| Pharmaceutical Information |
| Drug Name |
Mobocertinib |
| Drug ID |
BADD_D02573 |
| Description |
Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR). It is used specifically in the treatment of non-small cell lung cancer (NSCLC) caused by exon 20 insertion mutations in the _EGFR_ gene,[L38368] which are typically associated with a poorer prognosis (as compared to "classical" _EGFR_ mutants causing NSCLC) and are associated with resistance to standard targeted EGFR inhibitors.[A238828] Mobocertinib appears to be an effective means of treating this otherwise treatment-resistant NSCLC, exerting an inhibitory effect on _EGFR_ exon 20 insertion mutant variants at concentrations 1.5- to 10-fold lower than those required to inhibit wild-type EGFR.[L38319]
Mobocertinib, under the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated approval by the FDA in September 2021 for the treatment of locally advanced or metastatic NSCLC in patients with _EGFR_ exon 20 insertion mutations who have failed previous therapies.[L38368] |
| Indications and Usage |
Mobocertinib is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations whose disease has progressed on or after platinum-based chemotherapy.[L38319] |
| Marketing Status |
approved; investigational |
| ATC Code |
L01EB10 |
| DrugBank ID |
DB16390
|
| KEGG ID |
D12001
|
| MeSH ID |
C000720862
|
| PubChem ID |
118607832
|
| TTD Drug ID |
DI4HA7
|
| NDC Product Code |
48957-0104; 63020-040 |
| UNII |
39HBQ4A67L
|
| Synonyms |
mobocertinib | propan-2-yl 2-(4-(2-(dimethylamino)ethyl-methylamino)-2-methoxy-5-(prop-2-enoylamino)anilino)-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate | TAK-788 |
|
| Chemical Information |
| Molecular Formula |
C32H39N7O4 |
| CAS Registry Number |
1847461-43-1 |
| SMILES |
CC(C)OC(=O)C1=CN=C(N=C1C2=CN(C3=CC=CC=C32)C)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)
C)OC |
| Chemical Structure |
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| ADRs Induced by Drug |
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