Mobotinib Instructions

Mobocertinib is a first-in-class oral tyrosine kinase inhibitor (TKI) specifically designed to selectively target epidermal growth factor receptor (EGFR) exon 20 insertion mutations. The approval of mobotinib was based on results from a Phase 1/2 clinical trial in patients with metastatic non-small cell lung cancer harboring an EGFR exon 20 insertion mutation who were pretreated with a platinum-based agent. EGFR is a protein that helps cells grow and divide. When an exon 20 insertion mutation occurs, it drives abnormal cell growth and division, leading to EGFR-positive cancers.

Indications ：

Mobotinib is a prescription drug used to treat adults with NSCLC that is locally advanced or has spread to other parts of the body (metastatic) and cannot be removed with surgery, and has an abnormal EGFR gene caused by an exon 20 insertion mutation, and the disease worsens during or after platinum-based chemotherapy. Your doctor will perform tests to make sure mobotinib is right for you. It is not known whether mobotinib is safe and effective in children.

Mechanism of Action: Mobotinib is a kinase inhibitor specifically designed to selectively target the epidermal growth factor receptor (EGFR) Exon20 insertion mutation at lower concentrations than wild-type (WT) EGFR. Following oral administration of mobotinib, two pharmacologically active metabolites (AP32960 and AP32914) with similar inhibitory properties to mobotinib were found in plasma. Mobotinib also inhibits the activity of other EGFR family members (HER2 and HER4) and another kinase (BLK) in vitro at clinically relevant concentrations (IC50 values u200bu200b<2 nM).

Dosage: Mobotinib is provided as an oral capsule. The recommended dose is 160 mg orally once daily until disease progression or unacceptable toxicity. Take mobotinib at the same time each day with a meal or alone. Swallow the mobotinib capsule whole. Do not open, chew, or dissolve capsule contents. If you miss a dose by more than 6 hours, skip the dose and take the next dose at the scheduled time the next day. If a dose is vomited, do not take additional doses. Take your next dose as prescribed the next day.

Side effects:

Mobotinib may cause serious side effects, including:

Lung problems. Mobotinib may cause serious lung problems and possibly death. Symptoms may be similar to those of lung cancer. Tell your doctor right away if you develop any new or worsening symptoms, including: difficulty breathing or shortness of breath; cough; chest pain; fever.

Heart problems, including heart failure. Mobotinib may cause heart problems that can lead to death. Your doctor should check your heart function before you start treatment with mobotinib and during treatment. Tell your doctor right away if you have any signs or symptoms of a heart problem, including: feeling like your heart is racing; shortness of breath; chest pain; swelling in your ankles and feet; feeling faint.

Diarrhea. Diarrhea is common during treatment with mobotinib and can sometimes be severe. Diarrhea can cause you to lose too much fluid (dehydration) and cause kidney problems. Your primary care doctor may tell you to start drinking more fluids and electrolytes to replace salt in your body or to start taking an antidiarrheal medication. Tell your doctor right away if you have any loose stools or have more frequent bowel movements than normal.

The most common side effects of mobotinib include: diarrhea; rash; nausea; mouth sores; vomiting; decreased appetite; infection of the skin around the nails; tiredness; dry skin; muscle or bone pain.

Mobotinib may affect fertility in women and men, which may affect your ability to have a baby. If you are concerned about this issue, please consult your primary care physician.

These are not all possible side effects of mobotinib. Regardless of any physical discomfort the patient experiences while taking Mobotinib, the patient should go to the hospital immediately for medical treatment.

Precautions: Mobotinib can cause life-threatening heart rate corrections QT (QTc) prolongation, including potentially fatal torsades de pointes (Torsades de Pointes), requiring QTc and electrolyte monitoring at baseline and periodically during treatment. treat. Increase frequency of monitoring in patients with risk factors for QTc prolongation. Avoid concomitant use of drugs known to prolong the QTc interval and avoid use with mobotinibstrong or moderate CYP3A inhibitors, which may further prolong QTc. Withhold, reduce dose, or permanently discontinue mobotinib based on severity of QTc prolongation.

Storage: Store mobotinib at room temperature 68°F to 77°F (20°C to 25°C). Keep mobotinib and all medicines out of the reach of children.