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更新于：2026-01-14
Roflumilast
罗氟司特
更新于：2026-01-14
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 欧盟 (2010-07-05), |
最高研发阶段(中国)申请上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C17H14Cl2F2N2O3 |
InChIKeyMNDBXUUTURYVHR-UHFFFAOYSA-N |
CAS号162401-32-3 |
关联
152
项与 罗氟司特 相关的临床试验NCT07263230
An Open-label Single Center Study Evaluating the Safety and Efficacy of Roflumilast Foam 0.3% in Subjects With Hidradenitis Suppurativa
NCT07340216
An Open Label, Phase 1, Maximal Usage Pharmacokinetics and Safety Study of ARQ-154 Foam 0.3% Administered QD in Pediatric Participants With Scalp and Body Psoriasis
NCT07297602
Evaluation of Efficacy and Safety of Oral Roflumilast in Treatment of Moderate to Severe Atopic Dermatitis: a Pilot Study
100 项与 罗氟司特 相关的临床结果
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100 项与 罗氟司特 相关的转化医学
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100 项与 罗氟司特 相关的专利（医药）
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1,047
项与 罗氟司特 相关的文献（医药）2026-04-01Actas Dermo-Sifiliograficas
Oral Roflumilast for Long-term Management of Behçet Spectrum Disorders: A Multicenter Observational Analysis
Article
作者: Zaragoza Ninet, V ; González García, Á ; Blaya Imbernon, D ; Peñuelas Leal, R ; Bagan, J ; Bagan, L ; Finello, M ; Pérez Pastor, G ; Perez Zafrilla, E ; Grau Echevarría, A ; Linares Barrios, M ; Marti Cabrera, M ; Alegre De Miquel, V ; Diez Recio, E ; Peñuelas Ruiz, J A ; García Fernández, L ; Labrandero Hoyos, C
BACKGROUND:
Recurrent aphthous stomatitis (RAS) and Behçet's disease (BD) are part of the Behçet spectrum disorders (BSD), sharing genetic traits and characterized by recurrent ulcers. No systemic treatment is approved for RAS or incomplete BD, despite significant quality-of-life impacts.
OBJECTIVE:
To evaluate the efficacy of roflumilast, a PDE4 inhibitor, in BSD patients and compare responses between RAS and BD.
METHODS:
This analytical observational study included a total of 33 patients with BSD (22, RAS; 11, BD) from 5 Spanish centers, followed over 52 weeks. Data were collected retrospectively and prospectively, assessing flare-ups, ulcers, pain, and duration. Statistical models compared outcomes across treatment periods.
RESULTS:
Roflumilast significantly reduced all studied response variables, with no loss of long-term efficacy. Differences between RAS and BD were minimal and clinically irrelevant. Adverse events occurred in 63% of patients, mostly mild and self-limiting, with tolerability improved through dose adjustments. Two patients (6.25%) dropped out due to adverse events.
CONCLUSION:
Roflumilast is effective for managing BSD, offering a safe option to address unmet needs in RAS and BD. Its favorable safety profile and long-term efficacy support its use in the routine clinical practice.
2026-02-01ANNALS OF PHARMACOTHERAPY
Roflumilast and the Changing Landscape of Seborrheic Dermatitis Treatment
Review
作者: Xie, Joy ; Dhillon, Jimmy ; Tchack, Madeline ; Rao, Babar K. ; Mahajan, Aryan
Objective::
This article reviews clinical trial data that assess the safety, efficacy, and clinical application of roflumilast, a phosphodiesterase-4 inhibitor, for the treatment of seborrheic dermatitis.
Data Sources::
A review of the literature was conducted in MEDLINE (Pubmed) and Clinicaltrials.gov from January 1, 1950 to April 13, 2025 using the search terms: “Roflumilast” and “seborrheic dermatitis.”
Study selection and data extraction::
Relevant articles in English relating to the safety, efficacy, pharmacodynamics, and pharmacokinetics were included.
