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更新于：2026-08-08
Ripretinib
瑞派替尼
更新于：2026-08-08
概要
基本信息
药物类型 小分子化药 |
别名 Ripretinib (USAN)、里普替尼、DCC-2618 + [2] |
作用方式 抑制剂 |
作用机制 PDGFRα抑制剂(血小板衍生生长因子受体α抑制剂)、c-Kit抑制剂(干细胞生长因子受体抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2020-05-15), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、快速通道 (美国)、孤儿药 (美国)、附条件批准 (中国)、孤儿药 (日本)、孤儿药 (澳大利亚)、优先审评 (澳大利亚)、优先审评 (中国) |
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结构/序列
分子式C24H21BrFN5O2 |
InChIKeyCEFJVGZHQAGLHS-UHFFFAOYSA-N |
CAS号1442472-39-0 |
关联
17
项与 瑞派替尼 相关的临床试验NCT07618377
A Phase 1 Study to Evaluate the Safety of DCC-2618 in Patients With Unresectable, Metastatic, or Recurrent Gastrointestinal Stromal Tumor (GIST) Who Are Refractory or Intolerant to at Least 3 Prior Therapies
NCT06619275
Ripretinib in Patients With Previously Treated Advanced Gastrointestinal Stromal Tumor (GIST): a Prospective, Longitudinal, Multicenter, Observational Study in Germany
CTIS2022-501477-40-00
A study to learn the effects of ripretinib (study drug) on how midazolam behaves in the body of people with advanced gastrointestinal stromal tumor
100 项与 瑞派替尼 相关的临床结果
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100 项与 瑞派替尼 相关的转化医学
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100 项与 瑞派替尼 相关的专利（医药）
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194
项与 瑞派替尼 相关的文献（医药）2026-12-31Future Science OA
A comprehensive analysis of the adverse drug events of metastatic and unresectable gastrointestinal stromal tumor treatment options: avapritinib, imatinib, regorafenib, ripretinib, and sunitinib safety insights and implications
Article
作者: Andrews, Michael B. ; Thompson, Cameron M. ; Adler, Douglas G.
BACKGROUND:
Treatments for metastatic, unresectable, or treatment-resistant gastrointestinal stromal tumors (GIST) include avapritinib, imatinib, regorafenib, ripretinib, and sunitinib. The FDA Adverse Event Reporting System (FAERS) database collects medication-related adverse events (AEs).
DESIGN AND METHODS:
Reports in the FAERS database from each medication's FDA approval to June 30, 2025 were analyzed. Reports containing other medications or indications outside of GIST treatment were excluded.
RESULTS:
Avapritinib was associated with fatigue (n = 826, 10.2%), nausea/vomiting (n = 574, 7.1%), eye/facial swelling (n = 631, 7.8%), diarrhea n = 361, 4.5%), peripheral edema (n = 231, 2.5%). Imatinib was associated with nausea/vomiting (n = 677, 4.4%), fatigue (n = 549, 3.6%), anemia (n = 404, 2.6%), abdominal pain (n = 400, 2.6%), and rash (n = 340, 2.2%), hemorrhage (317 AEs, 2.1%). Regorafenib was associated with fatigue (n = 104, 8.6%), palmar-plantar erythrodyesthesia syndrome (n = 66, 5.4%), diarrhea (n = 60, 4.9%). Ripretinib was associated with fatigue (n = 534, 8.4%), alopecia (n = 355, 5.6%), nausea/vomiting (n = 273, 4.3%). Sunitinib was associated with fatigue (n = 420, 6.1%%), nausea/vomiting (n = 284, 4.2%), diarrhea (n = 262, 3.8 %), hemorrhage (n = 149, 2.2%).
CONCLUSIONS:
The FAERS database revealed multiorgan AEs associated with five GIST treatment medications. Novel findings include eye/facial and peripheral edema with avapritinib, palmar-plantar erythrodyesthesia syndrome, headache/migraine, and gait abnormalities across all five medications, pancytopenia with imatinib, and hemorrhage with imatinib and sunitinib.
2026-07-01JOURNAL OF CUTANEOUS PATHOLOGY
Benign Keratoses With Inverted Follicular Keratosis‐Like Features in a Patient Receiving Ripretinib: A Case Report
Article
作者: Curry, Jonathan L. ; Aung, Phyu P. ; Kundert, Peter N. ; Perkins, Benjamin H. ; George, Saira ; Ibrahim, Elsayed
ABSTRACT:
Inverted follicular keratosis (IFK) is a rare benign neoplasm of the follicular infundibulum and typically presents as a solitary, nonpigmented verrucous papule on the head and neck of older males and can mimic viral warts, basal cell carcinoma (BCC), or squamous cell carcinoma (SCC). We report a case of multiple benign keratoses with IFK‐like features in an 82‐year‐old woman undergoing ripretinib therapy for metastatic gastrointestinal stromal tumor (GIST). Eight weeks into therapy, the patient developed multiple darkly pigmented, scaly, raised papules, primarily on the bilateral lower extremities. Histopathologic examination revealed a well‐circumscribed endophytic keratinocytic proliferation with a broad, smooth base and numerous squamous eddies. No significant cytologic atypia or brisk mitotic activity was observed. These findings supported a diagnosis of benign keratoses with IFK‐like features. The patient remains alive with stable disease 10 months after initiating ripretinib. No specific treatment was required for the benign keratoses with IFK‐like features, and ripretinib therapy was continued. Ripretinib, a switch control tyrosine kinase inhibitor that targets KIT and PDGFRA kinases, is associated with an increased risk of cutaneous neoplasms, including actinic keratosis, seborrheic keratosis, SCC, keratoacanthoma, and melanoma. Patients treated with small‐molecule inhibitors that target MAPK pathway may develop various keratinocytic dermatologic toxicities. To the best of our knowledge, this represents the first reported association between repretinib treatment and benign keratoses with IFK‐like features. Further studies are needed to clarify the clinical significance and biological implications of this observation.
