[Translation] A randomized, open-label, two-formulation, single-dose, two-cycle, double-crossover bioequivalence study of dotenoradine tablets in healthy study participants.

以江西泰吉立生物制药有限公司研制的多替诺雷片为受试制剂，以株式会社富士薬品持证的多替诺雷片（商品名：URECE®）为参比制剂，考察两制剂在空腹及餐后状态下单次给药的药代动力学参数及相对生物利用度，评价两制剂是否具有生物等效性。

[Translation]

Using dotenorum tablets developed by Jiangxi Taijili Biopharmaceutical Co., Ltd. as the test formulation and dotenorum tablets (trade name: URECE®) certified by Fuji Pharmaceutical Co., Ltd. as the reference formulation, the pharmacokinetic parameters and relative bioavailability of the two formulations under fasting and postprandial conditions after a single dose were investigated to evaluate whether the two formulations are bioequivalent.

Start Date29 Dec 2025

Sponsor / Collaborator

Jiangxi Taijili Bio-Pharmaceutical Co., Ltd.

CTR20255025

/ Active, not recruitingNot Applicable

多替诺雷片人体生物等效性研究

[Translation] Human bioequivalence study of dotenorazole tablets

本试验旨在研究单次空腹和餐后口服江苏德源药业股份有限公司研制、生产的多替诺雷片（2 mg）的药代动力学特征；以株式会社富士藥品生产的多替诺雷片（URECE®，2 mg）为参比制剂，比较两制剂中药动学参数Cmax、AUC0-t、AUC0-∞，评价两制剂的人体生物等效性。

[Translation]

This study aimed to investigate the pharmacokinetic characteristics of dotenoradine tablets (2 mg) developed and manufactured by Jiangsu Deyuan Pharmaceutical Co., Ltd., taken orally on an empty stomach and after a meal. Dotenoradine tablets (URECE®, 2 mg) manufactured by Fuji Pharmaceutical Co., Ltd. were used as a reference formulation. The pharmacokinetic parameters Cmax, AUC0-t, and AUC0-∞ of the two formulations were compared to evaluate their bioequivalence in humans.

Start Date26 Dec 2025

Sponsor / Collaborator

Jiangsu Deyuan Pharmaceutical Co., Ltd.

CTR20254366

/ Active, not recruitingNot Applicable

多替诺雷片在健康受试者中单中心、随机、开放、单剂量、双周期、双交叉空腹和餐后状态下的生物等效性试验

[Translation] A single-center, randomized, open-label, single-dose, two-period, two-crossover bioequivalence study of dotenoradine tablets in healthy subjects in fasting and postprandial settings.

主要试验目的：比较空腹和餐后给药条件下，桂林南药股份有限公司生产的多替诺雷片（2mg）与株式会社富士薬品持证的多替诺雷片（2mg，商品名：ユリス®/URECE®）在健康成年人群中吸收程度和速度的差异，评价其生物等效性。次要试验目的：评价空腹和餐后给药条件下，桂林南药股份有限公司生产的多替诺雷片（2mg）与株式会社富士薬品持证的多替诺雷片（2mg，商品名：ユリス®/URECE®）在健康成年人群中的安全性。

[Translation]

Primary objective: To compare the absorption rate and extent of dotenorazole tablets (2 mg) manufactured by Guilin Nanfang Pharmaceutical Co., Ltd. with that of dotenorazole tablets (2 mg, brand name: URECE®) certified by Fuji Pharmaceutical Co., Ltd. in a healthy adult population under fasting and postprandial administration conditions, and to evaluate their bioequivalence. Secondary objective: To evaluate the safety of dotenorazole tablets (2 mg) manufactured by Guilin Nanfang Pharmaceutical Co., Ltd. with that of dotenorazole tablets (2 mg, brand name: URECE®) certified by Fuji Pharmaceutical Co., Ltd. in a healthy adult population under fasting and postprandial administration conditions.

Start Date04 Dec 2025

Sponsor / Collaborator

Guilin Pharmaceutical Co., Ltd.

