Rozlytrek

About Entrecitinib

Entrectinib is a prescribed medicine for the treatment of: 

Adult patients with metastatic non-small cell lung cancer (NSCLC) with ROS1-positive tumors.
Adults and children aged 12 and up with solid malignancies that:

• contain a neurotrophic tyrosine receptor kinase (NTRK) gene fusion in the absence of a known acquired resistance mutation,

• are metastatic or when surgical excision would result in considerable morbidity; and 
• have progressed following treatment or have no suitable alternative therapy.

Strength

100 mg and 200 mg capsules

Recommended Dosage:

• The recommended dosage for ROS1-positive non-small cell lung cancer is 600 mg orally once daily.
• The recommended dosage for NTRK Gene Fusion-Positive Solid Tumors is 600 mg orally once daily for adults and for pediatric patients 12 years or above, the recommended dosage for Entrectinib capsules depends on body surface area (BSA)
• BSA more than 1.50 m2: 600 mg once daily
• BSA 1.11–1.50 m2: 500 mg once daily
• BSA 0.91–1.10 m2: 400 mg once daily

Important

Encourage patients to communicate with their healthcare providers about all concurrent medications, encompassing prescription drugs, over-the-counter medications, vitamins, and herbal products. Additionally, advise patients to refrain from consuming grapefruit juice while undergoing Rozlytrek treatment.

Warnings & Precautions

• Prior to initiating Rozlytrek, assess the left ventricular ejection fraction in patients with CHF symptoms or risk factors (Congestive Heart Failure). Monitor for clinical signs and symptoms, and consider withholding Entrectinib for new or worsening CHF. Reassess LVEF and implement appropriate management. 
• Entrectinib capsules might cause CNS side effects such as cognitive impairment, mood problems, dizziness, and sleep disruptions. Withhold and then restart at the same or lower dose when symptoms improve, or cease Rozlytrek completely dependent on severity. 
• Rozlytrek increases the possibility of fractures (Skeletal Fractures). Consulting doctors must evaluate patients with fracture indications or symptoms immediately.
• The consulting doctor must asses the liver tests, such as ALT and AST, every two weeks for the first month of therapy, then monthly after that, and as clinically necessary (Hepatotoxicity). Depending on the severity, withhold or permanently cease Rozlytrek. If withheld, restart Entrectinib at the same or lower dose according to severity. 
• Patients with or at risk of QTc interval prolongation should be closely monitored (QT Interval Prolongation). Assess the QT interval and electrolytes at the start of treatment and on a regular basis. Withhold and then restart at the same or decreased dose, or quit Entrectinib permanently dependent on severity. 
• Withhold for new visual changes or changes that interfere with everyday activities until improvement or stabilization occurs. If necessary, the treating doctor should perform an ophthalmological examination (Vision Disorders). Upon improvement or stability, the same or reduced dosage can be resumed.
•  There are chances of fetal damage (Embryo-Fetal Toxicity). The treating doctors must inform females of reproductive potential about the potential risk of pregnancy and the need of using effective contraception.

Common Entrectinib Side Effects

• Fatigue
• Constipation
• Dysgeusia
• Edema
• Dizziness
• Diarrhea
• Nausea
• Dysesthesia
• Dyspnea
• Myalgia
• Cognitive impairment
• Increased weight
• Cough
• Vomiting
• Pyrexia
• Arthralgia
• Vision disorders

Use in specific population 

• Rozlytrek carries a risk of fetal harm in pregnant women, with insufficient data on its use in this population. 
• Do not breastfeed while taking Rozlytrek. Information on the presence of entrectinib or its metabolites in human milk and their impact on breastfeeding infants and milk production is unavailable. Due to potential adverse reactions in breastfed children, lactating women are advised to cease breastfeeding during Rozlytrek treatment and for 7 days after the final dose. 
• Before initiating Rozlytrek, assess the pregnancy status of females of reproductive potential, advising effective contraception during treatment and for at least 5 weeks post-final dose. 
• Male patients with female partners of reproductive potential should employ effective contraception during treatment and for 3 months following the final dose. 
• Rozlytrek’s safety and effectiveness have not been established in pediatric patients under 12 years old with solid tumors harboring an NTRK gene fusion or in pediatric patients with ROS1-positive NSCLC. 
• No dose adjustment is recommended for mild or moderate renal impairment, but its use has not been studied in patients with severe renal impairment. 
• For hepatic impairment, no dose adjustment is recommended for mild impairment, while Rozlytrek’s use has not been studied in patients with moderate to severe hepatic impairment.

Storage and Handling

Store below 30ºC