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VITRAKVI 25mg hard capsules

⚠ This medicine appears to have been discontinued

The electronic medicines compendium (emc) no longer publishes a Summary of Product Characteristics for this product, which usually means it is no longer marketed in the UK. The patient leaflet below is kept for reference, but the product may not be available.

If you were prescribed this medicine, other products containing Larotrectinib sulfate may still be available. Do not stop your treatment — ask your pharmacist or GP what to use instead.

Active substance: Larotrectinib sulfate
Source: electronic medicines compendium (emc)
Official leaflet: Read the PIL on emc

What it is and what it is used for

for

What VITRAKVI is used for VITRAKVI contains the active substance larotrectinib. It is used in adults, adolescents and children to treat solid tumours (cancer) in various parts of the body that are caused by a change in the NTRK gene (neurotrophic tyrosine receptor kinase). VITRAKVI is only used when these cancers are advanced or have spread to other parts of the body or if a surgery to remove the cancer is likely to cause severe complications and there are no satisfactory treatment options. Before you are given VITRAKVI, your doctor will do a test to check if you have the change in the NTRK gene. GB-v003_1

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How VITRAKVI works In patients whose cancer is due to an altered NTRK gene, the change in the gene causes the body to make an abnormal protein called TRK fusion protein, which can lead to uncontrolled cell growth and cancer. VITRAKVI blocks the action of TRK fusion proteins and so may slow or stop the growth of the cancer. It may also help to shrink the cancer. If you have any questions on how VITRAKVI works or why it has been prescribed for you, ask your doctor, pharmacist or nurse. 2.

What you need to know before you take it

e VITRAKVI

Do not take VITRAKVI if you are allergic to larotrectinib or any of the other ingredients of this medicine (listed in section 6). Tests and checks VITRAKVI can increase the amount of the liver enzymes ALT and AST and bilirubin in your blood. Your doctor will do blood tests before and during treatment to check the level of ALT, AST and bilirubin and check how well your liver is working. Other medicines and VITRAKVI Tell your doctor, pharmacist or nurse if you are taking, have recently taken or might take any other medicines. This is because some medicines may affect the way VITRAKVI works or VITRAKVI may affect how other medicines work. In particular, tell your doctor, pharmacist or nurse if you are taking any of the following medicines: medicines used to treat fungal or bacterial infections called itraconazole, voriconazole, clarithromycin, telithromycin, troleandomycin a medicine used to treat Cushing's syndrome called ketoconazole medicines used to treat HIV infection called atazanavir, indinavir, nelfinavir, ritonavir, saquinavir, rifabutin, efavirenz a medicine used to treat depression called nefazodone medicines used to treat epilepsy called phenytoin, carbamazepine, phenobarbital a herbal medicine used to treat depression called St. John's wort a medicine used to treat tuberculosis called rifampicin a medicine used for strong pain relief called alfentanil medicines used to prevent organ rejection after an organ transplant called ciclosporin, sirolimus, tacrolimus a medicine used to treat an abnormal heart rhythm called quinidine medicines used to treat migraines called dihydroergotamine, ergotamine a medicine used to treat long-term pain called fentanyl a medicine used to control involuntary movements or sounds called pimozide a medicine to help you stop smoking called bupropion medicines to reduce blood sugar levels called repaglinide, tolbutamide a medicine that prevents blood clots called warfarin a medicine used to reduce the amount of acid produced in the stomach called omeprazole a medicine used to help control high blood pressure called valsartan a group of medicines used to help lower cholesterol called statins hormonal medicines used for contraception, see section "contraception – for men and women" below. If any of the above apply to you (or you are not sure), talk to your doctor, pharmacist or nurse. Taking VITRAKVI with food and drink Do not eat grapefruit or drink grapefruit juice while taking VITRAKVI. This is because it may increase the amount of VITRAKVI in your body.

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Pregnancy and breast-feeding Pregnancy If you are pregnant, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine. You should not use VITRAKVI during pregnancy since the effect of VITRAKVI on the unborn is not known. Breast-feeding Do not breast-feed while taking this medicine and for 3 days after the last dose. This is because it is not known if VITRAKVI passes into breast milk. Contraception – for men and women You should avoid getting pregnant while taking this medicine. If you are able to become pregnant, your doctor should do a pregnancy test before you start treatment. You must use effective methods of contraception while taking VITRAKVI and for at least 1 month after the last dose, if you are able to become pregnant. If you use hormonal contraceptives, you should also use a barrier method, such as a condom. you have sex with a woman able to become pregnant. Ask your doctor about the best method of contraception for you. Driving, cycling and using machines VITRAKVI may make you feel dizzy or tired. If this happens, do not drive, cycle or use any tools or machines. 3.

