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Rozlytrek

Last reviewed on RxList: 9/7/2020
Rozlytrek Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

What Is Rozlytrek?

Rozlytrek (entrectinib) is a kinase inhibitor indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are ROS1-positive; and adult and pediatric patients 12 years of age and older with solid tumors that have a neurotrophic tyrosine receptor kinase (NTRK) gene fusion without a known acquired resistance mutation, are metastatic or where surgical resection is likely to result in severe morbidity, and have progressed following treatment or have no satisfactory alternative therapy.

What Are Side Effects of Rozlytrek?

Common side effects of Rozlytrek include:

Dosage for Rozlytrek

The recommended dosage of Rozlytrek for ROS1-Positive non-small cell lung cancer is 600 mg orally once daily. The recommended adult dosage of Rozlytrek for NTRK gene fusion-positive solid tumors is 600 mg orally once daily. The recommended dosage of Rozlytrek is based on body surface area.

What Drugs, Substances, or Supplements Interact with Rozlytrek?

Rozlytrek may interact with grapefruit and grapefruit products, strong or moderate CYP3A inhibitors or inducers, and medications that prolong the QT/QTc interval. Tell your doctor all medications and supplements you use.

Rozlytrek During Pregnancy and Breastfeeding

Rozlytrek is not recommended for use during pregnancy; it may harm a fetus. Females of reproductive potential are advised to use effective contraception during treatment with Rozlytrek and for 5 weeks following the final dose. Males with female partners of reproductive potential are advised to use effective contraception during treatment with Rozlytrek and for 3 months after the final dose. It is unknown if Rozlytrek passes into breast milk. Because of the potential adverse reactions in breastfed children, breastfeeding is not recommended during treatment with Rozlytrek and for 7 days after the final dose.

Additional Information

Our Rozlytrek (entrectinib) Capsules, for Oral Use Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

QUESTION

Lung cancer is a disease in which lung cells grow abnormally in an uncontrolled way. See Answer
Rozlytrek Consumer Information

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • bone pain or problems moving;
  • fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness (like you might pass out);
  • nausea, vomiting, loss of appetite, right-sided upper stomach pain;
  • swelling in your lower legs, rapid weight gain;
  • cough, wheezing, shortness of breath, trouble breathing while lying down;
  • confusion, hallucinations, problems with memory or concentration;
  • dizziness, mood changes, trouble sleeping; or
  • blurred vision, double vision, increased sensitivity to light, or seeing flashes of light or "floaters" in your vision.

Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.

Common side effects may include:

  • changes in your mental status;
  • vision changes;
  • nausea, vomiting, diarrhea, constipation;
  • fever, cough;
  • dizziness, tiredness;
  • weight gain, swelling;
  • muscle or joint pain;
  • trouble breathing; or
  • changes in your sense of taste or touch.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Rozlytrek (Entrectinib Capsules)

SLIDESHOW

Lung Cancer: Early Signs, Symptoms, Stages See Slideshow
Rozlytrek Professional Information

SIDE EFFECTS

The following clinically significant adverse reactions are described elsewhere in the labeling:

  • Congestive Heart Failure [see WARNINGS AND PRECAUTIONS]
  • Central Nervous System Effects [see WARNINGS AND PRECAUTIONS]
  • Skeletal Fractures [see WARNINGS AND PRECAUTIONS]
  • Hepatotoxicity [see WARNINGS AND PRECAUTIONS]
  • Hyperuricemia [see WARNINGS AND PRECAUTIONS]
  • QT Interval Prolongation [see WARNINGS AND PRECAUTIONS]
  • Vision Disorders [see WARNINGS AND PRECAUTIONS]

Clinical Trial Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Data in WARNINGS AND PRECAUTIONS and below reflect exposure to ROZLYTREK in 355 patients, including 172 (48%) patients exposed for 6 months or longer and 84 (24%) patients exposed for 1 year or longer. ROZLYTREK was studied in one dose-finding trial in adults [ALKA (n = 57)], one dose-finding and activity-estimating trial in adults [STARTRK-1 (n = 76)], one dose-finding and activity-estimating trial in pediatric and adult patients [STARTRK-NG (n = 16)], and one single arm, activity-estimating trial in adults [STARTRK-2 (n = 206)].

