Larotrectinib

What is Larotrectinib?

• Larotrectinib (Vitrakvi) is a kinase inhibitor used for the treatment of adult and pediatric patients with solid tumors.

Larotrectinib

What are the uses of this medicine?

Larotrectinib (Vitrakvi) is a prescription medicine that is used to treat adults and children with solid tumors (cancer) that:

• are caused by certain abnormal NTRK genes and
• have spread or if surgery to remove their cancer is likely to cause severe complications, and
• there is no acceptable treatment option or the cancer grew or spread on other treatment

How does this medicine work?

• Larotrectinib (lar" oh trek' ti nib) is an orally available, small molecule inhibitor of the tropomyosin receptor kinases (TRK-A, -B and -C). The genes of TRK are found to be oncogenic drivers in many solid tumors including gliomas and sarcomas.
• The tumors harbor a fusion product of the proto-oncogene family and overexpress the neurotrophin receptor kinases which results in abnormal cell growth.
• Larotrectinib has activity against all three forms of TRK and has been shown to be effective in prolonging progression free survival in children and adults with various solid tumors harboring an NTRK gene fusion.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following:

• certain antifungals such as itraconazole (Onmel, Sporanox) and ketoconazole
• avanafil (Stendra)
• buspirone
• clarithromycin (Biaxin, in PrevPac)
• certain medications for human immunodeficiency virus (HIV) or acquired immunodeficiency syndrome (AIDS) such as efavirenz (Sustiva, in Atripla), indinavir (Crixivan), nelfinavir (Viracept), nevirapine (Viramune), ritonavir (Norvir, in Kaletra), and saquinavir (Invirase)
• certain medications that suppress the immune system such as everolimus (Afinitor, Zortress), sirolimus (Rapamune), and tacrolimus (Astagraf, Envarsus XR, Prograf)
• lovastatin
• midazolam
• nefazodone
• pioglitazone (Actos)
• rifabutin (Mycobutin)
• rifampin (Rifadin, Rimactane, in Rifamate, in Rifater)
• certain medications for seizures such as carbamazepine (Carbatrol, Epitol, Tegretol, others), phenobarbital, and phenytoin (Dilantin, Phenytek) sildenafil (Revatio, Viagra),simvastatin (Flolipid, Zocor); and vardenafil (Levitra, Staxyn).
• Tell your doctor what herbal products you are taking, especially St. John's wort. Do not take St. John's wort while taking larotrectinib.

Is this medicine FDA approved?

• Larotrectinib received accelerated approval for use in the United States in 2018 for the treatment of advanced or metastatic solid tumors that have NTRK gene fusion.

How should this medicine be used?

• Select patients for treatment with Vitrakvi based on the presence of a NTRK gene fusion.

Recommended dosage: Recommended Dosage in Adult and Pediatric Patients with Body Surface Area of at Least 1.0 Meter-Squared:

• The recommended dosage of Vitrakvi is 100 mg orally twice daily, with or without food, until disease progression or until unacceptable toxicity.

Recommended Dosage in Pediatric Patients with Body Surface Area of Less Than 1.0 Meter-Squared:

• The recommended dosage of Vitrakvi is 100 mg/m2 orally twice daily, with or without food, until disease progression or until unacceptable toxicity.

Administration:

• Vitrakvi comes in capsules and as an oral solution.

If your healthcare provider prescribes Vitrakvi oral solution:

• Your healthcare provider will provide you with the Vitrakvi oral solution and oral syringes or send you to a pharmacy that can provide you with Vitrakvi oral solution and oral syringes.
• Your healthcare provider should show you how to correctly measure and give a dose of Vitrakvi oral solution.

• Vitrakvi is usually taken by mouth 2 times a day.
• Swallow Vitrakvi capsules whole.
• Do not chew or crush the capsules.
• Take Vitrakvi with or without food.
• If you vomit after taking a dose of Vitrakvi, wait and take the next dose at your scheduled time
• If you miss a dose of Vitrakvi, take it as soon as you remember unless your next scheduled dose is due within 6 hours. Take the next dose at your regular time.

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

This medicine is available in fallowing doasage form:

• As Capsules: 25 mg, 100 mg
• Oral Solution: 20 mg/mL

This medicine is available in fallowing brand namesː Vitrakvi

What side effects can this medication cause?

The most common side effects of this medicine include:

• tiredness
• nausea
• dizziness
• vomiting
• cough
• constipation
• diarrhea

• Vitrakvi may affect fertility in females and may affect your ability to become pregnant.

Vitrakvi may cause serious side effects, including:

• Nervous system problems
• Liver problems

What special precautions should I follow?

• Vitrakvi can make you feel dizzy. Do not drive or operate machinery until you know how Vitrakvi affects you.
• Avoid taking St.John’s wort, eating grapefruit, or drinking grapefruit juice during treatment with Vitrakvi.
• Neurologic adverse reactions of any grade occurred. Advise patients and caretakers of the risk of neurologic adverse reactions. Advise patients not to drive or operate hazardous machinery if experiencing neurotoxicity. Withhold and modify dosage, or permanently discontinue Vitrakvi based on severity.
• Increased AST and ALT leading to dose modifications occurred in 4% and 6% of patients, respectively. Monitor liver tests including ALT and AST every 2 weeks during the first month of treatment, then monthly thereafter and as clinically indicated. Withhold and modify dosage, or permanently discontinue Vitrakvi based on severity.
• Vitrakvi Can cause fetal harm. Advise females with reproductive potential of potential risk to the fetus and to use effective contraception.
• Larotrectinib is associated with a high rate of serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent liver injury with jaundice.

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?

• Vitrakvi can cause embryo-fetal harm when administered to a pregnant woman.
• There are no available data on Vitrakvi use in pregnant women.

Can this medicine be used in children?

• It is not known if Vitrakvi is safe and effective in children younger than 1 month of age.

What are the active and inactive ingredients in this medicine?

• Active ingredient: larotrectinib
• Inactive ingredients:
• Capsule: gelatin, titanium dioxide and edible ink
• Oral Solution: purified water, hydroxypropyl betadex, sucrose, glycerin, sorbitol, citric acid, sodium phosphate, sodium citrate dihydrate, propylene glycol and flavoring. Preserved with methylparaben and potassium sorbate.

Who manufactures and distributes this medicine?

• Manufactured for: Loxo Oncology, Inc., Stamford, CT

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

• Store Vitrakvi capsules at room temperature between 68°F to 77°F (20°C to 25°C).
• Store Vitrakvi oral solution in the refrigerator between 36° F to 46° F (2° C to 8° C). Do not freeze.
• Throw away (dispose of) any unused Vitrakvi oral solution remaining after 90 days of first opening the bottle.

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• Dailymed label info on Larotrectinib
• FDA Larotrectinib

Larotrectinib Resources
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Larotrectinib Resources
Latest articles Most recent articles Ongoing trials	Wikipedia