Ripretinib

What is Ripretinib?

• Ripretinib (Qinlock) is a kinase inhibitor used to treat adults with advanced gastrointestinal stromal tumor (GIST) who have received 3 or more prior treatments for their GIST.

What are the uses of this medicine?

• This medicine is indicated for the treatment of adult patients with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with 3 or more kinase inhibitors, including imatinib.

How does this medicine work?

• Ripretinib is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor A (PDGFRA) kinase, including wild type, primary, and secondary mutations.
• Ripretinib also inhibits other kinases in vitro, such as PDGFRB, TIE2, VEGFR2, and BRAF.
• Upon oral administration, ripretinib targets and binds to both wild-type and mutant forms of KIT and PDGFRa specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms.
• This abrogates KIT/PDGFRa-mediated tumor cell signaling and prevents proliferation in KIT/PDGFRa-driven cancers.
• DCC-2618 also inhibits several other kinases, including vascular endothelial growth factor receptor type 2 (VEGFR2; KDR), angiopoietin-1 receptor (TIE2; TEK), PDGFR-beta and macrophage colony-stimulating factor 1 receptor (FMS; CSF1R), thereby further inhibiting tumor cell growth.
• KIT and PDGFRa are tyrosine kinase receptors that are upregulated or mutated in a variety of cancer cell types; mutated forms play a key role in the regulation of tumor cell proliferation and resistance to chemotherapy.

Who Should Not Use this medicine ?

• This medication have no usage limitations.

What drug interactions can this medicine cause?

Avoid Coadministration of Qinlock with fallowing:

• Strong CYP3A Inhibitors
• Strong CYP3A Inducers
• Moderate CYP3A Inducers

Is this medicine FDA approved?

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

How should this medicine be used?

• The recommended dosage of Qinlock is 150 mg orally once daily with or without food until disease progression or unacceptable toxicity.

Administration

• Take Qinlock exactly as your healthcare provider tells you to.
• Your healthcare provider may temporarily or permanently stop treatment or change your dose of Qinlock if you develop side effects during treatment.
• Do not change your dose or stop taking Qinlock unless your healthcare provider tells you to.
• Take Qinlock 1 time each day, at the same time each day.
• Take Qinlock with or without food.
• Swallow Qinlock tablets whole.
• If you vomit after taking a dose of Qinlock, do not take an extra dose. Take your next dose of Qinlock at your scheduled time.
• If you miss a dose of Qinlock, take it as soon as you remember if it is within 8 hours of the scheduled dose. If more than 8 hours have passed, wait until your next scheduled dose.
• If you take more than the prescribed dose of Qinlock, call your healthcare provider.

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

This medicine is available in fallowing doasage form:

• As Tablets: 50 mg

This medicine is available in fallowing brand namesː

• Qinlock

What side effects can this medication cause?

Common possible side effects of this medicine include: Common possible side effects of this medicine include:

• hair thinning or hair loss
• nausea
• constipation
• diarrhea
• vomiting
• tiredness
• abdominal pain
• muscle pain
• decreased appetite

Qinlock may cause serious side effects, including:

• A skin problem called palmar-plantar erythrodysesthesia syndrome
• New skin cancers
• High blood pressure (Hypertension)
• Heart problems
• Risk of wound healing problems

Qinlock may cause serious side effects, including:

• A skin problem called palmar-plantar erythrodysesthesia syndrome
• New skin cancers
• High blood pressure (Hypertension)
• Heart problems
• Risk of wound healing problems

What special precautions should I follow?

• Palmar-Plantar Erythrodysesthesia Syndrome may occur. Based on severity, withhold Qinlock and resume at same or reduced dose.
• Perform dermatologic evaluations when initiating Qinlock and routinely during treatment.
• Do not initiate Qinlock in patients with uncontrolled hypertension and monitor blood pressure during treatment. Based on severity, withhold Qinlock and then resume at same or reduced dose or permanently discontinue.
• Permanently discontinue Qinlock for Grade 3 or 4 left ventricular systolic dysfunction.
• This medicine increases the risk of impaired wound healing. Withhold Qinlock for at least 1 week prior to elective surgery. Do not administer for at least 2 weeks after major surgery and until adequate wound healing.
• Advise females of reproductive potential of the potential risk to a 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?

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

Can this medicine be used in children?

• The safety and effectiveness of Qinlock in pediatric patients have not been established.

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

• Store in the original container with the desiccant to protect from moisture and light. Replace cap securely each time after opening. Do not discard desiccant.
• Store at 20°C to 25°C (68°F to 77°F); excursion permitted between 15°C to 30°C (59°F to 86°F)

• Dailymed label info on Ripretinib
• FDA Ripretinib

Ripretinib Resources
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