How to take VITRAKVI

Always take this medicine exactly as your doctor or pharmacist has told you. Check with your doctor, pharmacist or nurse if you are not sure. How much to take Adults (from 18 years) The recommended dose of VITRAKVI is 100 mg (1 capsule of 100 mg or 4 capsules of 25 mg), two times a day. Your doctor will review your dose and change it as needed. Children and adolescents Your child's doctor will work out the right dose for your child based on their height and weight. The maximum recommended dose is 100 mg (1 capsule of 100 mg or 4 capsules of 25 mg), two times a day. Your child's doctor will review the dose and change it as needed. An oral solution of VITRAKVI is available for patients who cannot swallow the capsules.

How to take it

this medicine VITRAKVI can be taken with or without food. Do not eat grapefruit or drink grapefruit juice while taking this medicine. Swallow the VITRAKVI capsules whole with a glass of water. Do not open, chew or crush the capsule as it has a very bitter taste. If you take more VITRAKVI than you should Talk to your doctor, pharmacist or nurse or go to a hospital straight away. Take the medicine pack and this leaflet with you.

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If you miss a dose of VITRAKVI Do not take a double dose to make up for a forgotten dose or if you vomit after taking this medicine. Take your next dose at the usual time. If you stop taking VITRAKVI Do not stop taking this medicine without talking to your doctor first. It is important to take VITRAKVI for as long as your doctor tells you. If you are not able to take the medicine as your doctor prescribed talk to your doctor straight away. If you have further questions on the use of this medicine, ask your doctor, pharmacist or nurse. 4.

Possible side effects

Like all medicines, this medicine can cause side effects, although not everybody gets them. You should immediately contact your doctor if you experience any of the following serious side effects: feeling dizzy (very common side effect, may affect more than 1 in 10 people), tingling, feeling numb, or a burning feeling in your hands and feet, difficulty walking normally (common side effect, may affect up to 1 in 10 people). This could be symptoms of nervous system problems. Your doctor may decide to lower the dose, or pause or stop the treatment. Tell your doctor, pharmacist or nurse if you notice any of the following side effects: Very common (may affect more than 1 in 10 people): you may look pale and feel your heart pumping, which could be symptoms of low red blood cells (anaemia) flu like symptoms including fever, which could be symptoms of low white blood cells (neutropenia, leukopenia) feeling or being sick (nausea or vomiting) diarrhoea constipation muscle pain (myalgia) feeling tired (fatigue) increased amount of liver enzymes in blood tests weight increase. Common (may affect up to 1 in 10 people): you may bruise or bleed more easily, which could be symptoms of reduced number of platelets (thrombocytopenia) change in how things taste (dysgeusia) muscle weakness increased amount of "alkaline phosphatase" in blood tests (very common in children). Not known (not known how often they occur) you may experience a combination of tiredness, upper right stomach pain, loss of appetite, nausea or vomiting, yellowing of your skin or eyes, bruising or bleeding more easily, and dark urine. These could be symptoms of liver problems. Reporting of side effects If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects directly (see details below). By reporting side effects you can help provide more information on the safety of this medicine. Yellow Card Scheme Website: https://yellowcard.mhra.gov.uk or search for MHRA Yellow Card in the Google Play or Apple App Store. GB-v003_1

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5.

How to store it

VITRAKVI

–

Keep this medicine out of the sight and reach of children. Do not use this medicine after the expiry date which is stated on the carton and the bottle label after EXP. The expiry date refers to the last day of that month. This medicine does not require any special storage conditions. Do not use this medicine if you notice that capsules look damaged. Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help to protect the environment.

–

6.

Contents of the pack and other information

What VITRAKVI contains The active substance is larotrectinib. Each VITRAKVI 25 mg capsule contains 25 mg of larotrectinib (as sulfate). Each VITRAKVI 100 mg capsule contains 100 mg of larotrectinib (as sulfate). The other ingredients are: Capsule shell: Gelatin Titanium dioxide (E 171) Printing ink: Shellac, bleached dewaxed Indigo carmine aluminium lake (E 132) Titanium dioxide (E 171) Propylene glycol (E 1520) Dimeticone 1000 What VITRAKVI looks like and the contents of the bottle VITRAKVI 25 mg is supplied as white opaque hard gelatine capsule, (18 mm long x 6 mm wide), with blue printing of BAYER-cross and "25 mg" on the body of the capsule VITRAKVI 100 mg is supplied as white opaque hard gelatine capsule, (22 mm long x 7 mm wide), with blue printing of BAYER-cross and "100 mg" on the body of the capsule Each carton contains 1 child-resistant plastic bottle containing 56 hard gelatine capsules. Marketing Authorisation Holder Bayer plc 400 South Oak Way Reading RG2 6AD Manufacturer Bayer AG Kaiser-Wilhelm-Allee 51368 Leverkusen Germany For any information about this medicine, please contact Bayer plc, Tel. 0118 206 3000. This leaflet was last revised in March 2023. Product Licence Number Vitrakvi 25 mg hard capsules – PLGB 00010/0742 Vitrakvi 100 mg hard capsules – PLGB 00010/0743 GB-v003_1

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This medicine has been given 'conditional approval'. This means that there is more evidence to come about this medicine. The MHRA will review new information on this medicine at least every year and this leaflet will be updated as necessary.

