预约演示
更新于：2026-04-07
Apecotrep
更新于：2026-04-07
概要
基本信息
药物类型 小分子化药 |
别名 [4-(6-aminopyridazin-3-yl)piperidin-1-yl][5-(4-fluorophenoxy)-4-methoxypyridin-2-yl]methanone、阿佩可普、BI 764198 + [2] |
靶点 |
作用方式 拮抗剂 |
作用机制 TRPC6拮抗剂(transient receptor potential cation channel subfamily C member 6 antagonists) |
在研适应症 |
非在研机构- |
权益机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评孤儿药 (欧盟)、突破性疗法 (中国)、孤儿药 (日本)、儿科研究计划 (欧盟) |
登录后查看时间轴
关联
14
项与 Apecotrep 相关的临床试验NCT07355296
PODOMOUNT-Basket, a Phase II, Multicentre, Randomised, 2-arm Parallel-group, Double-blind, Placebo-controlled Basket Trial to Assess Safety, Tolerability, PK, and Efficacy of BI 764198 in Four Proteinuric Kidney Diseases
NCT07220083
A Multicentre, Randomised, Double-blind, Parallel Group, Placebo-controlled Trial to Assess the Effects of Oral TRPC6 Inhibitor BI 764198 Taken Over a 104 Week Treatment Period in Adult and Adolescent Participants With Primary Focal Segmental Glomerulosclerosis (pFSGS) or Genetic FSGS Related to TRPC6 Gene Variants
NCT07308652
The Effect of Multiple Doses of Itraconazole on the Single-dose Pharmacokinetics of BI 764198 Following Oral Administration in Healthy Male Trial Participants (an Open-label, Non-randomised, Two-period, Fixed-sequence Design Study)
100 项与 Apecotrep 相关的临床结果
登录后查看更多信息
100 项与 Apecotrep 相关的转化医学
登录后查看更多信息
100 项与 Apecotrep 相关的专利（医药）
登录后查看更多信息
4
项与 Apecotrep 相关的文献（医药）2026-02-01LANCET
TRPC6 inhibition for the treatment of focal segmental glomerulosclerosis: a randomised, placebo-controlled, phase 2 trial of BI 764198
Article
作者: Kretzler, Matthias ; Prasad, Srinivasa ; Cross, Nicholas ; Gesualdo, Loreto ; Licarião Rocha, Fabia T ; Retlich, Silke ; Trachtman, Howard ; Kaufeld, Jessica ; Ye, Zhiming ; Meijers, Björn ; Lobmeyer, Maximilian T ; Chen, Qinkai ; Derebail, Vimal K ; Soleymanlou, Nima ; Ng, Monica Suet Ying ; Ji, Bo ; Workeneh, Biruh
BACKGROUND:
In focal segmental glomerulosclerosis (FSGS), transient receptor potential cation channel, subfamily C, member 6 (TRPC6) overactivity might cause podocyte loss and progressive kidney function decline. This exploratory study assessed the safety and efficacy of a novel once-daily oral selective TRPC6 inhibitor, BI 764198.
METHODS:
This multicentre phase 2, double-blind, placebo-controlled, randomised controlled trial assessed BI 764198 (20 mg, 40 mg, or 80 mg once daily) versus placebo over 12 weeks in participants aged 18-75 years with biopsy-confirmed primary FSGS (based on the absence of clinical evidence of secondary cause) or with a disease-causing TRPC6 variant. The study took place in 31 sites in ten countries, and random allocation was performed centrally in blocks in a 1:1:1:1 ratio and was stratified according to use of corticosteroids. Participants were receiving stable conservative and immunosuppressive therapy, with screening urine protein-creatinine ratio (UPCR) at 1·0 g/g or greater and estimated glomerular filtration rate at 30 mL/min per 1·73 m2 or greater. The primary endpoint was the proportion of participants with proteinuria response (≥25% UPCR reduction from baseline) at week 12. Other key outcomes were safety and tolerability. The study was registered with ClinicalTrials.gov on Jan 27, 2022 (NCT05213624) and is complete as of Jan 3, 2025.
