Dasatinib vs. Nilotinib: Comparing Two Tyrosine Kinase Inhibitors

Chronic Myeloid Leukemia (CML) is a form of cancer-related to the blood and bone marrow. This is a rather rare condition as it affects nearly 1 to 2 cases among every 100,000 people.

Furthermore, it is more common in men than in women. Even though science has made much progress in its treatment, selecting the right medicine is quite important.

There two prominent contenders in this case, dasatinib and nilotinib, and both have proven their effectiveness in treating and managing this condition. However, one cannot take both drugs at the same time which is why we will compare them in detail and find out which one if better for your individual needs.

What is Dasatinib?

Dasatinib is a medication used to manage specific types of leukemia. It is prescribed as an initial treatment for chronic myeloid leukemia (CML) in adults and for those who no longer respond to other CML drugs, such as imatinib (Gleevec), or cannot use them due to side effects.

Additionally, dasatinib was approved by the FDA for treating chronic CML in children aged 1 year or older in 2017 [ref].

For acute lymphoblastic leukemia (ALL), it is used in adults who cannot benefit from or tolerate other leukemia treatments. This is also combined with chemotherapy to treat certain types of ALL in children aged 1 year or older.

What is Nilotinib?

This medication is used to treat specific types of chronic myeloid leukemia (CML), a cancer of WBCs, in adults and children aged 1 year and older.

Additionally, it is used for adults whose CML could not be successfully treated with imatinib (Gleevec) or who cannot tolerate imatinib due to side effects.

Similarly, it is prescribed for children aged 1 year or older whose CML could not be managed with other tyrosine kinase inhibitors or who experience intolerable side effects from these treatments.

Mechanism of action of Dasatinib and Nilotinib:

Dasatinib

Dasatinib works by blocking specific proteins called tyrosine kinases that help cancer cells grow and divide. By stopping these proteins, dasatinib slows down or stops the growth of leukemia cells in chronic myeloid leukemia (CML) and other types of blood cancer.

Nilotinib

Nilotinib works by blocking a specific protein called BCR-ABL, which is abnormal in people with chronic myeloid leukemia (CML). This protein sends signals that make leukemia cells grow and divide uncontrollably. By stopping this protein, nilotinib helps slow down or completely stop the growth of cancer cells.

Dosage and administration

Dasatinib

Dosage:

The medication is available in tablet form (20mg, 50mg, 70mg, 80mg, 100mg, and 140mg). For freshly diagnosed adults with Philadelphia chromosome-positive (Ph+) CML in the chronic phase, the dose is 100mg once daily, adjustable to 140mg if the response is inadequate. For advanced CML (chronic, accelerated, or blast phases) with resistance or intolerance to previous therapy, the dose is 140mg once daily, adjustable to 180mg if necessary. It can be taken in the morning or evening.

Administration:

Take the tablet whole without cutting, crushing, or chewing, either with or without meals, in the morning or evening. Follow special handling and disposal procedures, and avoid exposure to crushed or broken tablets, especially if pregnant.

Nilotinib

Dosage:

Capsules are available in 150 mg and 200 mg strengths. For newly diagnosed Philadelphia chromosome-positive (Ph+) chronic phase (CP) chronic myeloid leukemia (CML), the recommended dose is 300 mg orally every 12 hours. For treatment-resistant or intolerant CP and accelerated phase (AP) Ph+ CML following prior therapy (e.g., imatinib), the dosage is 400 mg orally every 12 hours.

Administration

Take the medication twice daily at approximately 12-hour intervals unless otherwise directed. Take on an empty stomach, avoiding food for at least 2 hrs before and 1 hr after the dose.

Swallow capsules whole with water. If swallowing is difficult, then capsule contents can be mixed with 1 teaspoon of applesauce and consumed immediately (within 15 minutes). Do not store the mixture. If a dose is missed, continue with the next scheduled dose; do not double up.

Efficacy of Dasatinib vs. Nilotinib:

A study from 2021 found that nilotinib had a greater major molecular response (39% nilotinib vs 12% dasatinib) and complete cytogenetic response (24% nilotinib vs 16% dasatinib) response outcomes. This suggests that nilotinib is more effective than dasatinib in achieving these important response measures. [ref]

A study found that nilotinib and dasatinib work equally well for treating newly diagnosed chronic-phase chronic myeloid leukemia (CML).

Bosutinib showed slightly better results in achieving a major molecular response (MMR) after 24 months, but the difference wasn’t significant. This means nilotinib and dasatinib are still reliable first-choice treatments for CML. [ref]

A 2023 study, found that nilotinib and dasatinib work equally well in helping patients with CML and improving their health. However, nilotinib was more likely to cause blood-related side effects, while dasatinib was more likely to lead to fluid buildup. This means both medicines are good options, but the choice should depend on the patient’s specific needs and the balance between risks and benefits. [ref]

Research from 2024 found that nilotinib and dasatinib had comparable efficacy to each other, with significantly higher therapy responses and failure-free survival rates than imatinib. However, there were no proper differences in progression-free survival or overall survival between nilotinib and dasatinib. [ref]