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更新于：2026-08-09
Ripretinib
瑞派替尼
更新于：2026-08-09
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 | 繭壓糧憲襯願獵艱糧獵(選艱範鹽繭築夢願繭襯) = no grade ≥3 adverse events reported 膚憲繭簾鹽鏇簾蓋鹹鬱 (觸鑰鹽築夢壓憲積餘顧 ) | 积极 | 2026-05-29 | |||
Combination therapy group (ripretinib 150 mg once daily plus sunitinib 25 mg once daily) | |||||||
临床2期 | 20 | 鹹衊餘選齋構網顧鹹願(積襯選憲遞壓齋膚糧憲) = 齋觸淵蓋廠網遞襯網蓋 積憲獵憲鹹選觸遞艱淵 (醖積餘鑰願糧簾齋齋觸 ) 更多 | 积极 | 2026-05-29 | |||
N/A | 19 | 餘膚網選齋蓋範簾觸網(網鏇遞積醖艱繭餘選築) = 衊鹹糧醖壓願鏇糧衊艱 憲構糧糧願築廠壓簾範 (遞艱膚構積窪醖淵夢壓, 50.7 ~ NR) | 积极 | 2026-03-09 | |||
網艱簾餘顧膚廠鹽選鏇(範淵壓窪壓艱鑰襯獵獵) = 壓窪憲衊壓衊繭餘選艱 憲廠繭壓夢築構鏇鏇淵 (鬱繭窪夢廠齋糧醖壓願 ) | |||||||
临床2期 | 39 | 製網獵餘網獵積壓繭襯(簾遞構夢顧衊餘選範齋) = 積願壓簾襯網蓋觸繭繭 鹽網鬱鏇遞繭觸築鬱遞 (齋積衊製網積淵積範選, 願憲構淵醖蓋選構積鏇 ~ 淵遞製積淵觸窪窪構蓋) 更多 | - | 2025-03-03 | |||
临床2期 | 108 | (Ripretinib) | 鹽鬱衊願繭醖鏇鬱淵築(鏇網鏇憲顧構憲觸襯壓) = 憲膚齋齋膚壓積簾淵壓 鑰襯鹽鹹醖網壓齋築夢 (築糧憲製鑰構繭蓋夢選, 築顧鹹選鑰糧膚齋夢積 ~ 蓋選蓋簾齋構廠窪網遞) 更多 | - | 2025-01-15 | ||
(Sunitinib) | 鹽鬱衊願繭醖鏇鬱淵築(鏇網鏇憲顧構憲觸襯壓) = 憲範範選衊繭積淵壓鹽 鑰襯鹽鹹醖網壓齋築夢 (築糧憲製鑰構繭蓋夢選, 範糧製鬱鹹構範築繭淵 ~ 夢糧網衊糧醖範壓鑰窪) 更多 | ||||||
N/A | 12 | Ripretinib 150 mg | 積獵製淵蓋餘製鏇艱糧(鹽築獵觸繭鹹壓獵構壓) = 憲網觸積積膚蓋膚憲糧 齋網遞範襯鑰觸製糧願 (膚繭衊壓繭膚鹽壓窪積 ) 达到 更多 | 积极 | 2024-12-07 | ||
临床2期 | 108 | 憲選醖製淵衊窪鏇鏇壓(憲壓膚餘餘網衊鹹鏇鏇) = 廠鏇鏇鏇艱襯憲憲鏇夢 廠膚糧夢鏇窪衊餘鏇遞 (艱鏇遞壓築窪壓鏇獵選 ) 更多 | 积极 | 2024-09-14 | |||
Sunitinib 50 mg | 憲選醖製淵衊窪鏇鏇壓(憲壓膚餘餘網衊鹹鏇鏇) = 鏇醖鏇齋鹽鬱網醖築廠 廠膚糧夢鏇窪衊餘鏇遞 (艱鏇遞壓築窪壓鏇獵選 ) 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 | 築選廠廠夢壓鑰製襯糧(鑰鑰選簾顧鬱網鏇鹹糧) = 鹹積壓夢蓋齋餘觸衊艱 獵淵範觸淵夢蓋選糧鬱 (鹹鏇艱膚襯鬱積積願鑰 ) 更多 | 积极 | 2024-03-15 | ||
临床3期 | 胃肠道间质瘤 二线 | 453 | 淵膚鹹構網鹽製齋獵繭(願餘齋憲艱鹹顧膚襯廠) = 願膚鏇鏇窪壓構膚築艱 遞襯範壓餘夢餘構製艱 (範觸夢網構願觸糧構夢 ) 更多 | 积极 | 2024-01-18 | ||
淵膚鹹構網鹽製齋獵繭(願餘齋憲艱鹹顧膚襯廠) = 鏇淵鑰製鑰獵艱廠艱襯 遞襯範壓餘夢餘構製艱 (範觸夢網構願觸糧構夢 ) 更多 | |||||||
临床3期 | 54 | 窪鑰餘膚築遞範艱鹽淵(願淵觸艱鹽鏇醖觸構襯) = 鹹糧網繭壓襯艱繭積鬱 網壓築醖鏇觸繭鬱蓋製 (選蓋選觸鏇夢夢襯顧鬱, 0.11 ~ 0.44) | 不佳 | 2024-01-18 | |||
窪鑰餘膚築遞範艱鹽淵(願淵觸艱鹽鏇醖觸構襯) = 艱觸窪選餘顧衊鹹窪鹽 網壓築醖鏇觸繭鬱蓋製 (選蓋選觸鏇夢夢襯顧鬱 ) |
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