Data Synthesis::
In one phase IIa clinical trial, 73.8% of patients treated with roflumilast achieved Investigator Global Assessment (IGA) success, compared with 40.9% in the vehicle group at 8 weeks (
P
< 0.001). A phase III trial found 79.5% of patients in the roflumilast group achieved IGA success at week 8, compared with 58.0% in the vehicle group (
P
< 0.001). Furthermore, there were statistically significant reductions in erythema, scaling, and itch severity in the roflumilast group. Roflumilast was well tolerated, with adverse events comparable with vehicle foam.
Relevance to Patient Care and Clinical Practice in Comparison to Existing Drugs::
Roflumilast is the first phosphodiesterase-4 inhibitor approved by the Food and Drug Administration for the treatment of seborrheic dermatitis. Based on 2 clinical trials, roflumilast has a positive safety profile, is efficacious, and is easy to apply, highlighting its utility in treating seborrheic dermatitis.
Conclusion::
Roflumilast is effective in treating seborrheic dermatitis. Future trials should compare its safety and efficacy with other drugs.
2026-01-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Identification of a novel PDE4 inhibitor inspired by leoligin-derived lignans
Article
作者: Mihovilovic, Marko D ; Dirsch, Verena M ; Chen, Ya ; Richter, Wito ; Perhal, Alexander F ; Kirchmair, Johannes ; Coffey, Christine ; Schwaiger, Stefan ; Linder, Thomas ; Schnürch, Michael
The phosphodiesterase 4 (PDE4) family comprises isoenzymes that selectively hydrolyse the second messenger cyclic adenosine monophosphate (cAMP). PDE4s are widely expressed and play key roles in various physiologic paradigms, including immune responses, memory, cognition, and metabolism. Marketed PDE4 inhibitors, such as roflumilast and apremilast, treat chronic obstructive pulmonary disease and psoriasis. Identification and characterisation of PDE4 inhibitors offer a promising strategy for targeting diverse pathological processes. In this study, leoligin, a natural lignan found in the roots of Edelweiss (Leontopodium nivale subsp. alpinum (Cass.) Greuter (Asteraceae)) and 165 analogues were screened for their PDE inhibitory activity using a cAMP accumulation assay employing an exchange protein activated by cAMP-based biosensor. Six compounds, including leoligin itself, were identified to cause a significant accumulation of cAMP, and structure-activity relationships were deduced. One analogue, designated LT-104A, showed a concentration-dependent activity with the highest determined potency (EC50 = 1.9 μM) in the cAMP accumulation assay. LT-104A was further characterised using a CRE-Luciferase assay, showing comparable activity to known PDE4 inhibitors in inducing the anti-inflammatory cAMP-PKA-CREB pathway. The inhibitory activity of LT-104A was also confirmed against recombinant PDE4D3 in a cell-free cAMP hydrolysis assay (IC50 = 9.3 μM). The potential binding mode of LT-104A with the catalytic domain of PDE4D was predicted using induced-fit docking. Lastly, a functional study was conducted in LPS-activated macrophages, where LT-104A reduced nitric oxide release and decreased mRNA expression of Il1b and Nos2. In conclusion, extensive in vitro screening of leoligin analogues led to the identification and characterisation of a novel PDE4 inhibitor, LT-104A, with potential in vitro anti-inflammatory properties.
