| 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 |
|
|
| ADRs Induced by Drug |
|
|
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice.
|
|
|
