Atrasentan
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Atrasentan is an experimental drug that is being studied for the treatment of various types of
cancer Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal b ...
, including non-small cell
lung cancer Lung cancer, also known as lung carcinoma (since about 98–99% of all lung cancers are carcinomas), is a malignant lung tumor characterized by uncontrolled cell growth in tissues of the lung. Lung carcinomas derive from transformed, malign ...
. It is also being investigated as a therapy for diabetic kidney disease. Atrasentan failed a phase 3 trial for prostate cancer in patients unresponsive to hormone therapy. A second trial confirmed this finding. It is an
endothelin receptor antagonist An endothelin receptor antagonist (ERA) is a drug that blocks endothelin receptors. Three main kinds of ERAs exist: * selective ETA receptor antagonists ( sitaxentan, ambrisentan, atrasentan, BQ-123, zibotentan, edonentan), which affect e ...
selective for subtype A (ETA). While other drugs of this type ( sitaxentan, ambrisentan) exploit the
vasoconstrictive Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vessel ...
properties of endothelin and are mainly used for the treatment of pulmonary arterial hypertension, atrasentan blocks endothelin induced cell proliferation. In April 2014, de Zeeuw et al. showed that 0.75 mg and 1.25 mg of atrasentan reduced urinary albumin by 35 and 38% respectively with modest side effects. Patients also had decreased home blood pressures (but no change in office readings) decrease total cholesterol and LDL. Patients in the 1.25 mg dose group had increased weight gain which was presumably due to increased edema and had to withdraw from the study more than the placebo or 0.75 mg dose group. Reductions in proteinuria have been associated with beneficial patient outcomes in diabetic kidney disease with other interventions but is not an accepted end-point by the FDA. In 2013, SONAR trial was initiated to determine if atrasentan reduces kidney failure in diabetic kidney disease.


References

{{Chemotherapeutic agents Endothelin receptor antagonists Experimental cancer drugs Benzodioxoles Carboxylic acids