1. Indications and Usage
\nNeurofibromatosis Type 1 (NF1): Treatment of pediatric patients 3 years of age and older with symptomatic, inoperable plexiform neurofibromas (PNs) associated with NF1 .
\nNote: Approved specifically for children; data for adult use as initial treatment is limited .
\n2. Dosage and Administration
\nAdministration: Oral administration. Capsules must be swallowed whole with water (do not crush, chew, or open). Can be taken with or without food .
\nStandard Dose:
\nRecommended Dose: 25 mg\/m\u00b2 twice daily (approximately every 12 hours).
\nCalculation: Dose is calculated based on Body Surface Area (BSA) and rounded to the nearest 5 mg or 10 mg (maximum single dose 50 mg) .
\nMissed Dose: If a dose is missed, take it as soon as possible if it is more than 6 hours before the next scheduled dose. Otherwise, skip the missed dose.
\nVomiting: If vomiting occurs after administration, do not re-administer the dose .
\n3. Mechanism of Action
\nSelumetinib is a selective inhibitor of mitogen-activated protein kinase 1 and 2 (MEK1 and MEK2).
\nMEK proteins are upstream regulators of the ERK signaling pathway, which promotes cell proliferation.
\nIn NF1, the loss of neurofibromin function leads to overactivation of this pathway.
\nBy inhibiting MEK, selumetinib blocks ERK phosphorylation, thereby reducing tumor cell proliferation and inducing apoptosis .
\n4. Safety and Warnings
\nEmbryo-Fetal Toxicity: May cause fetal harm. Contraception is required for females of reproductive potential during treatment and for 1 week after the final dose .
\nCardiomyopathy: Can cause a decrease in left ventricular ejection fraction (LVEF). Echocardiograms are recommended before initiation and periodically during treatment .
\nOcular Toxicity: Retinal vein occlusion (RVO) and uveitis may occur. Periodic ophthalmologic examinations are recommended .
\nRash and Acneiform Rash: Severe skin reactions are common. Dermatologic monitoring is necessary.
\nElevated Creatine Phosphokinase (CPK): Monitor CPK levels periodically, especially in patients with muscle pain or weakness .
\n5. Adverse Reactions
\nCommon adverse reactions (incidence \u226520%) in pediatric patients include:
\nGastrointestinal: Vomiting, diarrhea, nausea, abdominal pain.
\nDermatologic: Acneiform rash, dry skin, paronychia (nail bed inflammation), pruritus.
\nGeneral: Fatigue, fever (pyrexia), stomatitis .
\n6. Drug Interactions
\nCYP3A4 and CYP2C19 Inhibitors: Avoid co-administration with strong or moderate inhibitors (e.g., ketoconazole, clarithromycin) as they increase Selumetinib exposure. If unavoidable, dose reduction is required .
\nCYP3A4 Inducers: Avoid co-administration with strong inducers (e.g., rifampin) as they reduce efficacy .
\n7. Pharmaceutical Information
\nChemical Name: 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-6-[2-(hydroxyethoxy)carbamoyl]-1-methyl-1H-benzimidazole hydrogen sulfate .
\nMolecular Formula: C17H15BrClFN4O3 \u00b7 H2SO4 .
\nStorage: Store at 25\u00b0C (77\u00b0F); excursions permitted to 15\u00b0C-30\u00b0C (59\u00b0F-86\u00b0F). Keep out of reach of children .<\/p>\n","protected":false},"excerpt":{"rendered":"
Brand Name:\u79d1\u8d5b\u4f18\u00ae (Koselugo\u00ae)<\/p>\n
Generic Name:Selumetinib Hydrogen Sulfate<\/p>\n
Strength:Two specifications: 10 mg per capsule \/ 25 mg per capsule; 60 capsules per bottle, 1 bottle per box<\/p>\n
Manufacturer:Patheon Pharmaceuticals Incorpated(USA)<\/p>\n
Marketing Authorization Holder:AstraZeneca UK Limited\uff08\u963f\u65af\u5229\u5eb7\u82f1\u56fd\u6709\u9650\u516c\u53f8\uff09\uff0c\u56fd\u5185\u4e0a\u5e02\u8bb8\u53ef\u6301\u6709\u4eba\u5173\u8054\u4f01\u4e1a\u4e3a\u963f\u65af\u5229\u5eb7\u6295\u8d44\uff08\u4e2d\u56fd\uff09\u6709\u9650\u516c\u53f8<\/p>\n
Approval Date in China:April 28, 2023<\/p>\n
Registration Number:10mg \u89c4\u683c\uff1a\u56fd\u836f\u51c6\u5b57HJ20230044;25mg \u89c4\u683c\uff1a\u56fd\u836f\u51c6\u5b57HJ20230045<\/p>\n
Storage:Store in original sealed bottle at 25\u00b0C; short-term transportation is permitted between 15\u201330\u00b0C. Keep the desiccant inside the bottle, protect from moisture and light, and keep out of reach of children<\/p>\n
Price&Cost:Contact Us now for the best price of Selumetinib Hydrogen Sulfate\uff08Koselugo\uff09<\/p>\n","protected":false},"featured_media":2858,"comment_status":"open","ping_status":"closed","template":"","meta":[],"product_brand":[75],"product_cat":[26],"product_tag":[],"class_list":["post-2857","product","type-product","status-publish","has-post-thumbnail","product_brand-astrazeneca","product_cat-capsules","first","instock","shipping-taxable","product-type-simple"],"yoast_head":"\n