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What is Xalkori, and How Does It Compare to Other Lung Cancer Medications?

Sonja Jacobsen, PharmD, BCPS, BCOPEmmeline C. Academia, PharmD, BCOP
Published on July 7, 2022

Key takeaways:

  • Xalkori (crizotinib) is a targeted therapy medication used to treat certain types of non-small cell lung cancer (NSCLC).

  • Xalkori treats lung cancer by blocking cancer-causing proteins made from ALK and ROS1 gene fusions.

  • Xalkori may cause side effects, including fatigue and changes in vision. More serious side effects are also possible. 

Senior man with face mask coughing. He has his hand in front of his face mask in a fist.
PonyWang/E+ via Getty Images

If you've been diagnosed with lung cancer, you may be wondering about all the testing and treatment options available to you. In recent years, the landscape of lung cancer treatment has grown and changed, making it hard to keep up with the latest treatments. 

Advancements in tumor testing, like biomarker testing, are one of the biggest areas of growth. Biomarker testing looks for changes in genes, proteins, and other molecules that may reveal treatment options that could be beneficial for you, like targeted therapy and/or immunotherapy. Some of these changes for people living with non-small cell lung cancer (NSCLC) happen in genes called ALK or ROS1. 

These genes may just sound like alphabet soup, but fusions with ALK or ROS1 are known drivers of lung cancer growth. About 4% of people with NSCLC test positive for the ALK fusions (ALK+), and about 2% of people test positive for the ROS1 fusions (ROS1+). If your lung cancer has one of these fusion genes, certain treatments could be a good option for you. 

One of these treatments is called Xalkori (crizotinib). Here, we'll discuss how Xalkori works to treat lung cancer, how effective it is, and how it stacks up against other treatment options for ALK+ and ROS1+ lung cancer.

What is Xalkori?

Xalkori is an oral targeted therapy medication. It’s used to treat metastatic lung cancer, meaning cancer that has spread to other parts of the body. More specifically, it treats metastatic NSCLC that has a genetic change in the ALK gene or ROS1 gene. When NSCLC has one of these fusions, it’s called ALK-positive (ALK+) or ROS1-positive (ROS1+) NSCLC. 

Your cancer specialist should test your lung cancer for one or more of these gene changes. Testing your tumor for biomarkers can let your cancer specialist know which mutation(s) may be fueling your lung cancer’s growth. This can help improve treatment decisions.

How does Xalkori work?

Xalkori works by targeting and blocking proteins that are made from ALK and ROS1 gene fusions. Specifically, when ALK and ROS1 genes change — or mutate — they form a fusion with another gene. These gene fusions create an overactive protein that causes cancer.

By blocking the effects of these fusion genes, Xalkori helps slow the growth of lung cancer cells and causes cancer cells to die. Because of this, targeted therapy is a preferred treatment option for people who have ALK+ or ROS1+ NSCLC.

How do you take Xalkori?

Xalkori comes as a capsule that's taken by mouth. For NSCLC, it's usually recommended to take 1 capsule (250 mg) by mouth 2 times a day. If you have liver or kidney problems, your cancer specialist may recommend you only take Xalkori once a day.

Xalkori can be taken with or without food. But you shouldn’t eat or drink anything containing grapefruit, like grapefruit juice, while you’re taking Xalkori. This is because grapefruit can cause a higher amount of Xalkori in your body. This interaction may be harmful and could lead to more side effects.

Xalkori capsules should be swallowed whole. You shouldn’t try to break open or crush the capsule.

How long do you have to take Xalkori for?

Xalkori is usually taken for as long as it continues working and you aren't having unmanageable side effects. This could be temporary, or it could be for months to years.

However, your cancer specialist may recommend lowering your dose or stopping Xalkori if you experience severe side effects. If your cancer worsens, your cancer specialist may recommend stopping Xalkori or switching to another treatment altogether.

How effective is Xalkori for lung cancer?

Xalkori has been shown to be effective for treating ALK+ and ROS1+ NSCLC in multiple studies.

ALK+ NSCLC

In one study of more than 300 people with metastatic ALK+ NSCLC, participants received either Xalkori or standard chemotherapy for metastatic NSCLC. People in this study had not received any prior treatment for their cancer. 

This study found that people who received Xalkori had about 4 months longer of progression-free survival than people who received chemotherapy. This means that their cancer did not get worse, or progress, for a longer period of time than those who received chemotherapy. 

Overall, Xalkori reduced the risk of lung cancer disease progression or death by 55% compared to chemotherapy.

ROS1+ NSCLC

Another study looked at 50 people with metastatic ROS1+ NSCLC who received Xalkori. Unlike the study mentioned above, this study didn’t compare Xalkori to chemotherapy. This study aimed to see if people with this gene mutation would respond well to Xalkori. 

The study found that 72% of people saw their tumors get smaller while taking Xalkori. Some people in this study went about 18 months (1.5 years) before seeing their tumors get bigger or spread after initially responding to Xalkori.

What are the common side effects of Xalkori?

