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Entrectinib

Class: Antineoplastic Agents
- ALK Inhibitors
- ALK Tyrosine Kinase Inhibitors
- Anaplastic Lymphoma Kinase Inhibitors
- C-ros Oncogene Inhibitor
- ROS Inhibitor
- Tropomyosin Kinase Inhibitor
- TRK Inhibitor
- Kinase Inhibitors
- Receptor Tyrosine Kinase Inhibitors
- Tyrosine Kinase Inhibitors
Chemical Name: N-{5-[(3,5-Difluorophenyl)methyl]-1H-indazol-3-yl}-4-(4-methylpiperazin-1-yl)-2-[(oxan-4-yl)amino]benzamide
Molecular Formula: C31H34F2N6O2
CAS Number: 1108743-60-7
Brands: Rozlytrek

Medically reviewed by Drugs.com on Aug 31, 2020. Written by ASHP.

Introduction

Antineoplastic agent; potent inhibitor of multiple receptor tyrosine kinases including tropomyosin receptor kinases (Trk) A, TrkB, TrkC, c-ros oncogene-1 (ROS-1), and anaplastic lymphoma kinase (ALK).

Uses for Entrectinib

Non-small Cell Lung Cancer (NSCLC)

Treatment of ROS-1-positive metastatic NSCLC (based on an objective response rate of 78% in a cohort of patients with ROS-1-positive locally advanced or metastatic NSCLC).

Designated an orphan drug by FDA for treatment of TrkA-positive, TrkB-positive, TrkC-positive, ROS-1-positive, and ALK-positive NSCLC.

Confirmation of ROS-1 fusion necessary prior to initiation of therapy. In clinical studies, presence of ROS-1 fusion was determined by fluorescence in situ hybridization (FISH) or next-generation sequencing (NGS).

Solid Tumors with Neurotrophic Receptor Tyrosine Kinase (NTRK) Gene Fusion

Treatment of solid tumors harboring an NTRK gene fusion (without a known acquired mutation for resistance) in patients who have metastatic disease or who may experience severe morbidity following surgical resection and whose disease progressed following prior therapy or those who are not candidates for other treatment options.

Accelerated approval based on objective response rate and duration of response. Continued approval may be contingent on verification and description of clinical benefit in confirmatory studies.

Designated an orphan drug by FDA for treatment of solid tumors harboring NTRK gene fusion.

Confirmation of NTRK fusion necessary prior to initiation of therapy. In clinical studies, presence of NTRK fusion status was determined by NGS or other nucleic acid-based tests.

Entrectinib Dosage and Administration

General

  • Confirm presence of ROS-1 fusion in tumor specimens of patients with metastatic NSCLC prior to initiation of therapy. (See Non-small Cell Lung Cancer [NSCLC] under Uses.)

  • Confirm presence of NTRK fusion prior to initiation of therapy for the treatment of locally advanced or metastatic solid tumors. (See Solid Tumors with Neurotrophic Receptor Tyrosine Kinase [NTRK] Gene Fusion under Uses.)

Restricted Distribution

  • Obtain entrectinib through designated specialty pharmacies and distributors.

Administration

Oral Administration

Administer orally once daily without regard to food.

Swallow capsules whole; do not open, crush, chew, or dissolve.

Dosage

Pediatric Patients

Solid Tumors with NTRK Fusion
Oral

Adolescents ≥12 years of age with body surface area (BSA) >1.5 m2: 600 mg once daily. If concomitant use with moderate or potent CYP3A inhibitors cannot be avoided, adjust dosage of entrectinib. (See Interactions.)

Adolescents ≥12 years of age with BSA of 1.11–1.5 m2: 500 mg once daily.

Adolescents ≥12 years of age with BSA of 0.91–1.1 m2: 400 mg once daily.

Continue therapy until disease progression or unacceptable toxicity occurs.

Dosage Modification for Toxicity
Oral

Temporary interruption of therapy, dosage reduction, and/or permanent discontinuance of drug may be necessary (see Table 2). When dosage modification is required in pediatric patients, reduce dosage of entrectinib as described in Table 1.