100 Clinical Results associated with Dotinurad

100 Translational Medicine associated with Dotinurad

100 Patents (Medical) associated with Dotinurad

Literatures (Medical) associated with Dotinurad

01 Feb 2026·EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Benzoheterocyclic analogues of dotinurad as orally efficacious human urate transporter 1 inhibitors: Design, synthesis, structure-activity relationships, and pharmacokinetic studies

Article

Author: Zhou, Jian ; Liang, Jiaqi ; Li, Xiang ; Zhang, Linjian ; Zhang, Guowei ; Zhang, Xiaojin ; Zhang, Haoshu ; Su, Kaijun

A series of benzoheterocyclic analogues of Dotinurad were designed and synthesized as URAT1 inhibitors via bioisosterism and linker modification strategies. Among the 19 synthesized derivatives, compounds 9, 13, and 14 (bearing benzimidazole, benzotetrahydropyrrole, and benzo[b]thiazine 1,1-dioxide scaffolds, respectively) exhibited acceptable inhibitory potency (IC₅₀: 69.81-441.51 nM), favorable metabolic stability, and improved pharmacokinetic profiles compared to Dotinurad. Notably, despite showing weaker in vitro URAT1 inhibition than the Dotinurad, these three candidates demonstrated significantly superior uricosuric activity in hyperuricemic rats. Mechanistic investigation revealed that the substantial excretion of unchanged prototype compounds into the urine ensured a high local concentration within the renal tubule lumen, which effectively compensated for their moderate in vitro affinity. These findings validated the design strategy and highlighted compounds 9, 13, and 14 as promising candidates for hyperuricemia treatment.

01 Dec 2025·Clinical Drug Investigation

A Single- and Multiple-Dose Study to Characterize the Pharmacokinetics and Safety of Dotinurad in Healthy Chinese Adults

Article

Author: Sun, Hui ; Kokan, Rieko ; Cai, Cuiyuan ; Kawamura, Kotomi ; Nomoto, Maiko ; Liu, Yun ; Chen, Qian

BACKGROUND AND OBJECTIVES:

Dotinurad is a selective uricosuric drug for patients with gout with hyperuricemia. To our knowledge, this is the first study to evaluate the pharmacokinetics (PK) of dotinurad, following single and multiple oral doses in healthy Chinese adults.

METHODS:

This single-center, open-label, parallel group, phase 1 study had 3 cohorts: A (1-mg single dose), B (single and multiple doses of 4 mg once daily for 7 days), and C (10-mg single dose). Dotinurad was administered on an empty stomach. Healthy nonsmoking Chinese adults aged 18-45 years with body mass index 19-24 k/m² and weight ≥ 50 kg were enrolled; Cohort B required serum urate ≥ 5.5 mg/dL at screening.

RESULTS:

In total, 26 subjects were included. After single oral doses of 1, 4, and 10 mg, mean ± standard deviation (SD) plasma dotinurad concentration reached maximum observed plasma concentration (C_max) of 104 ± 18.5, 365 ± 35.2, and 964 ± 101 ng/mL at 3.00-3.50 h, respectively. The mean ± SD terminal elimination phase half-life was 10.1 ± 1.26, 9.87 ± 1.47, and 10.9 ± 1.53 h for the 1, 4, and 10 mg doses, respectively; both area under the plasma concentration-time curve and C_max increased in a dose-proportional manner across the 1-10-mg dose range. During once-daily doses for 7 days, steady state was reached by the 2nd day after the initiation of multiple dosing, with an average steady-state plasma concentration of 186 ± 31.8 ng/mL, indicating minimal accumulation. Treatment-emergent adverse events (TEAEs) occurred in four subjects (15.4%); all were mild and resolved without treatment. No dose-dependent TEAEs were observed.

CONCLUSION:

Single- and multiple-dose PK of dotinurad in healthy Chinese adults showed rapid absorption, rapid elimination, linear PK, and no accumulation with once-daily dosing. Dotinurad was well-tolerated during the 7-day treatment course.

TRIAL REGISTRATION:

ClinicalTrials.gov: NCT05278676.

01 Dec 2025·Arthritis & Rheumatology

Efficacy and Safety of Dotinurad Versus Febuxostat for the Treatment of Gout: A Randomized, Multicenter, Double‐Blind, Phase 3 Trial in China

Article

Author: Lu, Yibing ; Jiang, Zhenyu ; Yi, Bin ; Yu, Shihao ; Kokan, Rieko ; Ishikawa, Kohei ; Cheng, Yongjing ; Guo, Dongmei ; Kong, Xiaodan ; Sun, Jia ; Liu, Yu ; Xu, Baijie ; Li, Changgui ; Zhang, Hongfeng ; Zhang, Zhuoli ; Hu, Jiankang ; Liu, Dongzhou ; Kawakatsu, Mikiko ; Gao, Zhengnan ; Wang, Yu

Objective:

Dotinurad is a selective urate reabsorption inhibitor that reduces serum urate levels. We compared the efficacy and safety of dotinurad with febuxostat in Chinese patients with gout.