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Frequently asked questions about VITRAKVI 25mg hard capsules

How do I take VITRAKVI 25mg hard capsules?

VITRAKVI 25mg hard capsules comes as capsule containing 25mg. Always follow the dose your doctor or pharmacist has given you, and read the leaflet that comes with the medicine.

What is the active substance in VITRAKVI 25mg hard capsules?

The active substance in VITRAKVI 25mg hard capsules is larotrectinib sulfate.

Where does this information come from?

This leaflet reproduces the patient information leaflet approved for VITRAKVI 25mg hard capsules, as published on the electronic medicines compendium (emc). The version printed inside your medicine’s packaging is the one that applies to you.

Can I get VITRAKVI 25mg hard capsules without a prescription?

Whether a medicine is available over the counter or on prescription only depends on its licence. Check the leaflet, or ask your pharmacist — they can tell you straight away.

About this leaflet

The text above reproduces the patient information leaflet approved for this medicine, restructured for easier reading.

Medical disclaimer: This page is for information only and does not replace advice from your doctor or pharmacist. Always read the leaflet supplied with your medicine. If you are unwell, call NHS 111; in an emergency, call 999.

Medicines with the same active substance: Larotrectinib sulfate (3 medicines)
See every medicine containing this substance, or browse the full A–Z of active substances.
⚕For healthcare professionals — Summary of Product Characteristics (SmPC)Full SmPC: dosage, interactions, contraindications, warnings+
Technical information intended for healthcare professionals (doctors and pharmacists). The Summary of Product Characteristics (SmPC) is the official document approved by the MHRA/EMA. It does not replace the patient leaflet or a doctor’s advice.

4.1. Therapeutic indications

VITRAKVI as monotherapy is indicated for the treatment of adult and paediatric patients with solid tumours that display a Neurotrophic Tyrosine Receptor Kinase (NTRK) gene fusion,

- who have a disease that is locally advanced, metastatic or where surgical resection is likely to result in severe morbidity, and

- who have no satisfactory treatment options (see sections 4.4 and 5.1).

4.2. Posology and method of administration

Treatment with VITRAKVI should be initiated by physicians experienced in the administration of anticancer therapies.

The presence of an NTRK gene fusion in a tumour specimen should be confirmed by a validated test prior to initiation of treatment with VITRAKVI.

Posology

Adults

The recommended dose in adults is 100 mg larotrectinib twice daily, until disease progression or until unacceptable toxicity occurs.

Paediatric population

Dosing in paediatric patients is based on body surface area (BSA). The recommended dose in paediatric patients is 100 mg/m2 larotrectinib twice daily with a maximum of 100 mg per dose until disease progression or until unacceptable toxicity occurs.

For paediatric patients from birth to less than 3 months the recommended starting dose is 50 mg/m2 twice daily (see section 5.2).

Missed dose

If a dose is missed, the patient should not take two doses at the same time to make up for a missed dose. Patients should take the next dose at the next scheduled time. If the patient vomits after taking a dose, the patient should not take an additional dose to make up for vomiting.

Dose modification

For all grade 2 adverse reactions, continued dosing may be appropriate, though close monitoring to ensure no worsening of the toxicity is advised.

For all grade 3 or 4 adverse reactions not referring to liver function test abnormalities:

- VITRAKVI should be withheld until the adverse reaction resolves or improves to baseline or grade 1. Resume at the next dose modification if resolution occurs within 4 weeks.

- VITRAKVI should be permanently discontinued if an adverse reaction does not resolve within 4 weeks.

The recommended dose modifications for VITRAKVI for adverse reactions are provided in Table 1.

Table 1: Recommended dose modifications for VITRAKVI for adverse reactions

Dose modification

Adult and paediatric patients with body surface area of at least 1.0 m2

Paediatric patients aged 3 months or older with body surface area less than 1.0 m2

Paediatric patients aged less than 3 months

First

75 mg twice daily

75 mg/m2 twice daily

25 mg/m2 twice daily

Second

50 mg twice daily

50 mg/m2 twice daily

-

Third

100 mg once daily

25 mg/m2 twice dailya

-

a Paediatric patients on third dose modification at 25 mg/m² twice daily should remain on this dose (25 mg/m2 twice daily) even if body surface area increases during the treatment.

