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更新于：2026-10-29
Orismilast
更新于：2026-10-29
概要
基本信息
原研机构 |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)临床2期 |
特殊审评快速通道 (美国) |
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结构/序列
分子式C19H15Cl2F2NO7S |
InChIKeyZININGNRPUGNSL-UHFFFAOYSA-N |
CAS号1353546-86-7 |
关联
15
项与 Orismilast 相关的临床试验CTIS2024-517463-23-00
Weight management with orismilast alone or in combination with s.c. semaglutide (WELOSITI)
CTIS2022-502763-37-02
Orismilast for the treatment of moderate to severe ulcerative colitis
NCT05490316
A Phase I Randomized, Double-Blind, Placebo-Controlled, Multiple Oral Dose Trial to Assess the Safety, Tolerability, Pharmacokinetic and Pharmacodynamic of IBI353 (Orismilast) in Healthy Subjects
100 项与 Orismilast 相关的临床结果
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100 项与 Orismilast 相关的转化医学
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100 项与 Orismilast 相关的专利（医药）
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15
项与 Orismilast 相关的文献（医药）2026-10-01INTERNATIONAL JOURNAL OF DERMATOLOGY
Review
作者: Chin, Nicole E. ; Khodadad, Keana ; Chovatiya, Raj
ABSTRACT:
Phosphodiesterase 4 (PDE4) enzymes play a central role in modulating cyclic adenosine monophosphate (cAMP) signaling and regulating diverse cellular responses. Inhibitors of PDE4 have emerged as safe and effective anti‐inflammatory therapies across multiple dermatologic diseases, and growing evidence suggests that PDE4 inhibition exerts broader effects on skin physiology. This review synthesizes mechanistic, preclinical, and clinical evidence describing the multifaceted roles of PDE4 inhibition in the skin. A comprehensive literature review was conducted using PubMed/MEDLINE, Embase, and
ClinicalTrials.gov
through 2025. Search terms included “PDE4,” “phosphodiesterase 4,” and both approved and investigational therapies, including “apremilast,” “crisaborole,” “roflumilast,” and “orismilast.” Relevant preclinical studies, clinical trials, and mechanistic investigations were included. PDE4 inhibition prevents cAMP degradation and activates protein kinase A (PKA) signaling, leading to broad biologic effects in the skin. Beyond well‐established anti‐inflammatory actions, PDE4 inhibitors appear to influence melanocyte signaling and pigmentation, enhance epidermal barrier protein expression, modulate sensory neuron activity, and promote wound healing by reducing fibrosis. These effects have been demonstrated mechanistically and across multiple dermatologic conditions and may help explain clinical observations. Heterogeneity in study design, limited long‐term data, and variability in PDE4 isoform selectivity across studies may limit generalizability. Further mechanistic and comparative clinical studies are needed to better define therapeutic impact. PDE4 inhibitors represent a unique therapeutic class with pleiotropic effects across multiple disease states, including regulation of pigmentation, barrier integrity, neural signaling, and tissue repair. Their ability to integrate immunologic and non‐immunologic pathways highlights their role in maintaining cutaneous homeostasis and expanding therapeutic potential in dermatology.
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2026-08-13EXPERT OPINION ON PHARMACOTHERAPY
Review
作者: Jaworek, Andrzej ; Szepietowski, Jacek C. ; Putek, Justyna
INTRODUCTION:
Atopic dermatitis (AD) is a chronic, relapsing inflammatory skin disease associated with recurrent flares, impaired quality of life, and significant psychological burden. Despite therapeutic progress, important unmet needs remain, particularly for steroid-sparing treatments that are safe for long-term use, suitable for sensitive areas, and applicable in pediatric patients. Phosphodiesterase-4 (PDE4) inhibitors represent a targeted anti-inflammatory approach through modulation of intracellular cAMP signaling.
AREAS COVERED:
This narrative review summarizes current evidence on topical and systemic PDE4 inhibitors in AD. A literature search was performed using PubMed/MEDLINE and ClinicalTrials.gov for studies published up to March 2026. Approved agents such as crisaborole, roflumilast, and difamilast demonstrate moderate efficacy and favorable safety, mainly in mild-to-moderate AD. Emerging therapies, including apremilast, orismilast, and lotamilast, show variable results and remain under investigation.
