Augtyro

Pronunciation: Aug-TYE-ro
Generic name: repotrectinib
Dosage form: capsules (40mg)
Drug class: Multikinase inhibitors

Medically reviewed by Melisa Puckey, BPharm. Last updated on Jun 14, 2024.

What is Augtyro?

Augtyro (repotrectinib) is a next-generation TKI (Tyrosine Kinase Inhibitor) cancer medicine used to treat types of ROS1-Positive NSCLC (Non-Small Cell Lung Cancer). In ROS1-positive cancer, the ROS1 gene joins with part of another gene, which activates the ROS1 gene and causes uncontrolled cell growth and cancer. Augtyro works by inhibiting the ROS1 gene and the receptor tyrosine kinases; this helps control cancer growth and decrease tumor size.

Augtyro received FDA approval on November 15, 2023, to treat adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC). FDA approval was based on positive results from the Phase 1/2 trial.

In this trial for ROS1-Positive NSCLC patients who had not previously been treated with a TKI:

• 79% of patients had a partial response (reduction in tumor size)
• 6 % of patients had a complete response (no longer have signs of cancer)
• The median duration of response (mDOR) was 34.1 months.
• 7 out of 8 patients who had brain tumors had a response.

As a next-generation TKI, Augtyro was designed to have improved activity against brain tumors, and Augtyro treatment can last a longer time before cancers become resistant to treatment.

On June 13, 2024, the FDA approval for Augtyro was extended under the accelerated approval designation to include adults and children 12 years of age and older with solid tumors that:

• are caused by certain abnormal NTRK genes, and
• have spread to other parts of the body, or if surgery to remove your cancer is likely to cause severe complications, and
• have grown or spread after other treatments or there is no satisfactory alternative treatment option.

Continued approval for this indication may be contingent upon positive benefits being shown in further clinical trials.

Augtyro side effects

The most common Augtyro side effects are dizziness, change in taste, numbness or tingling in your arms or legs, constipation, nausea, difficulty breathing, tiredness, issues with thinking, being forgetful or confused, memory problems, hallucinations, trouble with balance, coordination, and walking.

Serious Augtyro side effects

Augtyro may cause serious side effects, including:

Central nervous system (CNS) effects.  Tell your healthcare provider right away if you experience any new or worsening of these symptoms during treatment with Augtyro:

• dizziness
• problems with thinking, such as forgetfulness or confusion
• seeing or hearing things that are not real (hallucinations)
• problems with concentration, attention, memory, and sleep
• vertigo
• changes in mood, such as anxiety, irritability, and depression
• balance or coordination problems.

Lung problems (pneumonitis).  Tell your healthcare provider if you have any new or worsening symptoms of lung problems, including a dry cough (without mucus), productive cough (with mucus), wheezing, or trouble breathing.

Liver problems.  Your healthcare provider will do blood tests to check your liver function before starting and during treatment with this medicine. Tell your healthcare provider right away if you develop symptoms of liver problems, such as:

• your skin or the white part of your eyes turns yellow
• loss of appetite
• dark or “tea-colored” urine
• nausea or vomiting
• light-colored stools (bowel movements)
• pain on the upper right side of your stomach area.

Muscle problems.  Your healthcare provider will do blood tests before you start treatment with Augtyro, at least every 2 weeks for the first month and as needed during treatment. Tell your healthcare provider right away if you get new or worsening signs and symptoms of muscle problems, including unexplained muscle pain or muscle pain that does not go away, tenderness, or weakness.

Increased uric acid levels in your blood (hyperuricemia). This medicine may cause an excess of uric acid in your blood. Your healthcare provider will do tests before and during your treatment with Augtyro to check the uric acid level in your blood. If you have high blood uric acid levels, your healthcare provider may prescribe medications to reduce it. Tell your healthcare provider if you experience symptoms of increased uric acid, including:

• red, hot, tender, or swollen joints, especially in your big toe
• decrease in your amount of urine or no urine at all
• nausea or vomiting
• pain in your stomach area or sides
• pink or brown urine or blood in your urine.

Bone fractures.  Augtyro may increase your risk for bone fractures. Bone fractures may happen with or without a fall or other injury. Tell your healthcare provider right away if you have pain, changes in movement, or bone abnormalities.

It is not known if Augtyro is safe and effective in children with ROS1-positive NSCLC or in children younger than 12 years with NTRK-positive solid tumors.

Related/similar drugs

Before taking this medicine

Before taking this medicine, tell your healthcare provider about all your medical conditions, including if you: 

• have nervous system (neurological) problems
• have lung or breathing problems other than lung cancer
• have liver problems.