VITRAKVI should be permanently discontinued in patients who are unable to tolerate VITRAKVI after three dose modifications.

The recommended dose modifications in case of liver function tests abnormalities during treatment with VITRAKVI are provided in Table 2.

Table 2: Recommended dose modifications and management for VITRAKVI for liver function test abnormalities

Laboratory parameters

Recommended measures

Grade 2 ALT and/or AST (>3x ULN and ≤5x ULN)

- Conduct serial laboratory evaluations frequently after the observation of grade 2 toxicity, until resolved, to establish whether a dose interruption or reduction is required.

Grade 3 ALT and/or AST (>5x ULN and ≤20x ULN)

or

Grade 4 ALT and/or AST (>20x ULN), with bilirubin <2x ULN

- Withhold treatment until the adverse reaction resolves or improves to baseline. Monitor liver function frequently until resolution or return to baseline. Permanently discontinue treatment if an adverse reaction does not resolve.

- Resume at the next dose modification if adverse reactions resolve. Treatment should only be resumed in patients where the benefit outweighs the risk.

- Permanently discontinue treatment if a grade 4 ALT and/or AST elevation occurs after resuming treatment.

ALT and/or AST ≥3x ULN with bilirubin ≥2x ULN

- Withhold treatment and monitor liver function frequently until resolution or return to baseline.

- Consider permanent treatment discontinuation.

- Treatment should only be resumed in patients where the benefit outweighs the risk.

- If resumed, start at the next lower dose. Monitor liver function frequently upon restart.

- Permanently discontinue treatment if adverse reaction recurs after resuming treatment.

ALT Alanine aminotransferase

AST Aspartate aminotransferase

ULN upper limit of normal

Special populations

Elderly

No dose adjustment is recommended in elderly patients (see section 5.2).

Hepatic impairment

The starting dose of VITRAKVI should be reduced by 50% in patients with moderate (Child‑Pugh B) to severe (Child‑Pugh C) hepatic impairment. No dose adjustment is recommended for patients with mild hepatic impairment (Child‑Pugh A) (see section 5.2).

Renal impairment

No dose adjustment is required for patients with renal impairment (see section 5.2).

Co‑administration with strong CYP3A4 inhibitors

If co‑administration with a strong CYP3A4 inhibitor is necessary, the VITRAKVI dose should be reduced by 50%. After the inhibitor has been discontinued for 3 to 5 elimination half‑lives, VITRAKVI should be resumed at the dose taken prior to initiating the CYP3A4 inhibitor (see section 4.5).

Method of administration

VITRAKVI is for oral use.

VITRAKVI is available as a capsule or oral solution with equivalent oral bioavailability and may be used interchangeably.

The patient should be advised to swallow the capsule whole with a glass of water. Due to the bitter taste, the capsule should not be opened, chewed or crushed.

The capsules can be taken with or without food but should not be taken with grapefruit or grapefruit juice.

4.3. Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

4.4. Special warnings and precautions for use

Efficacy across tumour types

The benefit of VITRAKVI has been established in single arm trials encompassing a relatively small sample of patients whose tumours exhibit NTRK gene fusions. Favourable effects of VITRAKVI have been shown on the basis of overall response rate and response duration in a limited number of tumour types. The effect may be quantitatively different depending on tumour type, as well as on concomitant genetic alterations (see section 5.1). For these reasons, VITRAKVI should only be used if there are no treatment options for which clinical benefit has been established, or where such treatment options have been exhausted (i.e., no satisfactory treatment options).

Neurologic reactions

Neurologic reactions including dizziness, gait disturbance and paraesthesia were reported in patients receiving larotrectinib (see section 4.8). For the majority of neurologic reactions, onset occurred within the first three months of treatment. Withholding, reducing, or discontinuing VITRAKVI dosing should be considered, depending on the severity and persistence of these symptoms (see section 4.2).

Hepatotoxicity

Abnormalities of liver function tests including increased ALT, AST, alkaline phosphatase (ALP) and bilirubin have been observed in patients receiving larotrectinib (see section 4.8). The majority of ALT and AST increases occurred within 3 months of starting treatment. Cases of hepatotoxicity with increases in ALT and/or AST of grade 2, 3 or 4 severity and increases in bilirubin ≥ 2x ULN have been reported.

In patients with hepatic transaminase elevations, withhold, modify dose or permanently discontinue VITRAKVI based on the severity (see section 4.2).

Liver function including ALT, AST, ALP and bilirubin should be monitored before the first dose, then every 2 weeks during the first month of treatment, then monthly for the next 6 months of treatment, then periodically during treatment. In patients who develop transaminase elevations, more frequent testing is needed (see section 4.2).