The population characteristics were: median age 55 years (range: 4 to 86 years); 5% (n = 17) were less than 18 years of age; 55% were female; and 66% were White, 23% were Asian, and 5% were Black; 3% were Hispanic/Latino. The most common tumors (≥ 5%) were lung (56%), sarcoma (8%), and colon (5%). ROS1 gene fusions were present in 42% and NTRK gene fusions were present in 20%. Most adults (75%) received ROZLYTREK 600 mg orally once daily. The doses ranged from 100 mg/m² to 1600 mg/m² once daily in adults and 250 mg/m² to 750 mg/m² once daily in pediatric patients. ROZLYTREK is not indicated for pediatric patients less than 12 years of age [see Use In Specific Populations].

Serious adverse reactions occurred in 39% of patients. The most frequent serious adverse reactions (≥ 2%) were pneumonia (3.9%), dyspnea (3.7%), pleural effusion (3.4%), sepsis (2.5%), pulmonary embolism (2.3%), respiratory failure (2%), and pyrexia (2%). Grade 3 or 4 adverse reactions occurred in 60% of patients; the most common (≥ 2%) were lung infection (5%), increased weight (7%), dyspnea (6%), fatigue/asthenia (5%), cognitive disorders (4.5%), syncope (2.5%), pulmonary embolism (3.4%), hypoxia (3.4%), pleural effusion (3.1%), hypotension (2.8%), diarrhea (2%), and urinary tract infection (2.5%). Fatal events included dyspnea (0.6%), pneumonia (0.6%), sepsis (0.6%), completed suicide (0.3%), large intestine perforation (0.3%) and tumor lysis syndrome (0.3%). One patient developed Grade 4 myocarditis after one dose of ROZLYTREK which resolved after discontinuation of ROZLYTREK and administration of high-dose corticosteroids.

Permanent discontinuation due to an adverse reaction occurred in 9% of patients who received ROZLYTREK. The most frequent adverse reactions (< 1% each) that resulted in permanent discontinuation were pneumonia, cardio-respiratory arrest, dyspnea, and fatigue.

Dose interruptions due to adverse reactions occurred in 46% of patients. The most frequent adverse reactions (≥ 2%) that resulted in interruption were increased blood creatinine (4%), fatigue (3.7%), anemia (3.1%), diarrhea (2.8%), pyrexia (2.8%), dizziness (2.5%), dyspnea (2.3%), nausea (2.3%), pneumonia (2.3%), cognitive disorder (2%) and neutropenia (2%).

Dose reductions due to adverse reactions occurred in 29% of patients who received ROZLYTREK. The most frequent adverse reactions resulting in dose reductions (≥ 1%) were dizziness (3.9%), increased blood creatinine (3.1%), fatigue (2.3%), anemia (1.7%), and increased weight (1.4%).

The most common adverse reactions (≥ 20%) were fatigue, constipation, dysgeusia, edema, dizziness, diarrhea, nausea, dysesthesia, dyspnea, myalgia, cognitive impairment, increased weight, cough, vomiting, pyrexia, arthralgia and vision disorders.

Table 4 summarizes the adverse reactions observed in these 355 patients.

Table 4: Adverse Reactions (≥ 10%) in Patients Receiving ROZLYTREK in ALKA, STARTRK-1, STARTRK-2, and STARTRK-NG

