Selpercatinib is the generic name for the trade name drug Retevmo™. In some cases, health care professionals may use trade name Retevmo™ or the generic name Selpercatinib when referring to the drug.
Drug Type: Selpercatinib is a targeted therapy. This medication is classified as a RET tyrosine kinase inhibitor (for more detail, see “How Selpercatinib Works” below).
What Selpercatinib Is Used For
- Treatment of non-small cell lung cancer and thyroid cancer with an abnormal RET gene (RET gene mutation or RET gene fusion-positive)
Note: If a drug has been approved for one use, physicians may elect to use this same drug for other problems if they believe it may be helpful.
How Selpercatinib Is Given
- Selpercatinib is taken as a capsule by mouth, usually 2 times a day with or without food.
- Swallow selpercatinib capsules whole. Do not crush, chew, open, or dissolve the contents of the capsule.
- Selpercatinib doses should be separated by 12 hours.
- If you vomit after taking a dose of selpercatinib, do not take an extra dose. Take the next dose of selpercatinib at your scheduled time.
- Do not take a missed dose of Selpercatinib unless it is more than 6 hours until your next scheduled dose.
- If you take too much selpercatinib, call your healthcare provider or go to the nearest hospital emergency room right
The amount of selpercatinib that you will receive depends on many factors, including your weight, your general health or other health problems, and the type of cancer or condition you have. Your doctor will determine your exact dosage and schedule.
Important things to remember about the side effects of selpercatinib:
- Most people will not experience all of the side effects listed
- Side effects are often predicatble in terms of their onset, duration, and severity
- Most side effects will improve after therapy is complete
- There are things your treatment team can do to minimize or prevent side effects
The following side effects common (occurring in greater than or equal to 30%) for patients taking selpercatinib:
These are less common side effects (occurring in 10-29%) for patients taking selpercatinib:
These are rare serious side effects for patients receiving selpercatinib:
Not all side effects are listed above. Side effects that are very rare -- occurring in less than about 10 percent of patients -- are not listed here. But you should always inform your health care provider if you experience any unusual symptoms.
When to Contact Your Doctor or Health Care Provider/
Contact your health care provider immediately, day or night, if you should experience any of the following symptoms:
- Fever of 100.4º F (38º C) or higher, chills (possible signs of infection)
The following symptoms require medical attention, but are not an emergency. Contact your health care provider within 24 hours of noticing any of the following:
- Nausea (interferes with ability to eat and unrelieved with prescribed medication)
- Vomiting (vomiting more than 4-5 times in a 24-hour period)
- Diarrhea (4-6 episodes in a 24-hour period)
- Unusual bleeding or bruising
- Black or tarry stools, or blood in your stools
- Blood in the urine
- Pain or burning with urination
- Extreme fatigue (unable to carry on self-care activities)
- Mouth sores (painful redness, swelling or ulcers)
Always inform your health care provider if you experience any unusual symptoms.
- Before starting selpercatinib treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.)
- Avoid taking acid-reducing agents such as proton pump inhibitors (dexlansoprazole, esomeprazole, lansoprazole, omeprazole, pantoprazole, rabeprazole), H2 blockers (famotidine), and locally-acting antacids (TUMS®, calcium carbonate; Maalox®, alum-mag hydroxide-simethicone) during treatment with selpercatinib
- If you cannot avoid taking an antacid:
- Take selpercatinib with food when also administered with a proton pump inhibitor
- Take selpercatinib 2 hours before or 10 hours after administration of H2 blocker
- Take selpercatinib 2 hours before or 2 hours after administration of locally-acting antacid.
- Do not receive any kind of immunization or vaccination without your doctor’s approval while taking Selpercatinib.
- You should stop taking Selpercatinib at least 7 days before your planned surgery
- Inform your health care professional if you are pregnant or may be pregnant prior to starting this treatment. This drug must not be given to a pregnant woman or a woman who intends to become pregnant. If you become pregnant while taking Selpercatinib, stop taking the medication immediately and call your doctor for further instructions.
- For both men and women: Use contraceptives, and do not conceive a child (get pregnant) while taking Selpercatinib. Barrier methods of contraception, such as condoms, are recommended for up to 1 week after last dose of Selpercatinib.
- Do not breast feed while taking Selpercatinib and for 1 week after the last dose.
- Drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise.
- You may be at risk of infection so try to avoid crowds or people with colds, and report fever or any other signs of infection immediately to your health care provider.
- Wash your hands often.
- Use an electric razor and a soft toothbrush to minimize bleeding.
- Avoid contact sports or activities that could cause injury.
- To reduce nausea, take anti-nausea medications as prescribed by your doctor, and eat small, frequent meals.
- Follow regimen of anti-diarrhea medication as prescribed by your health care professional.
- Eat foods that may help reduce diarrhea (see managing side effects - diarrhea).
- Avoid sun exposure. Wear SPF 30 (or higher) sunblock and protective clothing.
- In general, drinking alcoholic beverages should be kept to a minimum or avoided completely. You should discuss this with your doctor.
- Get plenty of rest.
- Maintain good nutrition.
- Remain active as you are able. Gentle exercise is encouraged such as a daily walk.
- If you experience symptoms or side effects, be sure to discuss them with your health care team. They can prescribe medications and/or offer other suggestions that are effective in managing such problems.
Monitoring and Testing While Taking Selpercatinib
You will be checked regularly by your doctor while you are taking selpercatinib, to monitor side effects and check your response to therapy. Periodic blood work will be obtained to monitor your complete blood count (CBC) as well as the function of other organs (such as your kidneys and liver) will also be ordered by your doctor.
How Selpercatinib Works
Cancer is a disease caused by changes, also known as mutations, in DNA that change the way cells grow and divide. Cancer cells can be destroyed using many different types of medications that work in very different ways. Examples of medications that destroy cancer cells include cytotoxic chemotherapy, targeted therapy, immunotherapy, and antibody-drug conjugates.
Targeted therapy is about identifying the other features of cancer cells. Scientists look for specific differences in the cancer cells and the normal cells. This information is used to create a targeted therapy to attack the cancer cells without damaging the normal cells, thus leading to fewer side effects. Many targeted therapies are small molecule drugs. These drugs are small enough to enter the cell and affect other molecules such as proteins or DNA. Each type of targeted therapy works a little bit differently but all interfere with the ability of the cancer cell to grow, divide, repair and/or communicate with other cells.
Selpercatinib is a targeted therapy that is a highly selective anti-RET (REarranged during Transfection) kinase inhibitor. Selpercatinib binds and inhibits abnormal RET genes. By binding to these receptors Selpercatinib blocks an important pathway that promotes cell growth. Selpercatinib has anti-tumor activity in cancer cells with abnormal RET genes.
Note: We strongly encourage you to talk with your health care professional about your specific medical condition and treatments. The information contained in this website is meant to be helpful and educational but is not a substitute for medical advice.