Ensartinib

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A medication used in the treatment of non-small cell lung cancer


Ensartinib
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Ensartinib is a tyrosine kinase inhibitor (TKI) used in the treatment of non-small cell lung cancer (NSCLC) that is positive for anaplastic lymphoma kinase (ALK) rearrangements. It is a small molecule inhibitor that targets the ALK receptor tyrosine kinase, which is involved in the growth and spread of cancer cells.

Mechanism of Action[edit | edit source]

Ensartinib works by selectively inhibiting the activity of the ALK tyrosine kinase. ALK is a receptor tyrosine kinase that, when altered by genetic mutations or rearrangements, can drive the proliferation of cancer cells. By inhibiting ALK, ensartinib disrupts the signaling pathways that promote tumor growth and survival, leading to cancer cell death.

Clinical Use[edit | edit source]

Ensartinib is primarily used in patients with ALK-positive NSCLC. It is often prescribed for patients who have developed resistance to other ALK inhibitors or who cannot tolerate other treatments. Ensartinib has shown efficacy in both treatment-naïve patients and those who have previously been treated with other ALK inhibitors.

Pharmacokinetics[edit | edit source]

Ensartinib is administered orally and is absorbed into the bloodstream, where it exerts its effects on cancer cells. The drug is metabolized in the liver and excreted primarily through the feces. The pharmacokinetic profile of ensartinib allows for once-daily dosing, which can improve patient compliance.

Side Effects[edit | edit source]

Common side effects of ensartinib include fatigue, nausea, diarrhea, and rash. More serious side effects can include liver toxicity, interstitial lung disease, and cardiac effects such as QT prolongation. Patients receiving ensartinib require regular monitoring to manage these potential adverse effects.

Development and Approval[edit | edit source]

Ensartinib was developed as part of ongoing efforts to improve the treatment of ALK-positive NSCLC. It has undergone clinical trials to establish its safety and efficacy, leading to its approval in several countries for the treatment of this specific type of lung cancer.

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