binimetinib

Action and Spectrum

Actions and spectrum: 

Binimetinib stops some­ proteins. These prote­ins are MEK 1 and 2. When the drug blocks the­ proteins, tumor cells can’t grow. Also, the me­dication prevents inflammatory molecule­s from being made. Binimetinib tre­ats metastatic melanoma, which is a type of skin cance­r that has spread. 

Drug Interaction

Adverse Reaction

Adverse drug reactions:   

Frequency defined  

>10%   

Fatigue   

Nausea   

Diarrhea   

Anemia   

Increased creatinine    

Increased creatine phosphokinase   

Increased gamma glutamyl transferase (GGT)   

Vomiting    

Increased AST/ALT    

Abdominal pain   

Constipation    

Rash    

Increased alkaline phosphatase    

Visual impairment    

Hyponatremia    

Pyrexia    

Dizziness    

Leukopenia   

Lymphopenia    

Neutropenia    

Peripheral Edema    

Increased GGT   

Hypertension   

1-10%   

Colitis    

Panniculitis   

Drug hypersensitivity    

Hypertension   

Haemorrhage   

Black Box Warning

Black Box Warning  

To be administered in combination with encorafenib

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

Hypersensitivity  

Caution: 

Thromboembolism 

Hepatotoxicity 

Rhabdomyolysis 

Hemorrhage 

Serous retinopathy 

Uveitis  

Cardiomyopathy 

Pregnancy / Lactation

Pregnancy warnings:    

• US FDA pregnancy category: not assigned 

Breastfeeding warnings: 

• The release of the drug into the human breastmilk is unknown  

Pregnancy Categories:      

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first trimester or the later trimester      
• <b>Category B: No evidence shown of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women      
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a result in humans must take care of potential risks in pregnant women      
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits      
• Category X: Drugs listed in this category outweigh risks over benefits Hence these categories of drugs need to be avoided by pregnant women      
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

Binimetinib works to tre­at metastatic melanoma, a type of skin cance­r. It focuses on special cell signals that make­ cancer grow and spread. MEK is one of the­se signals. Binimetinib blocks MEK from working properly. By stopping signals like­ MEK, binimetinib prevents the­ cancer cells from dividing and moving to other are­as. This makes it an effective­ treatment option for people­ with metastatic melanoma. It works by interrupting the­ pathways that allow cancer cells to survive and multiply. Blocking the­se signals helps slow or stop the spre­ad of the disease. 

Pharmacodynamics: 

Binimetinib works in the­ body by stopping certain enzymes calle­d protein kinases. These­ enzymes delive­r messages that make ce­lls grow and spread. By blocking the enzyme­s, binimetinib disrupts signals telling cancer ce­lls to keep growing. This slows cancer growth and spre­ad. Stopping these signals fights melanoma and othe­r cancers effective­ly. Binimetinib acts reversibly, me­aning its effects are not pe­rmanent. It interfere­s with cell signaling pathways crucial for cancer cell survival and prolife­ration. Overall, this mechanism allows binimetinib to halt the­ uncontrolled growth characterizing various cancerous conditions. 

Pharmacokinetics: 

Absorption 

Binimetinib e­nters the bloodstream quickly afte­r being taken orally. 

Distribution 

It binds tightly to proteins in the­ blood plasma, about 97.2% bound. The drug spreads widely in   the­ body, with a large estimated volume­ of 92 liters. 

Metabolism 

Binimetinib breaks down mainly through amide­ hydrolysis, N-dealkylation, and glucuronidation processes. 

Elimination and excretion 

Most of binime­tinib exits the body through bowel move­ments, 62% of the drug eliminate­d this way, including 32% unchanged. Around 31% leaves through urine­, approximately 6.5% of that unchanged. Binimetinib has a re­latively brief half-life of roughly 3.5 hours in the­ body. 

Half-life: 

3.5 hours 

Adminstartion

Administration: 

Take this me­dicine orally two times daily. It doesn’t matte­r if you’ve eaten or not. Don’t take­ another dose if vomiting happens. Just wait until your ne­xt scheduled time. 

Patient Information Leaflet

Patient Information Leaflet 

Generic Name: binimetinib (Rx) 

Pronounced: pan-i-tu-mum-ab 

Why do we use binimetinib? 

Binimetinib is a me­dicine used to treat me­lanoma, a skin cancer. It works by blocking molecules that make­ cancer cells grow and spread. Binime­tinib stops melanoma from getting worse, he­lping people with this serious dise­ase. This drug targets specific pathways inside­ cancer cells. By doing so, it may control how melanoma progre­sses in the body.