as salt: InChI=1S/C32H39N7O4.C4H6O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26;5-3(6)1-2-4(7)8/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36);1-2H2,(H,5,6)(H,7,8)
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 moleculetyrosine kinase inhibitor structurally similar toosimertinib (differs only by the presence of an additional isopropylester group).[9] Its molecular target isepidermal growth factor receptor (EGFR) bearing mutations in theexon 20 region.[10][11] Mobocertinib is anirreversible 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]
Mobocertinib is indicated for adults with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or afterplatinum-based chemotherapy.[6]
The volume of distribution of Mobocertinib at steady state is 3,509 L.[13] The mean oral bioavailability of Mobocertinib is 37%.[13] The median Tmax is 4 hours.[13] The average half-life of Mobocertinib and its metabolites is 18 hours.[13] Mobocertinib is metabolized by CYP3A enzymes.[13]
More serious side effects of Mobocertinib may include agitation, bloating of the eyes, lips, feet, blurred vision, coma, decreased urine output, headache, hostility, diarrhea, depression, dizziness, fainting, lethargy, anxiety, nausea, seizures, weight gain, fatigue as well as edema.[14] Other side effects which may be less frequent are: chills, cough, dilated neck veins, ill-feeling and trouble with breathing.[14] Other notable side effects of taking Mobocertinib are: having an acidic stomach, heartburn, acidity, hair loss/thinning, bone pain, sore throat, stuffy nose, trouble swallowing, vomiting and weakness in hands and feet.[14]
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