Mobocertinib

Mobocertinib is a type of drug called a kinase inhibitor, which is used to treat a rare type of non-small cell lung cancer (NSCLC).

Mobocertinib is used to treat NSCLC caused by a specific type of gene mutation called an epidermal growth factor receptor (EGFR) exon 20 insertion mutation. Only about 2000 to 4000 people are diagnosed with this type of cancer in the US each year.

EGFR is a protein that helps cells to grow and divide. When an exon 20 insertion mutation occurs, it drives cells to grow and divide abnormally, causing an EGFR-positive cancer.

Mobocertinib works by binding to and blocking EGFR exon 20 insertion mutations, which helps to slow the growth of cancer cells.

Mobocertinib was granted accelerated approval by the US Food and Drug Administration (FDA) in 2021. It is used with the Oncomine Dx Target Test, which identifies patients with exon 20 insertion mutations.

Mobocertinib is a prescription medicine used to treat adults with NSCLC:

• that is locally advanced or has spread to other parts of the body (metastatic) and cannot be removed by surgery, and
• has an abnormal EGFR gene caused by an exon 20 insertion mutation
• whose disease has worsened while on or after chemotherapy that contains platinum

Your healthcare provider will perform a test to make sure that mobocertinib is right for you.

It is not known if mobocertinib is safe and effective in children.

• Take mobocertinib exactly as your healthcare provider tells you to take it.
• Take your prescribed dose of mobocertinib 1 time each day.
• Take mobocertinib with or without food.
• Swallow mobocertinib capsules whole. Do not open, chew, or dissolve the contents of the capsules.
• Do not change your dose or stop taking mobocertinib unless your healthcare provider tells you to.
• Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with mobocertinib if you develop certain side effects.

Mobocertinib may cause serious side effects, including:

• Changes in the electrical activity of your heart called QTc prolongation and Torsades de Pointes. QTc prolongation can cause irregular heartbeats that can be life-threatening and may lead to death. Your healthcare provider will check the electrical activity of your heart with a test called an electrocardiogram (ECG) and do blood tests to check your electrolytes before starting and during treatment with mobocertinib. Tell your healthcare provider right away if you feel dizzy, lightheaded, faint or have an irregular heartbeat.

See "What are the side effects of mobocertinib?" below for more information about side effects.

Before taking mobocertinib, tell your healthcare provider about all of your medical conditions, including if you:

• have heart problems, including a condition called long QTc syndrome
• have problems with your electrolytes, such as sodium, potassium, calcium or magnesium
• have lung or breathing problems other than lung cancer

Mobocertinib may cause serious side effects, including:

• See "Important information" above.
• Lung problems. Mobocertinib may cause severe lung problems that may lead to death. Symptoms may be similar to those symptoms from lung cancer. Tell your healthcare provider right away if you develop any new or worsening symptoms, including: trouble breathing or shortness of breath cough chest pain fever
• Heart problems, including heart failure. Mobocertinib may cause heart problems that may lead to death. Your healthcare provider should check your heart function before you start and during treatment with mobocertinib. Tell your healthcare provider right away if you have any signs or symptoms of a heart problem, including: feeling like your heart is pounding or racing shortness of breath chest pain swelling of your ankles and feet feeling faint
• Diarrhea. Diarrhea is common during treatment with mobocertinib, and may sometimes be severe. Diarrhea can cause you to lose too much body fluid (dehydration) and kidney problems. Your healthcare provider may tell you to start drinking more fluids and electrolytes to replace body salts or start taking your antidiarrheal medicines. Tell your healthcare provider right away if you have any loose stools or have stools more often than is normal for you.

The most common side effects of mobocertinib include:

• diarrhea
• rash
• nausea
• mouth sores
• vomiting
• decrease appetite
• infection of skin around nails
• tiredness
• dry skin
• muscle or bone pain

Mobocertinib may affect fertility in females and males, which may affect your ability to have a child. Talk to your healthcare provider if this is a concern for you.

These are not all of the possible side effects of mobocertinib.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

The recommended dose of mobocertinib is 160 mg taken orally once a day. Mobocertinib can be taken with or without food.

See full prescribing information for further details about mobocertinib dosing.

If you miss a dose of mobocertinib, and it has been more than 6 hours, skip the dose and take your next dose at your regularly scheduled time the next day.

If you vomit a dose of mobocertinib, do not take an extra dose. Take your next dose at your regularly scheduled time the next day.

Avoid eating grapefruit or drinking grapefruit juice during treatment with mobocertinib. Grapefruit may increase the amount of mobocertinib in your blood.

Tell your healthcare provider about all the medicines you take, including prescription medicines and over-the-counter medicines, vitamins, and herbal supplements. Tell your healthcare provider if you take medicines for heart problems.

Mobocertinib and other medicines may affect each other causing serious side effects.

Tell your doctor if you are pregnant or plan to become pregnant. Mobocertinib can harm your unborn baby.

Females who are able to become pregnant:

• Your healthcare provider should do a pregnancy test before you start treatment with mobocertinib.
• You should use an effective form of non-hormonal birth control during treatment and for 1 month after your last dose of mobocertinib.
• Birth control pills (oral contraceptives) and other hormonal forms of birth control may not work as well during treatment with mobocertinib.
• Talk to your healthcare provider about birth control methods that might be right for you during this time.
• Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with mobocertinib.

Males who have female partners who are able to become pregnant:

• You should use effective birth control during treatment and for 1 week after your last dose of mobocertinib.

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if mobocertinib passes into your breast milk. Do not breastfeed during treatment and for 1 week after your last dose of mobocertinib.

• Store mobocertinib at room temperature between 68°F to 77°F (20°C to 25°C).

Keep mobocertinib and all medicines out of the reach of children.

Active ingredient: mobocertinib

Inactive ingredients: None

Capsule shells: gelatin and titanium dioxide. The printing ink contains shellac, dehydrated alcohol, isopropyl alcohol, butyl alcohol, propylene glycol, strong ammonia solution, black iron oxide, potassium hydroxide, and purified water.

Mobocertinib is distributed under the brand name Exkivity by Takeda Pharmaceuticals America, Inc., Lexington, MA 02421.