Like many other cancer medications, Xalkori can cause side effects. Some common side effects of Xalkori include:

  • Vision changes like blurry vision, double vision, or flashes of light

  • Feeling tired

  • Nausea or vomiting

  • Diarrhea

  • Constipation

  • Loss of appetite

  • Upset stomach

  • Feeling dizzy

  • Numbness or tingling in hands or feet

  • Swelling

  • Upper respiratory tract infection

What are the serious side effects of Xalkori?

Xalkori can cause some serious side effects as well. These include:

  • Signs of liver problems, like yellowing of the skin or eyes

  • Signs of lung problems, such as cough and shortness of breath

  • Changes in heart rate

  • Vision loss

  • Severe nausea, vomiting, or diarrhea

  • Harm to an unborn baby if you take this medication while pregnant

If you experience any of these serious side effects, you should notify your healthcare provider right away.

Which medications are comparable to Xalkori?

In 2011, Xalkori became the first ALK inhibitor approved to treat lung cancer. Since then, many newer ALK inhibitors have been approved for the same use. They are sometimes referred to as “next-generation” ALK inhibitors. They include:

While these newer medications work similarly to Xalkori, they each have their own nuances. 

For example, Xalkori doesn’t work for cancer that has spread to the brain, but the newer ALK inhibitors are able to work in the brain. Next-generation ALK inhibitors also are more potent (stronger) than Xalkori. Over time, people treated with Xalkori may become resistant to Xalkori, meaning it stops working. The next-generation ALK inhibitors have been shown to work for people when Xalkori stopped working. 

Because of all these reasons, next-generation ALK inhibitors are preferred over Xalkori in the treatment of ALK+ NSCLC. Xalkori is usually only used if a next-generation ALK inhibitor isn’t available.

Xalkori was also the first ROS1 inhibitor approved to treat lung cancer. There are now a few other medications that work the same way:

Similarly, Rozlytrek is preferred over Xalkori because it works better for cancer that has spread to the brain. Lorbrena is usually only used after cancer has gotten worse on a medication like Xalkori.

If you experience unwanted side effects from one ALK or ROS1 inhibitor, rest assured that there are other options you can try.

What are the alternatives to Xalkori?

If Xalkori or other similar medications aren’t options for you, there are other treatments you and your cancer care team can consider for NSCLC. This usually means treatment with chemotherapy, immunotherapy, and/or another type of targeted therapy. 

Is there a best medication for lung cancer?

No. There isn’t one best medication for treating lung cancer. There are many different types of lung cancer, and they're not all treated the same way or with the same medications. The best treatment depends on your type and stage of lung cancer. Your insurance coverage status can also play a role. 

Your cancer specialist likely will test your lung cancer for a number of different biomarkers before determining the best treatment option(s) for you.

The bottom line

There are different types of lung cancer and a variety of treatment options. Targeted therapy medications like Xalkori are most beneficial for people with ALK+ or ROS1+ NSCLC. Xalkori can cause some side effects, like vision problems and liver problems. To see if Xalkori may be a treatment option for you, speak with a cancer specialist.

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Why trust our experts?

Sonja Jacobsen, PharmD, BCPS, BCOP
Sonja Jacobsen, PharmD, BCPS, BCOP,  is a clinical oncology pharmacy specialist currently practicing in Seattle. She has been practicing as a pharmacist since 2015 and is licensed to practice in Washington state and North Carolina.
Joshua Murdock, PharmD, BCBBS
Joshua Murdock, PharmD, BCBBS, is a licensed pharmacist in Arizona, Colorado, and Rhode Island. He has worked in the pharmacy industry for more than 10 years and currently serves as a pharmacy editor for GoodRx.
Emmeline C. Academia, PharmD, BCOP
Emmeline C. Academia, PharmD, BCOP, has been a practicing clinical pharmacist in adult oncology since 2020. She is a clinical pharmacy specialist in oncology at Beth Israel Deaconess Medical Center, in Boston.

References

American Cancer Society. (2019). What is lung cancer?

American Lung Association. (2021). ALK and lung cancer.

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Food and Drug Administration. (2016). FDA approves crizotinib capsules.

National Cancer Institute. (2021). Biomarker testing for cancer treatment.

National Cancer Institute. (2022). Targeted therapy to treat cancer.

National Comprehensive Cancer Network. (2021). Non-small cell lung cancer early and locally advanced patient guideline.

Pfizer Labs. (2021). Xalkori [package insert].

Sahu, A., et al. (2013). Crizotinib: A comprehensive review. South Asian Journal of Cancer.

Shaw, A. T., et al. (2014). Crizotinib in ROS1-rearranged non–small-cell lung cancer. New England Journal of Medicine.

Solomon, B. J., et al. (2014). First-line crizotinib versus chemotherapy in ALK-positive lung cancer. New England Journal of Medicine.

Villalobos, P., et al. (2018). Lung cancer biomarkers. Hematology/Oncology Clinics of North America.

Wu, J., et al. (2016). Second- and third-generation ALK inhibitors for non-small cell lung cancer. Journal of Hematology & Oncology.

GoodRx Health has strict sourcing policies and relies on primary sources such as medical organizations, governmental agencies, academic institutions, and peer-reviewed scientific journals. Learn more about how we ensure our content is accurate, thorough, and unbiased by reading our editorial guidelines.

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