2026-05-01AMERICAN JOURNAL OF PATHOLOGY
Epidermal Growth Factor Receptor/KIT-Linked Proliferative Bias in Normal Breast Lobules from Matched Non-Hispanic Black and White Women Is Rapidly Reversible by Receptor Tyrosine Kinase Inhibition
Article
作者: Arnold, Amanda ; Pacheco-Spann, Laura ; Cruz-Reyes, Nicole ; McLaughlin, Sarah ; Radisky, Derek C ; Winham, Stacey J ; Ogony, Joshua W ; Sherman, Mark E ; Degnim, Amy C
Basal-like/triple-negative breast cancers occur disproportionately at younger ages among non-Hispanic Black women (NHBW), but whether normal breast epithelium shows measurable, reversible differences in proliferative signaling is unclear. Histologically normal lobules from parity-, age-, and body mass index-matched NHBW and non-Hispanic White women (NHWW) donors (10 versus 10) were profiled using targeted transcriptomics (IO360/BC360) and whole-slide quantitative immunohistochemistry for epidermal growth factor receptor (EGFR), KIT, and cytokeratin-5. Eighty-nine transcripts differed between groups at false discovery rate < 0.10, with EGFR and KIT elevated in NHBW lobules and enrichment of basal/receptor tyrosine kinase-linked programs. Quantitative immunohistochemistry confirmed higher protein in NHBW tissue; in lobule-level models, the group effect (NHBW - NHWW) was EGFR β = 0.055, P = 0.010; KIT β = 0.093, P = 0.0027; and cytokeratin-5 β = 0.126, P = 0.027. In prestasis human mammary epithelial cells, 24-hour treatment with EGFR (lapatinib) or KIT (ripretinib) inhibitors increased cyclin-dependent kinase inhibitors, decreased cyclins/cyclin-dependent kinase 4/6, and enforced G1 arrest; EGFR inhibition also increased apoptosis. Together, these data identify a coordinated EGFR/KIT-linked proliferative bias in NHBW epithelium that is rapidly reversible in vitro, supporting validation in larger cohorts and pharmacodynamic window studies.
100 项与 瑞派替尼 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 |
|---|---|---|---|
| 胃肠道间质瘤 | 美国 | 2020-05-15 |
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 |
|---|---|---|---|---|
| 不可切除的胃肠道间质瘤 | 临床1期 | 日本 | 2026-07-07 | |
| 黑色素瘤 | 临床1期 | 美国 | 2015-11-01 | |
| 黑色素瘤 | 临床1期 | 加拿大 | 2015-11-01 | |
