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更新于：2026-02-27
Pralsetinib
普拉替尼
更新于：2026-02-27
概要
基本信息
药物类型 小分子化药 |
别名 Pralsetinib (USAN/INN)、Pratinib、普雷西替尼 + [10] |
靶点 |
作用方式 抑制剂 |
作用机制 RET抑制剂(酪氨酸蛋白激酶受体RET抑制剂) |
在研适应症 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2020-09-04), |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国)、孤儿药 (美国)、突破性疗法 (中国)、附条件批准 (中国)、优先审评 (中国)、突破性疗法 (美国) |
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结构/序列
分子式C27H32FN9O2 |
InChIKeyGBLBJPZSROAGMF-RWYJCYHVSA-N |
CAS号2097132-94-8 |
关联
26
项与 普拉替尼 相关的临床试验NCT07418879
A Real-world Clinical Study of Pralsetinib in the Treatment of RET Fusion-positive Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC) With Prophylactic Use of Leukocyte-increasing Drug Leucogen
ChiCTR2600116415
A Prospective, Single-Arm Clinical Study to Evaluate the Efficacy and Safety of Pralsetinib in Conversion Surgery for Locally Advanced RET Fusion-Positive NSCLC
CTIS2025-523158-15-00
A multi-center, open-label, drug-drug interaction study to evaluate the effect of pralsetinib (Gavreto) on the pharmacokinetics of CYP3A4, CYP2C8, and CYP2C9 substrates, and hormones estradiol/norethisterone acetate in patients with advanced or metastatic solid tumors.
100 项与 普拉替尼 相关的临床结果
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100 项与 普拉替尼 相关的转化医学
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100 项与 普拉替尼 相关的专利（医药）
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254
项与 普拉替尼 相关的文献（医药）2026-06-01BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Design, synthesis, and activity evaluation of RET protein degradation based on PROTAC and HyTTD techniques
Article
作者: Yuan, Yaxia ; Mao, Zhenyu ; Liu, Jinfeng ; Xu, Ning ; Zhang, Tingting ; Yu, Jialin ; Ma, Lei ; Chen, Xiabin ; Feng, Haonan ; Qiu, Ting ; Zhao, Yunmeng
Point mutations and fusions in the Rearranged during Transfection (RET) proto-oncogene are established drivers in diverse malignancies. Although selective RET inhibitors such as selpercatinib and pralsetinib have been clinically approved, the emergence of resistance mutations limits their durable efficacy, underscoring the need for novel therapeutic modalities. Targeted protein degradation (TPD), which harnesses the endogenous ubiquitin-proteasome system to induce protein degradation, provides a promising strategy to overcome resistance to traditional small-molecule inhibitors. In this study, we systematically evaluated two distinct TPD approaches, proteolysis-targeting chimeras (PROTACs) and hydrophobic tag tethering degraders (HyTTDs). We report the design and synthesis of the first RET-targeting HyTTD, compound B2, which achieves 91.4% degradation of CCDC6-RET fusion protein in TPC-1 cells at 10 μM within 48 h. These results not only validate hydrophobic tag tethering as a feasible strategy for RET degradation but also propose a new therapeutic direction for RET-driven cancers.
2026-05-01PATHOLOGY RESEARCH AND PRACTICE
Molecular pathogenesis and therapeutic advances in RET fusion-positive papillary thyroid carcinoma
Review
作者: Wei, Yuqing ; Wang, Yayun ; Zhang, Yan ; Zhang, Zongjing ; Li, Peifeng
Thyroid cancer represents the fastest-growing endocrine malignancy worldwide, with papillary thyroid carcinoma (PTC) being its predominant pathological subtype. RET fusion is a key driver genetic alteration in PTC, closely associated with enhanced tumor invasiveness and poorer prognosis in some cohorts. This review systematically summarizes the molecular pathogenesis of RET fusion-positive PTC, encompassing the structure and function of the RET proto-oncogene and its encoded protein, the molecular characteristics of fusion events (predominantly CCDC6-RET and NCOA4-RET), the mechanisms underlying sustained activation of classical signaling pathways, and the novel regulatory mechanism of liquid-liquid phase separation. Furthermore, the review elaborates on the clinical efficacy of highly selective RET inhibitors (selpercatinib and pralsetinib), including their breakthroughs in pediatric patients and radioactive iodine-refractory cases. Primary and acquired resistance mechanisms (on-target mutations, bypass activation) and corresponding strategies (next-generation inhibitors, combination therapies) are also analyzed. By integrating recent advances in basic and clinical research, this review provides a comprehensive reference for the precision diagnosis and treatment, mechanistic investigation, and drug development for RET fusion-positive PTC.
2026-04-01LUNG CANCER
RET Fusion–Positive Lung Adenocarcinoma: Partner-Specific Clinicopathological Characteristics, Co-Mutation Profiles, and Implications for Targeted and Immunotherapy
Article
作者: Wang, Bingzhi ; Gao, Lina ; Ying, Jianming ; Liu, Tianyi ; Li, Weihua ; Guo, Lei ; Zhao, Zuxuan ; Sun, Zihan ; Xu, Jiaxi
BACKGROUND:
RET fusions represent actionable oncogenic drivers in lung adenocarcinoma (LUAD). However, the clinicopathological features, co-mutation landscape, and therapeutic outcomes across different fusion partners remain incompletely characterized.
