A Guide to Tyrosine Kinase Inhibitors: Uses, Benefits, and Drawbacks

In the world of cancer treatment, things move fast. Every day, researchers learn more about how cancer grows and spreads. This helps them drill down to specific targets that might be useful in fighting cancer.

Tyrosine kinase inhibitors (TKIs) are a specific group of targeted cancer medications. All TKIs are oral medications. But don’t let these pills fool you — they pack a punch. If you’ve been diagnosed with cancer, there’s a good chance you’ll encounter a TKI at some point in your treatment.

Here, we’ll discuss common TKI uses, in addition to some of their pros and cons.

What are tyrosine kinase inhibitors​ (TKIs)?

Tyrosine kinase inhibitors (TKIs) are a broad class of oral cancer medications. They generally work by blocking proteins involved in cell growth. Changes in your DNA may cause overactive or high amounts of proteins in cancer cells, so blocking them stops cancer growth. The specific protein that’s involved varies by person and cancer type.

Your oncologist may take a sample of your tumor or blood to see if you have unwanted changes in these proteins. This is called biomarker testing; it helps your oncologist decide if a TKI is right for you.

What are some of the most common TKIs?

TKIs are used in the treatment of many different types of cancers. Let’s dive deeper into the most common TKIs used to treat cancers such as leukemia, breast cancer, and lung cancer, among others.

Good to know: This article does not capture all possible TKIs used for each specific cancer.

Blood cancer

Gleevec (imatinib) paved the way as the first TKI approved. It’s an effective, first-choice option if you have a blood cancer called chronic myeloid leukemia (CML). Gleevec targets a specific protein, or tyrosine kinase, called BCR-ABL1. But there are now several other TKIs available that treat CML, too, including:

• Sprycel (dasatinib)

• Bosulif (bosutinib)

• Tasigna (nilotinib)

• Iclusig (ponatinib)

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A different protein, called Bruton’s tyrosine kinase (BTK), contributes to the growth of other blood cancers, such as chronic lymphocytic leukemia (CLL) and certain lymphomas. TKIs that block BTK and treat these cancers include:

• Imbruvica (ibrutinib)

• Calquence (acalabrutinib)

• Brukinsa (zanubrutinib)

• Jaypirca (pirtobrutinib)

Lung cancer

TKIs play a particularly large role in a type of lung cancer called non-small cell lung cancer (NSCLC). There are several proteins that are overactive or found in high amounts in NSCLC. These are prime targets for NSCLC TKIs. The likelihood of having one of these overactive proteins varies from person to person.

If you have metastatic NSCLC — cancer that has spread to other parts of your body — and your oncologist finds a specific change in one of these proteins, TKIs are often a first choice for fighting your cancer.

TKIs used in NSCLC

Breast cancer

About 1 in 5 people with breast cancer have too much of a protein called HER2 on their cancer cells. If you have a high enough amount of HER2, your breast cancer is considered “HER2-positive.” There are several TKIs available to treat HER2-positive breast cancer. These include:

• Tukysa (tucatinib)

• Tykerb (lapatinib)

• Nerlynx (neratinib)

Tukysa and Tykerb are only used in breast cancer that has spread (advanced breast cancer). They’re used in combination with other medications to make them more effective.

Nerlynx can be used alone in early breast cancer or in combination with other treatments in advanced breast cancer.

Skin cancer

Melanoma is a type of skin cancer. About half of melanomas have overactive BRAF proteins. The same TKIs that target BRAF in NSCLC are also used in melanoma. These include:

• Tafinlar

• Braftovi

• Zelboraf

Another protein, called MEK, contributes to BRAF’s cancer growth. For this reason, you’ll often find TKIs that block BRAF are combined with TKIs that block MEK to make them both work better. TKIs that target MEK include:

• Mekinist 

• Mektovi

• Cotellic (cobimetinib)

Kidney and liver cancer

TKIs are important for treating kidney and liver cancer. Unlike with the previously mentioned cancers, testing for specific mutations or changes in proteins is not needed to qualify for a TKI. In addition to cutting off blood supply to tumors, these TKIs target several proteins that are known to contribute to cancer growth in liver and kidney cancers.

There’s a lot of overlap between the TKIs approved for each of these cancers, so here’s a table to help keep them straight.

In kidney cancer, many of these TKIs are combined with another type of treatment called immunotherapy.

Soft tissue cancer

TKIs are also used in a type of cancer that affects the lining of your gut, called a gastrointestinal stromal tumor (GIST). Gleevec is most commonly used for GIST, while Sutent, Stivarga, and Qinlock (ripretinib) can be used later on if Gleevec or other TKIs stop working. Ayvakit (avapritinib) can also be helpful if you have a change in a gene called PDGFRA.

What are the main benefits of TKIs?

One of the main benefits of TKIs is that they block specific proteins that lead to cancer growth, allowing for more targeted cancer treatment. This helps spare healthy cells and makes side effects more manageable (compared with nonspecific treatments such as chemotherapy).

Another plus is that TKIs come as oral medications. You can take them in the comfort of your own home. This cuts down on the need for visits to your oncologist’s office or an infusion center.

What are the main drawbacks of TKIs?

TKIs are only effective if you take them as prescribed. If you have trouble remembering to take pills, TKIs may not be the best choice for you. Fortunately, there are several ways to help you remember your doses — including using medication reminder apps, trying personal alarms, and setting a medication routine around daily tasks.

Be aware that certain foods and medications could affect how well your specific TKI is absorbed. You have to be able to swallow pills, too. If you’re having trouble, taking a pill with a large glass of water or trying specific swallowing techniques can be helpful. And remember, many cancer pills can’t be crushed, split, or put into certain foods. This includes TKIs.

Unlike chemotherapy and other medications given through a vein, TKIs are often given at a set dose. This means that everyone gets the same dose, despite differences in body size. This can increase the chance of side effects in certain people.

On the topic of side effects, TKIs still have the potential to cause troublesome side effects, despite being a targeted therapy. For example, EGFR TKIs often cause an acne-like skin rash, while VEGF TKIs can cause high blood pressure, blood clots, and bleeding.

What’s more, TKIs can be quite expensive. Some cost anywhere from $5,000 to $10,000 per month without insurance or any discounts. If your copays are too high or you don’t have insurance, you may need to apply for financial assistance programs to afford the medication.

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Written by:

Rachel Feaster, PharmD, BCOP, BCPS

Rachel Feaster has over 10 years of professional experience in ambulatory, inpatient, pharmacogenomics, and oncology care. She is board certified in oncology and pharmacotherapy.

Edited by:

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.

Reviewed by:

Vanessa Carranza, PharmD

Vanessa Carranza, PharmD, is a pharmacist who has dedicated her career to the advancement of medical education for healthcare providers, patients, and caregivers, most notably in the oncology space.

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