| Pharmaceutical Information |
| Drug Name |
Asciminib |
| Drug ID |
BADD_D02528 |
| Description |
Asciminib is a tyrosine kinase inhibitor (TKI) used in the treatment of chronic-phase Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML). More specifically, it is an inhibitor of the ABL1 kinase activity of the BCR-ABL1 fusion protein[L38995] which serves as a driver of CML proliferation in most patients with the disease.[L39005] It has also shown benefit in Ph+ CML with the T315I mutation, which produces a mutant BCR-ABL1 which is typically treatment-resistant as compared to wild-type BCR-ABL1.
Existing inhibitors of ABL compete at the ATP binding sites of these proteins and can be classified into those that target the active conformation of the kinase domain ([dasatinib], [bosutinib]) and those that target the inactive kinase domain ([imatinib], [nilotinib], [ponatinib]).[A241065] Asciminib is unique in that it acts as an allosteric inhibitor, binding at the myristoyl pocket of the BCR-ABL1 protein and locking it into an inactive conformation.[L38995,A241055]
Asciminib received FDA approval on October 29, 2021 (Scemblix, Novartis AG).[L39000] |
| Indications and Usage |
Asciminib is indicated for the treatment of adult patients with Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) in chronic phase who have been previously treated with ≥2 tyrosine kinase inhibitors.[L38995] It is also indicated in the treatment of Ph+ CML in adult patients with the T315I mutation.[L38995] |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EA06 |
| DrugBank ID |
DB12597
|
| KEGG ID |
D11403
|
| MeSH ID |
C000621806
|
| PubChem ID |
72165228
|
| TTD Drug ID |
DSHT18
|
| NDC Product Code |
0078-1091; 0078-1098 |
| UNII |
L1F3R18W77
|
| Synonyms |
asciminib | ABL001 | asciminib hydrochloride |
|
| Chemical Information |
| Molecular Formula |
C20H18ClF2N5O3 |
| CAS Registry Number |
1492952-76-7 |
| SMILES |
C1CN(CC1O)C2=C(C=C(C=N2)C(=O)NC3=CC=C(C=C3)OC(F)(F)Cl)C4=CC=NN4 |
| Chemical Structure |
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| ADRs Induced by Drug |
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