Co‑administration with CYP3A4/P‑gp inducers

Avoid co‑administration of strong or moderate CYP3A4/P‑gp inducers with VITRAKVI due to a risk of decreased exposure (see section 4.5).

Contraception in female and male

Women of childbearing potential must use highly effective contraception while taking VITRAKVI and for at least one month after stopping treatment (see sections 4.5 and 4.6).

Males of reproductive potential with a non‑pregnant woman partner of childbearing potential should be advised to use highly effective contraception during treatment with VITRAKVI and for at least one month after the final dose (see section 4.6).

4.5. Interaction with other medicinal products and other forms of interaction

Effects of other agents on larotrectinib

Effect of CYP3A, P‑gp and BCRP inhibitors on larotrectinib

Larotrectinib is a substrate of cytochrome P450 (CYP) 3A, P‑glycoprotein (P‑gp) and breast cancer resistance protein (BCRP). Co‑administration of VITRAKVI with strong or moderate CYP3A inhibitors, P‑gp and BCRP inhibitors (e.g. atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, troleandomycin, voriconazole or grapefruit) may increase larotrectinib plasma concentrations (see section 4.2).

Clinical data in healthy adult subjects indicate that co‑administration of a single 100 mg VITRAKVI dose with itraconazole (a strong CYP3A inhibitor and P‑gp and BCRP inhibitor) 200 mg once daily for 7 days increased larotrectinib Cmax and AUC by 2.8‑fold and 4.3‑fold, respectively.

Clinical data in healthy adult subjects indicate that co‑administration of a single 100 mg VITRAKVI dose with a single dose of 600 mg rifampicin (a P‑gp and BCRP inhibitor) increased larotrectinib Cmax and AUC by 1.8‑fold and 1.7‑fold, respectively.

Effect of CYP3A and P‑gp inducers on larotrectinib

Co‑administration of VITRAKVI with strong or moderate CYP3A inducers and strong P‑gp inducers (e.g. carbamazepine, phenobarbital, phenytoin, rifabutin, rifampicin, or St. John's Wort) may decrease larotrectinib plasma concentrations and should be avoided (see section 4.4).

Clinical data in healthy adult subjects indicate that co‑administration of a single 100 mg VITRAKVI dose with rifampicin (a strong CYP3A and P‑gp inducer) 600 mg once daily for 11 days decreased larotrectinib Cmax and AUC by 71% and 81%, respectively. No clinical data is available on the effect of a moderate inducer, but a decrease in larotrectinib exposure is expected.

Effects of larotrectinib on other agents

Effect of larotrectinib on CYP3A substrates

Clinical data in healthy adult subjects indicate that co‑administration of VITRAKVI (100 mg twice daily for 10 days) increased the Cmax and AUC of oral midazolam 1.7‑fold compared to midazolam alone, suggesting that larotrectinib is a weak inhibitor of CYP3A.

Exercise caution with concomitant use of CYP3A substrates with narrow therapeutic range (e.g. alfentanil, ciclosporin, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, or tacrolimus) in patients taking VITRAKVI. If concomitant use of these CYP3A substrates with narrow therapeutic range is required in patients taking VITRAKVI, dose reductions of the CYP3A substrates may be required due to adverse reactions.

Effect of larotrectinib on CYP2B6 substrates

In vitro studies indicate that larotrectinib induces CYP2B6. Co‑administration of larotrectinib with CYP2B6 substrates (e.g. bupropion, efavirenz) may decrease their exposure.

Effect of larotrectinib on other transporter substrates

In vitro studies indicate that larotrectinib is an inhibitor of OATP1B1. No clinical studies have been performed to investigate interactions with OATP1B1 substrates. Therefore, it cannot be excluded whether co‑administration of larotrectinib with OATP1B1 substrates (e.g. valsartan, statins) may increase their exposure.

Effect of larotrectinib on substrates of PXR regulated enzymes

In vitro studies indicate that larotrectinib is a weak inducer of PXR regulated enzymes (e.g. CYP2C family and UGT). Co‑administration of larotrectinib with CYP2C8, CYP2C9 or CYP2C19 substrates (e.g. repaglinide, warfarin, tolbutamide or omeprazole) may decrease their exposure.

Hormonal contraceptives

It is currently unknown whether larotrectinib may reduce the effectiveness of systemically acting hormonal contraceptives. Therefore, women using systemically acting hormonal contraceptives should be advised to add a barrier method.

4.6. Fertility, pregnancy and lactation

Women of childbearing potential / Contraception in males and females

Based on the mechanism of action, foetal harm cannot be excluded when administering larotrectinib to a pregnant woman. Women of childbearing potential should have a pregnancy test prior to starting treatment with VITRAKVI.

