Leukemia targeted therapy guide | Introduction and comparison of drugs classified by target
Leukemia is a blood cancer that originates in the bone marrow and is often caused by abnormal proliferation and dysfunction of white blood cells. Traditional treatment is mainly chemotherapy, but with the development of precision medicine, many "targeted drugs" targeting genetic abnormalities in cancer cells have been introduced. Blocking specific targets can greatly improve treatment outcomes and reduce side effects.
This article will classify according to targets and introduce the current common leukemia targeted drugs and their differences in clinical applications.
🔹 1. BCR-ABL fusion protein inhibitor
Indications : Chronic myeloid leukemia (CML), Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL)
BCR-ABL is a fusion protein produced by chromosomal rearrangement with abnormally active tyrosine kinase. It is an oncogenic driver of CML and some Ph+ ALL.
Common drug comparisons:
| Drug Name | generations | Features and Differences |
|---|---|---|
| Imatinib (Glivec) | First Generation | The world's first targeted anticancer drug lays the foundation for CML to become a chronic disease, but it is easy to develop drug resistance |
| Dasatinib (Sprycel) | Second Generation | Stronger in strength, can penetrate the central nervous system, suitable for Ph+ ALL or those who are ineffective against imatinib |
| Ponatinib (Iclusig) | Third Generation | It can fight against many mutations, including T315I, but it has severe side effects and should be used with caution. |
| Assimil (Scemblix) | Third Generation | Specifically targeting the T315I mutation, with milder side effects, it will gradually become the first choice for drug resistance after 2022 |
📌Brief analysis : Imatinib or dasatinib are often used as the first line. If drug resistance occurs, aximinib or ponatinib will be used instead, depending on the mutation type and tolerance.
🔹 2. BTK (Bruton's tyrosine kinase) inhibitors
Indications : Chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), mantle cell lymphoma (MCL)
BTK is a key enzyme for B cell development and survival. BTK inhibitors can cut off cancer cell signals and inhibit their proliferation.
Common drug comparisons:
| Drug Name | generations | Features and Differences |
|---|---|---|
| Ibrutinib (Imbruvica) | First Generation | The first approved BTK inhibitor, effective but with more side effects, such as arrhythmia and bleeding risk |
| Acalabrutinib (Calquence) | Second Generation | More specific to BTK, with fewer side effects, it is the first choice for many patients |
| Pitobrutinib (Jaypirca) | Third Generation | It can be used for patients with C481S drug-resistant mutations and is a next-generation therapy designed for those who have failed to respond to previous generations of treatments. |
📌Brief analysis : Currently, the second-generation drug (acalabrutinib) is commonly used as the first-line drug, and its side effect tolerance is better than that of the first-generation drugs; for drug-resistant mutations, pitubutinib is used instead.
🔹 3. BCL-2 inhibitors
Indications : Chronic lymphocytic leukemia (CLL), acute myeloid leukemia (AML, specific groups)
BCL-2 is an anti-apoptotic protein that makes cancer cells "immortal". BCL-2 inhibitors can restore the cell suicide mechanism and promote the natural apoptosis of cancer cells.
Common drugs:
| Drug Name | Features and Applications |
|---|---|
| Venetoclax (Venclexta) | Used alone or in combination with chemotherapy or anti-CD20 antibodies; especially suitable for elderly patients with poor physical strength |
📌Brief analysis : Venetoclax is an oral small molecule and a very important treatment option for AML and CLL, with significant effects in combination with traditional therapies.
💡 Conclusion
Targeted therapy is one of the core strategies for modern leukemia treatment, but each patient has different genetic backgrounds, disease progression, and side effect tolerance. Therefore , doctors need to select the most appropriate drugs and treatment sequence through genetic testing and disease assessment .
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