预约演示
更新于：2026-04-16
Tunlametinib
妥拉美替尼
更新于：2026-04-16
概要
基本信息
药物类型 小分子化药 |
别名 HL 085、HL-085、HL085 + [1] |
作用方式 抑制剂 |
作用机制 MEK1抑制剂(双特异性丝裂原活化蛋白激酶激酶1抑制剂)、MEK2抑制剂(双特异性丝裂原活化蛋白激酶激酶2抑制剂) |
原研机构 |
非在研机构 |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2024-03-12), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、突破性疗法 (中国)、附条件批准 (中国) |
登录后查看时间轴
结构/序列
分子式C16H12F2IN3O3S |
InChIKeyUFZJUVFSSINETF-UHFFFAOYSA-N |
CAS号1801756-06-8 |
关联
26
项与 妥拉美替尼 相关的临床试验NCT07170293
An Exploratory, Prospective, Single Arm, Open Label, Single Center, Basket, Phase II Clinical Study of Tunlametinib (HL-085) in Patients With NRAS Mutant Non-melanoma Refractory Solid Tumors
NCT07507526
A Study on the Efficacy and Safety of Disitamab Vedotin Combined With Tunlametinib and PD-1 Antibody in Third-Line and Above Treatment of Patients With HER2-Overexpressing Advanced Gastric Cancer
NCT07463677
A Study Protocol for Evaluating the Efficacy and Safety of Tunlametinib Combination Therapy in KRAS-Mutated Unresectable Locally Advanced or Metastatic Non-Small Cell Lung Cancer
100 项与 妥拉美替尼 相关的临床结果
登录后查看更多信息
100 项与 妥拉美替尼 相关的转化医学
登录后查看更多信息
100 项与 妥拉美替尼 相关的专利（医药）
登录后查看更多信息
11
项与 妥拉美替尼 相关的文献（医药）2026-04-01ANTI-CANCER DRUGS
Multimodal treatment with thiotepa, bevacizumab, teniposide, and tunlametinib in a patient with neurofibromatosis type 1-associated oligodendroglioma: a rare case report
Article
作者: Zhou, Shizhen ; Tao, Rongjie ; Chen, Yanfei ; Gao, Guoliang ; Sun, Peng ; Pan, Xueqiang
Neurofibromatosis type 1 (NF1) is a common autosomal dominant disorder associated with central nervous system gliomas, most frequently optic pathway gliomas; however, oligodendrogliomas in the setting of NF1 are exceedingly rare, with no prior documented cases and no established treatment strategies to date. A 53-year-old female with NF1-associated oligodendroglioma experienced multiple recurrences following surgery, radiotherapy, chemotherapy, and targeted therapy. Upon further disease progression, she was treated with a novel combination of thiotepa, bevacizumab, teniposide, and the mitogen-activated protein kinase kinase 1/2 (MEK1/2) inhibitor tunlametinib. After one treatment cycle, the patient achieved a marked reduction in tumor volume, consistent with a complete response (CR). She subsequently completed eight additional cycles of the regimen and has maintained CR. The treatment was well-tolerated, with manageable grade 3 myelosuppression controlled by supportive care. As of June 2025, the patient has achieved a CR with a progression-free survival of 9 months before experiencing disease recurrence. This rare case of NF1-associated oligodendroglioma was managed with thiotepa, bevacizumab, teniposide, and tunlametinib, highlighting the potential of MEK inhibition in NF1-related gliomas.
2025-11-15RAPID COMMUNICATIONS IN MASS SPECTROMETRY
Characterization of 12 Unknown Photodegradation Impurities of Tunlametinib Capsules Using Liquid Chromatography Coupled With ion Trap/Time‐Of‐Flight Mass Spectrometry
Article
作者: Gao, Jiarui ; Yang, Ying ; Zeng, Hongxia
ABSTRACT:
Rationale:
In March 2024, tunlametinib capsules, a Class 1 new drug (referring to active pharmaceutical ingredients and formulations not previously marketed either nationally or globally), were approved in China for treating patients with advanced melanoma and neuroblastoma RAS viral oncogene homologue mutations who experienced disease progression or intolerance to anti‐PD‐1/PD‐L1 therapy. Risk assessment of impurity profiles is essential for drug safety and efficacy in clinical applications. This study characterized impurity profiles in tunlametinib capsules induced by photodegradation.
Methods:
Initial high‐performance liquid chromatography coupled with ion trap/time‐of‐flight mass spectrometry (HPLC/IT‐TOF MS) in positive ion mode was first performed to determine the
m
/
z
values of protonated ions and predict the formulas of the detected impurities. Subsequent LC‐MS
n
analyses (
n
= 2–4) of target compounds elucidated comprehensive structural features.
Results:
Twelve previously unidentified photodegradation impurities in tunlametinib capsules were characterized using HPLC/IT‐TOF MS.
Conclusions:
Structural elucidation of 12 previously uncharacterized photodegradation impurities was achieved through HPLC/IT‐TOF MS. These findings establish a scientific foundation for refining quality specifications of tunlametinib.