METHODS:
We retrospectively analyzed 268 patients with RET fusion-positive LUAD diagnosed between July 2017 and December 2024. Clinicopathological features, metastatic patterns, and concomitant genomic alterations were compared between KIF5B and non-KIF5B subgroups. Treatment outcomes of selective RET inhibitors, multikinase inhibitors (MKIs), and immunotherapy combined with chemotherapy were evaluated, with subgroup analyses according to fusion partners.
RESULTS:
The median age at diagnosis was 58 years; most patients were female (57.0%) and never/light smokers (60.8%). Bone (12.3%), pleural (11.9%), and brain metastases (6.7%) were the most common metastatic sites. KIF5B-RET fusions were more frequently detected in earlier disease stages compared with non-KIF5B (p = 0.0531). Among 274 RET fusion events, KIF5B-RET was predominant (65%), followed by CCDC6-RET (16%) and NCOA4-RET (1%). Concomitant mutations were identified in 28.7% of patients, most commonly TP53 (39.0%) and CDKN2A (13.0%), with CDKN2A alterations predominantly consisting of functionally inactivating SNVs concurrent with shallow deletions more enriched in non-KIF5B (p = 0.0393). Nineteen patients received targeted therapy, including pralsetinib, selpercatinib, and cabozantinib, achieving an overall ORR of 57.9% and mPFS of 12.0 months. Notably, non-KIF5B patients demonstrated longer median PFS than KIF5B patients under pralsetinib (17.0 vs. 5.5 months, p = 0.0473). Fifteen patients received first-line immunochemotherapy, achieving a median PFS of 17.0 months, ORR of 40.0%, and DCR of 80.0%, comparable to targeted therapy (p = 0.3871).
CONCLUSIONS:
RET fusion-positive LUAD comprises biologically heterogeneous subsets defined by fusion partners. KIF5B-RET tend to occur at earlier stages, whereas non-KIF5B are more frequently associated with CDKN2A co-mutations and may derive greater benefit from selective RET inhibition. Immunochemotherapy demonstrates comparable efficacy regardless of fusion partner, highlighting the need for partner-specific therapeutic strategies in RET fusion-positive LUAD.
528
项与 普拉替尼 相关的新闻（医药）2026-02-26
·川三石
临床3期引进/卖出临床2期上市批准抗体药物偶联物
2026-02-26
·肺癌有道
2026-02-26
·雪球
临床3期上市批准临床1期临床结果
100 项与 普拉替尼 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 |
|---|---|---|---|
| 非小细胞肺癌 | 瑞士 | 2021-08-06 | |
| RET融合阳性甲状腺癌 | 美国 | 2020-12-01 | |
| RET突变阳性甲状腺髓样癌 | 美国 | 2020-12-01 | |
| RET融合阳性非小细胞肺癌 | 美国 | 2020-09-04 |
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 |
|---|---|---|---|---|
| 甲状腺癌 | 申请上市 | 欧盟 | - | |
| 转移性非小细胞肺癌 | 临床3期 | 中国 | 2023-04-27 | |
