Table 1.

R_x data of mobocertinib.

Parameter	Summary
Drug data	Proprietary name: Exkivity; Active ingredient: Mobocertinib succinate; Dosage Form: Capsule; Route: Oral; Strength: 48.06 mg of mobocertinib succinate (Equivalent to 40 mg of mobocertinib base); Applicant: Takeda Pharmaceuticals [33]
Application data	Application number: N215310; Review type: Priority review; Orphan status: Orphan drug; Approval date: 15 September 2021; Marketing Status: Prescription [33]
Exclusivity data	Exclusivity type (Expiry date): New chemical entity (September 15, 2026) [33]
Indication (Use Code)	NSCLC with EGFR exon 20 exon insertion mutations whose disease has progressed on or after platinum-based chemotherapy (U-3220) [30,33]
Recommended Dose	160 mg/day with/without food till disease progression/unacceptable toxicity. The dose can be reduced based on the adverse reactions [29,30,34,35]
Warning/Precautions	Exkivity may lead to QTc prolongation and/or torsades de pointes. If this happens, reduce the dose or discontinue Exkivity based on the severity of QTc prolongation. Discontinue Exkivity if the patient shows induction of interstitial lung disease/pneumonitis, cardiac toxicity, diarrhea, and embryo-fetal toxicity. Additionally, avoid concomitant use of CYP3A inhibitors with Exkivity that can prolong QTc [29,30]
Adverse effects	Diarrhoea, rash, nausea, stomatitis, vomiting, decreased appetite, paronychia, fatigue, dry skin, musculoskeletal pain, increased amylase/lipase/creatinine, and decreased potassium/hemoglobin/magnesium/lymphocytes [29,30,34]
Contraindication	No data is available [29,30]
Drug interaction	Avoid concomitant use of CYP3A inhibitors as well as inducers like itraconazole and rifampin [24,30]
Absorption	Tmax = 4 h; Absolute bioavailability = 37%; Cmax 45.8 ng/mL; AUC0-inf = 862 ngh/mL [34]
Volume of distribution	3509 L (38%) at steady-state [29,30]
Metabolism	Mobocertinib is metabolized by CYP3A via N-demethylation to produce two equipotent metabolites, namely, AP32960 (Figure 2) and AP32914 (Figure 2) [24]
Protein binding	Mobocertinib = 99.3%; AP32960 = 99.5%; AP32914 = 98.6% [25,29,30]
Route of elimination	Mobocertinib (Faeces, 76%; Urine, 4%), AP32960 (Faeces, 12%; Urine, 1%), AP32914 (Undetected) [29,30]
Half-life	Mobocertinib = 18 h; AP32960 = 24 h; AP32914 = 18 h [29,30]
Clearance	Mobocertinib = 138 L/h; AP32960 = 149 L/h; AP32914 = 159 L/h [29,30]
Toxicity	Cardiac toxicity; Ocular toxicity; embryo-fetal toxicity [29,30] Grade 3 or 4 abnormality: Decreased red blood cells (3.5%); Decreased lymphocytes (15%); Decreased platelets (0.9); Decreased leukocytes (0%); Increased creatinine (2.7%); Increased amylase (13%); Increased lipase (10%); Decreased potassium (5.3%); Increased alkaline phosphatase (1.8%); Decreased albumin (1.8%); Decreased magnesium (2.7%); Increased alanine aminotransferase (2.7%); Increased aspartate aminotransferase (1.8%); Decreased sodium (0.9%) [29,30] No data about overdose are available [29,30]