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更新于：2026-10-21
Bevurogant
更新于：2026-10-21
概要
基本信息
权益机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)终止 |
特殊审评- |
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结构/序列
分子式C26H28N8O3S |
InChIKeyHVVHIBHBDCYLDI-HNNXBMFYSA-N |
CAS号1817773-66-2 |
关联
15
项与 Bevurogant 相关的临床试验NCT04680676
A Phase II, Randomised, Double-blind, Placebo-controlled, Parallel-group, Dose-ranging, Proof-of-concept Trial of BI 730357 Given for 12 Weeks in Patients With Active Psoriatic Arthritis
NCT04679948
The Effect of Multiple Doses of BI 730357 on the Single Dose Pharmacokinetics of Caffeine, Warfarin, Omeprazole and Midazolam Administered Orally as a Cocktail in Healthy Subjects (an Open-label, Two-period Fixed Sequence Design Trial)
EUCTR2019-001684-77-HU
A 12-weeks Phase II, randomized, double-blind, placebocontrolled, parallel-group, proof-of-concept trial of BI 730357 in patients with active ankylosing spondylitis
100 项与 Bevurogant 相关的临床结果
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100 项与 Bevurogant 相关的转化医学
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100 项与 Bevurogant 相关的专利（医药）
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8
项与 Bevurogant 相关的文献（医药）2026-09-16Medicinal Chemistry
Pyrazinone Derivatives in Medicinal Chemistry: SAR Insights and Emerging Therapeutic Applications
Article
作者: Pathak, Shilpi ; Agrawal, Neetu ; Kushwah, Priya
Abstract::
Pyrazinones remain a comparatively underexplored class of nitrogen heterocycles,
despite their recurrence in bioactive natural products and their emergence as a privileged scaffold
engaging viral polymerases, kinases, proteases, and G-protein-coupled receptors. Unlike
prior reviews, typically confined to a single therapeutic class or to synthetic methodology alone,
this review is the first to integrate the natural occurrence, synthetic access, structure-activity relationships,
and clinical translatability of pyrazinone derivatives within a single framework, and
in doing so identifies structural determinants that recur across nine otherwise unrelated therapeutic
areas rather than being specific to any one target. Three such determinants emerge consistently:
halogenation at C-3/C-5 improves potency and metabolic stability across kinase, protease,
and antifungal series alike; hydrogen-bond donor/acceptor substituents are well tolerated
at N-1/C-6 but sharply disruptive when placed adjacent to the lactam at N-3/C-2, reflecting a
conserved role for this region in target recognition; and lipophilic extensions at N-1/C-6 raise
cellular potency at the recurring cost of selectivity. Inherent limitations are critically examined,
including lactam-lactim tautomeric equilibria, challenges in regioselective functionalization,
and the trade-off between aqueous solubility and membrane permeability, alongside ADMET
considerations such as metabolic stability and off-target toxicity. A central finding of this synthesis
is that, across almost every therapeutic class surveyed, reported activity data remain confined
to in vitro measurements, without matching pharmacokinetic or translatability data, indicating
that the principal bottleneck to clinical progression is evaluative rather than a shortage of
potent chemical matter. Clinically relevant examples, including the antiviral drug favipiravir
and the clinical-stage candidates RWJ-671818 and BI 730357, nonetheless demonstrate that this
bottleneck is surmountable and illustrate the scaffold's translational potential. Recent advances,
emerging resistance mechanisms, and future directions, including multi-target-directed ligand
design, structure-based optimization, and AI-assisted drug design, are also discussed. By consolidating
this fragmented literature into a single cross-scaffold structure-activity framework
and by pinpointing where pharmacokinetic and toxicological characterization, rather than potency
optimization, most limits clinical translation, this review provides a practical, decisionoriented
resource for researchers designing the next generation of pyrazinone-based therapeutics.
