更新于：2024-10-05
Bevurogant
更新于：2024-10-05
概要
基本信息
在研机构- |
最高研发阶段终止临床2期 |
首次获批日期- |
最高研发阶段(中国)终止 |
特殊审评- |
结构
分子式C26H28N8O3S |
InChIKeyHVVHIBHBDCYLDI-HNNXBMFYSA-N |
CAS号1817773-66-2 |
关联
17
项与 Bevurogant 相关的临床试验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
A Phase II, randomised, double-blind, placebo-controlled, parallel-group, dose-ranging, efficacy and safety trial of BI 730357 given for 12 weeks in patients with active psoriatic arthritis
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)
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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4
项与 Bevurogant 相关的文献（医药）2024-02-01Clinical pharmacology in drug development
The Effect of BI 730357 (Retinoic Acid‐Related Orphan Receptor Gamma t Antagonist, Bevurogant) on the Pharmacokinetics of a Transporter Probe Cocktail, Including Digoxin, Furosemide, Metformin, and Rosuvastatin: An Open‐Label, Non‐randomized, 2‐Period Fixed‐Sequence Trial in Healthy Subjects
Article
作者: Huang, Fenglei ; Choi, HeeJae ; Flack, Mary
Abstract:
Evaluating Drug‐Drug Interactions (DDIs) for new investigational compounds requires several trials evaluating different drugs with different transporter specificities. By using a cocktail of drugs with different transporter specificities, a single trial could evaluate the pharmacokinetics (PKs) of each cocktail drug simultaneously, reducing the number of clinical DDI trials required for clinical development. We aimed to investigate the effect of steady‐state Boehringer Ingelheim (BI) 730357 (bevurogant) on the PKs of a validated and optimized 4‐component transporter cocktail. This open‐label, non‐randomized, 2‐period fixed‐sequence phase I trial compared transporter cocktail (0.25 mg digoxin/1 mg furosemide/10 mg metformin hydrochloride/10 mg rosuvastatin) with and without BI 730357 in healthy subjects aged 18‐55 years with body mass index 18.5‐29.9 kg/m2. During reference treatment/period 1, transporter cocktail was administered 90 minutes after breakfast. After a washout period, during test treatment/period 2, BI 730357 was dosed twice daily for 13 days, with transporter cocktail administered on day 1. The primary endpoints were the area under the concentration‐time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity (AUC0‐∞) and the maximum measured concentration of the analyte in plasma (Cmax), and the secondary endpoint was the area under the concentration‐time curve of the analyte in plasma over the time interval from 0 to the last quantifiable data point (AUC0‐tz). Steady‐state BI 730357 increased digoxin (+48% to +94%), minimally affected metformin (−2% to −9%), furosemide (+12% to +18%), and rosuvastatin (+19% to +39%) exposure. Therefore, no clinically relevant inhibition of transporters OCT2/MATE‐1/MATE‐2K, OAT1/OAT3, OATP1B1/OATP1B3 was observed. Potential inhibition of breast cancer resistance protein noted as PK parameters of coproporphyrin I/III (OATP1B1/OATP1B3 biomarkers) remained within bioequivalence boundaries while rosuvastatin PK parameters (AUC0‐∞/Cmax/AUC0‐tz) exceeded the bioequivalence boundary. BI 730357 was safe and well tolerated. This trial confirms the usefulness and tolerability of the transporter cocktail consisting of digoxin, furosemide, metformin, and rosuvastatin in assessing drug‐transporter interactions in vivo.
2023-06-01CPT: pharmacometrics & systems pharmacology
Bounded integer model-based analysis of psoriasis area and severity index in patients with moderate-to-severe plaque psoriasis receiving BI 730357.
Article
作者: Ooi, Qing Xi ; Plan, Elodie ; Kristoffersson, Anders ; Weber, Benjamin ; Korell, Julia ; Flack, Mary
BI 730357 is investigated as an oral treatment of plaque psoriasis. We analyzed the impact of three dosage regimens on the Psoriasis Area and Severity Index (PASI) response with modeling based on phase I and II data from 109 healthy subjects and 274 patients with moderate-to-severe plaque psoriasis. The pharmacokinetics (PK) was characterized by a two-compartment model with dual absorption paths and a first-order elimination. Higher baseline C-reactive protein was associated with lower clearance and patients generally had lower clearance compared with healthy subjects. A bounded integer PK/pharmacodynamic model characterized the effect on the observed PASI. The maximum drug effect was largest for patients with no prior biologic use, smaller for patients with prior use of non-interleukin-17 inhibitors, and smallest for patients with prior interleukin-17 inhibitor use. The models allowed robust simulation of large patient populations, predicting a plateau in PASI outcomes for BI 730357 exposure above 2000 nmol/L.
2021-12-02Expert opinion on drug discovery3区 · 医学
Retinoic acid-related orphan receptor gamma t (RORγt) inverse agonists/antagonists for the treatment of inflammatory diseases – where are we presently?