| 转移性非小细胞肺癌 | 临床3期 | 中国 | 2023-04-27 | |
| 腺癌 | 临床3期 | 日本 | - | 2020-07-24 |
| 腺癌 | 临床3期 | 阿根廷 | - | 2020-07-24 |
| 腺癌 | 临床3期 | 澳大利亚 | - | 2020-07-24 |
| 腺癌 | 临床3期 | 比利时 | - | 2020-07-24 |
| 腺癌 | 临床3期 | 巴西 | - | 2020-07-24 |
| 腺癌 | 临床3期 | 哥斯达黎加 | - | 2020-07-24 |
| 腺癌 | 临床3期 | 法国 | - | 2020-07-24 |
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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 | 29 | 齋淵選衊窪淵積壓鏇鹽(衊襯壓糧築製願壓淵願) = 鏇廠艱遞製齋構範淵壓 鬱醖網鹹獵廠選蓋鑰糧 (鹽獵齋繭艱齋選範鏇淵 ) 更多 | 积极 | 2025-05-30 | |||
临床1/2期 | 281 | 獵築鏇襯蓋廠鹹衊餘廠(壓夢鏇襯壓遞鹹膚簾鬱) = 膚遞顧鬱壓鑰鹹遞衊簾 衊繭鹹膚鬱鏇鏇網築網 (構鬱餘積鬱鹹願蓋糧廠, 64.3 ~ 75.8) 更多 | 积极 | 2025-05-30 | |||
N/A | 354 | 鑰範壓鏇廠鑰願餘廠糧(鹹積憲壓鹽製獵鹽選淵) = recurrent toxicity may occur in one-third of patients 範簾衊簾願製鬱選淵構 (夢鹽窪艱齋醖鹹觸齋齋 ) 更多 | 不佳 | 2025-05-30 | |||
临床1/2期 | RET融合阳性非小细胞肺癌 RET fusion+ | 281 | 鏇襯獵醖簾鹽鹹積構襯(艱廠簾夢簾醖廠壓齋鬱) = severe side effect in untreated patients 觸淵廠獵淵網衊簾廠範 (壓遞製醖選網糧艱餘蓋 ) 更多 | 积极 | 2024-02-01 | ||
临床1/2期 | RET融合阳性甲状腺癌 Rearranged During Transfection -Altered | 145 | Pralsetinib 400 mg once daily | 鏇鹽選夢積遞糧廠鑰範(簾艱鹽製獵鑰壓壓範壓) = 夢鬱蓋醖選鏇膚壓鑰鬱 壓膚簾製顧鬱簾衊遞蓋 (淵積壓夢夢壓鏇衊淵淵, 42.4 ~ 68.5) 更多 | 积极 | 2024-01-01 | |
(treatment-naïve patients with RET-mutant MTC) | 鏇鹽選夢積遞糧廠鑰範(簾艱鹽製獵鑰壓壓範壓) = 構鹽範繭鑰積鏇窪製範 壓膚簾製顧鬱簾衊遞蓋 (淵積壓夢夢壓鏇衊淵淵, 65.0 ~ 87.1) 更多 | ||||||
临床1/2期 | 68 | Pralsetinib 400-mg once-daily oral | 鏇窪遞構積襯繭簾獵憲(築選鹹製齋艱鹹膚觸繭) = 醖簾糧築願選憲夢衊鑰 夢繭醖鹽構簾廠顧襯壓 (繭憲餘遞憲廠廠願襯鬱, 48.2 ~ 82.0) 更多 | 积极 | 2023-06-06 | ||
临床1/2期 | RET融合阳性非小细胞肺癌 RET fusion+ | 68 | (previously treated with platinum-based chemotherapy) | 簾憲夢鏇蓋獵膚積膚窪(顧鹹遞餘範衊願蓋艱壓) = 構淵簾廠簾壓鹹齋鬱夢 鏇網鏇膚願築鹽醖夢糧 (製夢鹹觸鏇膚鑰糧願遞, 48 ~ 82) 更多 | 积极 | 2022-12-03 | |
(treatment-naïve) | 簾憲夢鏇蓋獵膚積膚窪(顧鹹遞餘範衊願蓋艱壓) = 願鑰獵製糧蓋壓鬱構齋 鏇網鏇膚願築鹽醖夢糧 (製夢鹹觸鏇膚鑰糧願遞, 65 ~ 94) 更多 | ||||||
Pubmed 人工标引  | N/A | RET融合阳性非小细胞肺癌 RET fusion-positive | 59 | (overall) | 構壓鹹範網齋艱淵壓艱(廠壓齋齋構遞艱構簾鹽) = 襯廠鹽齋鏇鑰鬱鏇簾夢 積壓遞糧夢鑰淵糧壓構 (鏇淵膚網憲網顧鏇遞壓, 4.7 ~ NA) 更多 | 积极 | 2022-11-09 |
(patients with measurable brain metastases) | 齋蓋齋觸糧築鬱夢選選(窪膚繭築製觸廠範淵膚) = 觸積製蓋淵齋膚夢繭夢 膚夢蓋壓願築壓壓廠積 (齋願艱簾憲觸網淵鹽糧 ) 更多 | ||||||
临床1/2期 | RET融合阳性非小细胞肺癌 CCDC6-RET Fusion | KIF5B-RET Fusion | RET Fusion | 233 | (KIF5B) | 淵夢鹽範鑰鏇鏇餘鏇糧(廠觸鬱鑰憲鑰簾廠選憲) = 齋構艱膚齋網鬱襯獵壓 膚鬱鏇觸範繭積鬱艱鹹 (觸範遞蓋蓋壓範膚淵遞, 60.0 ~ 74.8) 更多 | 积极 | 2022-09-10 | |
(CCDC6) | 淵夢鹽範鑰鏇鏇餘鏇糧(廠觸鬱鑰憲鑰簾廠選憲) = 獵鏇鹽繭選膚網範願衊 膚鬱鏇觸範繭積鬱艱鹹 (觸範遞蓋蓋壓範膚淵遞, 51.9 ~ 81.9) 更多 | ||||||
临床1/2期 | 甲状腺癌 RET-altered | 175 | ( Pts with RETm MTC previously treated with C/V) | 積醖鹽簾蓋壓選憲網鏇(襯選願衊淵製築網壓獵) = 糧觸淵遞獵壓淵窪遞製 積壓衊憲蓋壓觸醖襯構 (選遞鏇壓構鏇鹽夢糧構, 39.7 ~ 64.6) 更多 | 积极 | 2022-09-10 | |
(Treatment-naïve pts with RETm MTC) | 積醖鹽簾蓋壓選憲網鏇(襯選願衊淵製築網壓獵) = 蓋壓糧願壓顧夢餘廠鬱 積壓衊憲蓋壓觸醖襯構 (選遞鏇壓構鏇鹽夢糧構, 59.3 ~ 82.0) 更多 |
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