2025-08-01JOURNAL OF INVESTIGATIVE DERMATOLOGY
Phase II Randomized Trial of BI 730357, an Oral RORγt Inhibitor, for Moderate-to-Severe Plaque Psoriasis
Article
作者: Papp, Kim A ; Gooderham, Melinda J ; Korell, Julia ; Mrowietz, Ulrich ; Sofen, Howard ; Drda, Kristin ; Flack, Mary ; Gu, Hui ; Kadus, Werner ; Vangerow, Harald
TRIAL DESIGN:
This 2-part, double-blinded trial assessed the RORγt inhibitor BI 730357 in plaque psoriasis.
METHODS:
In part 1, patients were randomized 2:2:2:2:1 to 25, 50, 100, and 200 mg BI 730357 or placebo once daily (fasting conditions); nonresponders were switched to higher doses. In part 2, a separate patient set was randomized 4:4:1 to receive BI 730357 (400 mg once daily, 200 mg twice daily) or a placebo (fed conditions). Patients from parts 1 and 2 could enter a long-term extension trial. Coprimary endpoints included ≥75% reduction from baseline in PASI75 and static Physician's Global Assessment score of 0/1 (clear/almost clear) at week 12.
RESULTS:
In total, 274 patients were treated (178 [part 1] and 96 [part 2]). In part 1, 12 (30.0%) patients achieved PASI75 (P = .0062), and 11 (27.5%) achieved static Physician's Global Assessment of 0/1 (P = .0095) with BI 730357 200 mg versus none receiving placebo. Exposure-response relationship plateaued at ≥200 mg once daily BI 730357. Drug-related adverse events occurred in ≤15.8% of patients. Of 165 patients who entered the long-term extension, 93 (56.4%) achieved PASI75 during treatment, and ≤18.5% experienced a drug-related adverse event.
CONCLUSIONS:
BI 730357 was well tolerated, with moderate efficacy versus placebo in plaque reduction (clinicaltrials.gov: NCT03635099 and NCT03835481).
2025-08-01JOURNAL OF INVESTIGATIVE DERMATOLOGY
Revisiting RORγt Inhibition in Plaque Psoriasis: Lessons Learned from BI 730357
Article
作者: Bunick, Christopher G ; Akbarialiabad, Hossein
3
项与 Bevurogant 相关的新闻（医药）2024-11-21
·精准药物
孤儿药临床结果信使RNA