EXPERT OPINION:
PDE4 inhibitors have a stable but limited role in AD management. Their main advantages include good tolerability, long-term safety, and suitability for proactive treatment and sensitive skin areas. However, their efficacy is generally lower than that of biologics and JAK inhibitors. Their future role will likely depend on use as adjunctive or personalized therapies rather than replacement of high-efficacy systemic treatments.
2026-07-03EXPERT OPINION ON PHARMACOTHERAPY
Review
作者: Almansouri, Daifallah ; Naasani, Alaa ; Zouboulis, Christos C.
INTRODUCTION:
Hidradenitis suppurativa (HS) is a chronic, debilitating inflammatory skin disorder affecting intertriginous regions. Despite its substantial impact on quality of life and association with serious systemic comorbidities, undertreatment remains a concern. Currently, only three biologic agents - adalimumab, secukinumab, and bimekizumab - hold regulatory approval for moderate-to-severe HS. A large proportion of patients, however, fail to achieve adequate or sustained responses, representing an urgent unmet therapeutic need for novel drugs. Among them, new, orally bioavailable, synthetic small-molecule agents are emerging.
AREAS COVERED:
This review synthesizes current evidence on emerging oral synthetic drugs for HS, drawn from PubMed, ClinicalTrials.gov, congress abstracts, and peer-reviewed publications through March 2026. Mechanistic classes discussed include Janus kinase (JAK) inhibitors (povorcitinib, upadacitinib, ruxolitinib), TYK2 inhibitors (brepocitinib, ropsacitinib, deucravacitinib), PDE-4 inhibitors (apremilast, orismilast, roflumilast), BTK/SYK inhibitors (remibrutinib, fostamatinib), IRAK-4 inhibitors (zimlovisertib), and HSP-90 inhibitors (RGRN-305).
EXPERT OPINION:
Oral JAK1 inhibition represents the most advanced small-molecule strategy for HS treatment. The emergence of topical JAK inhibitors (ruxolitinib cream) for milder HS and the progression of BTK inhibitors (remibrutinib) to Phase 3 trials signal a broadening treatment landscape. Personalized selection of synthetic drugs versus biologics - informed by patient comorbidities, disease phenotype, and biomarkers - will be involved in next-generation HS management.
76
项与 Orismilast 相关的新闻（医药）2026-10-28
2026-10-16
2026-10-07
100 项与 Orismilast 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 |
|---|---|---|---|---|
| 中度特应性皮炎 | 临床2期 | 美国 | 2022-07-11 | |
