RETEVMO Capsule (2020)
Βιβλιογραφική αναφορά
Συγγραφείς
Eli Lilly and Company
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1. Indications and Usage
1.1 Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer RETEVMO is indicated for the treatment of adult patients with metastatic <em>RET</em> fusion-positive non-small cell lung cancer (NSCLC). ...
2. Dosage and Administration
2.1 Patient Selection Select patients for treatment with RETEVMO based on the presence of a <em>RET</em> gene fusion (NSCLC or thyroid cancer) or specific <em>RET</em> gene mutation (MTC) in tumor specimens ...
3. Dosage Forms and Strengths
Capsules: 40 mg: gray opaque capsule imprinted with Lilly, 3977 and 40 mg in black ink. 80 mg: blue opaque capsule imprinted with Lilly, 2980 and 80 mg in black ink.
4. Contraindications
None.
5. Warnings and Precautions
5.1 Hepatotoxicity Serious hepatic adverse reactions occurred in 2.6% of patients treated with RETEVMO. Increased AST occurred in 51% of patients, including Grade 3 or 4 events in 8% and increased ALT ...
6. Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: Hepatotoxicity <em>[see Warnings and Precautions (5.1)]</em> Hypertension <em>[see Warnings and Precautions ...
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 RETEVMO Acid-Reducing Agents Concomitant use of RETEVMO with acid-reducing agents decreases selpercatinib plasma concentrations <em>[see Clinical Pharmacology (12.3)],</em> ...
8.1. Pregnancy
Risk Summary Based on findings from animal studies, and its mechanism of action <em>[see Clinical Pharmacology (12.1)]</em>, RETEVMO can cause fetal harm when administered to a pregnant woman. There are ...
8.2. Lactation
Risk Summary There are no data on the presence of selpercatinib or its metabolites in human milk or on their effects on the breastfed child or on milk production. Because of the potential for serious adverse ...
8.3. Females and Males of Reproductive Potential
Based on animal data, RETEVMO can cause embryolethality and malformations at doses resulting in exposures less than or equal to the human exposure at the clinical dose of 160 mg twice daily <em>[see Use ...
8.4. Pediatric Use
The safety and effectiveness of RETEVMO have been established in pediatric patients aged 12 years and older for medullary thyroid cancer (MTC) who require systemic therapy and for advanced <em>RET</em> ...
8.5. Geriatric Use
Of 702 patients who received RETEVMO, 34% (239 patients) were ≥65 years of age and 10% (67 patients) were ≥75 years of age. No overall differences were observed in the safety or effectiveness of RETEVMO ...
8.6. Renal Impairment
No dosage modification is recommended for patients with mild to moderate renal impairment (creatinine clearance [CLcr] ≥30 mL/min, estimated by Cockcroft-Gault). The recommended dosage has not been established ...
8.7. Hepatic Impairment
Reduce the dose when administering RETEVMO to patients with severe [total bilirubin greater than 3 to 10 times upper limit of normal (ULN) and any AST] hepatic impairment <em>[see Dosage and Administration ...
11. Description
Selpercatinib is a kinase inhibitor. The molecular formula for selpercatinib is C<sub>29</sub>H<sub>31</sub>N<sub>7</sub>O<sub>3</sub> and the molecular weight is 525.61 g/mol. The chemical name is 6-(2-hydroxy-2-methylpropoxy) ...
12.1. Mechanism of Action
Selpercatinib is a kinase inhibitor. Selpercatinib inhibited wild-type RET and multiple mutated RET isoforms as well as VEGFR1 and VEGFR3 with IC<sub>50</sub> values ranging from 0.92 nM to 67.8 nM. In ...
12.2. Pharmacodynamics
Exposure-Response Relationship Selpercatinib exposure-response relationships and the time course of pharmacodynamic response have not been fully characterized. Cardiac Electrophysiology The effect of RETEVMO ...
12.3. Pharmacokinetics
The pharmacokinetics of selpercatinib were evaluated in patients with locally advanced or metastatic solid tumors administered 160 mg twice daily unless otherwise specified. Steady-state selpercatinib ...
13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility
Carcinogenicity studies have not been conducted with selpercatinib. Selpercatinib was not mutagenic in the in vitro bacterial reverse mutation (Ames) assays, with or without metabolic activation, or clastogenic ...
14. Clinical Studies
14.1 Metastatic RET Fusion-Positive Non-Small Cell Lung Cancer The efficacy of RETEVMO was evaluated in patients with advanced <em>RET</em> fusion-positive NSCLC enrolled in a multicenter, open-label, ...
16.1. How Supplied
RETEVMO (selpercatinib) capsules are supplied as follows: 40 mg: Gray opaque, imprinted with Lilly, 3977 and 40 mg in black ink. 60 count bottle NDC# 0002-3977-60 80 mg: Blue opaque, imprinted with Lilly ...
16.2. Storage and Handling
Store at 20°C to 25°C (68°F to 77°F); excursions between 15°C and 30°C (59°F to 86°F) are permitted [see USP Controlled Room Temperature].
17. Patient Counseling Information
Advise the patient to read the FDA-approved patient labeling (Patient Information). Hepatotoxicity Advise patients that hepatotoxicity can occur and to immediately contact their healthcare provider for ...