Zykadia (ceritinib) is used for the treatment of people with non-small cell lung cancer (NSCLC) that has spread to other parts of the body and whose tumors are positive for a specific genetic marker called ALK. ALK is detected by a test approved by the U.S. Food and Drug Administration (FDA).
How Zykadia works
Zykadia is a potent anaplastic lymphoma kinase (ALK) inhibitor. ALK is part of a family of proteins called receptor tyrosine kinases (RTKs), which transmit signals from a cell’s surface into the cell through a process called signal transduction. This process begins when the RTK is stimulated by a ligand, which makes it bind, or dimerize, to another RTK. After dimerization, the RTKs are tagged with a cluster of oxygen and phosphorus atoms called a phosphate group. This activates the RTK, which then transfers the phosphate group to another protein inside the cell, in turn activating that protein, and so on, in a cascading effect. The last activated protein binds to the DNA itself and triggers the expression of other genes. This signaling cascade is important in different cellular processes, such as cell growth, division, and maturation.
The ALK gene has been associated with more than 20 distinct molecules, including some that trigger the formation of human cancers.
Zykadia inhibits the phosphorylation of ALK, interrupting the signaling cascade and proliferation of ALK-dependent cancer cells in vitro and in vivo.
Zykadia in clinical trials
Different clinical trials have proven that inhibiting ALK signaling may lead to remarkable clinical improvement, as well as improvements in the quality of life of ALK-positive cancer patients.
A Phase 3 study (NCT01828099) called ASCEND-4 assessed Zykadia’s effectiveness and safety in previously untreated adult patients with advanced ALK-positive NSCLC compared with standard chemotherapy. The trial included 376 participants who either received 750 mg of Zykadia daily or standard chemotherapy.
The results showed a clinically significant improvement in progression free survival (PFS) in participants treated with Zykadia compared to standard chemotherapy. Other clinically important secondary objectives were also achieved, including objective response rate (ORR, defined as the proportion of patients with tumor size reduction of a predefined amount and for a minimum time period), and response duration (RD), measured from the time of initial response until documented tumor progression.
Zykadia is for oral use. The usual adult dose for the treatment of NSCLC is 750 mg once daily on an empty stomach (at least one hour before or two hours after a meal). Capsules should be swallowed whole with water and should not be chewed or crushed.
The treatment should be maintained until the disease progresses or signs of unacceptable toxicity appear.
Zykadia’s common side effects include gastrointestinal problems (stomach pain, loss of appetite, nausea, vomiting, and diarrhea), fatigue, and weight loss.
It may also cause liver, heart, or lung problems, and may cause harm to an unborn baby. Women who may become pregnant should use effective birth control for six months after stopping Zykadia.
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