TEPMETKO Film-coated tablet (2021)

Βιβλιογραφική αναφορά

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EMD Serono, Inc.

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1. Indications and Usage

TEPMETKO is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition (MET) exon 14 skipping alterations. This ...

2. Dosage and Administration

2.1 Patient Selection for METex14 Skipping Alterations Select patients for treatment with TEPMETKO based on the presence of MET exon 14 skipping alterations in plasma or tumor specimens. Testing ...

3. Dosage Forms and Strengths

Tablets: 225 mg, white-pink, oval, biconvex film-coated tablets with embossment M on one side and plain on the other side.

4. Contraindications

None.

5. Warnings and Precautions

5.1 Interstitial Lung Disease (ILD)/Pneumonitis ILD/pneumonitis, which can be fatal, occurred in patients treated with TEPMETKO [see Adverse Reactions (6.1)]. ILD/pneumonitis occurred in 2.2% ...

6. Adverse Reactions

The following adverse reactions are described in greater detail elsewhere in the labeling: Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.1)] Hepatotoxicity [see Warnings ...

6.1. Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another ...

7. Drug Interactions

7.1 Effects of Other Drugs on TEPMETKO Dual Strong CYP3A Inhibitors and P-gp Inhibitors The effect of strong CYP3A inhibitors or P-gp inhibitors on TEPMETKO has not been studied clinically. However, metabolism ...

8.1. Pregnancy

Risk Summary Based on findings in animal studies and the mechanism of action [see Clinical Pharmacology (12.1)], TEPMETKO can cause fetal harm when administered to a pregnant woman. There are ...

8.2. Lactation

Risk Summary There are no data regarding the secretion of tepotinib or its metabolites in human milk or its effects on the breastfed infant or milk production. Advise women not to breastfeed during treatment ...

8.3. Females and Males of Reproductive Potential

Based on animal data, TEPMETKO can cause malformations at doses less than the human exposure based on AUC at the 450 mg clinical dose [see Use in Specific Populations (8.1)]. Pregnancy Testing ...

8.4. Pediatric Use

The safety and efficacy of TEPMETKO in pediatric patients have not been established.

8.5. Geriatric Use

Of 255 patients with METex14 skipping alterations in VISION who received 450 mg TEPMETKO once daily, 79% were 65 years or older, and 43% were 75 years or older. No clinically important differences ...

8.6. Renal Impairment

No dosage modification is recommended in patients with mild or moderate renal impairment (creatinine clearance [CLcr] 30 to 89 mL/min, estimated by Cockcroft-Gault). The recommended dosage has not been ...

8.7. Hepatic Impairment

No dosage modification is recommended in patients with mild (Child Pugh Class A) or moderate (Child Pugh Class B) hepatic impairment. The pharmacokinetics and safety of tepotinib in patients with severe ...

11. Description

Tepotinib is a kinase inhibitor. TEPMETKO (tepotinib) tablets for oral use are formulated with tepotinib hydrochloride hydrate. The chemical name for tepotinib hydrochloride hydrate is 3-{1-[(3-{5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl}phenyl)methyl]-6-oxo-1,6-dihydropyridazin-3-yl}benzonitrile ...

12.1. Mechanism of Action

Tepotinib is a kinase inhibitor that targets MET, including variants with exon 14 skipping alterations. Tepotinib inhibits hepatocyte growth factor (HGF)-dependent and -independent MET phosphorylation ...

12.2. Pharmacodynamics

Exposure-Response Tepotinib exposure-response relationships and the time course of pharmacodynamic response have not been fully characterized. Cardiac Electrophysiology At the recommended dosage, no large ...

12.3. Pharmacokinetics

The pharmacokinetics of tepotinib were evaluated in patients with cancer administered 450 mg once daily unless otherwise specified. Tepotinib exposure (AUC0-12h and Cmax) increases ...

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenicity studies have not been performed with tepotinib. Tepotinib and its major circulating metabolite were not mutagenic in vitro in the bacterial reverse mutation (Ames) assay, or a ...

14. Clinical Studies

The efficacy of TEPMETKO was evaluated in a single-arm, open-label, multicenter, non-randomized, multicohort study (VISION, NCT02864992). Eligible patients were required to have advanced or metastatic ...

16.1. How Supplied

TEPMETKO (tepotinib) tablets: 225 mg tepotinib, white-pink, oval, biconvex film-coated tablet with embossment M on one side and plain on the other side. NDC number Size 44087-5000-3 Box of 30 tablets: ...

16.2. Storage and Handling

Store TEPMETKO at 20°C-25°C (68°F-77°F); excursions permitted to 15°C-30°C (59°F-86°F) [see USP-NF Controlled Room Temperature]. Store in original package.

17. Patient Counseling Information

Advise the patient to read the FDA-approved patient labeling (Patient Information). Interstitial Lung Disease (ILD)/Pneumonitis Inform patients of the risk of severe or fatal ILD/pneumonitis. Advise patients ...