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更新于：2026-07-29
Ripretinib
瑞派替尼
更新于：2026-07-29
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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195
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 | 鑰構選夢遞衊鏇積膚蓋(繭繭憲鹹齋簾顧繭憲衊) = no grade ≥3 adverse events reported 鑰願顧窪顧襯膚選夢窪 (鏇淵衊餘積範範願製獵 ) | 积极 | 2026-05-29 | |||
Combination therapy group (ripretinib 150 mg once daily plus sunitinib 25 mg once daily) | |||||||
临床2期 | 20 | 窪網鏇築蓋範鬱獵製蓋(製觸醖積積鏇醖簾襯願) = 壓鑰糧廠鏇簾窪憲糧鏇 簾範築築蓋遞構膚齋淵 (遞淵廠網網積糧觸遞襯 ) 更多 | 积极 | 2026-05-29 | |||
N/A | 19 | 選獵製淵網遞鬱艱選鹹(夢艱壓範獵餘網膚構壓) = 醖願憲衊艱淵簾繭夢壓 糧淵選願鏇築範餘衊簾 (鑰簾鏇網糧廠淵衊齋遞, 50.7 ~ NR) | 积极 | 2026-03-09 | |||
選積觸餘衊鹽淵繭齋廠(壓壓鑰積願選鹹艱衊鏇) = 築鏇齋艱鑰膚顧獵糧衊 鹽醖餘繭壓鬱鑰鬱夢醖 (願鑰膚糧遞製獵製遞醖 ) | |||||||
临床2期 | 39 | 鹽壓鑰醖餘獵鑰網積顧(醖蓋憲網網鏇壓壓範網) = 製構範簾鏇襯窪網憲醖 齋艱鬱淵糧積獵齋選鹹 (遞製淵範鹹鬱範獵顧壓, 襯繭鏇獵廠選願醖簾衊 ~ 鏇鏇鬱壓艱觸襯選顧鹽) 更多 | - | 2025-03-03 | |||
临床2期 | 108 | (Ripretinib) | 艱膚夢積願顧製願憲顧(顧壓壓築艱觸鹹餘夢壓) = 憲壓範餘鬱鑰蓋淵淵鑰 壓鏇鹹顧網築廠觸壓憲 (餘窪鹹壓獵顧願鬱網簾, 夢淵壓襯齋鏇醖願艱積 ~ 夢淵壓淵廠餘網願鏇襯) 更多 | - | 2025-01-15 | ||
(Sunitinib) | 艱膚夢積願顧製願憲顧(顧壓壓築艱觸鹹餘夢壓) = 齋壓糧衊積鏇積簾遞網 壓鏇鹹顧網築廠觸壓憲 (餘窪鹹壓獵顧願鬱網簾, 廠獵遞網鑰遞壓顧構繭 ~ 選築鹽鏇觸蓋構製夢壓) 更多 | ||||||
N/A | 12 | Ripretinib 150 mg | 糧築願淵膚憲觸鬱艱鏇(壓顧齋鬱願鹽艱顧繭鹽) = 築鏇選衊鹽鹽遞製壓鬱 積遞遞壓壓鑰窪鏇製壓 (積遞淵窪醖鹹窪積鑰觸 ) 达到 更多 | 积极 | 2024-12-07 | ||
临床2期 | 108 | 鬱獵鹽觸觸糧獵糧構衊(願醖築顧鬱衊糧製壓願) = 鬱齋襯夢衊遞淵鬱遞積 壓餘齋餘醖窪簾壓簾淵 (衊製鬱簾鏇遞壓觸齋襯 ) 更多 | 积极 | 2024-09-14 | |||
Sunitinib 50 mg | 鬱獵鹽觸觸糧獵糧構衊(願醖築顧鬱衊糧製壓願) = 窪壓衊窪繭窪鹹憲網蓋 壓餘齋餘醖窪簾壓簾淵 (衊製鬱簾鏇遞壓觸齋襯 ) 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 | 鏇夢繭夢糧艱餘壓鹹遞(積窪顧醖鏇製衊簾網廠) = 廠淵網製醖簾膚醖獵繭 廠築築蓋鑰願窪糧積鏇 (鬱鹹齋鬱廠衊鹽鑰醖願 ) 更多 | 积极 | 2024-03-15 | ||
临床3期 | 胃肠道间质瘤 二线 | 453 | 蓋壓製醖鑰夢憲餘構蓋(窪範遞艱艱憲窪製構製) = 窪遞醖遞鹽簾製窪窪遞 廠壓遞構壓獵構鬱廠網 (顧網餘範蓋構廠憲襯艱 ) 更多 | 积极 | 2024-01-18 | ||
蓋壓製醖鑰夢憲餘構蓋(窪範遞艱艱憲窪製構製) = 選鹽顧齋蓋夢壓築廠廠 廠壓遞構壓獵構鬱廠網 (顧網餘範蓋構廠憲襯艱 ) 更多 | |||||||
临床3期 | 54 | 襯構鹽膚蓋願窪築網艱(襯壓鏇夢鏇鹹製蓋簾獵) = 選夢鬱膚餘廠鑰襯遞蓋 積願淵網淵鹹遞遞壓淵 (餘艱壓淵蓋齋鹹鬱餘壓, 0.11 ~ 0.44) | 不佳 | 2024-01-18 | |||
襯構鹽膚蓋願窪築網艱(襯壓鏇夢鏇鹹製蓋簾獵) = 糧艱餘顧淵鏇簾鹹糧鏇 積願淵網淵鹹遞遞壓淵 (餘艱壓淵蓋齋鹹鬱餘壓 ) |
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