| 黑色素瘤 | 临床1期 | 德国 | 2015-11-01 | |
| 黑色素瘤 | 临床1期 | 意大利 | 2015-11-01 | |
| 黑色素瘤 | 临床1期 | 荷兰 | 2015-11-01 | |
| 黑色素瘤 | 临床1期 | 英国 | 2015-11-01 | |
| 系统性肥大细胞增多症 | 临床1期 | 美国 | 2015-11-01 | |
| 系统性肥大细胞增多症 | 临床1期 | 加拿大 | 2015-11-01 | |
| 系统性肥大细胞增多症 | 临床1期 | 德国 | 2015-11-01 |
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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
N/A | 30 | 餘範構壓壓鬱廠繭餘積(鬱廠廠構願築築獵觸蓋) = no grade ≥3 adverse events reported 繭簾醖鏇顧窪鬱鏇構製 (鏇鑰鏇鏇蓋糧醖齋積蓋 ) | 积极 | 2026-05-29 | |||
Combination therapy group (ripretinib 150 mg once daily plus sunitinib 25 mg once daily) | |||||||
临床2期 | 20 | 範餘簾夢積膚選壓範襯(艱蓋鏇鏇襯憲餘鹹顧構) = 觸顧構顧積製糧鏇壓顧 簾壓衊構選襯積範選蓋 (衊憲鑰選鏇膚醖膚淵選 ) 更多 | 积极 | 2026-05-29 | |||
N/A | 19 | 餘鬱齋醖憲繭憲遞遞窪(觸醖觸齋壓蓋糧衊積顧) = 顧淵壓鏇蓋範鹽構餘築 襯獵鑰構繭壓壓製遞築 (蓋夢齋積簾網獵觸顧鬱, 50.7 ~ NR) | 积极 | 2026-03-09 | |||
淵積網積鹹廠鬱鑰夢蓋(選簾壓網壓蓋鑰顧衊鹹) = 鹽淵蓋簾觸膚糧網鹹餘 衊顧壓醖糧膚願憲衊鬱 (簾鬱鏇構壓鹹繭築膚艱 ) | |||||||
临床2期 | 39 | 鏇鑰鑰選鑰膚鑰鹽艱構(願選壓壓糧憲繭壓壓襯) = 鏇夢壓鑰夢膚遞淵鏇鏇 築鏇簾鬱製襯構糧憲選 (觸廠壓遞鬱憲壓鹽築廠, 壓窪鹽醖齋窪遞淵糧顧 ~ 壓窪網鹹淵衊簾糧衊鬱) 更多 | - | 2025-03-03 | |||
临床2期 | 108 | (Ripretinib) | 膚觸鏇餘糧壓醖鹽鹹簾(範淵遞鑰鏇蓋齋壓餘構) = 艱廠憲壓襯遞製齋鬱顧 鏇構膚鑰顧夢顧憲網網 (鏇鹹簾構醖積範鏇鹽範, 壓齋鹹廠襯壓憲製繭淵 ~ 艱觸衊齋選範顧糧憲鹽) 更多 | - | 2025-01-15 | ||
(Sunitinib) | 膚觸鏇餘糧壓醖鹽鹹簾(範淵遞鑰鏇蓋齋壓餘構) = 壓構齋簾衊糧窪夢鏇網 鏇構膚鑰顧夢顧憲網網 (鏇鹹簾構醖積範鏇鹽範, 製簾蓋築範鑰蓋鑰衊膚 ~ 鏇醖餘觸醖繭簾網製繭) 更多 | ||||||
N/A | 12 | Ripretinib 150 mg | 壓窪積膚獵窪築顧築鹽(齋蓋蓋夢壓淵構齋願壓) = 憲鏇淵積壓構壓艱廠廠 鏇齋觸範艱願鬱襯壓積 (願艱壓淵壓鏇艱構簾窪 ) 达到 更多 | 积极 | 2024-12-07 | ||
临床2期 | 108 | 糧觸鬱壓顧夢構獵壓衊(衊蓋鏇範鹽鬱觸窪網鑰) = 網鹹遞鹽範繭鹹鏇網鑰 蓋遞簾遞壓淵繭網範餘 (膚淵獵壓壓憲齋憲鬱遞 ) 更多 | 积极 | 2024-09-14 | |||
Sunitinib 50 mg | 糧觸鬱壓顧夢構獵壓衊(衊蓋鏇範鹽鬱觸窪網鑰) = 願夢鏇餘窪鹹夢築窪襯 蓋遞簾遞壓淵繭網範餘 (膚淵獵壓壓憲齋憲鬱遞 ) 更多 | ||||||
临床3期 | KIT外显子11和18突变胃肠道间质瘤 | KIT外显子11和17突变胃肠道间质瘤 KIT Exon 17 Mutation | KIT Exon 18 Mutation | KIT Exon 11 Mutation | 52 | 淵願鬱膚願醖艱繭憲淵(廠積製蓋艱糧鏇簾遞獵) = 衊製獵積鏇遞觸衊願獵 製積襯壓憲鬱築鑰夢鏇 (獵簾顧觸醖觸餘簾衊鹽 ) 更多 | 积极 | 2024-03-15 | ||
临床3期 | 胃肠道间质瘤 二线 | 453 | 範淵製願夢夢築齋遞網(繭簾築醖鹽鬱遞窪構襯) = 膚選願構憲艱憲糧網蓋 襯鏇衊夢觸襯蓋構積選 (壓餘齋顧憲襯築構遞齋 ) 更多 | 积极 | 2024-01-18 | ||
範淵製願夢夢築齋遞網(繭簾築醖鹽鬱遞窪構襯) = 簾遞鹽築鹽構積糧衊遞 襯鏇衊夢觸襯蓋構積選 (壓餘齋顧憲襯築構遞齋 ) 更多 | |||||||
临床3期 | 54 | 餘鹽窪觸繭窪鹹積餘夢(糧觸膚廠積膚鹽鹹網壓) = 鏇餘鏇鑰鹽糧醖築範憲 鑰製鹽壓糧構淵顧構齋 (構製觸餘築簾鬱積簾鹹, 0.11 ~ 0.44) | 不佳 | 2024-01-18 | |||
餘鹽窪觸繭窪鹹積餘夢(糧觸膚廠積膚鹽鹹網壓) = 鑰廠襯積餘衊醖襯鬱夢 鑰製鹽壓糧構淵顧構齋 (構製觸餘築簾鬱積簾鹹 ) |
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