How Far Is Too Far? The Ethics of Mini Brain Research
December 11, 2025
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Brand Name :
Rozlytrek
(United States) [Available]Synonyms :
entrectinib
Class :
Anti-cancer and Tyrosine Kinase Inhibitor
Brand Name :
Rozlytrek
(United States) [Available]Synonyms :
entrectinib
Class :
Anti-cancer and Tyrosine Kinase Inhibitor
Dosage forms & Strengths
capsule
100 mg
200 mg
600
mg
Capsule
Orally
once a day
600
mg
Capsule
Orally
once a day
Dosage forms & Strengths
capsule
100 mg
200 mg
Administer 600 mg four times daily orally
Safety and efficacy are not found in children below 12 years
600
mg
Capsule
Orally
once a day
Safety and efficacy are not found in children below 12 years
may enhance the concentration of serum when combined with entrectinib
may enhance the concentration of serum when combined with entrectinib
may enhance the concentration of serum when combined with entrectinib
may enhance the concentration of serum when combined with entrectinib
may enhance the concentration of serum when combined with entrectinib
may enhance the serum concentration of CYP3A4 inhibitors
may enhance the serum concentration of CYP3A4 Inhibitors
when used together, entrectinib and alfuzosin both increase the QTc interval
when used together, entrectinib and apomorphine both increase the QTc interval
when used together, entrectinib and bedaquiline both increase the QTc interval
when used together, entrectinib and citalopram both increase the QTc interval
when used together, entrectinib and degarelix both increase the QTc interval
when used together, entrectinib and eliglustat both increase the QTc interval
erythromycin stearate increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
etravirine decreases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
fluconazole increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
fostamatinib increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when used together, entrectinib and gilteritinib both increase the QTc interval
when used together, entrectinib and haloperidol both increase the QTc interval
idelalisib increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when used together, entrectinib and isoflurane both increase the QTc interval
ketoconazole increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when used together, entrectinib and lefamulin both increase the QTc interval
when used together, entrectinib and levofloxacin both increase the QTc interval
when used together, entrectinib and lithium both increase the QTc interval
when used together, entrectinib and lumefantrine both increase the QTc interval
when used together, entrectinib and methadone both increase the QTc interval
when used together, entrectinib and midostaurin both increase the QTc interval
nefazodone increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when used together, entrectinib and osimertinib both increase the QTc interval
when used together, entrectinib and panobinostat both increase the QTc interval
when used together, entrectinib and quinine both increase the QTc interval
when used together, entrectinib and ranolazine both increase the QTc interval
when used together, entrectinib and risperidone both increase the QTc interval
when used together, entrectinib and romidepsin both increase the QTc interval
when used together, entrectinib and midostaurin both increase the QTc interval
when used together, entrectinib and sorafenib both increase the QTc interval
when used together, entrectinib and midostaurin both increase the QTc interval
when used together, entrectinib and trazodone both increase the QTc interval
when used together, entrectinib and vandetanib both increase the QTc interval
verapamil increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when used together, entrectinib and vorinostat both increase the QTc interval
when used together, entrectinib and ziprasidone both increase the QTc interval
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
may have an increased QTc-prolonging effect when combined with QT-prolonging agents
may diminish the concentration of serum when combined with entrectinib
may diminish the concentration of serum when combined with entrectinib
may diminish the concentration of serum when combined with entrectinib
may diminish the concentration of serum when combined with entrectinib
may diminish the concentration of serum when combined with entrectinib
entrectinib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
entrectinib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
entrectinib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
entrectinib: they may increase the QTc-prolonging effect of QTc-prolonging Agents
QTc interval increases on taking entrectinib and lenvatinib together. Avoid or take an alternate drug