Women of reproductive potential should be advised to use highly effective contraception during treatment with VITRAKVI and for at least one month after the final dose. As it is currently unknown whether larotrectinib may reduce the effectiveness of systemically acting hormonal contraceptives, women using systemically acting hormonal contraceptives should be advised to add a barrier method.

Males of reproductive potential with a non‑pregnant woman partner of childbearing potential should be advised to use highly effective contraception during treatment with VITRAKVI and for at least one month after the final dose.

Pregnancy

There are no data from the use of larotrectinib in pregnant women.

Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity (see section 5.3).

As a precautionary measure, it is preferable to avoid the use of VITRAKVI during pregnancy.

Breast‑feeding

It is unknown whether larotrectinib/metabolites are excreted in human milk.

A risk to newborns/infants cannot be excluded.

Breast‑feeding should be discontinued during treatment with VITRAKVI and for 3 days following the final dose.

Fertility

There are no clinical data on the effect of larotrectinib on fertility. No relevant effects on fertility were observed in repeat‑dose toxicity studies (see section 5.3).

4.7. Effects on ability to drive and use machines

VITRAKVI has a moderate influence on the ability to drive and use machines. Dizziness and fatigue have been reported in patients receiving larotrectinib, mostly grade 1 and 2 during the first 3 months of treatment. This may influence the ability to drive and use machines during this time period. Patients should be advised not to drive and use machines, until they are reasonably certain VITRAKVI therapy does not affect them adversely (see section 4.4).

4.8. Undesirable effects

Summary of the safety profile

The most common adverse drug reactions (≥ 20%) of VITRAKVI in order of decreasing frequency were increased ALT (36%), increased AST (33%), vomiting (30%), anaemia (28%), constipation (28%), diarrhoea (27%), nausea (24%), fatigue (23%), and dizziness (20%).

The majority of adverse reactions were grade 2 or 3. Grade 4 was the highest reported grade for adverse reactions neutrophil count decreased (2%), ALT increased (1%), AST increased, leukocyte count decreased, platelet count decreased, muscular weakness and blood alkaline phosphatase increased (each in < 1%). The highest reported grade was grade 3 for adverse reactions anaemia (7%), weight increased (6%), diarrhoea (4%), gait disturbance and vomiting (each 1%), and fatigue, dizziness, paraesthesia, nausea, myalgia, and constipation (each in < 1%).

Permanent discontinuation of VITRAKVI for treatment emergent adverse reactions occurred in 2% of patients (2 cases each of neutrophil count decreased, ALT increased, and AST increased, 1 case each of gait disturbance, and muscular weakness). The majority of adverse reactions leading to dose reduction occurred in the first three months of treatment.

Tabulated list of adverse reactions

The safety of VITRAKVI was evaluated in 361 patients with TRK fusion‑positive cancer in one of three on‑going clinical trials, Studies 1, 2 (“NAVIGATE”), and 3 (“SCOUT”) and post‑marketing. The safety population characteristics were comprised of patients with a median age of 39.0 years (range: 0, 90) with 37% of patients being paediatric patients. Median time on treatment for the overall safety population (n=361) was 16.2 months (range: 0.1, 89.1).

The adverse drug reactions reported in patients (n=361) treated with VITRAKVI are shown in Table 3 and Table 4.

The adverse drug reactions are classified according to the System Organ Class.

Frequency groups are defined by the following convention: very common (≥ 1/10); common (≥ 1/100 to < 1/10); uncommon (≥ 1/1,000 to < 1/100); rare (≥ 1/10,000 to < 1/1,000); very rare (< 1/10,000), and not known (cannot be estimated from available data).

Within each frequency group, undesirable effects are presented in order of decreasing seriousness.

Table 3: Adverse drug reactions reported in TRK fusion‑positive cancer patients treated with VITRAKVI at recommended dose (overall safety population, n=361) and post‑marketing

System organ class

Frequency

All grades

Grades 3 and 4

Blood and lymphatic system disorders

Very common

Anaemia

Neutrophil count decreased (Neutropenia)

Leukocyte count decreased (Leukopenia)

Common

Platelet count decreased (Thrombocytopenia)

Anaemia

Neutrophil count decreased (Neutropenia)a

Leukocyte count decreased (Leukopenia)a

Uncommon

Platelet count decreased (Thrombocytopenia)a, b

Nervous system disorders

Very common

Dizziness

Common

Gait disturbance

Paraesthesia

Gait disturbance

Uncommon

Dizziness

Paraesthesia

Gastrointestinal disorders

Very common

Nausea

Constipation

Vomiting

Diarrhoea

Common

Dysgeusiac

Diarrhoea

Vomiting

Uncommon

Nausea

Constipation

Hepatobiliary disorders

Not known

Liver injuryd

Musculoskeletal and connective tissue disorders

Very common

Myalgia

Common

Muscular weakness

Uncommon

Myalgia

Muscular weaknessa, b

General disorders and administration site conditions

Very common

Fatigue

Uncommon

Fatigue

Investigations

Very common

Alanine aminotransferase (ALT) increased

Aspartate aminotransferase (AST) increased

Weight increased (Abnormal weight gain)