Table 1. Dosage Reduction for Entrectinib Toxicity in Pediatric Patients.1

Dosage Reduction after Recovery from Toxicity

Dose Reduction Level

Pediatric Patients ≥12 Years of Age with BSA >1.5 m2

(Initial Dosage = 600 mg once daily)

Pediatric Patients ≥12 Years of Age with BSA of 1.11–1.5 m2

(Initial Dosage = 500 mg once daily)

Pediatric Patients ≥12 years of Age with BSA of 0.91–1.1 m2

(Initial Dosage = 400 mg once daily)

First

Restart at 400 mg once daily

Restart at 400 mg once daily

Restart at 300 mg once daily

Second

Restart at 200 mg once daily

Restart at 200 mg once daily

Restart at 200 mg once daily

Third

Permanently discontinue entrectinib

Permanently discontinue entrectinib

Permanently discontinue entrectinib

If an adverse reaction occurs, modify treatment accordingly (see Table 2).

Table 2. Dosage Modification for Entrectinib Toxicity1

Adverse Reaction and Severity

Modification

Heart Failure

Grade 2 or 3

Withhold therapy; when toxicity resolves to grade 1 or less, resume at reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 4

Permanently discontinue therapy

CNS Effects

Grade 2 (intolerable)

Withhold therapy; when toxicity resolves to baseline or grade 1 or less, resume at same or reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 3

Withhold therapy; when toxicity resolves to baseline or grade 1 or less, resume at reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 4

Permanently discontinue therapy

Hepatotoxicity

Grade 3

Withhold therapy

Grade 3

If toxicity resolves to baseline or grade 1 or less within 4 weeks, resume at same dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 3

If toxicity does not resolve within 4 weeks, permanently discontinue therapy

Grade 3 (recurrent)

Withhold therapy; if toxicity resolves to baseline or grade 1 or less within 4 weeks, resume at reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 4

Withhold therapy

Grade 4

If toxicity resolves to baseline or grade 1 or less within 4 weeks, resume at reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 4

If toxicity does not resolve within 4 weeks, permanently discontinue therapy

Grade 4 (recurrent)

Permanently discontinue therapy

Elevated ALT or AST concentrations >3 times the ULN with concomitant total bilirubin concentrations >1.5 times the ULN in absence of cholestasis or hemolysis

Permanently discontinue therapy

Hyperuricemia

Symptomatic

Withhold therapy and initiate urate-lowering therapy; when toxicity improves, resume at same or reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 4

Withhold therapy and initiate urate-lowering therapy; when toxicity improves, resume at same or reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Prolongation of QT Interval

QTc interval >500 msec

If other etiology of QT-interval prolongation is present: Withhold therapy and correct other causes of QT-interval prolongation; resume at same dosage when toxicity resolves to baseline

QTc interval >500 msec

If no other etiology of QT-interval prolongation is present: Withhold therapy; resume at reduced dosage (see Table 1 for pediatric patients and Table 3 for adults) when toxicity resolves to baseline

Torsades de pointes, polymorphic ventricular tachycardia, or signs and/or symptoms of serious arrhythmia

Permanently discontinue therapy

Visual Disturbances

New visual symptoms, including changes that interfere with activities of daily living

Withhold therapy; when toxicity improves or stabilizes, resume at same or reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 2 or greater

Withhold therapy; when toxicity improves or stabilizes, resume at same or reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Hematologic Toxicity

Grade 3 or 4 anemia or neutropenia

Withhold therapy; when toxicity improves to grade 2 or less, resume at same or reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Other Toxicity

Grade 3 or 4 (clinically significant)

Withhold therapy

Grade 3 or 4 (clinically significant)

If toxicity resolves to baseline or grade 1 within 4 weeks, resume at same or reduced dosage (see Table 1 for pediatric patients and Table 3 for adults)

Grade 3 or 4 (clinically significant)

If toxicity does not resolve within 4 weeks, permanently discontinue therapy

Grade 4 (recurrent)

Permanently discontinue therapy

Adults

NSCLC
Oral

600 mg once daily. Continue therapy until disease progression or unacceptable toxicity occurs.

If concomitant use with moderate or potent CYP3A inhibitors cannot be avoided, adjust dosage of entrectinib. (See Interactions.)