Methods:

This phase 3, multicenter, randomized, double‐blind, parallel‐group study randomly allocated (1:1) eligible patients with gout to receive oral dotinurad or febuxostat. The primary end point was the responder rate (proportion of patients achieving serum urate levels ≤6.0 mg/dL) at week 24 in the full analysis set (FAS) to demonstrate superiority of dotinurad 4 mg/day to febuxostat 40 mg/day. The secondary end points included the responder rate at week 12 to show the noninferiority of dotinurad 2 mg/day to febuxostat 40 mg/day. Treatment‐emergent adverse events (TEAEs) were also recorded.

Results:

A total of 451 patients were randomized, and 441 were included in the FAS. Baseline characteristics were well balanced between treatment groups. The responder rate at week 24 was significantly higher for dotinurad 4 mg/day versus febuxostat 40 mg/day (73.6% vs 38.1%; adjusted difference 35.9% [95% confidence interval (CI) 27.4%–44.4%]; P < 0.0001), and at week 12, dotinurad 2 mg/day was noninferior to febuxostat 40 mg/day (55.5% vs 50.5%; adjusted difference 5.2% [95% CI −3.7% to 14.2%]). Incidences of TEAEs in the dotinurad and febuxostat groups were similar.

Conclusion:

Dotinurad 4 mg/day was superior to febuxostat 40 mg/day in achieving serum urate levels ≤6.0 mg/dL at week 24 and was well tolerated in Chinese patients with gout.

News (Medical) associated with Dotinurad

02 Feb 2026

·www.prnewswire.com

Crystalys Therapeutics Expands Phase 3 RUBY Study With First Patients Dosed at European Sites

SAN DIEGO, Feb. 2, 2026 /PRNewswire/ -- Crystalys Therapeutics, a clinical-stage biopharmaceutical company addressing the significant unmet medical needs of people living with gout, today announced that the first patients have been dosed at clinical sites in Europe in its Phase 3 RUBY study ( NCT07089875) evaluating dotinurad, a next-generation, once-daily oral URAT1 inhibitor for the treatment of hyperuricemia associated with gout. The RUBY study is part of Crystalys' global Phase 3 clinical development program for dotinurad, which is being evaluated as a potential second-line treatment option for patients with gout who do not respond adequately to allopurinol. "Expanding patient dosing into European sites is a key milestone for the RUBY study and we look forward to continued progress as enrollment advances" said James Mackay, Ph.D., President and Chief Executive Officer of Crystalys Therapeutics. About the RUBY Study The RUBY study (NCT07089875) is a Phase 3, randomized, double-blind, multicenter study to evaluate the safety and efficacy of dotinurad in approximately 500 patients with hyperuricemia associated with gout. Study participants will be given dotinurad orally once a day for up to 64 weeks. About Gout Gout is the most common form of inflammatory arthritis. It is a condition that is very debilitating for patients and characterized by sudden, severe attacks of pain, swelling, redness and tenderness in one or more joints. This disease arises from excess uric acid in the body, known as 'hyperuricemia,' which causes buildup of uric acid crystals and inflammation, leading to tophaceous gout in people with chronic or undertreated disease. Despite available therapies that aim to reduce uric acid levels below the target 6 mg/dL, a major treatment gap remains between first-line xanthine oxidase inhibitors (XOIs) and last-line uricase therapy. Currently, no suitable second-line options exist in the U.S. or E.U., leaving a critical unmet need for patients who fail to respond to first-line treatments. About Crystalys Therapeutics Crystalys Therapeutics is a clinical-stage biopharmaceutical company transforming the treatment of gout. Headquartered in San Diego, California, and co-founded by Catalys Pacific and Novo Holdings, Crystalys brings together a world-class team with deep expertise in gout drug development, dedicated to delivering more effective options for people living with gout. The company's lead candidate, dotinurad, is a next-generation, once daily oral, URAT1 inhibitor in clinical development as a second-line therapy aimed to reduce uric acid, gout flares and tophi. Dotinurad was invented by Fuji Yakuhin and has obtained regulatory approval in Japan, China, Philippines and Thailand. With best-in-class potential for both safety and efficacy, dotinurad is supported by clinical data from multiple Asian markets where it is approved. Crystalys is advancing dotinurad in global Phase 3 trials toward regulatory approval and commercial launch. For more information, visit and follow us on X and LinkedIn. SOURCE Crystalys Therapeutics 21% more press release views with Request a Demo