FINDINGS:
From March 10, 2022, to Sept 3, 2024, 139 participants were screened and 67 were randomly assigned to receive placebo or BI 764198 at doses of 20 mg, 40 mg, or 80 mg (five participants were randomly assigned in error and were not treated). 62 participants received treatment, two of whom had missing baseline or post-baseline UPCR measurements and were not included in the full analysis set. Overall, 37 participants (60%) were male and 25 participants (40%) were female; the mean age was 40·7 years (SD 12·6); and the majority of the trial cohort were White (39 [63%] of 62). Proteinuria responses were observed in eight (44%) of 18, two (14%) of 14, and six (43%) of 14 participants receiving BI 764198 20 mg, 40 mg, and 80 mg, respectively (16 [35%] of 46 for all BI 764198 doses) versus one (7%) of 14 receiving placebo; corresponding odds ratios (ORs) versus placebo were OR 10·0 (95% CI 1·6-118·1), 1·5 (0·2-19·5), and 6·0 (0·9-73·6) for the three doses of BI 764198, and 4·9 (1·0-48·8) for all doses combined. BI 764198 was well tolerated with no meaningful differences in adverse event frequencies across treatment arms; treatment-emergent adverse events were reported by 44 (71%) of 62 participants, with similar frequencies of adverse events observed in the placebo group (ten [71%] of 14) and BI 764198 groups (34 [71%] of 48).
INTERPRETATION:
BI 764198 lowered proteinuria and was well tolerated by participants in this trial. This is the first evidence of efficacy with a podocyte-targeted therapy in FSGS. Larger randomised controlled trials over longer treatment durations, enabling meaningful subgroup analyses, are planned to evaluate the safety and efficacy of BI 764198 treatment in FSGS and other conditions affected by podocytopathy.
FUNDING:
Boehringer Ingelheim.
2025-05-04EXPERT OPINION ON INVESTIGATIONAL DRUGS
A randomized, Phase I study of the safety, tolerability, and pharmacokinetics of BI 764198, a transient receptor potential channel 6 (TRPC6) inhibitor, in healthy Japanese men
Article
作者: Tachibana, Yoshifumi ; Retlich, Silke ; Soleymanlou, Nima ; Sarashina, Akiko ; Yonemura, Takuma
BACKGROUND:
BI 764198 is a selective, oral transient receptor potential cation channel, subfamily C, member 6 inhibitor under investigation for focal segmental glomerulosclerosis.
RESEARCH DESIGN AND METHODS:
Phase I study in 44 Japanese male volunteers. Single dose part: BI 764198 20 mg (n = 6) vs. placebo (n = 2); multiple dose part: BI 764198 40, 80, or 160 mg (n = 9 each) or placebo (n = 9) as a single dose then multiple daily dosing for 2 weeks. Primary endpoint: participants with drug-related adverse events (DRAEs); secondary endpoints: pharmacokinetic.
RESULTS:
DRAEs were reported in 20.5% (9/44) of participants (total BI 764198 21.2% [7/33]; placebo 18.2% [2/11]), mostly diarrhea (total BI 764198 15.2% [5/33]; placebo 18.2% [2/11]) and headache (BI 764198 80 mg 11.1% [1/9]; BI 764198 160 mg 33.3% [3/9]). BI 764198 exposure increased near dose proportionally to 80 mg and was slightly higher than anticipated with 160 mg. Pharmacokinetics were similar in Asians and non-Asians after accounting for body weight. Limitations include small sample size per dose and short trial duration.
CONCLUSIONS:
BI 764198 was well tolerated; exposure increased near dose proportionally to 80 mg, as previously observed in predominantly White volunteers.
CLINICAL TRIAL REGISTRATION:
This study was registered on Clinical Trials.gov, identifier NCT04665700.
2023-12-01Kidney international reports
TRPC6 Inhibitor BI 764198 in Focal Segmental Glomerulosclerosis: Phase 2 Study Design
Article
作者: Desmond, Hailey E ; Kretzler, Matthias ; Choi, Wansuk ; Soleymanlou, Nima ; Trachtman, Howard ; Manuel, Raymond C
Focal segmental glomerulosclerosis (FSGS), a leading glomerular cause of kidney failure, is a histological pattern characterized by podocyte injury and depletion.1 FSGS is found in 20–30% of adults with nephrotic syndrome and up to 20% of patients receiving dialysis.2,S1 FSGS can be broadly categorized into four causative classifications: primary (idiopathic), secondary (adaptive), familial (genetic), and of unknown cause.1,3,S2 Depending on patient selection and region, genetic variants have been reported in up to 14% of individuals with adult-onset FSGS.
