Simerta® (Osimertinib)

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40,80 mg TABLET

Simerta^® is a kinase inhibitor of epidermal growth factor receptor (EGFR) which binds irreversibly to certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions). Osimertinib also inhibited the activity of HER2, HER3, HER4, ACK1, and BLK at clinically relevant concentrations in vitro.

INDICATIONS

As adjuvant therapy after tumor resection in adult patients with non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 L858R mutations.
The first-line treatment of adult patients with metastatic NSCLC whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations.
The treatment of adult patients with metastatic EGFR T790M mutation-positive NSCLC, whose disease has progressed on or after EGFR TKI therapy.
It is not known if Osimertinib is safe and effective in children.

DOSAGE AND ADMINISTRATION

Adjuvant treatment of early stage NSCLC: 80 mg orally once daily, with or without food, until disease recurrence, or unacceptable toxicity, or for up to 3 years.
Metastatic NSCLC: 80 mg orally once daily, with or without food, until disease progression or unacceptable toxicity.

WARNINGS AND PRECAUTIONS

Simerta® may cause serious side effects including:

Lung problems. Osimertinib may cause Interstitial Lung Disease/Pneumonitis that may lead to death. Symptoms may be similar to those symptoms from lung cancer. Patients may experience new or worsening lung symptoms, including trouble breathing, shortness of breath, cough, or fever. Advise patients to contact their healthcare provider immediately to report new or worsening respiratory symptoms.
Heart problems, including heart failure. Osimertinib may cause heart problems that may lead to death. Osimertinib may cause heart rate-corrected QT (QTc) interval prolongation and cardiomyopathy (defined as cardiac failure, chronic cardiac failure, congestive heart failure, pulmonary edema or decreased ejection fraction). Symptoms of a heart problem may include: feeling like the heart is pounding or racing, shortness of breath, swelling of ankles and feet, dizziness, lightheadedness, and syncope. Patients’ heart function should be checked before starting Simerta^® and during treatment as needed. In patients who have a history or predisposition for QTc prolongation, or those who are taking medications that are known to prolong the QTc, electrocardiograms and electrolytes should be monitored. Advise patients to report these symptoms and to inform their physician about the use of any heart or blood pressure medications.
Eye problems (Keratitis). Patients treated with Osimertinib may experience eye problems. Symptoms suggestive of keratitis may include: watery eyes (lacrimation), eye inflammation, light sensitivity, eye pain, eye redness, blurred vision or vision changes. If patients get eye problems with Simerta^®, the healthcare provider will send them to see an eye specialist (ophthalmologist).
Skin problems. Stevens-Johnson syndrome (SJS) and erythema multiforme (EM) have been reported in patients receiving Osimertinib. Advise patients to contact their healthcare provider immediately if they experience developing target lesions (skin reactions that look like rings), severe blistering or peeling of the skin.
Inflammation of the blood vessels in skin (Cutaneous Vasculitis). Cutaneous vasculitis including leukocytoclastic vasculitis, urticarial vasculitis, and IgA vasculitis have been reported in patients receiving Osimertinib. Signs and symptoms that may be indicative of cutaneous vasculitis include: purple spots or redness of the skin that does not fade in color when pressed (non-blanching) on lower arms, lower legs, or buttocks or large hives on the main part of body (trunk) that do not go away within 24 hours and look bruised.

Call your healthcare provider right away if you have aforementioned symptoms.

The most common side effects

The most common side effects in people who take Osimertinib include:

Low white blood cell counts
Low platelet counts
Diarrhea
Muscle, bone, or joint pain
Changes in your nails, including: redness, tenderness, pain, inflammation, brittleness, separation from the nailbed, and shedding of nail
Dry skin
Mouth sores
Tiredness
Cough
Low red blood cell counts (anemia)
Rash

Tell your healthcare provider if you have any side effect that bothers you or that does not go away.

DRUG INTERACTIONS

Strong CYP3A Inducers: Co-administering Osimertinib with a strong CYP3A4 inducer decreased the exposure of Osimertinib compared to administering Osimertinib alone. Decreased Osimertinib exposure may lead to reduced efficacy. Avoid co-administration of Simerta® with strong CYP3A inducers. If co-administration of Simerta® with strong CYP3A inducers cannot be avoided, increase the Simerta® dosage. No dose adjustments are required when Simerta® is used with moderate and/or weak CYP3A inducers.
Breast Cancer Resistant Protein (BCRP) or P-glycoprotein (P-gp) substrate: Avoid co-administration of Simerta® with BCRP or P-gp substrate. Co-administering Simerta® increased the exposure of the substrate compared to administering it alone. Increased BCRP or P-gp substrate exposure may increase the risk of exposure related toxicity and adverse effects.
Drugs that prolong the QTc Interval: The effect of co-administering medicinal products known to prolong the QTc interval with Simerta® is unknown. When feasible, avoid concomitant administration of these drugs known to prolong the QTc interval with known risk of Torsades de pointes. If not feasible to avoid concomitant administration of such drugs, conduct periodic ECG monitoring.

simerta leaflet

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	osimertinib+En-02.12.16-Final.pdf	790.55 KB