Adverse ReactionsROZLYTREK
N =355
All Grades (%)Grade ≥ 3* (%)
General
Fatigue1485
Edema2401.1
Pyrexia210.8
Gastrointestinal
Constipation460.6
Diarrhea352.0
Nausea340.3
Vomiting240.8
Abdominal pain3160.6
Nervous System
Dysgeusia440.3
Dizziness4380.8
Dysesthesia5340.3
Cognitive impairment6274.5
Peripheral sensory neuropathy7181.1
Headache180.3
Ataxia8170.8
Sleep9140.6
Mood disorders10100.6
Respiratory, Thoracic and Mediastinal
Dyspnea306*
Cough240.3
Musculoskeletal and Connective Tissue
Myalgia11281.1
Arthralgia210.6
Muscular weakness120.8
Back pain121
Pain in extremity110.3
Metabolism and Nutritional
Increased weight257
Decreased appetite130.3
Dehydration101.1
Eye
Vision disorders12210.8
Infections
Urinary tract infection132.3
Lung infection13106*
Vascular
Hypotension14182.8
Skin and Subcutaneous Tissue
Rash15110.8
* Grades 3 - 5, inclusive of fatal adverse reactions, including 2 events of pneumonia and 2 events of dyspnea.
1Includes fatigue, asthenia
2 Includes face edema, fluid retention, generalized edema, localized edema, edema, edema peripheral, peripheral swelling
3 Includes abdominal pain upper, abdominal pain, lower abdominal discomfort, abdominal tenderness
4 Includes dizziness, vertigo, dizziness postural
5 Includes paresthesia, hyperesthesia, hypoesthesia, dysesthesia, oral hypoesthesia, palmar-plantar erythrodysesthesia, oral paresthesia, genital hypoesthesia
6 Includes amnesia, aphasia, cognitive disorder, confusional state, delirium, disturbance in attention, hallucinations, visual hallucination, memory impairment, mental disorder, mental status changes
7 Includes neuralgia, neuropathy peripheral, peripheral motor neuropathy, peripheral sensory neuropathy
8 Includes ataxia, balance disorder, gait disturbances
9 Includes hypersomnia, insomnia, sleep disorder, somnolence
10 Includes anxiety, affect lability, affective disorder, agitation, depressed mood, euphoric mood, mood altered, mood swings, irritability, depression, persistent depressive disorder, psychomotor retardation
11 Includes musculoskeletal pain, musculoskeletal chest pain, myalgia, neck pain
12 Includes blindness, cataract, cortical cataract, corneal erosion, diplopia, eye disorder, photophobia, photopsia, retinal hemorrhage, vision blurred, visual impairment, vitreous adhesions, vitreous detachment, vitreous floaters
13 Includes lower respiratory tract infection, lung infection, pneumonia, respiratory tract infection
14 Includes hypotension, orthostatic hypotension
15 Includes rash, rash maculopapular, rash pruritic, rash erythematous, rash papular

Clinically relevant adverse reactions occurring in ≤ 10% of patients include dysphagia (10%), fall (8%), pleural effusion (8%), fractures (6%), hypoxia (4.2%), pulmonary embolism (3.9%), syncope (3.9%), congestive heart failure (3.4%), and QT prolongation (3.1%).

Table 5 summarizes the laboratory abnormalities.

Table 5: Laboratory Abnormalities (≥ 20%) Worsening from Baseline in Patients Receiving ROZLYTREK in ALKA, STARTRK-1, STARTRK-2, and STARTRK-NG

Laboratory AbnormalityROZLYTREK NCI CTCAE Grade
All Grades (%)1Grade 3 or 4 (%)1
Hematology
Anemia679
Lymphopenia4012
Neutropenia287
Chemistry
Increased creatinine2732.1
Hyperuricemia5210
Increased AST442.7
Increased ALT382.9
Hypernatremia350.9
Hypocalcemia341.8
Hypophosphatemia307
Increased lipase2810
Hypoalbuminemia282.9
Increased amylase265.4
Hyperkalemia251.5
Increased alkaline phosphatase250.9
Hyperglycemia3NE33.8
AST: Aspartate Aminotransferase; ALT: Alanine Aminotransferase
1 Denominator for each laboratory parameter is based on the number of patients with a baseline and post-treatment laboratory value available which ranged from 111 to 346 patients.
2 Based on NCI CTCAE v5.0
3 NE = Not evaluable. Grade 1 and 2 could not be determined per NCI CTCAE v5.0, as fasting glucose values were not collected.

Read the entire FDA prescribing information for Rozlytrek (Entrectinib Capsules)

Related Resources for Rozlytrek

© Rozlytrek Patient Information is supplied by Cerner Multum, Inc. and Rozlytrek Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

QUESTION

Lung cancer is a disease in which lung cells grow abnormally in an uncontrolled way. See Answer

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