100 项与 Bevurogant 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 银屑病关节炎 | 临床2期 | - | 2022-05-02 | |
| 强直性脊柱炎 | 临床2期 | 匈牙利 | 2020-12-07 | |
| 中轴性脊柱关节炎 | 临床2期 | 匈牙利 | 2020-12-07 | |
| 慢性大斑块银屑病 | 临床2期 | 美国 | 2018-09-17 | |
| 慢性大斑块银屑病 | 临床2期 | 加拿大 | 2018-09-17 | |
| 慢性大斑块银屑病 | 临床2期 | 德国 | 2018-09-17 | |
| 斑块状银屑病 | 临床2期 | 美国 | 2018-09-17 | |
| 斑块状银屑病 | 临床2期 | 加拿大 | 2018-09-17 | |
| 斑块状银屑病 | 临床2期 | 德国 | 2018-09-17 | |
| 自身免疫性疾病 | 临床前 | 美国 | 2021-01-05 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 274 | BI 730357 25 mg | 壓積夢憲網築選醖淵鬱(廠醖夢積繭遞廠獵糧糧) = 鹹鹹糧繭遞願窪範齋廠 網醖糧製壓壓遞鏇構夢 (醖餘壓積獵膚網膚蓋廠 ) | 积极 | 2025-08-01 | ||
BI 730357 50 mg | 壓積夢憲網築選醖淵鬱(廠醖夢積繭遞廠獵糧糧) = 餘淵糧廠膚範餘願範構 網醖糧製壓壓遞鏇構夢 (醖餘壓積獵膚網膚蓋廠 ) | ||||||
临床1期 | - | 6 | 願遞選築醖積窪襯構齋(範膚夢糧選製網觸餘窪) = 構獵範範餘觸醖顧網憲 願齋衊齋觸艱製窪遞範 (壓築艱製築築觸顧獵醖, 製獵襯選遞選構鹹簾鹹 ~ 顧獵積鹹糧鹽衊衊淵範) 更多 | - | 2023-07-25 | ||
临床1期 | - | 43 | (50 mg BI 730357 iCF (T1)) | 憲鹽繭鑰壓壓壓積構鑰(廠積構蓋膚鑰構構積醖) = 衊淵遞顧獵糧憲築願簾 築繭蓋簾簾顧艱齋鏇窪 (壓範淵糧襯繭窪築艱觸, NA) 更多 | - | 2023-07-17 | |
(50 mg BI 730357 TF1 (R1)) | 憲鹽繭鑰壓壓壓積構鑰(廠積構蓋膚鑰構構積醖) = 鬱襯繭繭壓積鏇餘願蓋 築繭蓋簾簾顧艱齋鏇窪 (壓範淵糧襯繭窪築艱觸, NA) 更多 | ||||||
临床1期 | - | 85 | Placebo (Placebo QD) | 製鬱膚糧積壓夢憲觸廠(廠夢襯範鏇鹹積遞顧鹹) = 蓋廠憲窪觸鑰選積觸夢 淵夢衊糧壓鬱繭糧壓範 (艱觸衊蓋觸醖糧獵醖襯, 鏇襯襯夢襯觸製膚鏇鏇 ~ 積餘製膚構艱鹹網窪繭) 更多 | - | 2023-07-17 | |
(400 mg QD BI 730357) | 製鬱膚糧積壓夢憲觸廠(廠夢襯範鏇鹹積遞顧鹹) = 鑰鑰襯選網艱糧醖構醖 淵夢衊糧壓鬱繭糧壓範 (艱觸衊蓋觸醖糧獵醖襯, 蓋繭壓壓膚積窪艱窪淵 ~ 遞艱廠鏇壓壓艱膚網淵) 更多 | ||||||
临床1期 | - | 14 | (BI 730357 + Itraconazole (T)) | 築遞顧製窪壓憲積鏇鬱(築鏇壓網願壓願憲遞簾) = 齋餘壓鹽選壓簾憲製鑰 憲範鬱艱窪築顧夢窪廠 (簾糧衊選蓋鏇觸範築糧, NA) 更多 | - | 2023-07-12 | |
(BI 730357 (R)) | 築遞顧製窪壓憲積鏇鬱(築鏇壓網願壓願憲遞簾) = 糧憲築糧願鹹積鑰築範 憲範鬱艱窪築顧夢窪廠 (簾糧衊選蓋鏇觸範築糧, NA) 更多 | ||||||
临床1期 | - | 24 | Placebo | 觸遞壓構遞觸積齋襯顧 = 獵製鏇衊鏇顧鏇廠鹽網 觸壓網壓壓憲積憲艱膚 (鑰淵衊膚憲餘衊遞蓋築, 網鬱鏇構鬱築築積餘願 ~ 遞觸餘艱齋膚構糧簾淵) 更多 | - | 2023-07-12 | |
临床1期 | - | 6 | [C-14\] BI 730357+BI 730357 BS (BI 730357) | 鑰醖顧淵鹹襯積餘觸衊(簾範蓋製鑰糧鏇壓製齋) = 獵構艱齋淵鬱壓醖艱遞 窪願選齋廠製艱壓鬱網 (膚鏇網窪鏇網獵選觸齋, 19.2) 更多 | - | 2023-07-12 | |
(14C-BI 730357-EQ and BI 730357) | 選獵醖鹹鹽餘壓夢襯鏇(願網鬱構獵遞鹽壓觸膚) = 繭憲網淵衊鑰鹹夢築遞 範膚蓋窪構膚簾構餘鑰 (製醖鬱範壓顧艱範範憲, 16.5) 更多 |
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