the effect of entrectinib is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, both increase the QTC interval
lapatinib increases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, there may be an increased QTC interval goser
when both drugs are combined, there may be an increased QTC interval
CYP3A strong enhancers of the small intestine may reduce the bioavailability of entrectinib
midostaurin and entrecitinib, when used simultaneously, increase the QTc level
midostaurin and entrecitinib, when used simultaneously, increase the QTc level
when used together, entrectinib and albuterol both increase the QTc interval
when used together, entrectinib and arformoterol both increase the QTc interval
when used together, entrectinib and clomipramine both increase the QTc interval
when used together, entrectinib and imipramine both increase the QTc interval
when used together, entrectinib and protriptyline both increase the QTc interval
when used together, entrectinib and salmeterol both increase the QTc interval
tazemetostat decreases the effect of entrectinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
when used together, entrectinib and trimipramine both increase the QTc interval
when ajmaline is used together with entrectinib, the risk or seriousness of QTc prolongation is enhanced
When indisulam is used together with entrectinib, this leads to a reduction in entrectinib metabolism
entrectinib: it may increase the risk of methemoglobinemia with ambroxol
when both drugs are combined, there may be a reduced excretion rate of topotecan and result in an elevated level of serum concentration
when both drugs are combined, there may be an increased risk or severity of QTC prolongation
Actions and Spectrum:
Actions:
Entrectinib, a tyrosine kinase inhibitor, targets TRK, ROS1, and ALK receptors to disrupt cancer cell signaling pathways, inhibiting tumor growth, especially in lung cancers.
Spectrum
Entrecitinib is beneficial in treatment of solid tumors & ROS-1 positive NSCLC.
Frequency defined
>10%
Fatigue
Increased AST
Lymphopenia
Increased ALT
Hyponatremia
Diarrhea
Hypocalcemia
Hypophosphatemia
Dyspnea
Hypoalbuminemia
Neutropenia
Cognitive impairment
Hyperkalemia
Increased weight
Increased alkaline phosphatase
Pyrexia
Arthralgia
Headache
Hypotension
Ataxia
Abdominal pain
Urinary tract infection
Decreased appetite
Muscular weakness
Back pain
Extremity pain
1-10%
Mood disorders
Anemia
Neutropenia
Dyspnea
Pleural effusion
Pulmonary embolism
Respiratory failure
Pyrexia
<1%
Increased alkaline phosphatase
Hyponatremia
Vision disorders
Muscular weakness
Sleep disorders
Decreased appetite
Cough
Black Box Warning:
Avoid taking grapefruit drink or juice consumption while using entrecitinib.
Contraindication/Caution:
Contraindications
Cautions
Pregnancy consideration:
As per the mechanism of action of entrectinib, it is rendered unsafe for the fetus. Pregnant women are advised to know about the potential risks.
Lactation: No data available regarding the excretion of entrectinib in breast milk. Hence, potential adverse effects and potential benefits should be compared and considered.
Pregnancy category:
Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first trimester or the later trimester.
Category B: There is no affirmation of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women.
Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a product in humans; Pregnant women must take care of the potential risks.
Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential dangers may be used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh risks over benefits. The drug is not for pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology:
Entrecitinib acts as tyrosine kinase inhibitor.
Pharmacodynamics:
Entrectinib inhibits tyrosine kinase and blocks cancer-promoting pathways by binding to ATP sites on RTKs.
Pharmacokinetics:
Absorption
The Tmax is achieved within 4 to 6 hours after oral administration.
Distribution
Entrecitinib is moderately distributed in the body.
Metabolism
The metabolism occurs in the liver.
Excretion and Elimination
The drug is majorly excreted via feces with showing small portions through urine.
The half-life is 3.5 to 11.9 hours.
Administration:
The route of administration is oral
Generic Name: entrectinib
Pronounced: en-trek-ti-nib
Why do we use entrectinib?
Entrectinib is a kinase inhibitor used to treat specific types of advanced non-small cell lung cancer (NSCLC) in adults, as well as certain solid tumors in adults and children over 1 month old that are inoperable or have spread and progressed after other treatments. It works by blocking abnormal proteins that drive cancer cell growth, helping to slow or stop the spread of the disease.
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