Lucientre Entrectinib 200mg Capsules 90’s

Entrectinib is an oral targeted anticancer medicine that inhibits the activity of several receptor tyrosine kinases, particularly TRKA, TRKB, TRKC, and ROS1.

Certain cancers contain genetic abnormalities called NTRK gene fusions or ROS1 rearrangements, which can continuously activate these pathways and promote cancer-cell growth.

Entrectinib blocks these abnormal signaling pathways and can therefore inhibit the growth and survival of cancer cells.

Entrectinib is approved for selected patients whose tumors have the relevant NTRK gene fusion or ROS1-positive status, confirmed by an appropriate diagnostic test.

ROS1-positive metastatic NSCLC

Entrectinib is indicated for adults with ROS1-positive metastatic non-small-cell lung cancer (NSCLC).

NTRK fusion-positive solid tumors

It is also indicated for adult and pediatric patients older than 1 month with solid tumors that:

• Have an NTRK gene fusion
• Do not have a known acquired resistance mutation
• Are metastatic, or where surgical removal would likely cause severe morbidity.
• Have progressed following treatment, or have no satisfactory alternative therapy.

In cancers containing NTRK gene fusions or ROS1 rearrangements, these proteins can become abnormally activated and stimulate pathways responsible for:

• Cancer cell proliferation
• Cell survival
• Tumor growth
• Cancer-cell migration

Entrectinib blocks this signaling, thereby helping to slow or inhibit tumor growth.

In simple terms:

NTRK fusion / ROS1 rearrangement → abnormal kinase signaling → cancer-cell growth

Entrectinib → kinase inhibition → reduced abnormal signaling → inhibition of tumor growth

The medicine is therefore considered a molecularly targeted therapy rather than a conventional cytotoxic chemotherapy.

Recommended adult dose

For adult patients with either ROS1-positive metastatic NSCLC or NTRK fusion-positive solid tumors, 600 mg orally once daily.

Entrectinib can be taken:

• With or without food
• At approximately the same time every day.

Dosage in children

For pediatric patients with NTRK fusion-positive solid tumors, the dose is based on age and body-surface area (BSA) rather than simply using the adult 600-mg dose.

Capsules

Swallow capsules according to the prescribing instructions.

Entrectinib oral pellets are another dosage form for appropriate pediatric patients. Pellets should not be used for enteral tube administration; capsules prepared as a suspension are used for that purpose.

Missed dose

If a dose is missed or vomiting occurs after taking the dose, follow the prescribing physician's instructions rather than taking an extra dose. Do not double the dose without medical advice.

Common:

• Fatigue
• Constipation
• Altered taste (dysgeusia)
• Edema/swelling
• Dizziness
• Diarrhea
• Nausea
• Abnormal sensations (dysesthesia)
• Shortness of breath
• Muscle pain (myalgia)
• Cognitive impairment
• Weight gain
• Cough
• Vomiting
• Fever
• Joint pain (arthralgia)
• Vision disorders

Not every patient experiences these effects.

Serious:

Congestive heart failure

Entrectinib can cause congestive heart failure (CHF), including in patients without previous heart disease.

Central nervous system effects

Entrectinib can cause neurological and psychiatric effects.

Skeletal fractures

Fractures have been reported during treatment.

Hepatotoxicity

Entrectinib can cause liver toxicity, including elevations in liver enzymes.

Hyperuricemia

Entrectinib can cause increased uric acid levels.

QT prolongation

Entrectinib can prolong the QT interval, which can increase the risk of certain abnormal heart rhythms.

The prescribing information recommends evaluating the QT interval and electrolytes before starting treatment.

Vision disorders

Vision-related adverse effects can occur.

Always inform the oncologist about all prescription medicines, OTC medicines, vitamins, and herbal supplements.

Moderate and strong CYP3A inhibitors can increase the amount of entrectinib in the bloodstream and increase the risk of adverse reactions.

Examples can include certain:

• Antifungal medicines
• Antibiotics
• Antiviral medicines
• Other CYP3A-inhibiting drugs

These combinations should generally be avoided where possible. If unavoidable, the entrectinib dose may need to be reduced according to the prescribing information.

Grapefruit

Avoid grapefruit and grapefruit products, including grapefruit juice, because they can inhibit CYP3A and increase entrectinib exposure.

• Store at 20°C–25°C (68°F–77°F)
• Temperature excursions between 15°C and 30°C (59°F and 86°F) are permitted.
• Keep in the original container.
• Keep the bottle tightly closed.
• Protect from moisture.
• Keep all medicines out of reach of children.

• Confirm the relevant ROS1 alteration or NTRK gene fusion before treatment.
• Take the medicine exactly as prescribed.
• The usual adult dose is 600 mg once daily.
• It can be taken with or without food.
• Take it at approximately the same time every day.
• Avoid grapefruit and grapefruit juice.
• Inform your doctor about all medicines and supplements.
• Do not start a new medicine without checking for interactions.
• Report new or worsening shortness of breath or swelling.
• Report significant dizziness, confusion, hallucinations, or memory problems.
• Report new vision changes immediately.
• Report unexplained bone pain or injury.
• Attend scheduled heart, liver, electrolyte, and other laboratory monitoring.
• Do not drive if dizziness, confusion, blurred vision, or other neurological symptoms affect your ability to drive safely.
• Do not stop treatment without consulting your oncologist.