Description
Retevmo (Selpercatinib) is an oral medication aimed at treating cancer by targeting specific genetic changes. It falls under the category of targeted therapies, specifically acting as a receptor tyrosine kinase inhibitor (RET inhibitor). This drug zeroes in on cancers with RET genetic changes, such as non-small cell lung cancer (NSCLC) and certain types of thyroid cancer. By blocking the activity of the RET protein, Retevmo may slow the growth and survival of cancer cells with these genetic mutations.
F act Table |
Formula | C29H31N7O3 |
License | US FDA (2020) |
Bioavailability | ~73% (oral) |
Legal status | Prescription only (?) |
Chemical Name | 6-(2-Hydroxy-2-methylpropoxy)-2-[2-methoxy-4-[6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]anilino]pyrido[2,3-d]pyrimidin-7(8H)-one |
Elimination half-life | 32 hours |
Dosage (Strength) | 40 mg, 80 mg capsules |
Pregnancy | Not recommended (Category D) |
Brands | Retevmo |
Protein binding | 96% |
PubChem CID | 132968958 |
MedlinePlus | a620036 |
ChEBI | CHEBI:145825 |
ATC code | L01EX19 |
DrugBank | DB15340 |
KEGG | D11599 |
Routes of administration | Oral |
Directions
Retevmo should be taken exactly as prescribed by a healthcare professional. Patients typically take it orally with or without food, with the standard dosage varying based on the individual's condition and response to treatment. For managing specific cancers, such as locally advanced non-small cell lung cancer, medullary thyroid cancer (MTC), or other cancers with abnormal RET genes, the capsule is usually recommended twice daily at 12-hour intervals. Swallow capsules whole without chewing or crushing them.
Ingredients
The active ingredient in Retevmo is Selpercatinib. The inactive ingredients in the 40 mg and 80 mg capsules include microcrystalline cellulose and colloidal silicon dioxide.
Contraindications
There are no known contraindications on the drug label. However, it may need to be avoided in people with a known hypersensitivity or allergy to Selpercatinib or any of the ingredients in its formulation.
Cautions
- Talk to a healthcare provider about the following before starting treatment with Retevmo:
- Any allergies you may have.
- If you are currently pregnant or nursing.
- All other health conditions you're dealing with.
- Any medications you are presently taking.
- Before starting Retevmo, and during your treatment, your doctor will check your liver function through blood tests because Retevmo can affect liver health. Depending on how severe any liver issues are, your treatment plan may need to change.
- Keep an eye out for any new or worsening symptoms related to your lungs, such as difficulty breathing or coughing. If these occur, your doctor might adjust your dose of Retevmo or stop it altogether.
- If you have high blood pressure, it needs to be under control before you start Retevmo. Your blood pressure will be monitored closely once you begin treatment, especially during the first week and then monthly.
- Retevmo can affect your heart's rhythm, so your doctor will monitor this, especially if you're at risk for heart rhythm issues. This monitoring will be more frequent if you're taking other medications that can also affect your heart rhythm.
- If you experience severe bleeding while taking Retevmo, the medication may need to be stopped permanently.
- In case of an allergic reaction to Retevmo, your treatment may be paused and you might be given steroids. Once the reaction has resolved, you may be able to start taking Retevmo again at a lower dose and gradually increase it.
- This is a condition that can occur when cancer cells break down rapidly and release their contents into the blood. Your doctor will monitor you for signs of this syndrome and treat it if necessary.
- Retevmo can affect how well wounds heal. If you're planning to have surgery, you'll need to stop taking Retevmo at least 7 days before your surgery and not start it again until at least 2 weeks after surgery, once your wound has healed properly.
- Since Retevmo can affect your thyroid, your doctor will check your thyroid function before and during treatment. Depending on the results, your treatment may need to be adjusted.
- Retevmo can harm an unborn baby, so if you're able to become pregnant, you'll need to use effective birth control during treatment and for some time after the last dose. Your doctor will discuss the risks and the need for contraception with you.
Side Effects
Retevmo side effects commonly include swelling in the arms, legs, hands, and feet (edema), abdominal pain, diarrhea, constipation, tiredness, rash, dry mouth, nausea, high blood pressure, and headaches. These side effects are part of the body's response to the medication.
Serious side effects include liver problems, indicated by symptoms like yellowing of the skin or eyes, dark urine, and upper stomach pain. Severe lung inflammation, high blood pressure, heart rhythm changes, bleeding problems, allergic reactions, tumor lysis syndrome (a rapid breakdown of cancer cells causing various symptoms like nausea, vomiting, and weakness), wound healing complications, and low thyroid hormone levels are also potential serious side effects. Retevmo may affect fertility in both men and women. Regular monitoring by a healthcare provider, including liver function, blood pressure, heart activity, and thyroid function tests, is recommended. Immediate medical attention is required for any signs of severe side effects.
References:
- Retevmo (Selpercatinib) Product Monograph. Indianapolis, IN: Eli Lilly and Company; 2022.
- Retevmo (Selpercatinib) Drug Label Information. Indianapolis, IN: Eli Lilly and Company; 2023.
About Dr. Gerardo Sison (Page Author)
Dr. Sison graduated with honors from the University of Florida. He began his career in pharmacy counseling patients in a community setting and later served in hospitals and clinics. He has also worked in medication therapy management services. Read More....
IMPORTANT NOTE:
The above information is intended to increase awareness of health information and does not suggest treatment or diagnosis. This information is not a substitute for individual medical attention and should not be construed to indicate that use of the drug is safe, appropriate, or effective for you. See your health care professional for medical advice and treatment.
Product Code : 14603