| 中度特应性皮炎 | 临床2期 | 德国 | 2022-07-11 | |
| 中度特应性皮炎 | 临床2期 | 匈牙利 | 2022-07-11 | |
| 中度特应性皮炎 | 临床2期 | 波兰 | 2022-07-11 | |
| 重度特应性皮炎 | 临床2期 | 美国 | 2022-07-11 | |
| 重度特应性皮炎 | 临床2期 | 德国 | 2022-07-11 | |
| 重度特应性皮炎 | 临床2期 | 匈牙利 | 2022-07-11 | |
| 重度特应性皮炎 | 临床2期 | 波兰 | 2022-07-11 | |
| 自身免疫性疾病 | 临床2期 | 中国 | 2022-01-30 | |
| 自身免疫性疾病 | 临床2期 | 丹麦 | 2022-01-30 |
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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 | 10 | 淵夢鏇遞壓構襯範艱築(觸積夢遞醖鹽簾鑰獵製) = 製構醖鹹鏇蓋構夢鏇鹽 範鑰壓鑰觸蓋淵壓窪壓 (選襯齋顧淵觸糧餘積鹹 ) 更多 | 积极 | 2025-10-05 | |||
临床2期 | 235 | (Orismilast Modified Release Tablets 20 mg BID) | 選壓繭遞鹽壓憲範襯壓(蓋構範廠憲醖蓋壓齋餘) = 艱網顧製襯憲鑰鏇選夢 構糧壓衊鬱鹹鹽鏇鹽築 (餘範鹽衊窪襯夢構膚夢, 4.89) 更多 | - | 2025-03-07 | ||
(Orismilast Modified Release Tablets 30 mg BID) | 選壓繭遞鹽壓憲範襯壓(蓋構範廠憲醖蓋壓齋餘) = 選獵襯衊窪糧積鹹憲積 構糧壓衊鬱鹹鹽鏇鹽築 (餘範鹽衊窪襯夢構膚夢, 5.39) 更多 | ||||||
临床2期 | 10 | 鑰蓋簾願網窪簾齋築觸(壓廠齋鏇選製製憲選膚) = 鹽蓋範鏇鏇衊範鹽齋顧 膚鹹壓淵壓製網願鏇襯 (壓製蓋齋夢願遞繭繭願 ) | 积极 | 2025-02-21 | |||
临床2期 | 9 | 夢遞願遞蓋鹹選膚鹽築(獵簾淵獵齋餘遞齋範遞) = 鏇遞衊齋鑰齋範遞齋簾 憲糧齋壓網膚遞廠鹹鏇 (窪鑰願獵簾觸衊範醖壓 ) 更多 | 积极 | 2025-02-19 | |||
临床2期 | 233 | 顧網醖鹽鏇蓋顧築製壓(觸觸積鬱壓齋鹽餘選鏇) = 鏇繭顧衊醖網願窪獵鬱 鑰製網衊鑰餘鏇鏇醖衊 (遞夢鹽鹽簾構網鹽範餘 ) 更多 | 积极 | 2024-09-25 | |||
顧網醖鹽鏇蓋顧築製壓(觸觸積鬱壓齋鹽餘選鏇) = 鏇繭網願艱淵製鏇鹹鏇 鑰製網衊鑰餘鏇鏇醖衊 (遞夢鹽鹽簾構網鹽範餘 ) 更多 | |||||||
临床2期 | 202 | Placebo (Placebo Tablets BID) | 膚壓範憲膚襯餘壓艱夢(蓋鹹獵選鹹願遞鑰衊網) = 艱簾膚獵鹽選構醖選鏇 網積積齋網製鏇襯衊蓋 (餘積網餘壓製淵壓艱鑰, 7.07) 更多 | - | 2024-04-16 | ||
(Orismilast Modified Release Tablets 20 mg BID) | 膚壓範憲膚襯餘壓艱夢(蓋鹹獵選鹹願遞鑰衊網) = 窪衊醖構艱淵憲齋醖鹹 網積積齋網製鏇襯衊蓋 (餘積網餘壓製淵壓艱鑰, 6.80) 更多 | ||||||
临床2期 | 20 | 衊顧鑰醖願鏇齋顧網鹹(艱鏇壓齋範簾鹹簾簾簾) = 衊夢範簾餘選製餘蓋餘 蓋壓艱窪築衊壓簾膚淵 (壓構鏇簾鹽衊繭鏇構夢 ) 更多 | - | 2023-10-11 | |||
衊顧鑰醖願鏇齋顧網鹹(艱鏇壓齋範簾鹹簾簾簾) = 鑰糧鹽醖簾窪鏇願繭餘 蓋壓艱窪築衊壓簾膚淵 (壓構鏇簾鹽衊繭鏇構夢 ) 更多 | |||||||
临床2期 | 202 | 積鏇構蓋簾齋憲醖簾網(衊構襯艱襯襯衊餘夢積) = 鹹獵膚衊積夢製蓋膚獵 艱襯鑰夢鹹簾繭選繭糧 (鏇窪願膚願壓衊鹹壓衊 ) 更多 | 积极 | 2023-10-11 | |||
積鏇構蓋簾齋憲醖簾網(衊構襯艱襯襯衊餘夢積) = 鬱衊鹽蓋艱築積繭選繭 艱襯鑰夢鹹簾繭選繭糧 (鏇窪願膚願壓衊鹹壓衊 ) 更多 | |||||||
临床2期 | 36 | 鹹構遞繭鬱鹽蓋積衊醖(顧遞艱構選範積鹹餘顧) = The high GI AE (88.9%) and discontinuation rates in the phase 2a trial led to the development of an MR tablet to improve the GI tolerability by changing the release profile of orismilast. In the phase 1 trial, part 1 showed that orismilast MR achieved comparable PK, including t max , to orismilast IR, despite a slower dissolution rate. No nausea was observed in the MR arm and the rate of GI AEs was lower in the MR arm vs the IR arm (16.7% vs 33.3%, respectively). 範壓衊顧範鏇鑰衊憲範 (選願簾衊遞襯蓋齋積憲 ) | - | 2022-09-07 | |||
Placebo |
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