceptable representative signs and dates a written, informed consent form/Health Insurance Portability and Accountability Act (HIPAA) Authorization prior to the initiation of any study procedures. 2. The participant is male ≥50 ye...
Top 4 of 19 competitors
| Company | Ticker | Trials | Lead Phase | Drugs |
|---|---|---|---|---|
| United Therapeutics Corporation | UTHR | 1 | PHASE3 | Ralinepag |
| Roivant Sciences Ltd. | ROIV | 3 | PHASE3 | Mosliciguat |
| Eli Lilly and Company | LLY | 1 | PHASE3 | Lepodisiran |
| Illumina, Inc. | ILMN | 1 | PHASE1 | 18F-mFBG for administration |
Febuxostat is a small molecule drug developed by Takeda Pharmaceutical Company Limited (ticker TAK). It has been studied across several conditions, including gout, cardiovascular disease, hypertension, hyperuricosuria, joint damage, and renal impairment. Development has reached Phase 3, with seven completed clinical trials and no active trials currently listed.
Febuxostat targets XDH, also known as xanthine dehydrogenase, and acts as an inhibitor of this enzyme. This target class places Febuxostat among XDH inhibitors. Its clinical development has explored this mechanism across gout and cardiovascular-related conditions, including a dedicated Phase 2 study of its effect on blood pressure.
Febuxostat is developed by Takeda Pharmaceutical Company Limited, which trades under the ticker TAK. Takeda has sponsored the clinical program, including the Phase 3 CARES cardiovascular safety trial and Phase 2 studies in hypertension and renal impairment, as well as a Phase 1 food effect study.
Febuxostat has reached Phase 3 in its clinical development program. Seven trials are recorded as completed, with no active trials currently listed. The Phase 3 CARES trial evaluated cardiovascular safety in participants with gout and cardiovascular comorbidities, and earlier Phase 1 and Phase 2 studies have also completed.
Completed Febuxostat trials include NCT01101035, the Phase 3 CARES cardiovascular safety study in gout patients with cardiovascular comorbidities, which enrolled 6,198 participants. Other completed studies are NCT01496469 in hypertension, NCT01082640 in gout with renal impairment, and NCT02374164, a Phase 1 food effect study in healthy participants.
Yes, Febuxostat XR is an alternative name for Febuxostat. The extended-release designation appears in trial listings such as NCT02374164, a Phase 1 food effect study of Febuxostat XR in healthy participants. Searches for either name refer to the same Takeda compound targeting XDH.