Phase 3Drug Approval

17 Dec 2025

·www.biospace.com

Addition Debuts With $100M to Advance One-Time Therapies for Rare, Chronic Diseases

iStock, Ilija Erceg Addition joins a growing list of launches this year, following in the footsteps of startups like Crystalys Therapeutics and Ollin Biosciences. Addition Therapy launched on Wednesday, armed with $100 million in starting funds and two goals: one, transform the way rare and chronic diseases are treated, and two, develop one-time therapies that can overcome the shortcomings of current genetic medicines. To achieve these lofty aspirations, the California startup will leverage its proprietary PRINT platform, an all-RNA, non-viral technology making use of lipid nanoparticles to package and deliver therapeutic payloads. The tech is still very young: non-human primate studies are set for 2026. The biotech did not provide details about its pipeline or development timeline. Addition is backed by a group of high-pro including the Gates Foundation, Abingworth, SR One and Osage University Partners. The biotech also has ongoing research initiatives with certain unnamed pharma companies to advance its PRINT programs for undisclosed rare and chronic diseases. Aside from backing the launch, the Gates Foundation has also given Addition a grant to advance a PRINT-driven single-dose therapy that could help patients produce antibodies against HIV, potentially providing lifetime protection. Addition will be led by CEO Ron Park , a Roche alumnus who served as the pharma’s global co-lead of personalized healthcare. Park was previously an entrepreneur in residence at Third Rock Ventures. Joining Park on Addition’s masthead is Chief Scientific Officer Francine Gregoire , who was previously head of preclinical cardiovascular development at Moderna. Gregoire has also held leadership roles at CRISPR Therapeutics and Beam Therapeutics. Like Addition, several other startups have entered the biopharma arena this year. In September, for instance, Crystalys Therapeutics broke onto the scene with $205 million in series A funds to advance dotinurad, an oral URAT1 blocker being tested for gout. Ollin Biosciences also emerged from stealth that month, carrying $100 million in starting capital to develop its antibody OLN324, which blocks both VEGF and Ang2 pathways, for eye diseases.

15 Dec 2025

·www.fiercebiotech.com

Sobi pays $950M upfront to snap up phase 3 gout specialist Arthrosi Therapeutics

Under a new deal, Sobi gets its hands on Arthrosi Therapeutics’ pozdeutinurad, a next-gen, once-daily oral URAT1 inhibitor.\n Fresh off a $153 million series E round, Arthrosi Therapeutics is skipping an IPO route and is instead being bought up for a potential value of $1.5 billion from Swedish biopharma Sobi. Under the deal, San Diego-based Arthrosi will secure $950 million upfront as well as a contingent consideration of up to $550 million. For its part, Sobi gets its hands on Arthrosi’s pozdeutinurad, a next-gen, once-daily oral URAT1 inhibitor.This med is being assessed in several phase 3 tests for progressive and tophaceous gout, with initial readouts slated for next year.“The acquisition of Arthrosi allows us to expand our gout pipeline with a highly differentiated new asset,” Guido Oelkers, president and CEO of Sobi, said in a statement.“Pozdeutinurad has the potential to become the therapy of choice for patients who have progressive gout with persistent and unresolved symptoms despite first-line therapy,” the CEO added.Gout is a type of arthritis that causes sudden, severe joint pain. Common drug treatment includes simple pain relief, but pharma has been working on potential curative treatments for decades, though with mixed results.Arthrosi’s leading drug candidate is an inhibitor of URAT1, a transporter that has been a target for gout drugs going back to the approval of probenecid in 1951. Probenecid and other early gout drugs hit multiple targets but also caused a range of side effects. Seeking to avoid the adverse events, developers of subsequent waves of gout drugs tried to create more potent and specific URAT1 inhibitors.AstraZeneca acquired a URAT1 inhibitor in its $1.3 billion takeover of Ardea Biosciences in 2012 and won FDA approval for the drug in 2015. By 2020, the product, Zurampic, had, however, landed on the scrap heap.The commercial struggles of Zurampic, which carried a boxed warning, didn\'t deter others from trying to launch URAT1 inhibitors.A team behind Zurampic has reformed at Crystalys Therapeutics to advance dotinurad, a URAT1 inhibitor that is approved in Asian markets including Japan. And China’s Atom Therapeutic recently reported a phase 2b/3 win for its own URAT1 inhibitor, lingdolinurad.

