Difference between revisions of "Asciminib (Scemblix)"
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==Mechanism of action== | ==Mechanism of action== | ||
− | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/allosteric-bcr-abl-tyrosine-kinase-inhibitor-abl001 NCI Drug Dictionary]: An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. | + | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/allosteric-bcr-abl-tyrosine-kinase-inhibitor-abl001 NCI Drug Dictionary]: An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain, and is a so-called STAMP (Specifically Targeting the ABL Myristoyl Pocket) inhibitor. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. |
==Diseases for which it is used== | ==Diseases for which it is used== | ||
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[[Category:Oral medications]] | [[Category:Oral medications]] | ||
− | [[Category: | + | [[Category:STAMP inhibitors]] |
[[Category:Chronic myelogenous leukemia medications]] | [[Category:Chronic myelogenous leukemia medications]] | ||
[[Category:FDA approved in 2021]] | [[Category:FDA approved in 2021]] |
Revision as of 23:38, 8 December 2021
Mechanism of action
From the NCI Drug Dictionary: An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain, and is a so-called STAMP (Specifically Targeting the ABL Myristoyl Pocket) inhibitor. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies.
Diseases for which it is used
History of changes in FDA indication
- 10/29/2021: Granted accelerated approval for patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP), previously treated with two or more tyrosine kinase inhibitors (TKIs). (Based on ASCEMBL)
- 10/29/2021: Approved for adult patients with Ph+ CML in CP with the T315I mutation. (Based on CABL001X2101)
Also known as
- Code name: ABL001
- Brand name: Scemblix