.jpeg)
What is trametinib?
Trametinib is a kinase inhibitor indicated as a single agent for the treatment of BRAF inhibitor-naïve patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as tested in an FDA-approved trial. When used in combination with dabrafenib, it is indicated for: 1. Treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations detected in an FDA-approved test. 2. Adjuvant therapy for patients with melanoma with BRAF V600E or V600K mutations and involved lymph nodes after complete resection based on an FDA-approved test. 3. Treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose BRAF V600E mutation has been detected in an FDA-approved trial. 4. Treatment of patients with locally advanced or metastatic anaplastic thyroid cancer (ATC) who have BRAF V600E mutations and no satisfactory locoregional treatment options. 5. Treatment of adult and pediatric patients 1 year of age and older with unresectable or metastatic BRAF V600E-mutant solid tumors who have progressed after prior therapy and for whom satisfactory alternative treatment options are not available. This indication received accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and characterization of clinical benefit in confirmatory trials. 6. Treatment of pediatric patients 1 year of age and older with BRAF V600E-mutated low-grade glioma (LGG) who require systemic therapy.
The recommended dose of trametinib for adult patients is 2 mg orally once daily. The recommended dose of trametinib in pediatric patients is based on body weight. Take trametinib at least 1 hour before or 2 hours after a meal. Trametinib is a reversible inhibitor of mitogen-activated extracellular signal-regulated kinase 1 (MEK1) and MEK2 activation and MEK1 and MEK2 kinase activity. MEK protein is an upstream regulator of the extracellular signal-related kinase (ERK) pathway and promotes cell proliferation. The BRAF V600E mutation results in constitutive activation of the BRAF pathway including MEK1 and MEK2. Trametinib inhibits cell growth in various BRAF V600 mutation-positive tumors in vitro and in vivo. Trametinib and dabrafenib target two different kinases in the RAS/RAF/MEK/ERK pathway. The combination of trametinib and dabrafenib resulted in greater growth inhibition of BRAF V600 mutation-positive tumor cell lines in vitro and prolonged inhibition of tumor growth in BRAF V600 mutation-positive tumor xenografts compared with either agent alone. In the context of BRAF mutant colorectal cancer, induction of EGFR-mediated MAPK pathway reactivation is considered to be an intrinsic resistance mechanism to BRAF inhibitors. Administration of 1 mg and 2 mg mekinin tablets to patients with BRAF V600 mutation-positive melanoma resulted in dose-dependent changes in tumor biomarkers, including inhibition of phosphorylated ERK, inhibition of Ki67 (a marker of cell proliferation), and an increase in p27 (a marker of apoptosis). If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to learn more about high-quality overseas drugs for you.
[ 免责声明 ] 本页面内容来自公开渠道（如FDA官网、Drugs官网、原研药厂官网等），仅供持有医疗专业资质的人员用于医学药学研究参考，不构成任何治疗建议或药品推荐。所涉药品可能未在中国大陆获批上市，不适用于中国境内销售和使用。如需治疗，请咨询正规医疗机构。本站不提供药品销售或代购服务。