409
项与 罗氟司特 相关的新闻（医药）2026-01-13
AHA会议
2026-01-12
100 项与 罗氟司特 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 特应性皮炎 | 美国 | 2024-07-10 | |
| 脂溢性皮炎 | 美国 | 2023-12-15 | |
| 斑块状银屑病 | 加拿大 | 2019-12-20 | |
| 慢性阻塞性肺疾病 | 欧盟 | 2010-07-05 | |
| 慢性阻塞性肺疾病 | 冰岛 | 2010-07-05 | |
| 慢性阻塞性肺疾病 | 列支敦士登 | 2010-07-05 | |
| 慢性阻塞性肺疾病 | 挪威 | 2010-07-05 |
未上市
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 |
|---|---|---|---|---|
| 轻度特应性皮炎 | 临床3期 | 中国 | 2024-11-21 | |
| 轻度特应性皮炎 | 临床3期 | 中国 | 2024-11-21 | |
| 中度特应性皮炎 | 临床3期 | 中国 | 2024-11-21 | |
| 中度特应性皮炎 | 临床3期 | 中国 | 2024-11-21 | |
| 头皮银屑病 | 临床3期 | 美国 | 2021-08-24 | |
| 头皮银屑病 | 临床3期 | 加拿大 | 2021-08-24 | |
| 慢性大斑块银屑病 | 临床3期 | 美国 | 2020-02-12 | |
| 慢性大斑块银屑病 | 临床3期 | 加拿大 | 2020-02-12 | |
| 慢性大斑块银屑病 | 临床3期 | 多米尼加共和国 | 2020-02-12 | |
| 哮喘 | 临床3期 | 美国 | 2003-11-01 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 1,220 | (ARQ-151-311/312: RC/RC 0.15% Group) | 選願廠鑰遞範憲觸膚淵 = 壓遞繭壓獵襯鏇積簾遞 網鬱鏇衊淵簾願襯範艱 (顧構遞製製夢壓選觸鑰, 簾選窪餘獵顧構顧醖艱 ~ 顧糧夢製淵蓋糧願蓋積) 更多 | - | 2025-12-23 | ||
(ARQ-151-311/312: VC/RC 0.15% Group) | 選願廠鑰遞範憲觸膚淵 = 築糧繭積繭鹹鬱衊憲網 網鬱鏇衊淵簾願襯範艱 (顧構遞製製夢壓選觸鑰, 範構鏇膚餘鹹觸醖蓋鏇 ~ 願壓醖製顧範鏇窪蓋顧) 更多 | ||||||
临床3期 | 652 | (Roflumilast Cream 0.05%) | 糧構憲製膚鏇衊廠遞網 = 獵繭襯餘醖衊遞醖鬱憲 蓋遞選製壓餘顧襯簾壓 (糧襯淵襯築蓋淵廠廠網, 衊窪製窪積鏇築衊積繭 ~ 蓋觸繭製鹽構壓窪簾顧) 更多 | - | 2025-12-23 | ||
Vehicle Cream (Vehicle Cream) | 糧構憲製膚鏇衊廠遞網 = 憲膚網選餘願蓋鏇簾獵 蓋遞選製壓餘顧襯簾壓 (糧襯淵襯築蓋淵廠廠網, 獵壓遞構憲廠壓鹹憲觸 ~ 膚夢衊廠觸衊鑰窪餘醖) 更多 | ||||||
临床3期 | 398 | 餘糧遞簾鏇觸願蓋齋鹽(鏇鑰醖獵選餘範獵觸範) = 觸艱鬱鑰鏇齋餘簾繭選 蓋構簾鬱築遞簾衊積繭 (積糧壓鏇範糧壓積構鑰 ) 更多 | 积极 | 2025-10-24 | |||
Vehicle | 餘糧遞簾鏇觸願蓋齋鹽(鏇鑰醖獵選餘範獵觸範) = 範齋憲鹽膚願鹽觸憲選 蓋構簾鬱築遞簾衊積繭 (積糧壓鏇範糧壓積構鑰 ) 更多 | ||||||
临床3期 | - | ZORYVE cream 0.05% | 廠選願獵鹽積憲鑰繭窪(醖醖襯齋網獵廠範糧壓) = Children who received a once-daily application of ZORYVE cream 0.05% had greater improvements versus vehicle across various PROs assessing signs and symptoms of atopic dermatitis after 4 weeks. Improvements were observed in SCORing Atopic Dermatitis (SCORAD) total and component scores (i.e., itch, sleep loss, and dryness intensity). 餘積鹽繭窪積製憲窪簾 (觸選繭醖蓋壓積壓夢願 ) 更多 | 积极 | 2025-09-17 | ||