Pregnancy

Tell your healthcare provider if you are pregnant or plan to become pregnant.

Augtyro can harm your unborn baby. You should tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with this medicine.

Females who are able to become pregnant:

• Your healthcare provider should do a pregnancy test before you start treatment with this medicine.
• You should use effective non-hormonal birth control (contraception) during treatment and for 2 months after the last dose of Augtyro.
• Birth control methods that contain hormones (such as birth control pills, injections, or transdermal system patches) may not work as well during treatment with Augtyro.
• Talk to your healthcare provider about birth control methods that may be right for you.

Males with female partners who are able to become pregnant:

You should use effective birth control during treatment with Augtyro and for 4 months after the last dose.

Breastfeeding

Tell your healthcare provider if you are breastfeeding or plan to breastfeed. It is not known if Augtyro passes into your breast milk. Do not breastfeed during treatment and for 10 days after the last dose of Augtyro. Talk to your healthcare provider about the best way to feed your baby during this time.

How should I take Augtyro?

Take Augtyro exactly as your healthcare provider tells you to take it. Do not change your dose or stop taking Augtyro unless your healthcare provider tells you to. Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with Augtyro if you develop side effects.

Augtyro Instructions

Augtyro capsules are taken once daily for 14 days, then twice daily, with or without food.

Take Augtyro at about the same time each day. Swallow Augtyro capsules whole with water. Do not open, crush, chew or dissolve the capsule. Do not take a capsule if it is broken, cracked, or damaged.

If you miss a dose, or vomit at any time after taking a dose of Augtyro do not take an extra dose. Just skip the dose and take your next dose at the regularly scheduled time. Do not take 2 doses at the same time to make up a missed or vomited dose.

Dosing Information

Recommended dosage of Augtyro for adults and children aged 12 years and older:

• 160 mg taken once daily with or without food for 14 days, then increased to 160 mg twice daily.
• Continue until disease progression or unacceptable toxicity occurs.

What to avoid

• You should not drink grapefruit juice or eat grapefruit during your treatment with this medicine. It may increase the amount of Augtyro in your blood to a harmful level.
• Do not drive or operate machinery until you know how this medicine affects you. If you experience dizziness, blurred vision, memory loss, changes in mental status, confusion, hallucinations or have trouble with balance or coordination, or problems with concentration and attention, do not drive or operate machinery until your symptoms have resolved.

What other drugs will affect Augtyro?

Sometimes it is not safe to use certain medicines at the same time. Some drugs can affect your blood levels of other drugs you use, which may increase side effects or make the medicines less effective.

Tell your doctor about all your current medicines, is is especially important to tell your doctor if you take any of these medicines:

Contraceptives Augtyro can reduce the effectiveness of hormonal contraceptives. Advise females to use an effective nonhormonal contraceptive.

Strong and Moderate CYP3A Inhibitors Avoid using Augtyro with strong or moderate CYP3A inhibitors. Concomitant use of this medicine with a strong or moderate CYP3A inhibitor may increase repotrectinib exposure, which may increase the incidence and severity of adverse reactions.

P-gp Inhibitors Avoid using this medicine use with P-gp inhibitors. Concomitant use of Augtyro with a P-gp inhibitor may increase repotrectinib exposure, which may increase the incidence and severity of adverse reactions of AUGTYRO

Strong and Moderate CYP3A Inducers Avoid using this medicine with strong or moderate CYP3A inducers. Concomitant use of Augtyro with a strong or moderate CYP3A inducer may decrease repotrectinib plasma concentrations, which may decrease the efficacy of Augtyro.

Certain CYP3A4 Substrates Avoid using this medicine with use unless otherwise recommended in the Prescribing Information for CYP3A substrates, where minimal concentration changes can cause reduced efficacy. If concomitant use is unavoidable, increase the CYP3A4 substrate dosage in accordance with approved product labeling. Repotrectinib is a CYP3A4 inducer. Concomitant use of repotrectinib decreases the concentration of CYP3A4 substrates, which can reduce the efficacy of these substrates.

This list is not complete and many other drugs may interact with metronidazole. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

Storage

Store at room temperature between 68°F to 77°F (20°C to 25°C).

Ingredients

Active ingredient: repotrectinib

Inactive ingredients: microcrystalline cellulose, sodium lauryl sulfate, croscarmellose sodium, and colloidal silicon dioxide.

Capsule shell: contains gelatin and titanium dioxide.

Printing ink: contains shellac and FD & C blue #2 aluminum lake.

Company

Bristol-Myers Squibb Company, Princeton, NJ 08543 USA; U.S. License No. 1713.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Medical Disclaimer