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Mobocertinib
Small molecule tyrosine kinase inhibitor / From Wikipedia, the free encyclopedia
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Mobocertinib, sold under the brand name Exkivity, is used for the treatment of non-small cell lung cancer.[6][8]
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Trade names | Exkivity |
Other names | TAK-788, AP-32788 |
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Routes of administration | By mouth |
Drug class | Antineoplastic |
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Formula | C32H39N7O4 |
Molar mass | 585.709 g·mol−1 |
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The most common side effects include diarrhea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin, and musculoskeletal pain.[6]
Mobocertinib is a small molecule tyrosine kinase inhibitor structurally similar to osimertinib (differs only by the presence of an additional isopropyl ester group).[9] Its molecular target is epidermal growth factor receptor (EGFR) bearing mutations in the exon 20 region.[10][11] Mobocertinib is an irreversible kinase inhibitor, forming a covalent bond with the cysteine 797 in the EGFR active site, leading to sustained inhibition of EGFR enzymatic activity. The irreversible binding leads to increased potency via higher affinity binding, more sustained EGFR kinase activity inhibition, and greater overall selectivity, as only a limited number of other kinases possess a cysteine in the equivalent position.[12]
Mobocertinib was approved for medical use in the United States in September 2021.[6][8] It is a first-in-class oral treatment to target EGFR Exon20 insertion mutations.[8]