Selpercatinib

Non-Small-Cell Lung Carcinoma, Thyroid Neoplasms

Drug Status

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Government Approvals

US(FDA)

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WHO Essential Medicine

NO

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Known Teratogen

NO

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Pharmaceutical Class

Kinase Inhibitor

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Controlled Drug Substance

No

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Drug Ingredient

Selpercatinib

Summary

  • Selpercatinib is used to treat certain types of cancers, including non-small cell lung cancer, medullary thyroid cancer, and other solid tumors with specific genetic mutations. It is specifically used for cancers that have spread to other parts of the body and have specific genetic mutations or fusions.

  • Selpercatinib is a kinase inhibitor. It targets and blocks the action of abnormal proteins that signal cancer cells to multiply. By inhibiting these proteins, Selpercatinib helps slow or stop the spread of cancer cells.

  • For adults and adolescents 12 years or older, the usual daily dose of Selpercatinib is based on body weight. If less than 50 kg, it's 120 mg twice daily, and if 50 kg or greater, it's 160 mg twice daily. For children aged 2 to less than 12 years, the dose is based on body surface area, ranging from 40 mg three times daily to 160 mg twice daily.

  • Common side effects of Selpercatinib include edema, diarrhea, fatigue, dry mouth, hypertension, abdominal pain, constipation, nausea, and headache. More serious adverse effects can include hepatotoxicity, interstitial lung disease, hypertension, QT interval prolongation, and hemorrhagic events.

  • Important warnings for Selpercatinib include the risk of hepatotoxicity, interstitial lung disease, hypertension, QT interval prolongation, hemorrhagic events, hypersensitivity reactions, and tumor lysis syndrome. It is contraindicated in patients with known hypersensitivity to the drug.

Indications and Purpose

How does Selpercatinib work?

Selpercatinib is a kinase inhibitor that targets and blocks the action of abnormal proteins that signal cancer cells to multiply. By inhibiting these proteins, Selpercatinib helps slow or stop the spread of cancer cells, making it an effective treatment for certain types of cancers with specific genetic mutations.

Is Selpercatinib effective?

Selpercatinib has been shown to be effective in treating certain types of cancers, including non-small cell lung cancer, medullary thyroid cancer, and other solid tumors with specific genetic mutations. Clinical trials have demonstrated significant overall response rates and durations of response in patients with these conditions, supporting its use as a targeted cancer therapy.

What is Selpercatinib?

Selpercatinib is used to treat certain types of cancers, including non-small cell lung cancer, medullary thyroid cancer, and other solid tumors with specific genetic mutations. It works by inhibiting kinase proteins that signal cancer cells to multiply, thereby slowing or stopping the spread of cancer cells. This targeted approach helps manage cancer progression effectively.

Directions for Use

For how long do I take Selpercatinib?

Selpercatinib is typically used until disease progression or unacceptable toxicity occurs. The duration of use can vary significantly depending on the individual's response to treatment and the specific condition being treated. Always follow your doctor's guidance regarding the duration of treatment.

How do I take Selpercatinib?

Selpercatinib can be taken with or without food, but if you are taking a proton pump inhibitor, it should be taken with food. If taking H2 blockers, take Selpercatinib 2 hours before or 10 hours after the blocker. For antacids, take Selpercatinib 2 hours before or after. Avoid grapefruit and grapefruit juice, as they can interact with the medication.

How should I store Selpercatinib?

Selpercatinib should be stored at room temperature, between 68°F to 77°F (20°C to 25°C). It should be kept in its original container, tightly closed, and out of reach of children. Avoid storing it in the bathroom to prevent exposure to moisture.

What is the usual dose of Selpercatinib?

The usual daily dose of Selpercatinib for adults and adolescents 12 years or older is based on body weight: less than 50 kg is 120 mg twice daily, and 50 kg or greater is 160 mg twice daily. For children aged 2 to less than 12 years, the dose is based on body surface area, ranging from 40 mg three times daily to 160 mg twice daily. Always follow your doctor's specific dosage instructions.

Warnings and Precautions

Can I take Selpercatinib with other prescription drugs?

Significant drug interactions with Selpercatinib include acid-reducing agents like proton pump inhibitors, H2 receptor antagonists, and antacids, which can affect its absorption. Strong and moderate CYP3A inhibitors can increase Selpercatinib levels, while CYP3A inducers can decrease its effectiveness. Patients should inform their doctor of all medications they are taking to avoid interactions.

Can Selpercatinib be taken safely while breastfeeding?

Women are advised not to breastfeed during treatment with Selpercatinib and for 1 week after the last dose due to the potential for serious adverse reactions in breastfed children. It's important to discuss breastfeeding options with your healthcare provider before starting treatment.

Can Selpercatinib be taken safely while pregnant?

Selpercatinib can cause fetal harm based on animal studies, and it is advised that pregnant women avoid using it. Females of reproductive potential should use effective contraception during treatment and for 1 week after the last dose. Males with female partners of reproductive potential should also use contraception during treatment and for 1 week after the last dose. If pregnancy occurs, contact your doctor immediately.

Is Selpercatinib safe for the elderly?

There are no specific warnings or recommendations for the elderly using Selpercatinib. However, as with any medication, elderly patients should use Selpercatinib under the guidance of a healthcare provider, who will consider any age-related health conditions or other medications being taken.

Who should avoid taking Selpercatinib?

Important warnings for Selpercatinib include the risk of hepatotoxicity, interstitial lung disease, hypertension, QT interval prolongation, hemorrhagic events, hypersensitivity reactions, and tumor lysis syndrome. Patients should be monitored for these conditions, and the medication should be used with caution in those with pre-existing health issues. It's contraindicated in patients with known hypersensitivity to the drug.