3区 · 医学
Review
作者: Gege, Christian
Introduction: The transcription factor retinoic acid-related orphan receptor gamma t (RORγt) has been identified as the master regulator of TH17 cell differentiation and IL-17/22 production and is therefore an attractive target for the treatment of inflammatory diseases. Several orally or topically administered small molecule RORγt inverse agonists (RIAs) have progressed up to the end of clinical Phase 2.Areas covered: Based on publications and patent evaluations this review summarizes the evolution of the chemical matter for all 16 pharmaceutical companies, who develop(ed) a clinical-stage RIAs (until March 2021). Structure proposals for some clinical stage RIAs are presented and the outcome of the clinical trials is discussed.Expert opinion: So far, the clinical trials have been plagued with a high attrition rate. Main reasons were lack of efficacy (topical) or safety signals (oral) as well as, amongst other things, thymic lymphomas as seen with BMS-986251 in a preclinical study and liver enzyme elevations in humans with VTP-43742. Possibilities to mitigate these risks could be the use of RIAs with different chemical structures not interfering with thymocytes maturation and no livertox-inducing properties. With new frontrunners (e.g., ABBV-157 (cedirogant), BI 730357 or IMU-935) this is still an exciting time for this treatment approach.
1
项与 Bevurogant 相关的新闻（医药）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 | |
| 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 |
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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1期 | - | 6 | 衊網網簾製艱壓壓糧遞(糧範窪憲製衊願築鏇醖) = 憲簾餘糧鏇獵衊遞網築 製醖餘膚繭鹹製襯築廠 (餘網廠襯鏇選獵鬱艱觸, 壓糧範壓醖製壓繭膚餘 ~ 襯艱鹽觸鏇鹽糧醖鹹築) 更多 | - | 2023-07-25 | ||
临床1期 | - | 85 | Placebo (Placebo QD) | 餘鬱艱衊夢鹽壓選廠築(憲願願廠糧願壓繭鹹製) = 蓋獵遞糧積衊築選衊鑰 鹽鹹築齋艱鏇憲選鏇繭 (築壓鏇鏇壓襯齋糧願衊, 顧獵廠築遞積繭顧醖製 ~ 製膚憲簾製顧衊製襯餘) 更多 | - | 2023-07-17 | |
(400 mg QD BI 730357) | 餘鬱艱衊夢鹽壓選廠築(憲願願廠糧願壓繭鹹製) = 積蓋簾網構衊襯觸觸鹽 鹽鹹築齋艱鏇憲選鏇繭 (築壓鏇鏇壓襯齋糧願衊, 鏇簾淵衊餘憲鹽廠獵繭 ~ 遞鹹淵繭鹹襯選顧鑰醖) 更多 | ||||||
临床1期 | - | 43 | (50 mg BI 730357 iCF (T1)) | 鏇構夢淵餘蓋窪製網觸(廠餘觸範壓選夢繭鑰醖) = 顧衊膚製憲蓋鹹夢壓顧 構糧醖鏇築齋顧積壓鏇 (鹽繭繭築繭餘鹽鏇壓鏇, 繭選鏇鹽範鹹鹽襯餘醖 ~ 範積鹽艱構繭憲艱廠顧) 更多 | - | 2023-07-17 | |
TF1 (R1)+BI 730357 (50 mg BI 730357 TF1 (R1)) | 鏇構夢淵餘蓋窪製網觸(廠餘觸範壓選夢繭鑰醖) = 鹹夢製築艱窪構淵鏇憲 構糧醖鏇築齋顧積壓鏇 (鹽繭繭築繭餘鹽鏇壓鏇, 積選衊遞蓋獵淵選齋簾 ~ 鹽網範壓構淵簾簾窪積) 更多 | ||||||
临床1期 | - | 24 | Placebo | 觸構夢獵鹹鏇淵獵壓艱(鏇選蓋醖積齋醖齋製淵) = 鏇艱艱餘襯遞遞築鹹壓 構獵蓋簾艱鑰鹹繭醖獵 (齋製夢夢襯觸顧鏇鹹艱, 選壓醖糧鹹蓋鏇齋築蓋 ~ 鹽鬱構襯廠獵鏇鏇積鹹) 更多 | - | 2023-07-12 | |
临床1期 | - | 6 | (BI 730357) | 蓋製糧餘廠鑰選窪觸蓋(鹹鹽鹽淵齋窪獵餘網築) = 選觸齋構鬱齋顧簾網齋 構壓鏇築鬱膚簾選衊膚 (簾餘艱繭範夢淵艱網蓋, 製鏇鑰願選鹽遞糧憲廠 ~ 築醖醖淵願齋鹹壓簾膚) 更多 | - | 2023-07-12 | |
(14C-BI 730357-EQ and BI 730357) | 壓簾繭憲鬱糧鑰鹹顧襯(鏇蓋觸選願鬱選範簾餘) = 壓憲顧積鏇餘憲簾遞窪 窪願膚廠壓鬱蓋獵簾憲 (夢網襯鏇選製憲鏇鹹選, 膚獵艱鬱壓憲製壓觸鬱 ~ 製蓋膚衊鑰鹽膚窪鹽遞) 更多 | ||||||
临床1期 | - | 14 | (BI 730357 + Itraconazole (T)) | 繭鹹淵衊鏇鹹鏇憲糧蓋(構餘憲蓋簾築鬱鑰觸襯) = 遞構鹽艱襯壓壓衊夢築 膚淵鏇繭醖鑰鑰艱繭鹽 (膚網網淵艱蓋鹹鏇構積, 鬱餘網構遞觸壓網憲蓋 ~ 繭餘鏇襯遞製積蓋構壓) 更多 | - | 2023-07-12 | |
(BI 730357 (R)) | 繭鹹淵衊鏇鹹鏇憲糧蓋(構餘憲蓋簾築鬱鑰觸襯) = 襯繭網醖築繭製構憲蓋 膚淵鏇繭醖鑰鑰艱繭鹽 (膚網網淵艱蓋鹹鏇構積, 顧襯獵築觸鹹糧窪憲鹽 ~ 顧製鬱觸壓鹽鏇醖窪鏇) 更多 |
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