1. Indications and Usage
\nUnresectable or Metastatic Melanoma:
\nIndicated in combination with dabrafenib for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutation.
\nMetastatic Non-Small Cell Lung Cancer (NSCLC):
\nIndicated in combination with dabrafenib for the treatment of patients with metastatic NSCLC with BRAF V600E mutation.
\nAdjuvant Treatment of Melanoma:
\nIndicated in combination with dabrafenib for the adjuvant treatment of patients with melanoma with BRAF V600E or V600K mutation with involvement of lymph nodes following complete resection.
\n2. Dosage and Administration
\nRoute of Administration:
\nFor Oral Use ONLY.
\nRecommended Dosage:
\nDose: 2 mg once daily.
\nCombination: When used in combination with dabrafenib, trametinib and dabrafenib should be taken at the same time.
\nTiming:
\nAdminister at least 1 hour before or 2 hours after a meal.
\nMissed Dose:
\nIf a dose is missed, it should be taken as soon as possible unless it is less than 12 hours before the next scheduled dose. In that case, skip the missed dose.
\n3. Mechanism of Action
\nMEK Inhibition:
\nTrametinib is a reversible inhibitor of mitogen-activated protein kinase (MEK)1 and MEK2.
\nPathway Blockade:
\nMEK proteins are upstream regulators of the ERK signaling pathway, which promotes cell proliferation. Trametinib inhibits BRAF V600 mutant-positive tumor cell growth.
\nSynergistic Effect:
\nTrametinib and dabrafenib target two different kinases in the MAPK pathway. Their combination leads to greater inhibition of tumor cell growth compared to either agent alone and delays the development of drug resistance.
\n4. Safety and Warnings
\nCardiac Dysfunction (Cardiomyopathy):
\nReductions in Left Ventricular Ejection Fraction (LVEF) can occur. Evaluate LVEF prior to initiation and periodically during treatment.
\nOcular Toxicity:
\nRetinopathy, including Retinal Vein Occlusion (RVO) and Retinal Pigment Epithelium Detachment (RPED), can occur. Regular ophthalmologic examinations are recommended.
\nPulmonary Toxicity:
\nInterstitial Lung Disease (ILD)\/Pneumonitis has been reported. Discontinue trametinib if confirmed.
\nSevere Skin Toxicity:
\nMonitor for cutaneous toxicities.
\n5. Adverse Reactions
\nMost Common:
\nGeneral: Rash, diarrhea, and lymphedema.
\nWith Dabrafenib: Pyrexia (fever), chills, fatigue, nausea, vomiting, cough, headache, arthralgia, and night sweats.
\n6. Drug Interactions
\nMetabolic Pathway:
\nTrametinib is not metabolized by CYP enzymes but is a substrate of P-gp.
\nCYP3A4\/2C8 Substrates:
\nWhen used in combination with dabrafenib (a CYP3A4 inducer), trametinib may decrease the exposure of other CYP3A4 or CYP2C8 substrates (e.g., warfarin, cyclosporine), potentially leading to therapeutic failure of the co-administered drug.
\n7. Pharmaceutical Information
\nChemical Composition:
\nActive Ingredient: Trametinib Dimethyl Sulfoxide.
\nAppearance:
\n2 mg: Pink, round, film-coated tablets debossed with “GS HMJ”.
\n0.5 mg: Yellow, oval, film-coated tablets debossed with “GS TFC”.
\nStorage: Store at 20\u00b0C\u201325\u00b0C (68\u00b0F\u201377\u00b0F).<\/p>\n","protected":false},"excerpt":{"rendered":"
Brand Name: \u8fc8\u5409\u5b81\u00ae\uff08Mekinist\u00ae\uff09
\nGeneric Name: Trametinib
\nStrength: 2mg per tablet, 30 tablets per bottle
\nManufacturer: Novartis Pharma Stein AG
\nMarketing Authorization Holder: Novartis Pharmaceuticals (China) Co., Ltd.
\nApproval Date in China: March 06, 2019
\nRegistration Number: HJ20190009
\nStorage: Store below 25\u2103, sealed and protected from light; keep out of reach of children<\/p>\n
Price&Cost:Contact Us now for the best price of Trametinib \uff08Mekinist\uff09<\/p>\n","protected":false},"featured_media":3747,"comment_status":"open","ping_status":"closed","template":"","meta":[],"product_brand":[80],"product_cat":[27],"product_tag":[],"class_list":["post-3746","product","type-product","status-publish","has-post-thumbnail","product_brand-novartis","product_cat-tablets","first","instock","shipping-taxable","product-type-simple"],"yoast_head":"\n