Asciminib in chronic myeloid leukemia
Copyright 2022 Clarivate..
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.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:58 |
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| Enthalten in: |
Drugs of today (Barcelona, Spain : 1998) - 58(2022), 10 vom: 19. Okt., Seite 479-489 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Assanto, Giovanni Manfredi [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 01.11.2022 Date Revised 01.11.2022 published: Print Citation Status MEDLINE |
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| doi: |
10.1358/dot.2022.58.10.3441853 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM348198752 |
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| 520 | |a Copyright 2022 Clarivate. | ||
| 520 | |a 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 | ||
| 650 | 4 | |a Review | |
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Asciminib | |
| 650 | 4 | |a BCR-ABL kinase inhibitors | |
| 650 | 4 | |a Chronic myeloid leukemia | |
| 650 | 4 | |a Hematologic malignancies | |
| 650 | 4 | |a STAMP (specifically targeting the ABL myristoyl pocket) inhibitors | |
| 650 | 4 | |a T315I mutation | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a asciminib |2 NLM | |
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| 700 | 1 | |a Breccia, Massimo |e verfasserin |4 aut | |
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