100 项与 Apecotrep 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 局灶性节段性肾小球硬化症 | 临床3期 | 美国 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 中国 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 日本 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 阿根廷 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 澳大利亚 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 比利时 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 巴西 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 加拿大 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 克罗地亚 | 2026-02-16 | |
| 局灶性节段性肾小球硬化症 | 临床3期 | 丹麦 | 2026-02-16 |
登录后查看更多信息
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 | 62 | 艱淵觸蓋積膚鹹鑰憲窪(範襯衊獵鑰衊壓窪膚餘) = 遞獵觸願襯憲繭構艱鹹 範遞糧鏇糧壓憲餘襯鏇 (簾簾簾蓋鬱鬱觸廠廠醖 ) 更多 | 积极 | 2026-02-01 | |||
艱淵觸蓋積膚鹹鑰憲窪(範襯衊獵鑰衊壓窪膚餘) = 鏇襯憲糧齋繭壓窪繭鹹 範遞糧鏇糧壓憲餘襯鏇 (簾簾簾蓋鬱鬱觸廠廠醖 ) 更多 | |||||||
临床2期 | 67 | (BI 764198 20 mg) | 築餘構網衊齋觸糧齋壓 = 遞獵壓衊齋窪製鹽鏇廠 廠鹽觸鬱夢範餘壓製鹹 (鹽膚範壓遞範築遞願鹽, 選遞築憲蓋襯積鬱夢夢 ~ 膚壓膚簾鑰網鏇窪襯醖) 更多 | - | 2026-01-12 | ||
(BI 764198 40 mg) | 築餘構網衊齋觸糧齋壓 = 醖夢鏇廠衊範壓衊壓衊 廠鹽觸鬱夢範餘壓製鹹 (鹽膚範壓遞範築遞願鹽, 製範願網網艱糧遞齋壓 ~ 繭糧構淵鹹鹹鏇鹹襯憲) 更多 | ||||||
临床2期 | 60 | 糧襯窪獵蓋積衊獵夢遞(顧範襯願鹽顧獵襯鬱齋) = 範醖窪築製鏇構構鑰齋 鏇築夢糧鹽壓鏇顧夢顧 (膚廠簾廠齋廠觸壓廠蓋 ) | 积极 | 2025-11-08 | |||
糧襯窪獵蓋積衊獵夢遞(顧範襯願鹽顧獵襯鬱齋) = 壓製膚蓋艱醖選獵淵艱 鏇築夢糧鹽壓鏇顧夢顧 (膚廠簾廠齋廠觸壓廠蓋 ) | |||||||
临床1期 | 54 | 繭艱齋齋夢網觸觸築範(鹹醖築鹽鏇壓壓築鏇簾) = 1 participant (16.7%) experienced diarrhea 範繭觸構鑰鏇襯鹹壓鏇 (餘遞積艱鹽艱餘糧鏇鏇 ) 更多 | 积极 | 2025-06-08 | |||
Placebo | |||||||
临床1期 | TRPC6 | 44 | 齋鏇願膚鏇願餘選鏇衊(鏇願憲繭襯膚艱醖廠鹽) = 遞簾鹹衊壓夢憲鹹襯製 顧鬱網觸顧構壓觸鹽窪 (製遞醖觸糧襯構醖範選 ) 更多 | - | 2025-05-04 | ||
Placebo | 齋鏇願膚鏇願餘選鏇衊(鏇願憲繭襯膚艱醖廠鹽) = 鹹積壓鑰糧繭淵鑰齋顧 顧鬱網觸顧構壓觸鹽窪 (製遞醖觸糧襯構醖範選 ) 更多 | ||||||
临床2期 | - | 淵壓憲顧構襯構願衊夢(壓鹹齋廠餘願繭鑰艱糧): days = 3.41 (95% CI, 0.49 ~ 6.34) 更多 | 不佳 | 2023-04-06 | |||
Placebo | |||||||
临床2期 | 133 | (BI 764198 Treatment Group) | 衊積衊網蓋製選膚鬱窪 = 構繭鑰觸淵淵構齋鹽蓋 網淵壓齋選簾築觸衊淵 (膚網憲糧壓遞齋廠顧鑰, 積衊廠遞範製顧膚願醖 ~ 壓鏇壓遞衊齋醖築膚構) 更多 | - | 2022-04-11 | ||
Placebo (Placebo) | 衊積衊網蓋製選膚鬱窪 = 餘糧壓窪糧製築選觸築 網淵壓齋選簾築觸衊淵 (膚網憲糧壓遞齋廠顧鑰, 鑰鹽憲獵構鏇膚衊遞選 ~ 簾齋鬱繭鹹鹹淵簾繭壓) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用