Action and Spectrum

Tazemetostat is an oral, small-molecule inhibitor of EZH2, a protein that regulates gene expression. It is being investigated as a potential treatment for cancer, including certain types of lymphoma and solid tumors. 

Tazemetostat is thought to work by inhibiting the function of EZH2, which may lead to the inhibition of cancer cell growth and proliferation. It is being studied in several clinical trials for cancer treatment, including phase 3 trials for treating certain types of lymphoma and solid tumors. 

Drug Interaction

Adverse Reaction

>10%: 

Pain  

Decreased hemoglobin  

Fatigue  

Decreased lymphocytes 

Increased triglycerides  

Nausea 

Increased glucose  

Decreased sodium  

Decreased phosphate  

Decreased appetite  

Vomiting  

Decreased albumin  

Decreased WBC count  

Cough  

Hemorrhage  

Headache  

Decreased calcium  

Anemia  

Decreased weight  

Decreased glucose  

1-10%: 

Dyspnea  

Hemorrhage  

Decreased appetite  

Increased AST  

Increased ALT  

Increased triglycerides 

Increased alkaline phosphatase  

Decreased potassium  

Decreased sodium  

Decreased phosphate 

Fatigue  

Abdominal pain

Black Box Warning

Contraindication / Caution

Tazemetostat is contraindicated in patients hypersensitive to the active ingredient. 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the use of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the secretion of the drug in breast milk. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: 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 the 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 

Tazemetostat is a small molecule inhibitor of EZH2 (enhancer of zeste homolog 2), a protein that regulates gene expression. It is thought to work by inhibiting the activity of EZH2, which may lead to the inhibition of cancer cell growth and proliferation. Tazemetostat is generally well-tolerated; the most common side effects are fatigue, nausea, and constipation. 

Tazemetostat is metabolized primarily by the liver and is eliminated from the body through the kidneys. The half-life of tazemetostat in the body is approximately 14 hours, which means that it takes about 14 hours for the concentration of the drug in the body to be reduced by half. Tazemetostat is available in oral tablet form and is taken by mouth. It is typically given in combination with other cancer treatments, and the dosage and frequency of administration may vary depending on the treatment plan. 

Pharmacodynamics 

Tazemetostat is a small molecule inhibitor of EZH2 (enhancer of zeste homolog 2), a protein that regulates gene expression. 

Tazemetostat is thought to work by inhibiting the activity of EZH2, which may lead to the inhibition of cancer cell growth and proliferation. EZH2 is a component of a complex known as PRC2 (polycomb repressive complex 2), which is involved in regulating gene expression by adding a chemical modification called methylation to specific sites on histone proteins. By inhibiting EZH2, tazemetostat may disrupt the activity of PRC2, leading to changes in gene expression and potentially resulting in the death of cancer cells. 

Pharmacokinetics: 

Tazemetostat is metabolized primarily by the liver and is eliminated from the body through the kidneys. The half-life of tazemetostat in the body is approximately 14 hours. It takes about 14 hours for the concentration of the drug in the body to be reduced by half. Tazemetostat is available in oral tablet form and is taken by mouth. It is typically given in combination with other cancer treatments, and the dosage and frequency of administration may vary depending on the treatment plan. 

Absorption: 

The absorption of tazemetostat may be affected by several factors, including the GI tract’s pH, certain foods or medications, and any diseases or conditions that affect the GI tract. In addition, the absorption of tazemetostat may be affected by certain medications or conditions that affect the pH of the GI tract, such as the use of proton pump inhibitors or the presence of conditions such as gastric acid reflux. 

Distribution: 

After it is absorbed from the gastrointestinal (GI) tract into the bloodstream, tazemetostat is distributed to various tissues in the body. The distribution of a drug like tazemetostat is determined by several factors, including the drug’s physical and chemical properties, its affinity for specific tissues, and its perfusion (blood flow). 

Tazemetostat is thought to be widely distributed throughout the body, including to the liver, spleen, and bone marrow. The extent of distribution may be affected by several factors, including the patient’s age, weight, overall health, and other medications being taken. 

Metabolism: 

Tazemetostat is metabolized primarily by the liver. The gut microbiome also metabolizes a small portion. After it is absorbed from the gastrointestinal (GI) tract into the bloodstream, tazemetostat is carried to the liver, where cytochrome P450 enzymes metabolize it. 

Elimination and excretion: 

After tazemetostat is metabolized in the liver, the resulting metabolites are carried to the kidneys by the bloodstream. They are filtered out of the blood and eliminated in the urine. The rate of excretion of tazemetostat and its metabolites may be affected by several factors, including the patient’s age, weight, overall health, and other medications being taken. 

Adminstartion

Patient Information Leaflet

Patient information leaflet 

Generic Name: tazemetostat 

Pronounced: tah-zeh-met-o-stat 

Why do we use tazemetostat? 

Tazemetostat helps treat Epithelioid Sarcoma and Follicular Lymphoma.