Selpercatinib

What is Selpercatinib?

• Selpercatinib (Retevmo)™ is a kinase inhibitor used to treat certain cancers caused by abnormal RET genes.

What are the uses of this medicine?

This medicine is indicated used to treat certain cancers caused by abnormal RET genes in:

• adults with non-small cell lung cancer (NSCLC) that has spread.
• adults and children 12 years of age and older with advanced medullary thyroid cancer (MTC) or MTC that has spread who require a medicine by mouth or injection (systemic therapy).
• adults and children 12 years of age and older with advanced thyroid cancer or thyroid cancer that has spread who require a medicine by mouth or injection (systemic therapy) and who have received radioactive iodine and it did not work or is no longer working.

How does this medicine work?

• An orally bioavailable selective inhibitor of wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity.
• Upon oral administration, selpercatinib selectively binds to and targets wild-type RET as well as various RET mutants and RET-containing fusion products.
• This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity.
• In addition, selpercatinib targets, binds to and inhibits vascular endothelial growth factor receptor 1 (VEGFR1) and 3 (VEGFR3), and fibroblast growth factor receptor 1 (FGFR1), 2 (FGFR2), and 3 (FGFR3).
• RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.

Who Should Not Use this medicine ?

• This medication have no usage limitations.

What drug interactions can this medicine cause?

• Avoid Coadministration with acid-reducing agents. If coadministration cannot be avoided, take Retevmo with food (with PPI) or modify its administration time (with H2 receptor antagonist or locally-acting antacid).
• Avoid coadministration with strong and moderate CYP3A inhibitors
• Avoid coadministration with strong and moderate CYP3A Inducers
• Avoid coadministration with CYP2C8 and CYP3A Substrates

Is this medicine FDA approved?

• It was approved for use in the United States in 2020.

How should this medicine be used?

Recommended Dosage The recommended dosage of Retevmo based on body weight is:

• Less than 50 kg: 120 mg
• 50 kg or greater: 160 mg

Administration

• Take Retevmo exactly as your healthcare provider tells you.
• Your healthcare provider may stop treatment or change your dose of Retevmo if you have side effects. Do not change your dose or stop taking Retevmo unless your healthcare provider tells you.
• Retevmo is taken by mouth, usually 2 times a day with or without food.
• If you take a proton-pump inhibitor (PPIs such as dexlansoprazole, esomeprazole, lansoprazole, omeprazole, pantoprazole sodium, and rabeprazole), take Retevmo with food.
• Retevmo doses should be separated by 12 hours.
• If you take an antacid that contains aluminum, magnesium, calcium, simethicone, or buffered medicines, take Retevmo 2 hours before or 2 hours after taking the antacid.
• If you take an H2 blocker (such as famotidine, nizatidine, and cimetidine), take Retevmo 2 hours before or 10 hours after taking the H2 blocker.
• Swallow Retevmo capsules whole. Do not chew or crush the capsules.
• If you vomit after taking a dose of Retevmo, do not take an extra dose. Take the next dose of Retevmo at your scheduled time.
• Do not take a missed dose of Retevmo unless it is more than 6 hours until your next scheduled dose.
• If you take too much Retevmo, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 40 mg, 80 mg

This medicine is available in fallowing brand namesː

• Retevmo

What side effects can this medication cause?

Common possible side effects and laboratory abnormalities of this medicine include:

• increased levels of liver enzymes
• increased blood sugar levels
• decrease in white blood cell count
• decreased protein levels (albumin) in the blood
• decreased levels of calcium in the blood
• dry mouth
• diarrhea
• increased creatinine (kidney function test)
• high blood pressure
• tiredness
• swelling of your arms, legs, hands, and feet (peripheral edema)
• decrease in platelet count
• increased cholesterol levels
• rash
• decreased levels of salt (sodium) in the blood
• constipation

Retevmo may cause serious side effects, including:

• Liver problems
• High blood pressure (hypertension)
• Heart rhythm changes (QT prolongation)
• Bleeding problems
• Allergic reactions
• Tumor lysis syndrome (TLS)
• Risk of wound healing problems

What special precautions should I follow?

• This medicine may cause hepatotoxicity. Withhold, reduce dose, or permanently discontinue Retevmo based on severity.
• Do not initiate Retevmo in patients with uncontrolled hypertension. Optimize blood pressure (BP) prior to initiating Retevmo. Monitor BP after 1 week, at least monthly thereafter and as clinically indicated. Withhold, reduce dose, or permanently discontinue Retevmo based on severity.
• Monitor patients who are at significant risk of developing QTc prolongation.
• Permanently discontinue Retevmo in patients with severe or life-threatening hemorrhage.
• This medicine may cause hypersensitivity. Withhold Retevmo and initiate corticosteroids.
• Closely monitor patients at risk of Tumor Lysis Syndrome and treat as clinically indicated.
• Withhold Retevmo for at least 7 days prior to elective surgery. Do not administer for at least 2 weeks following major surgery and until adequate wound healing.
• Advise females of reproductive potential of the possible risk to the fetus and to use effective contraception.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Retevmo can cause fetal harm when administered to a pregnant woman.
• There are no available data on Retevmo use in pregnant women to inform drug-associated risk.

Can this medicine be used in children?

• The safety and effectiveness of Retevmo have been established in pediatric patients aged 12 years and older for medullary thyroid cancer (MTC) who require systemic therapy and for advanced RET fusion-positive thyroid cancer who require systemic therapy and are radioactive iodine-refractory (if radioactive iodine is appropriate).
• The safety and effectiveness of Retevmo have not been established in these indications in patients less than 12 years of age.
• The safety and effectiveness of Retevmo have not been established in pediatric patients for other indications.

What should I know about storage and disposal of this medication?

• Store Retevmo capsules at room temperature between 68˚F to 77˚F (20˚C to 25˚C).

• Dailymed label info on Selpercatinib
• FDA Selpercatinib

Selpercatinib Resources
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