Tyrosine kinase inhibitors (TKIs) used in the management of chronic myeloid leukaemia are associated with haematologic toxicities—Which TKI is the safest?

Abstract

Tyrosine kinase inhibitors (TKIs) used in the management of chronic myeloid leukaemia are associated with haematologic toxicities-Which TKI is the safest? Before imatinib, patients with chronic myeloid leukaemia (CML) received hydroxycarbamide, or interferon-alpha alone or in combination with low-dose cytarabine. Younger and fit patients with a suitable donor could be allografted, which was the only potentially therapeutic approach that would result in long-term disease-free survival; however, substantial morbidities or even mortality was observed. The discovery of tyrosine kinase inhibitors (TKIs) against the BCR-ABL1 oncogenic fusion protein has revolutionized the management of CML. Imatinib, the first BCR-ABL1 TKI, was introduced in early 2000s, and in the upcoming years, more potent second-generation TKIs

The Potential Protective Role of Naringenin against Dasatinib-Induced Hepatotoxicity

“…These drugs are highly efficacious in the treatment of leukemia, especially in CML and Ph+ ALL patients. Subsequently, TKIs are becoming a targeted approach and serving as an effective therapeutic plan for those patients with a variety of drug generation options [ 19 , 20 ]. DASA, as a member of the second-generation TKIs, was approved for the treatment of all CMLs and Ph + ALL patients, especially in cases of imatinib resistance.…”

COVID-19 Induced Pancytopenia in a Major Molecular Response CML patient on Dasatinib: A Case Report and Review of Literature

“…It was reported that, during the early stages of treatment, commercially available TKI might cause toxicity, including myelosuppression and cytopenia [11] . A higher grade of myelosuppression (grade III-IV) is generally seen in the initial stage of treatment and declines dramatically with longer duration of therapy [12] . Despite these findings, neither CML nor management with TKI triggers clinically significant immunosuppression in the chronic phase [5,10,13] .…”

Bosutinib – related pleural effusion in patients with chronic myeloid leukemia

“…Knowing the fact that second-generation TKIs (2GTKIs) are more potent than imatinib, inducing more rapid and profound responses with lower rates of transformation to advanced disease, these drugs are often considered as a better treatment option over imatinib in the upfront setting. Besides the potency and efficacy of these drugs, 2GTKIs can be associated with both hematologic and nonhematologic toxicities [3,4], which might interfere with patient health related quality of life [5]. In addition to targeting BCR-ABL1, 2GTKIs also inhibit other kinases and most of the nonhematologic adverse events (AEs) of these drugs are thought to be due to these off-target effects.…”