Common

Blood alkaline phosphatase increased

Alanine aminotransferase (ALT) increaseda

Aspartate aminotransferase (AST) increaseda

Weight increased (Abnormal weight gain)

Uncommon

Blood alkaline phosphatase increaseda, b

a grade 4 reactions were reported

b each grade frequency was less than <1%

c ADR dysgeusia includes the preferred terms “dysgeusia” and “taste disorder”

d includes cases with ALT/AST ≥3x ULN and bilirubin ≥2x ULN

Table 4: Adverse drug reactions reported in TRK fusion‑positive paediatric cancer patients treated with VITRAKVI at recommended dose (n=135); all grades

System organ class

Frequency

Infants and toddlers

(n=43)a

Children

(n=67)b

Adolescents

(n=25)c

Paediatric patients

(n=135)

Blood and lymphatic system disorders

Very common

Anaemia

Neutrophil count decreased (Neutropenia)

Leukocyte count decreased (Leukopenia)

Platelet count decreased (Thrombocytopenia)

Anaemia

Neutrophil count decreased (Neutropenia)

Leukocyte count decreased (Leukopenia)

Anaemia

Neutrophil count decreased (Neutropenia)

Leukocyte count decreased (Leukopenia)

Anaemia

Neutrophil count decreased (Neutropenia)

Leukocyte count decreased (Leukopenia)

Platelet count decreased (Thrombocytopenia)

Common

Platelet count decreased (Thrombocytopenia)

Platelet count decreased (Thrombocytopenia)

Nervous system disorders

Very common

Dizziness

Common

Dizziness

Dizziness

Paraesthesia

Gait disturbance

Paraesthesia

Gait disturbance

Dizziness

Paraesthesia

Gait disturbance

Gastrointestinal disorders

Very common

Nausea

Constipation

Vomiting

Diarrhoea

Nausea

Constipation

Vomiting

Diarrhoea

Nausea

Constipation

Vomiting

Diarrhoea

Nausea

Constipation

Vomiting

Diarrhoea

Common

Dysgeusia

Dysgeusia

Musculoskeletal and connective tissue disorders

Very common

Myalgia

Myalgia

Myalgia

Common

Muscular weakness

Muscular weakness

Muscular weakness

Muscular weakness

General disorders and administration site conditions

Very common

Fatigue

Fatigue

Fatigue

Fatigue

Investigations

Very common

Alanine aminotransferase (ALT) increased

Aspartate aminotransferase (AST) increased

Weight increased (Abnormal weight gain)

Blood alkaline phosphatase increased

Alanine aminotransferase (ALT) increased

Aspartate aminotransferase (AST) increased

Weight increased (Abnormal weight gain)

Blood alkaline phosphatase increased

Alanine aminotransferase (ALT) increased

Aspartate aminotransferase (AST) increased

Weight increased (Abnormal weight gain)

Blood alkaline phosphatase increased

Alanine aminotransferase (ALT) increased

Aspartate aminotransferase (AST) increased

Weight increased (Abnormal weight gain)

Blood alkaline phosphatase increased

a Infant/toddlers (28 days to 23 months): 5 grade 4 Neutrophil count decreased (Neutropenia) reactions and 2 Blood alkaline phosphatase increased reported. Grade 3 reactions included 11 cases of Neutrophil count decreased (Neutropenia), 4 cases of ALT increased, 3 cases each of Anaemia, Diarrhoea, and Weight increased (Abnormal weight gain), and 2 cases each of Blood alkaline phosphatase increased, and Vomiting and 1 case of AST increased.

b Children (2 to 11 years): 1 grade 4 Leukocytes count decreased reported. 9 reported grade 3 cases of Neutrophil count decreased (Neutropenia), 4 cases of Weight increased (Abnormal weight gain), 2 cases each of ALT increased, Anaemia, Diarrhoea, and Vomiting and 1 case each of AST increased, Gait disturbance, Paraesthesia and Myalgia.

c Adolescents (12 to <18 years): no grade 4 reactions were reported. Grade 3 reactions were reported in 1 case each of ALT increased, AST increased, Fatigue, Gait disturbance, and Muscular weakness.

