EPZ-5676 (Pinometostat) is a small molecule drug developed by Epizyme, Inc, for the treatment of acute leukemia. It is currently in clinical trials and has shown promising results in preclinical studies.
Chemical name: The chemical name of EPZ-5676 is N-((1-methylpiperidin-4-yl)methyl)-3-(6-(2-(2-methylpyridin-4-ylamino)pyrimidin-4-ylamino)pyridin-3-yl)acrylamide.
Molecular formula: The molecular formula for EPZ-5676 is C30H34N8O.
Formula weight: The formula weight for EPZ-5676 is 530.65 g/mol.
CAS No: The CAS number for EPZ-5676 is 1380288-87-8.
Top Ten Keywords and Synonyms:
Synonyms: Pinometostat; EPZ 5676; EPZ5676; EPZ-5676; N-[(1-Methyl-4-piperidinyl)methyl]-3-[6-(2-methyl-4-pyridinylamino)-3-pyridinyl]acrylamide; DOT1L Inhibitor EPZ-5676; N-(1-Methylpiperidin-4-ylmethyl)-3-[6-(2-methylpyridin-4-ylamino)pyridin-3-yl]acrylamide; EPZ5676-trifluoroacetate
Health Benefits of EPZ-5676: EPZ-5676 is designed to inhibit an enzyme called DOT1L, which plays a crucial role in the development of leukemia cells. By inhibiting DOT1L, EPZ-5676 may help to slow or stop the growth of leukemia cells, potentially leading to remission of the disease.
Potential Effects of EPZ-5676: Preclinical studies have shown that EPZ-5676 can inhibit the growth of leukemia cells both in vitro and in vivo, indicating its potential as a therapeutic agent for acute leukemia patients. Additionally, patients with genetic mutations that result in increased activation of DOT1L have been shown to respond well to EPZ-5676 treatment.
Product Mechanism: EPZ-5676 works by targeting and inhibiting the activity of DOT1L, an enzyme responsible for the methylation of histone H3 lysine 79 (H3K79). H3K79 methylation is associated with the activation of oncogenes, and DOT1L inhibition by EPZ-5676 leads to reduced levels of H3K79 methylation and subsequent suppression of leukemia cell growth.
Safety: As with any new drug, the safety of EPZ-5676 is being carefully evaluated in clinical trials. Preliminary studies suggest that EPZ-5676 is generally well-tolerated, with manageable side effects.
Side Effects: Common side effects of EPZ-5676 include fatigue, nausea, vomiting, and diarrhea. Less common but more serious side effects may include low white blood cell count or liver damage.
Dosing Information: The appropriate dose of EPZ-5676 depends on several factors, including the patient's age, weight, and overall health status. Dosage and duration of treatment are determined by the treating physician.
Conclusion: EPZ-5676 (Pinometostat) is a promising new drug under investigation for the treatment of acute leukemia. By inhibiting the activity of the DOT1L enzyme, it has the potential to slow or stop the growth of leukemia cells, leading to remission of the disease. While the drug is still in clinical trials, preliminary studies suggest that it is generally well-tolerated with manageable side effects. As research continues, EPZ-5676 may represent an exciting new option for patients with acute leukemia.
