Fruzaqla

Pronunciation: fru-zahk-la
Generic name: fruquintinib
Dosage form: oral capsules
Drug classes: Multikinase inhibitors, VEGF/VEGFR inhibitors

Medically reviewed by Carmen Pope, BPharm. Last updated on Nov 10, 2023.

What is Fruzaqla?

Fruzaqla is an oral kinase inhibitor that may be used to treat adults with metastatic colorectal cancer (mCRC), regardless of biomarker status, who have been previously treated with the following chemotherapy or targeted treatments:

fluoropyrimidine, oxaliplatin, and irinotecan
an anti-VEGF agent
and, if RAS is wild-type and medically appropriate, an anti-EGFR therapy.

Fruquintinib works by inhibiting vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3 VEGFR inhibitors help block tumor angiogenesis, which is the process by which new blood vessels form within a tumor. These blood vessels supply the tumor with the nutrients and oxygen it needs to grow and survive. This process plays a crucial role in the progression of cancer, as it enables tumors to increase in size and spread to other parts of the body. Fruzaqla has enhanced selectivity for these 3 VEGFR receptors that reduces its activity on other receptors, allowing for high drug exposure at the site of action, sustained inhibition of VEGFR-1,2, and 3, and flexibility for the potential use as part of combination therapy.

Fruzaqla is the first targeted treatment approved for mCRC regardless of biomarker status in more than a decade and was the first selective inhibitor of all three VEGF receptor kinases to be approved in the United States.

Fruzaqla was FDA approved on November 8, 2023.

Warnings

May cause high blood pressure. Blood pressure should be under control before treatment with antihypertensive medications if necessary. Your healthcare provider will monitor your blood pressure during treatment and manage it if necessary.

Can cause serious hemorrhagic events and gastrointestinal perforation, which may be fatal. The risk of hemorrhage is higher in people receiving anticoagulants. Also, tell your doctor if you have a recent history of blood clots in an artery.

May cause an increased risk of infections, some of which may be fatal, and may also impair wound healing. Fruzaqla should be withheld during active infections and for at least 2 weeks before and following major surgery.

Can cause liver injury and high protein levels in the urine. Conduct baseline laboratory tests before the start of treatment and periodically during treatment.

In clinical trials, Palmar-Plantar Erythrodysesthesia (PPE), also called hand-foot syndrome (symptoms include redness, swelling, and blistering on the palms of the hands and soles of the feet) was reported in 35% of people, including 8% with Grade 3 events. The average time to onset was 19 days from the first dose.

May cause Posterior Reversible Encephalopathy Syndrome (PRES) ( a type of brain swelling). Symptoms include seizures, headache, visual disturbances, confusion, or altered mental function. Immediately discontinue Fruzaqla if PRES is suspected and confirmed via Magnetic Resonance Imaging (MRI).

Fruzaqla capsules contain FD&C Yellow No. 5 (Tartrazine) and No. 6 (Sunset Yellow FCF) as color additives, which may cause allergic reactions (including bronchial asthma) in certain susceptible patients.

Can cause fetal harm. Adequate contraception should be used during treatment

It is not known if Fruzaqla is safe and effective in children.

Before taking

Before taking Fruzaqla, tell your healthcare provider about all of your medical conditions, including if you:

have high blood pressure
have bleeding problems
have an infection
have liver or kidney problems
plan to have surgery or have had recent surgery
have recently had a blood clot, stroke, or heart attack
are allergic to FD&C Yellow No. 5 (tartrazine) or FD&C Yellow No. 6 (sunset yellow FCF)
are pregnant or plan to become pregnant
are breastfeeding or plan to breastfeed.

Pregnancy and Breastfeeding

Fruzaqla can harm your unborn baby and you should avoid becoming pregnant during treatment if you are a woman who can become pregnant. Your healthcare provider will do a pregnancy test before you start treatment and you should use effective birth control (contraception) during treatment and for 2 weeks after your last dose of Fruzaqla. Tell your healthcare provider right away if you inadvertently become pregnant during treatment.

Males with female partners who can become pregnant should use effective birth control during treatment with Fruzaqla and for 2 weeks after their last dose. Tell your healthcare provider right away if your partner becomes pregnant during your treatment.

It is not known if Fruzaqla passes into your breast milk. Do not breastfeed during treatment and for 2 weeks after your last dose.

How should I take Fruzaqla?

Take Fruzaqla exactly as your healthcare provider tells you. Do not change your dose or stop taking it unless your healthcare provider tells you. Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment if you have certain side effects.

The recommended dosage of Fruzaqla is usually 5mg taken once a day for 21 days (3 weeks) and then stopped for 7 days (1 week).
This is 1 cycle of treatment. Repeat this cycle for as long as your healthcare provider tells you.
Take about the same time each day with or without food and swallow the capsule whole.

What happens if I miss a dose?

If you miss a dose of Fruzaqla, you can take the missed dose within 12 hours on the same day. If more than 12 hours have passed, take your regularly scheduled dose the next day at the usual time. Do not take 2 doses at the same time to make up for the missed dose.

Do not take another dose if you vomit after taking Fruzaqla. Take your regularly scheduled dose the next day at the usual time.

What happens if I overdose?

If you take too much Fruzaqla, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the side effects of Fruzaqla?