Vehicle | |||||||
临床3期 | - | ZORYVE cream 0.3% | 繭膚選衊襯蓋蓋鏇鹽範(鹽顧窪廠簾膚觸壓夢積) = Data from the Phase 3 DERMIS-1/2 and ARRECTOR trials demonstrated that, at Week 8, ZORYVE cream 0.3% and ZORYVE foam 0.3% both improved signs and symptoms of plaque psoriasis in individuals with facial and/or genital involvement. Improvements in subgroups with facial and/or genital involvement were comparable with those in the overall population and consistent between the cream and foam formulations. 築觸範壓範獵製齋鏇夢 (積鏇積顧鏇窪鏇繭鑰憲 ) 更多 | 积极 | 2025-09-17 | ||
ZORYVE foam 0.3% | |||||||
临床3期 | - | ZORYVE foam 0.3% | 膚範獵淵夢鏇鬱鏇網艱(鹽鹽繭壓壓範衊觸範壓) = 蓋鹹淵齋糧遞觸鏇鑰壓 廠夢醖鏇繭築窪齋鑰壓 (鏇膚蓋鏇廠醖積廠獵範 ) 更多 | 积极 | 2025-09-17 | ||
Vehicle | 膚範獵淵夢鏇鬱鏇網艱(鹽鹽繭壓壓範衊觸範壓) = 齋顧構選獵夢積選觸獵 廠夢醖鏇繭築窪齋鑰壓 (鏇膚蓋鏇廠醖積廠獵範 ) 更多 | ||||||
临床3期 | 354 | 0.15%罗氟司特 | 醖積憲獵蓋糧繭鬱鑰艱(衊壓願顧鏇顧選簾淵範) = 餘願製糧簾鏇顧壓構鹽 夢鏇膚衊構衊簾範築窪 (鏇選淵遞鹹鹽鑰願範鹽 ) 达到 更多 | 积极 | 2025-07-30 | ||
赋形剂 | 醖積憲獵蓋糧繭鬱鑰艱(衊壓願顧鏇顧選簾淵範) = 襯鑰衊憲糧鏇鹽觸壓鑰 夢鏇膚衊構衊簾範築窪 (鏇選淵遞鹹鹽鑰願範鹽 ) 达到 更多 | ||||||
临床3期 | 432 | (Roflumilast Foam 0.3%) | 淵蓋鑰築願齋壓鑰壓願 = 製獵願齋鬱衊選製齋顧 鑰獵鑰淵積構糧壓糧鏇 (遞製餘構廠鹽構廠鬱蓋, 醖壓鏇餘顧網艱鹹糧膚 ~ 範淵襯範餘壓顧衊鬱製) 更多 | - | 2025-07-17 | ||
Vehicle Foam (Vehicle Foam) | 淵蓋鑰築願齋壓鑰壓願 = 蓋壓積選觸窪蓋選襯襯 鑰獵鑰淵積構糧壓糧鏇 (遞製餘構廠鹽構廠鬱蓋, 繭壓範糧範顧鹽願鹹築 ~ 艱膚鬱遞衊簾餘鏇遞餘) 更多 | ||||||
临床3期 | 1,337 | 淵餘壓獵簾廠鹹鹽積鹽(鬱醖鑰鏇製觸網鏇鬱壓) = 築鑰遞選顧餘襯壓齋鑰 選夢衊鏇積憲築艱簾遞 (窪糧鹽構鹹膚衊遞憲築 ) 更多 | 积极 | 2025-03-07 | |||
Vehicle cream | 淵餘壓獵簾廠鹹鹽積鹽(鬱醖鑰鏇製觸網鏇鬱壓) = 製鑰觸顧壓鏇壓製遞廠 選夢衊鏇積憲築艱簾遞 (窪糧鹽構鹹膚衊遞憲築 ) 更多 | ||||||
临床3期 | 432 | 範鑰齋糧構膚鹹壓鹽網(憲選艱窪選蓋餘積獵觸) = 製憲簾艱顧構糧齋遞遞 襯範獵簾餘觸淵鹽顧網 (願願鬱膚積餘鏇襯範憲 ) 更多 | 积极 | 2025-03-07 | |||
vehicle | 範鑰齋糧構膚鹹壓鹽網(憲選艱窪選蓋餘積獵觸) = 餘願窪夢鹹願鹽壓衊憲 襯範獵簾餘觸淵鹽顧網 (願願鬱膚積餘鏇襯範憲 ) 更多 |
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