Solid Tumors with NTRK Fusion
Oral

600 mg once daily. Continue therapy until disease progression or unacceptable toxicity occurs.

If concomitant use with moderate or potent CYP3A inhibitors cannot be avoided, adjust dosage of entrectinib. (See Interactions.)

Dosage Modification for Toxicity
Oral

Temporary interruption of therapy, dosage reduction, and/or permanent discontinuance of drug may be necessary. Recommendations for dosage modification for toxicity in pediatric patients also apply to adults (see Table 2). When dosage modification is required in adults, reduce dosage of entrectinib as described in Table 3.

Table 3. Dosage Reduction for Entrectinib Toxicity in Adults.1

Dose Reduction Level

Dosage Reduction after Recovery from Toxicity - (Initial Dosage = 600 mg once daily)

First

Restart at 400 mg once daily

Second

Restart at 200 mg once daily

Third

Permanently discontinue entrectinib

Special Populations

Hepatic Impairment

Mild hepatic impairment (total bilirubin concentration ≤1.5 times the ULN): No dosage adjustment required. (See Hepatic Impairment under Cautions.)

Renal Impairment

Mild or moderate renal impairment (Clcr 30 to <90 mL/minute): No dosage adjustment required. (See Renal Impairment under Cautions.)

Geriatric Patients

No specific dosage recommendations. (See Geriatric Use under Cautions.)

Cautions for Entrectinib

Contraindications

  • Manufacturer states none known.

Warnings/Precautions

Heart Failure

Heart failure reported; median time to onset is 2 months. Resolves in 75% of patients following initiation of appropriate treatment for heart failure and interruption or discontinuance of drug.

Assess LVEF prior to initiation of therapy in patients with symptoms or known risk factors for heart failure. Monitor for signs and symptoms of heart failure (e.g., dyspnea, edema). For patients with myocarditis with or without a decreased ejection fraction, diagnosis may require magnetic resonance imaging (MRI) or cardiac biopsy. If new onset or worsening heart failure occurs, interrupt therapy, initiate appropriate therapy for heart failure, and reassess LVEF; dosage reduction or permanent discontinuance of therapy may be necessary. (See Dosage Modification for Toxicity under Dosage and Administration: Pediatric Patients and Dosage and Administration: Adults.)

CNS Effects

Entrectinib can cause a variety of adverse CNS effects including cognitive impairment, mood disorder, dizziness, and sleep disturbance.

Inform patients and their caregivers of the risk of adverse CNS effects. Advise patients not to drive or operate hazardous machinery if they are experiencing adverse CNS effects. If adverse CNS effects occur, interruption of therapy, dosage reduction, or permanent discontinuance of therapy may be necessary. (See Dosage Modification for Toxicity under Dosage and Administration: Pediatric Patients and Dosage and Administration: Adults.)

Fractures

Fractures, mostly involving the lower extremity (e.g., hip, femoral or tibial shaft) reported. Sometimes associated with trauma (e.g., fall) in adults and with minimal or no trauma in pediatric patients. Radiographic abnormalities potentially indicating bone metastases reported in some patients.

Promptly evaluate patients with signs or symptoms of fracture (e.g., pain, changes in mobility, deformity). Effect on healing of known fractures or long-term fracture risk is unknown.

Hepatotoxicity

Hepatotoxicity reported; median time to onset of elevated AST or ALT concentrations is 2 weeks.

Monitor liver function tests (e.g., ALT, AST), every 2 weeks during the first month of therapy, monthly thereafter, and as clinically indicated. If hepatotoxicity occurs, interruption of therapy, dosage reduction, or permanent discontinuance of therapy may be necessary. (See Dosage Modification for Toxicity under Dosage and Administration: Pediatric Patients and Dosage and Administration: Adults.)

Hyperuricemia

Hyperuricemia, sometimes symptomatic, reported. Grade 4 hyperuricemia (associated with tumor lysis syndrome) resulted in death in one patient.

