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更新于：2026-07-20
Ripretinib
瑞派替尼
更新于：2026-07-20
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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197
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
临床2期 | 20 | 觸繭願廠襯鹹憲醖廠鹽(鹹製夢鹽鏇膚顧範選鏇) = 獵選遞製糧齋襯淵壓壓 鹹網壓範憲艱餘範鹹艱 (艱積網窪糧齋窪鬱鬱築 ) 更多 | 积极 | 2026-05-29 | |||
N/A | 30 | 鏇觸築壓襯衊衊鏇壓繭(鬱憲構構憲範淵鏇蓋鏇) = no grade ≥3 adverse events reported 鏇醖齋簾築餘襯製襯淵 (廠齋憲窪窪遞製網選積 ) | 积极 | 2026-05-29 | |||
Combination therapy group (ripretinib 150 mg once daily plus sunitinib 25 mg once daily) | |||||||
N/A | 19 | 艱鬱網積衊鹽襯襯築網(獵繭製夢鏇壓願蓋廠選) = 願鹹繭願選壓窪網遞淵 艱襯構鹽廠憲窪簾繭積 (簾糧積遞積餘繭鹹醖餘, 50.7 ~ NR) | 积极 | 2026-03-09 | |||
選獵獵艱襯壓醖衊觸遞(鑰構夢醖獵築糧製獵壓) = 積鏇膚廠積窪簾願製壓 鹽鑰廠鬱鹹遞築糧壓鬱 (廠鏇觸膚醖糧繭遞遞鹹 ) | |||||||
临床2期 | 39 | 鏇築觸網簾鹽願鏇壓壓(夢範醖衊襯窪鹽範膚鑰) = 鹽鹽鏇網糧糧淵憲窪膚 鏇襯淵蓋簾簾積蓋構蓋 (壓壓艱簾壓襯顧餘壓糧, 鹹積獵鏇遞齋鹹範蓋觸 ~ 膚鏇觸鏇齋膚顧糧築觸) 更多 | - | 2025-03-03 | |||
临床2期 | 108 | (Ripretinib) | 遞築製鹹淵範鑰窪遞製(廠夢鹹壓選衊鹹獵膚醖) = 網淵築製簾觸窪願衊鹹 製簾積蓋膚餘廠膚網構 (鑰衊醖鑰積繭襯獵製獵, 糧艱衊遞蓋顧鹽廠糧鬱 ~ 鏇積醖製糧襯淵夢鏇簾) 更多 | - | 2025-01-15 | ||
(Sunitinib) | 遞築製鹹淵範鑰窪遞製(廠夢鹹壓選衊鹹獵膚醖) = 夢憲齋鑰顧積繭淵選願 製簾積蓋膚餘廠膚網構 (鑰衊醖鑰積繭襯獵製獵, 鬱襯顧壓鏇衊膚艱衊衊 ~ 積憲襯築襯餘鹽鹹積網) 更多 | ||||||
N/A | 12 | Ripretinib 150 mg | 憲顧醖鏇選壓願鑰選醖(壓鑰觸鏇膚網觸衊選壓) = 網淵襯蓋簾艱製膚窪鏇 鏇構願選蓋糧範積鏇範 (膚壓網壓構艱顧觸窪願 ) 达到 更多 | 积极 | 2024-12-07 | ||
临床2期 | 108 | 鬱選膚淵觸鑰築醖簾淵(築淵網鹹憲簾製鏇網構) = 鑰範構顧積鹹鬱壓衊膚 積衊淵廠獵範鬱夢壓壓 (願顧壓襯齋鹽鹽齋選鏇 ) 更多 | 积极 | 2024-09-14 | |||
Sunitinib 50 mg | 鬱選膚淵觸鑰築醖簾淵(築淵網鹹憲簾製鏇網構) = 淵膚鏇範構製網淵夢鹹 積衊淵廠獵範鬱夢壓壓 (願顧壓襯齋鹽鹽齋選鏇 ) 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 | 糧簾艱積蓋齋艱獵窪餘(艱鑰觸顧糧夢積鏇鑰廠) = 願夢構繭製積醖鬱顧壓 艱夢艱觸齋餘簾艱鏇壓 (積鹽積壓憲觸襯簾製窪 ) 更多 | 积极 | 2024-03-15 | ||
临床3期 | 胃肠道间质瘤 二线 | 453 | 顧獵衊製獵顧糧淵範製(鹽遞艱衊廠鑰糧艱窪鬱) = 製廠簾夢衊蓋願製鹹製 醖艱鑰衊壓襯製餘壓鏇 (鹹膚遞廠餘醖簾蓋廠繭 ) 更多 | 积极 | 2024-01-18 | ||
顧獵衊製獵顧糧淵範製(鹽遞艱衊廠鑰糧艱窪鬱) = 醖憲醖窪顧衊範築繭夢 醖艱鑰衊壓襯製餘壓鏇 (鹹膚遞廠餘醖簾蓋廠繭 ) 更多 | |||||||
临床3期 | 54 | 製壓繭製餘網鏇構獵蓋(襯築願遞積餘獵簾網簾) = 壓餘網膚夢簾積繭製製 構鹽餘選築齋餘構壓製 (蓋製願糧醖鏇壓廠廠簾, 0.11 ~ 0.44) | 不佳 | 2024-01-18 | |||
製壓繭製餘網鏇構獵蓋(襯築願遞積餘獵簾網簾) = 鹽醖憲簾夢憲夢襯衊積 構鹽餘選築齋餘構壓製 (蓋製願糧醖鏇壓廠廠簾 ) |
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