Fruzaqla may cause serious side effects, including:

High blood pressure (hypertension). Your healthcare provider will check your blood pressure before starting treatment, 1 time every week for the first month of treatment, and then at least 1 time a month or more often if needed during treatment. Your healthcare provider may prescribe medicine to treat your high blood pressure if needed. Tell your healthcare provider if you get any of the following symptoms of hypertension during treatment:

severe headache
chest pain
lightheadedness or dizziness
trouble breathing
confusion
nosebleeds
changes in vision
vomiting.

Severe bleeding (hemorrhage). Fruzaqla can cause bleeding that can be serious and may lead to death. Tell your healthcare provider if you get any of the following symptoms of bleeding during treatment:

unusual, severe, or bleeding that will not stop
blood in the urine or urine that looks red, pink, or brown
bruising
coughing up blood or blood clots
lightheadedness
menstrual bleeding that is heavier than normal
vomiting blood or your vomit looks like coffee o unusual vaginal bleeding grinds
blood in the stool or black stool that looks like tar
nose bleeds that happen often

Infections. Fruzaqla can increase the risk of infections, including serious infections that can lead to death. The most common infections happen in the urinary tract, nose or throat, and lungs. Tell your healthcare provider if you get any of the following symptoms of infection during treatment:

fever
trouble breathing
severe cough with or without an increase in mucus (sputum) production
burning or pain when you urinate
redness, swelling, or pain in any part of the body o severe sore throat.

A tear in your stomach or intestinal wall (gastrointestinal perforation). Fruzaqla can cause gastrointestinal perforation that can be serious and may lead to death. Tell your healthcare provider right away, if you get any of the following symptoms of gastrointestinal perforation during treatment:

severe stomach (abdominal) pain or stomach
blood in the stool or black stool that looks like tar
pain that does not go away
vomiting or vomiting blood
fever or chills
nausea.

Liver problems. Increased liver enzymes in your blood are common with Fruzaqla and can also be severe and may lead to death. Your healthcare provider will do blood tests before and during treatment to check for liver problems. Tell your healthcare provider if you get any of the following symptoms of liver problems during treatment:

yellowing of your skin or the white part of your eyes
loss of appetite
nausea or vomiting
dark colored (tea-colored) urine
bleeding or bruising
pain in your right upper stomach area (abdomen).

Protein in your urine (proteinuria). Protein in your urine is common with Fruzaqla and can also be severe. Your healthcare provider will check your urine for protein before starting and during treatment. Tell your healthcare provider if you have to urinate more than usual, or if you get swelling of your face, hands, arms, legs, or feet during treatment.
Hand-foot skin reactions (Palmar-Plantar Erythrodysesthesia [PPE]). Hand-foot skin reactions are common with Fruzaqla and can also be severe. Tell your healthcare provider if you get a severe rash or redness, pain, blisters, bleeding, or swelling on the palms of your hands or soles of your feet during treatment.
Posterior Reversible Encephalopathy Syndrome (PRES). PRES is a serious condition that can happen in your brain during treatment with Fruzaqla. Tell your healthcare provider right away if you get any of the following symptoms during treatment:

headache
changes in vision
seizures
problems thinking
confusion

Wound healing problems. Wounds may not heal properly during treatment with Fruzaqla. Tell your healthcare provider if you plan to have any surgery before starting treatment or during treatment.
Blood clots in your blood vessels (arteries). Fruzaqla can cause blood clots or blockage in your blood vessels that may lead to heart attack, stroke, or death. Get medical help right away if you get any of the following symptoms during treatment:

severe chest pain or pressure
sudden confusion, trouble talking, or understanding things
pain in your arms, legs, back, neck or jaw
trouble walking
shortness of breath
sudden severe headache
numbness or weakness of your face, arm, or leg, especially on one side of your body
sudden vision changes in one or both eyes
feeling lightheaded or faint
dizziness, or loss of balance or coordination
sweating more than usual.

Allergic reactions to tartrazine and sunset yellow FCF (contained in the capsules). Tell your healthcare provider if you get hives, rash, or trouble breathing during treatment.

The most common side effects of Fruzaqla affecting more than 20% of people include:

high blood pressure
Palmar-Plantar Erythrodysesthesia
proteinuria
voice changes or hoarseness
diarrhea
stomach-area (abdominal) pain
weakness, lack of strength and energy, and feeling very tired or sleepy (asthenia).

These are not all of the possible side effects of Fruzaqla. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

What other drugs will affect Fruzaqla?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements. Fruzaqla may affect the way other medicines work, and other medicines may affect how it works.

Especially tell your healthcare provider if you take blood thinners (anticoagulants).

Know the medicines you take. Keep a list of your medicines to show to your healthcare provider and pharmacist when you get a new medicine. See the prescribing information for a full list of interactions.

Storage

Store at room temperature between 68°F to 77°F (20°C to 25°C). Keep dry and away from moisture.

The bottle comes with a child-resistant closure, but keep Fruzaqla and all medicines out of the reach of children.

Ingredients

Active: fruquintinib 1mg, 5mg

Inactive: corn starch, microcrystalline cellulose, talc

Capsule shell:

1 mg capsule: FD&C Yellow No. 5 (tartrazine), FD&C Yellow No. 6 (sunset yellow FCF), gelatin, and titanium dioxide
5 mg capsule: FD&C Blue No. 1 (brilliant blue FCF), FD&C Red No. 40 (allura red AC), gelatin, and titanium dioxide

Printing ink: butanol, dehydrated alcohol, ferrosoferric oxide, isopropyl alcohol, potassium hydroxide, propylene glycol, purified water, shellac, and strong ammonia solution.