Assess serum uric acid levels prior to initiating entrectinib and then periodically during therapy. Monitor patients for signs and symptoms of hyperuricemia. In patients experiencing signs or symptoms of hyperuricemia, initiate urate-lowering therapy as clinically indicated and interrupt entrectinib therapy; dosage reduction may be necessary. (See Dosage Modification for Toxicity under Dosage and Administration: Pediatric Patients and Dosage and Administration: Adults.)

Prolongation of the QT Interval

Prolongation of QTc interval reported.

Monitor QT interval and electrolyte concentrations at baseline and periodically during therapy. More frequent monitoring may be necessary in patients with preexisting QTc-interval prolongation or risk factors for developing QTc-interval prolongation (e.g., long QT syndrome, clinically important bradyarrhythmia, severe or uncontrolled heart failure, electrolyte abnormalities, concomitant use of drugs known to prolong QT interval). If QTc-interval prolongation occurs, temporary interruption of entrectinib therapy, dosage reduction, or permanent discontinuance of therapy may be necessary. (See Dosage Modification for Toxicity under Dosage and Administration: Pediatric Patients and Dosage and Administration: Adults.)

Visual Disturbances

Visual disturbances (i.e., blurred vision, photophobia, diplopia, visual impairment, photopsia, cataract, vitreous floaters) reported.

In patients who report new visual symptoms, including changes that interfere with activities of daily living, temporarily interrupt entrectinib therapy and perform an ophthalmologic evaluation as clinically appropriate; dosage reduction may be necessary. (See Dosage Modification for Toxicity under Dosage and Administration: Pediatric Patients and Dosage and Administration: Adults.)

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm. Teratogenicity and embryofetal toxicity (i.e., reduced fetal weight, reduced skeletal ossification) demonstrated in animals.

Literature reports in individuals with congenital mutations in the tropomyosin receptor kinase (Trk) pathway suggest decreased Trk-mediated signaling may be associated with obesity, developmental delays, cognitive impairment, insensitivity to pain, and anhidrosis.

Avoid pregnancy during therapy. Perform pregnancy test prior to initiation of entrectinib in women of reproductive potential. Women of reproductive potential should use effective contraceptive methods while receiving the drug and for ≥5 weeks after the last dose. Men who are partners of such women should use effective methods of contraception while receiving the drug and for 3 months after the last dose. If used during pregnancy or if patient becomes pregnant, apprise patient of potential fetal hazard.

Specific Populations

Pregnancy

May cause fetal harm. (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Not known whether entrectinib or its metabolites distribute into human milk or affect milk production or nursing infants.

Discontinue nursing during therapy and for 1 week after the last dose.

Pediatric Use

Safety and efficacy not established in pediatric patients with NSCLC.

Safety and efficacy in pediatric patients ≥12 years of age with solid tumors harboring NTRK gene fusion are supported by extrapolation of data from 3 noncomparative studies in adults and limited safety data in 30 pediatric patients. Grade 3 or 4 neutropenia, fractures, weight gain, thrombocytopenia, lymphopenia, elevations in γ-glutamyltransferase (GGT, γ-glutamyltranspeptidase, GGTP) concentrations, and device-related infection occurred more frequently in pediatric patients compared with adults.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether efficacy and safety are similar to those in younger adults.

Hepatic Impairment

Mild hepatic impairment (total bilirubin concentration ≤1.5 times the ULN): No clinically important effect on pharmacokinetics.

Effect of moderate to severe hepatic impairment (total bilirubin concentration >1.5 times the ULN) on pharmacokinetics not established.

Renal Impairment

Mild to moderate renal impairment (Clcr 30 to <90 mL/minute): No clinically important effect on pharmacokinetics.

Effect of severe renal impairment (Clcr <30 mL/minute) on pharmacokinetics not established.

Common Adverse Effects

Fatigue, constipation, dysgeusia, edema, dizziness, diarrhea, nausea, dysesthesia, dyspnea, myalgia, cognitive impairment, increased weight, cough, vomiting, pyrexia, arthralgia, and vision disorders.

Interactions for Entrectinib

Metabolized principally by CYP3A4 to form M5 (major active metabolite), and to a lesser extent by CYP isoenzymes 2C9 and 1C19.

Entrectinib is not a substrate of P-glycoprotein (P-gp) or breast cancer resistance protein (BCRP), but M5 is a substrate of both P-gp and BCRP.