Description of selected adverse reactions

Neurologic reactions

In the overall safety database (n=361), the maximum grade neurologic adverse reaction observed was grade 3 or 4 which was observed in 10 (3%) patients and included gait disturbance (4 patients, 1%), dizziness (3 patients, <1%), and paraesthesia (3 patients, <1%). The overall incidence was 20% for dizziness, 7% for paraesthesia and 5% for gait disturbance. Neurologic reactions leading to dose modification or interruptions included dizziness (1%), gait disturbance (<1%), and paraesthesia (<1%). One patient permanently discontinued the treatment due to grade 3 gait disturbance. In all cases except of one, patients with evidence of anti‑tumour activity who required a dose reduction were able to continue dosing at a reduced dose and/or schedule (see section 4.4).

Hepatotoxicity

Abnormalities of liver function tests including ALT, AST, ALP and bilirubin have been observed in patients treated with VITRAKVI.

In the overall safety database (n=361), the maximum grade transaminase elevation observed was grade 4 ALT increase in 7 patients (2%) and AST increase in 4 patients (1%). Grade 3 ALT and AST increases in 26 (7%) and 22 (6%) of patients, respectively. Majority of grade 3 elevations were transient appearing in the first three months of treatment and resolving to grade 1 by months 3‑4. Grade 2 ALT and AST increases were observed in 37 (10%) and 33 (9%) of patients, respectively, and grade 1 ALT and AST increases were observed in 173 (48%) and 177 (49%) of patients, respectively.

ALT and AST increases leading to dose modifications or interruptions occurred in 25 (7%) patients and 21 (6%) patients, respectively (see section 4.4). Two patients permanently discontinued the treatment with 1 patient due to grade 3 ALT and grade 3 AST increases.

Cases of hepatotoxicity with increases in ALT and/or AST of grade 2, 3 or 4 severity and increases in bilirubin ≥ 2x ULN have been reported. In some cases, the dose of VITRAKVI was withheld and restarted at a reduced dose, while in other cases treatment was permanently discontinued (see section 4.4).

Additional information on special populations

Paediatric patients

Of the 361 patients treated with VITRAKVI, 135 (37%) patients were from birth to < 18 years of age (n=13 from birth to < 3 months, n=4 ≥ 3 months to < 6 months, n=17 ≥ 6 months to < 12 months, n=9 ≥ 12 months to < 2 years, n=30 ≥ 2 years to < 6 years, n=37 ≥ 6 years to < 12 years, n=25 ≥ 12 years to < 18 years). The majority of adverse reactions were grade 1 or 2 in severity and were resolved without VITRAKVI dose modification or discontinuation. Adverse reactions of grade 3 or 4 in severity were generally observed more frequently in patients < 6 years of age. They were reported in 77% of patients from birth to < 3 months and in 47% of patients ≥ 3 months to < 6 years. Decreased neutrophil count has been reported to have led to study drug discontinuation, dose modification and dose interruption.

Elderly

Of the 361 patients in the overall safety population who received VITRAKVI, 69 (19%) patients were 65 years or older and 22 (6%) patients were 75 years or older. The safety profile in elderly patients (≥ 65 years) is consistent with that seen in younger patients. The adverse reaction dizziness (30% versus 28% in all adults), anaemia (36% versus 28% in all adults), diarrhoea (25% versus 23% in all adults), muscular weakness (13% versus 11% in all adults), platelet count decreased (12% versus 6% in all adults), gait disturbance (9% versus 5% in all adults), and dysgeusia (9% versus 6% in all adults) were more frequent in patients of 65 years or older.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via https://yellowcard.mhra.gov.uk or search for MHRA Yellow Card in the Google Play or Apple App Store.

4.9. Overdose

There is limited experience of overdose with VITRAKVI. Symptoms of overdose are not established. In the event of overdose, physicians should follow general supportive measures and treat symptomatically.

🇷🇴 Known in Romania as

Medicines sold in Romania with the same active substance: Cunoscut în România ca

  • VITRAKVI 100 mg prescriptionLAROTRECTINIBUM · taken by mouth
  • VITRAKVI 20 mg/ml prescriptionLAROTRECTINIBUM · taken by mouth

Same active substance. The strength, the form and whether you need a prescription can differ. Always ask a pharmacist before you switch. Romanian medicines in the UK →

🇵🇱 Known in Poland as

Medicines sold in Poland with the same active substance: W Polsce znany jako

⚠ Same active substance, but a different pharmaceutical form (for example a gel instead of a tablet). Not interchangeable — ask a pharmacist.

  • VitrakviLarotrectinibum

Same active substance. The strength, the form and whether you need a prescription can differ. Always ask a pharmacist before you switch. Polish medicines in the UK →

💬 Ask about this leaflet

Ask anything about VITRAKVI 25mg hard capsules. The assistant answers only from this leaflet — if the leaflet does not cover it, it will say so. It does not give medical advice.

Answers come from the patient leaflet published on the electronic medicines compendium (emc). They are not medical advice. Ask a pharmacist or your GP if you are unsure. For urgent help call NHS 111, or 999 in an emergency.

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