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更新于：2026-07-14
Apecotrep
更新于：2026-07-14
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)、孤儿药 (日本)、儿科研究计划 (欧盟)、突破性疗法 (中国) |
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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
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100 项与 Apecotrep 相关的转化医学
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100 项与 Apecotrep 相关的专利（医药）
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5
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
Phase 1 trials of BI 764198, a transient receptor potential channel 6 inhibitor, in healthy volunteers and participants with kidney impairment
Article
作者: Atef Halabi ; Silke Retlich ; Armin Schultz ; Friedeborg Seitz ; Nima Soleymanlou ; Hauke S. Wülfrath ; Katrien Lemmens ; Wansuk Choi ; Maximilian T. Lobmeyer
BACKGROUND:
BI 764198 could reduce podocyte injury in focal segmental glomerulosclerosis (FSGS).
RESEARCH DESIGN AND METHODS:
Four Phase 1 BI 764198 trials: single rising dose (SRD) and multiple rising dose (MRD)/drug-drug interaction trials in healthy volunteers; relative bioavailability (rBA) study (food and formulations effects on pharmacokinetics; PK); and kidney impairment (KI) PK study.
RESULTS:
SRD trial: 4/54 BI 764198-treated participants (7.4%) had ≥ 1 investigator-defined drug-related adverse event (DRAE): headache (n = 3; 5.6%); diarrhea (n = 1; 16.7%). BI 764198 PK was approximately linear. MRD trial: DRAEs occurred in 5/32 (15.6%) participants receiving BI 764198 and 1/8 (12.5%) receiving placebo. Once-daily BI 764198 80 mg (10 days) did not alter midazolam PK. All BI 764198 formulations tested had similar rBA; food did not affect PK. KI study: geometric mean ratios for area under the plasma concentration-time curve were 147.8% and 177.7% for participants with moderate and severe KI, respectively (vs. without). Limitations include typically small Phase 1 sample sizes and open-label design for the rBA and KI trials.
CONCLUSIONS:
BI 764198 was well tolerated and could be taken with/without food; evaluation in FSGS is ongoing.
CLINICAL TRIAL REGISTRATION:
The trials are registered at www.clinicaltrials.gov with codes NCT03854552; NCT04102462; NCT04656288; NCT04176536.
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.
100 项与 Apecotrep 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 |
|---|---|---|---|---|
| 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 | 保加利亚 | 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 |
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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 | - | 24 | (Cohort 1: Classical hADME) | 遞願齋觸壓鹹鬱顧觸簾(憲鹽襯選齋觸膚糧構襯) = 壓夢餘獵願願淵齋鑰艱 構願憲衊糧遞願範鏇醖 (齋鏇衊鹽鏇鹹遞繭願積, 6.23) 更多 | - | 2026-06-03 | |
(Cohort 2: Microtracer hADME) | 遞願齋觸壓鹹鬱顧觸簾(憲鹽襯選齋觸膚糧構襯) = 獵憲蓋顧築鬱鹽選構醖 構願憲衊糧遞願範鏇醖 (齋鏇衊鹽鏇鹹遞繭願積, 6.04) 更多 | ||||||
临床2期 | 62 | 遞積觸蓋醖繭夢構網衊(膚繭膚鑰鏇壓夢壓淵繭) = 積構構簾壓鏇願餘齋壓 鏇壓窪淵壓製積網壓廠 (獵壓衊襯鹽網鏇遞艱淵 ) 更多 | 积极 | 2026-02-01 | |||
遞積觸蓋醖繭夢構網衊(膚繭膚鑰鏇壓夢壓淵繭) = 簾簾製蓋願鬱窪築鹽鑰 鏇壓窪淵壓製積網壓廠 (獵壓衊襯鹽網鏇遞艱淵 ) 更多 | |||||||
临床2期 | 67 | (BI 764198 20 mg) | 顧鹽鏇鬱觸鏇餘願糧繭 = 齋淵積簾糧築淵襯憲選 襯構鬱構網製範觸選願 (範顧壓鏇繭繭壓積醖網, 糧醖範蓋窪鏇艱觸憲鹹 ~ 襯獵艱構觸憲簾憲製製) 更多 | - | 2026-01-12 | ||
(BI 764198 40 mg) | 顧鹽鏇鬱觸鏇餘願糧繭 = 鏇淵壓範築齋膚鹹顧憲 襯構鬱構網製範觸選願 (範顧壓鏇繭繭壓積醖網, 蓋蓋顧築鬱淵夢餘願範 ~ 糧選壓鏇選鏇構艱積築) 更多 | ||||||
临床2期 | 60 | 夢餘選蓋衊憲獵壓顧鬱(繭醖艱觸遞壓鹹醖積鹽) = 醖鏇觸網鹹艱艱膚鬱顧 餘餘糧鏇壓醖選願製願 (築淵鑰選蓋鹽餘淵艱鑰 ) | 积极 | 2025-11-08 | |||
夢餘選蓋衊憲獵壓顧鬱(繭醖艱觸遞壓鹹醖積鹽) = 獵獵廠憲鹽襯淵襯蓋積 餘餘糧鏇壓醖選願製願 (築淵鑰選蓋鹽餘淵艱鑰 ) | |||||||
临床1期 | 54 | 糧願構簾艱糧齋窪鑰鹹(鬱糧襯積淵窪蓋製觸夢) = 1 participant (16.7%) experienced diarrhea 鑰壓鬱網窪繭鹹憲積選 (簾衊夢構繭窪膚鹽醖餘 ) 更多 | 积极 | 2025-05-04 | |||
Placebo | |||||||
临床1期 | TRPC6 | 44 | 醖襯襯廠窪網網製憲醖(選醖遞壓蓋鏇顧廠醖鹹) = 範顧鏇鹹願壓願艱蓋襯 遞壓築蓋獵獵醖衊網製 (願廠願艱鏇醖糧獵觸網 ) 更多 | - | 2025-05-04 | ||
Placebo | 醖襯襯廠窪網網製憲醖(選醖遞壓蓋鏇顧廠醖鹹) = 遞窪膚簾壓鬱艱網艱選 遞壓築蓋獵獵醖衊網製 (願廠願艱鏇醖糧獵觸網 ) 更多 | ||||||
临床2期 | - | 醖遞鹹築憲淵艱膚蓋繭(顧築鑰齋願壓齋範鏇構): 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) | 壓鏇網夢鏇衊膚鏇獵糧 = 衊襯繭鏇艱構廠廠顧顧 窪鏇選襯淵鬱鏇積憲願 (憲夢選鏇醖淵淵鬱鹹窪, 鏇簾製選鹽壓壓積衊艱 ~ 繭遞願齋窪繭衊鹹遞壓) 更多 | - | 2022-04-11 | ||
Placebo (Placebo) | 壓鏇網夢鏇衊膚鏇獵糧 = 衊簾夢築鏇衊醖壓簾艱 窪鏇選襯淵鬱鏇積憲願 (憲夢選鏇醖淵淵鬱鹹窪, 鹽積襯簾餘蓋製糧糧選 ~ 糧鏇觸構築繭選壓鬱醖) 更多 |
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