Neither entrectinib nor M5 is a substrate of organic anion transport protein (OATP) 1B1 or 1B3.

Drugs and Foods Affecting Hepatic Microsomal Enzymes

Potent inhibitors of CYP3A: Possible increased systemic exposure to, and increased toxicity of, entrectinib. Avoid concomitant use. If concomitant use cannot be avoided in adults and pediatric patients ≥12 years of age with BSA >1.5 m2, reduce entrectinib dosage to 100 mg once daily. When concomitant use of the potent CYP3A inhibitor is discontinued, return entrectinib dosage (after 3–5 elimination half-lives of the CYP3A inhibitor) to dosage used prior to initiation of the potent CYP3A inhibitor.

Moderate inhibitors of CYP3A: Possible increased systemic exposure to, and increased toxicity of, entrectinib. Avoid concomitant use. If concomitant use cannot be avoided in adults and pediatric patients ≥12 years of age with BSA >1.5 m2, reduce entrectinib dosage to 200 mg once daily. When concomitant use of the moderate CYP3A inhibitor is discontinued, return entrectinib dosage (after 3–5 elimination half-lives of the CYP3A inhibitor) to dosage used prior to initiation of the moderate CYP3A inhibitor.

Inducers of CYP3A: Possible decreased systemic exposure to, and decreased therapeutic efficacy of, entrectinib. Avoid concomitant use.

Drugs that Prolong the QT Interval

Because entrectinib has been associated with QT-interval prolongation, avoid concomitant use with other drugs with known potential to prolong the QT interval.

Specific Drugs and Foods

Drug or Food

Interaction

Comments

Digoxin

Digoxin peak concentrations and AUC increased by 28 and 18%, respectively

Efavirenz

Decreased systemic exposure of entrectinib expected

Avoid concomitant use

Erythromycin

Increased systemic exposure of entrectinib expected

Avoid concomitant use; if concomitant use cannot be avoided in adults and pediatric patients ≥12 years of age with BSA >1.5 m2, reduce entrectinib dosage to 200 mg once daily

When erythromycin is discontinued, return entrectinib dosage (after 3–5 elimination half-lives of erythromycin) to prior dosage

Grapefruit juice

Possible increased systemic exposure of entrectinib

Avoid concomitant use

Itraconazole

Increased peak plasma concentration and AUC of entrectinib 1.7- and 6-fold, respectively

Avoid concomitant use; if concomitant use cannot be avoided in adults and pediatric patients ≥12 years of age with BSA >1.5 m2, reduce entrectinib dosage to 100 mg once daily

When itraconazole is discontinued, return entrectinib dosage (after 3–5 elimination half-lives of itraconazole) to prior dosage

Lansoprazole

Entrectinib peak concentrations and AUC decreased by 23 and 25%, respectively

Midazolam

Midazolam peak concentrations decreased by 21% and AUC increased by 50%

Rifampin

Entrectinib peak concentrations and AUC decreased by 56 and 77%, respectively

Avoid concomitant use

Entrectinib Pharmacokinetics

Absorption

Bioavailability

Pharmacokinetics of entrectinib and its active metabolite are linear and time-independent over a dosage range of 100–400 mg/m2 when coadministered with food.

Peak plasma concentrations achieved in 4–6 hours following oral administration.

Steady-state concentrations of entrectinib and its active metabolite achieved within 1–2 weeks; systemic accumulation is approximately 2-fold.

Food

Administration with a high-fat, high-calorie meal has no clinically important effect on systemic exposure.

Special Populations

Age (12–86 years), sex, race, or body weight (32–130 kg) do not affect pharmacokinetics.

Distribution

Extent

Not known whether entrectinib or its metabolites are distributed into human milk.

Crosses blood-brain barrier in animals.

Plasma Protein Binding

Entrectinib and M5: >99% bound to plasma proteins.

Elimination

Metabolism

Principally metabolized by CYP3A4 to form M5.

Elimination Route

Eliminated in the feces (83% [36% as unchanged drug, 22% as M5]) and urine (3%).

Half-life

Entrectinib: 20 hours.