2025-08-18BRITISH JOURNAL OF DERMATOLOGY
Targeting the MAPK pathway for NRAS mutant melanoma: from mechanism to clinic
Review
作者: Xia, Hongwei ; Wang, Yi ; Xu, Guangchao
Abstract:
Mutant NRAS is the second-most common type of mutation in melanoma. The prognosis in patients with NRAS mutant melanoma is poor, and effective targeted treatment strategies are still lacking. Mutant NRAS mainly acts by activating RAF–MEK–ERK signalling to promote carcinogenesis in melanoma. In recent years, significant clinical advances have been made in targeting the NRAS–MAPK (mitogen-activated protein kinase) pathway, with novel therapies such as the MEK inhibitor tunlametinib and a combination therapy of the pan-RAF inhibitor naporafenib + trametinib leading the way. In this review, we systematically summarize the recent advances made in the direct targeting of mutant NRAS proteins and their downstream RAF and MEK proteins, as well as targeting the MAPK pathway in combination with other therapeutic targets, including immunotherapy, to treat NRAS mutant melanoma. Additionally, we discuss the current issues and emerging countermeasures related to targeted therapy for NRAS mutant melanoma.
149
项与 妥拉美替尼 相关的新闻（医药）2026-04-13
细胞疗法免疫疗法抗体药物偶联物
2026-04-13
2026-04-13
100 项与 妥拉美替尼 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| NRAS突变黑色素瘤 | 中国 | 2024-03-12 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| BRAF V600E突变结直肠癌 | 临床3期 | 中国 | 2023-10-16 | |
| BRAF V600E突变非小细胞肺癌 | 临床2期 | 中国 | 2023-11-28 | |
| 转移性结直肠癌 | 临床2期 | 中国 | 2022-02-24 | |
| NF1突变型丛状神经纤维瘤 | 临床2期 | 中国 | 2021-11-01 | |
| 神经纤维瘤病1型 | 临床2期 | 中国 | 2021-10-18 | |
| BRAF突变阳性黑色素瘤 | 临床2期 | 中国 | 2021-09-23 | |
| 局部晚期黑色素瘤 | 临床2期 | 中国 | 2021-09-06 | |
| 黑色素瘤 | 临床1期 | 中国 | 2026-04-16 | |
| RAS/RAF 突变的实体瘤 | 临床1期 | 中国 | 2020-08-17 | |
| KRAS突变非小细胞肺癌 | 临床1期 | 中国 | 2020-05-21 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床1期 | BRAF突变实体瘤 BRAF V600 | 72 | 繭糧願製鏇壓遞簾艱壓(簾齋願壓醖鏇簾願顧襯) = All 72 patients had treatment-related adverse events (TRAEs) 鹹鹹積簾窪鹽餘顧餘衊 (築醖壓蓋餘壓餘廠膚觸 ) 更多 | 积极 | 2024-06-12 | ||
(RP2D) | |||||||
临床2期 | BRAF V600 突变阳性黑色素瘤 BRAF V600-mutant | 17 | 願願鑰餘艱範窪壓壓鏇(築廠網膚鬱憲網獵衊顧) = 淵鏇鬱顧鹽艱築簾獵淵 窪衊糧顧顧夢壓遞遞憲 (窪膚觸鑰壓夢醖築淵廠, 44.0 ~ 89.7) 更多 | 积极 | 2024-05-24 | ||
(pre-treated pts) | 願願鑰餘艱範窪壓壓鏇(築廠網膚鬱憲網獵衊顧) = 齋遞鏇憲淵衊簾廠繭壓 窪衊糧顧顧夢壓遞遞憲 (窪膚觸鑰壓夢醖築淵廠, 46.2 ~ 95.0) 更多 | ||||||
临床2期 | 100 | 襯憲齋鬱簾獵蓋積積鹹(膚壓鑰遞餘積壓積齋選) = 構糧築顧廠餘築簾衊獵 蓋廠壓窪願壓襯製願夢 (遞窪願顧醖願顧醖觸齋, 26.3% ~ 46.3%) 更多 | 积极 | 2024-05-24 | |||
临床1期 | 晚期恶性实体瘤 BRAF V600 mutation | 72 | 遞廠鏇襯膚鏇顧鑰簾餘(網獵鑰繭網築蓋艱選餘) = The most common AE were CK elevation, anemia and rash which were predominantly grade 1/2. 願顧願窪鹽範觸鹽夢憲 (齋廠願醖淵壓窪簾壓積 ) | 积极 | 2023-10-23 | ||
(NSCLC) | |||||||
临床2期 | NRAS突变黑色素瘤 NRAS Mutation | 100 | 遞糧襯醖積獵壓鑰襯簾(獵餘鏇顧築選構蓋獵艱) = 壓觸簾壓淵觸鏇繭餘淵 網襯鹽齋襯艱廠糧觸構 (鹹餘襯遞襯觸願鬱範壓, 25.3 ~ 45.2) 更多 | 积极 | 2023-05-26 | ||
临床1期 | 42 | 網網膚鹹範齋簾鏇鬱簾(獵襯壓壓簾醖齋鏇鬱齋) = 憲顧範築繭鹹簾鑰網艱 鹹鹹襯糧夢構餘廠構遞 (膚鏇遞襯選蓋膚醖淵廠 ) 更多 | - | 2023-01-04 | |||
临床1/2期 | 33 | 製遞鹹願醖願鹽鬱淵網(醖餘繭觸壓夢醖鹹獵餘) = the most common drug-related AEs were aspartate aminotransferase 繭繭鹽願餘繭膚獵鹽廠 (繭願餘膚窪廠壓齋顧窪 ) 更多 | 积极 | 2020-05-25 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用