Drug ApprovalPhase 3AcquisitionIPO

100 Deals associated with Dotinurad

External Link

KEGG	Wiki	ATC	Drug Bank
D11071	Dotinurad	M04AB	DB16145

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Gout	Japan	Fuji Yakuhin Co., Ltd.	23 Jan 2020
Hyperuricemia	Japan	Fuji Yakuhin Co., Ltd.	23 Jan 2020

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Chronic tophaceous gout	Phase 3	United States	Crystalys Therapeutics	04 Aug 2025
Primary gout	Phase 3	China	Eisai Co., Ltd.	21 Dec 2021

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05278676 (Pubmed \| Clin Drug Investig)	Phase 1	-	26	Dotinurad 1 mg	nbyntnqami(nuqwdetpyv) = xbaqxzizvx vxofzotieo (kvjkcwucxy, 18.5) View more	Positive	19 Oct 2025
				Dotinurad 4 mg single and multiple doses	nbyntnqami(nuqwdetpyv) = aubyhinqaw vxofzotieo (kvjkcwucxy, 35.2) View more
NCT05007392 (CTgov)	Phase 3	Gout \| Primary gout \| Arthritis, Gouty	451	Febuxostat (Febuxostat)	zzmtoaputp = citvfsikwo okfztdrvtf (bmvlyrdxdf, fcelpphnng - cwumauafgh) View more	-	30 Jul 2025
				Dotinurad (Dotinurad)	zzmtoaputp = ptaoqbtgyf okfztdrvtf (bmvlyrdxdf, nyzggdqjfi - ikbrbkffvj) View more
NCT05007392 (EULAR 12024 \| EULAR 22024) Manual	Phase 3	Gout	451	Dotinurad 4mg	mdwyimvzwq(zlrwedkkno) = tognqhhutk knprobexyi (meqfofermp, 67.8 - 79.5) Met	Superior	14 Jun 2024
				Febuxostat 40mg	mdwyimvzwq(zlrwedkkno) = vlbixmxuzf knprobexyi (meqfofermp, 31.6 - 44.5) Met View more
NCT03100318 (Pubmed \| Pediatr Int \| Clin Exp Nephrol) Manual	Phase 3	Gout \| Hyperuricemia	201	Dotinurad	kksdmycsno(zhzccslkkw) = xgrhzwwute hyqftwjhcj (uwjgupbivc )	Positive	01 Mar 2020
				benzbromarone	kksdmycsno(zhzccslkkw) = kzeqgworsk hyqftwjhcj (uwjgupbivc )
NCT03372200 (Pubmed) Manual	Phase 3	Hyperuricemia \| Gout	203	dotinurad	nmmrlvnugi(didvaoiyqg) = vtbonnrvay vrhawtgnzc (mskiprqiak )	Non-inferior	01 Mar 2020
				febuxostat	nmmrlvnugi(didvaoiyqg) = rmkssdmtxk vrhawtgnzc (mskiprqiak )
NCT03006445 (Pubmed \| Pediatr Int \| Clin Exp Nephrol) Manual	Phase 3	Gout \| Hyperuricemia	-	dotinurad	jatfdxsetw(hzpycjdrmg) = -46.73% (2 mg), -54.92% (4 mg) rekxflhifo (llurnrbgve ) View more	Positive	01 Mar 2020
				Dotinurad 4 mg
NCT02344862 (Pubmed \| Clin Exp Nephrol)	Phase 2	Gout \| Hyperuricemia	80	Dotinurad 1 mg	uqcorjuwrg(rlihecywxl) = ydnvrqsimf ewjqnacxcj (bqcfsoywwa )	-	01 Mar 2020
				Dotinurad 2 mg	uqcorjuwrg(rlihecywxl) = ddsmrwalqw ewjqnacxcj (bqcfsoywwa )
NCT02416167 (Pubmed \| Clin Exp Nephrol)	Phase 2	Hyperuricemia \| Gout	200	Dotinurad 0.5 mg	vpizboqfmv(uuzwmazrwo) = dwouzxfccp kgjrfqxwjx (pebohutxen )	-	01 Mar 2020
				Dotinurad 1 mg	vpizboqfmv(uuzwmazrwo) = zkovayfhmx kgjrfqxwjx (pebohutxen )

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