M5: 40 hours.

Stability

Storage

Oral

Capsules

<30°C.

Actions

  • Potent inhibitor of TrkA, TrkB, TrkC, ROS-1, and ALK.

  • TrkA, TrkB, and TrkC are encoded by NTRK1, NTRK2, and NTRK3 and are involved in the initiation of various cascades of intracellular signaling events (i.e., Ras/MAPK/ERK, PI3K/Akt, and PLCγ1/Pkc signal transduction pathways) that lead to cell proliferation, differentiation, apoptosis, and regulation of processes critical to neuron survival in the central and peripheral nervous systems.

  • Chromosomal rearrangements of NTRK1, NTRK2, and NTRK3 genes result in formation of a constitutively active chimeric Trk oncogenic fusion protein and dysregulation of Trk signaling and subsequent tumorigenesis.

  • Fusion proteins including ROS-1 or ALK kinase domains also activate tumorigenesis through hyperactivation of downstream signaling pathways.

  • Inhibits cancer cell lines derived from multiple tumor types harboring NTRK, ROS-1, and ALK fusion genes.

  • Major metabolite, M5, has similar inhibitory activity for TrkA, TrkB, TrkC, ROS-1, and ALK to that of entrectinib.

  • In vitro, 10- to 100-fold more potent than crizotinib in activity against ROS-1, and 7- to 8-fold more potent than crizotinib in activity against ALK.

  • Inhibits Janus kinase 2 (JAK2) and tyrosine kinase nonreceptor 2 (TNK2).

  • Clinical resistance attributed to secondary point mutations of NTRK kinase domain (e.g., G595R and G667C point mutations in the TrkA kinase domain; G623R point mutation in the TrkC kinase domain) reported.

Advice to Patients

  • Importance of advising patients to read the FDA-approved patient information.

  • Importance of advising patients to swallow entrectinib capsules whole and to avoid grapefruit juice while taking entrectinib. If a dose is missed, importance of taking missed dose as soon as it is remembered unless the next dose is due within 12 hours. If a dose is vomited immediately after administration, an additional dose should be administered to make up for the vomited dose.

  • Risk of heart failure. Importance of informing clinician promptly if new or worsening signs or symptoms of heart failure (e.g., dyspnea, edema) occur.

  • Risk of CNS effects. Importance of informing clinician if new or worsening CNS effects (i.e., cognitive impairment, mood disorders, dizziness, sleep disturbance) occur. Necessity of advising patients to avoid driving or operating hazardous machinery if they experience CNS effects.

  • Risk of hepatotoxicity and importance of monitoring liver function. Importance of informing clinician promptly if symptoms of hepatotoxicity (e.g., loss of appetite, nausea, vomiting, upper right abdominal pain) occur.

  • Risk of fractures. Importance of informing clinician if symptoms such as pain, changes in mobility, or deformity occur.

  • Risk of hyperuricemia. Importance of informing clinician if signs or symptoms associated with hyperuricemia occur.

  • Risk of QT-interval prolongation. Importance of informing clinician promptly if abnormal heartbeat or feelings of faintness, lightheadedness, or dizziness occur.

  • Risk of visual disturbances. Importance of informing clinician if visual disturbances (e.g., blurring, photophobia, diplopia, photopsia, light sensitivity, new or increased floaters) occur.

  • Risk of fetal harm. Necessity of advising women of reproductive potential to use effective methods of contraception while receiving entrectinib and for ≥5 weeks after the last dose. Importance of advising men with female partners of reproductive potential to use effective methods of contraception while receiving the drug and for 3 months after the last dose. Importance of women informing clinicians if they are or plan to be pregnant. If pregnancy occurs, advise pregnant women of potential risk to the fetus.

  • Importance of advising women to avoid nursing while receiving the drug and for 1 week after the last dose.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and herbal supplements, as well as any concomitant illnesses.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Distribution of entrectinib is restricted. (See Restricted Distribution under Dosage and Administration.)

Entrectinib

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

100 mg

Rozlytrek

Genentech

200 mg

Rozlytrek

Genentech

AHFS DI Essentials™. © Copyright 2021, Selected Revisions August 31, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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