ENMD-2076 (CAS: 934353-76-1) is a small molecule drug developed by EntreMed Inc., a biopharmaceutical company based in Maryland, USA. ENMD-2076 is an orally available kinase inhibitor that targets multiple pathways involved in cancer progression, including angiogenesis, cell proliferation, and DNA damage response. It has shown promising results in preclinical studies and is currently being evaluated in several clinical trials.
Chemical name: 4-[(4'-{3,5-dimethyl-4-[(4-methylpiperazin-1-yl)carbonyl]-1H-pyrrol-2-yl}-[1,1'-biphenyl]-4-yl)amino]-3-cyano-7-ethoxyquinoline
Molecular formula: C29H31N7O3
Formula weight: 525.61 g/mol
CAS No: 934353-76-1
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Health benefits of ENMD-2076: ENMD-2076 has the potential to offer several health benefits, primarily as a cancer drug. In preclinical studies, the drug has demonstrated efficacy against various types of cancer, including ovarian, breast, lung, and leukemia. ENMD-2076's mechanism of action involves inhibiting tumor angiogenesis and cell proliferation, which are essential processes for cancer growth and spread. In addition, it can also inhibit DNA damage response, making it potentially useful in combination with other chemotherapy agents.
Potential effects: ENMD-2076 has shown promising effects in preclinical and clinical studies. One Phase II study evaluated the drug's efficacy in patients with platinum-resistant ovarian cancer and found a response rate of 39%. Another Phase II study tested the drug in triple-negative breast cancer and reported a response rate of 20%, with a median progression-free survival of 3.7 months. ENMD-2076's potential effect on cancer stem cells, which are known to be resistant to chemotherapy, is also being investigated.
Product mechanism: ENMD-2076 functions as a multitargeted kinase inhibitor, targeting several pathways involved in cancer progression. It inhibits angiogenesis by blocking the VEGFR, FGFR, and PDGFR signaling pathways, which play crucial roles in tumor growth and metastasis. The drug also inhibits Aurora A kinase, which regulates cell division and is overexpressed in many types of cancer. Additionally, ENMD-2076 can inhibit DNA damage response by targeting the ATR/Chk1 pathway, which is involved in repairing DNA damage caused by chemotherapy.
Safety: ENMD-2076 has been generally well-tolerated in clinical studies, with most adverse events being mild to moderate in severity. The most common side effects reported include fatigue, nausea, diarrhea, and hypertension. However, some serious adverse events have been reported, such as pulmonary embolism and interstitial lung disease. Patients with a history of cardiac disease should use caution when taking this drug, as it can cause QT interval prolongation.
Dosing information: ENMD-2076 is administered orally and is available in capsule form. The recommended dose varies depending on the indication and the patient's condition. In clinical studies, doses range from 160 mg to 300 mg per day, usually given once or twice daily. The drug should be taken with food to increase absorption and reduce gastrointestinal side effects.
Conclusion: ENMD-2076 is a promising cancer drug that targets multiple pathways involved in tumor growth and metastasis. Its ability to inhibit angiogenesis, cell proliferation, and DNA damage response makes it a potentially valuable agent in the treatment of various types of cancer, including ovarian, breast, and lung cancers. Although the drug has shown promising results in early clinical studies, further research is needed to determine its long-term efficacy and safety
