: Despite the fact that, in the last years, life expectancy of chronic myeloid leukemia (CML) patients has reached that of the normal population, a significant proportion of CML patients is likely to fail treatment with first- or second-generation tyrosine kinase inhibitors (TKIs). Failure to first-line treatment is commonly due to molecular resistance or unbearable toxicity. New specific compounds are tested in this setting to fulfill this unmet clinical need in CML; of these, asciminib has shown efficacy based on allosteric inhibition which allows to overcome resistance and off-target toxicity. This review aims to cover how asciminib will change the therapeutic scenario of CML, highlighting its mechanism of action, pharmacokinetics, efficacy and toxicity. Asciminib will be a possible option as third-line therapy for patients carrying resistant mutations, such as T315I, and/or not eligible for treatment with other TKIs.

Asciminib in chronic myeloid leukemia / Assanto, Giovanni Manfredi; Scalzulli, Emilia; Breccia, Massimo. - In: DRUGS OF TODAY. - ISSN 1699-3993. - 58:10(2022), pp. 479-489. [10.1358/dot.2022.58.10.3441853]

Asciminib in chronic myeloid leukemia

Assanto, Giovanni Manfredi;Scalzulli, Emilia;Breccia, Massimo
2022

Abstract

: Despite the fact that, in the last years, life expectancy of chronic myeloid leukemia (CML) patients has reached that of the normal population, a significant proportion of CML patients is likely to fail treatment with first- or second-generation tyrosine kinase inhibitors (TKIs). Failure to first-line treatment is commonly due to molecular resistance or unbearable toxicity. New specific compounds are tested in this setting to fulfill this unmet clinical need in CML; of these, asciminib has shown efficacy based on allosteric inhibition which allows to overcome resistance and off-target toxicity. This review aims to cover how asciminib will change the therapeutic scenario of CML, highlighting its mechanism of action, pharmacokinetics, efficacy and toxicity. Asciminib will be a possible option as third-line therapy for patients carrying resistant mutations, such as T315I, and/or not eligible for treatment with other TKIs.
2022
Asciminib; BCR-ABL kinase inhibitors; Chronic myeloid leukemia; Hematologic malignancies; STAMP (specifically targeting the ABL myristoyl pocket) inhibitors; T315I mutation
01 Pubblicazione su rivista::01a Articolo in rivista
Asciminib in chronic myeloid leukemia / Assanto, Giovanni Manfredi; Scalzulli, Emilia; Breccia, Massimo. - In: DRUGS OF TODAY. - ISSN 1699-3993. - 58:10(2022), pp. 479-489. [10.1358/dot.2022.58.10.3441853]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11573/1669707
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