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Tartseva
Last reviewed: 03.07.2025
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Tarceva, an antitumor drug and a tyrosine kinase inhibitor, belongs to the category of antineoplastic agents.
Indications Tartsevs
The main indications for prescribing Tarceva are the following:
- Maintenance treatment of localized or metastatic non-small cell lung cancer, if there is no progression of the disease after 4 courses of chemotherapy.
- Lung cancer, localized or metastatic, if one or more courses of chemotherapy have not had the expected effect.
- Localized or metastatic inoperable cancer in the pancreas (as a first-line drug, in combination with Gemcitabine).
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Release form
Tarceva is produced in tablet form, with a protective shell coating. The active ingredient is the antitumor substance erlotinib.
The tablets are round, with smooth edges, covered with a light yellowish film. On one side there is an inscription reflecting the name and dosage of the tablet in mg:
- Tarceva 25;
- Tarceva 100;
- Tarceva 150.
One blister plate contains ten tablets. A cardboard pack contains three blister plates and a paper instruction.
Pharmacodynamics
Tarceva, based on erlotinib, is the most powerful drug that inhibits the tyrosine kinase of the EGF (human epidermal growth factor) receptor.
Tyrosine kinase is responsible for the processes of phosphorylation of EGF, which are expressed on the surface of healthy and tumor cell structures, inside the cell. Inhibition of the activity of phosphotyrosine growth factor inhibits the development of cancer cells and/or causes their death.
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Pharmacokinetics
The active component of Tarceva is well absorbed after oral administration. The maximum serum concentration is observed after four hours. Bioavailability in a healthy person is estimated at 59%. The presence of food masses in the stomach can increase the bioavailability of the drug.
The serum trough level is 1.995 ng/mL. Equilibrium is observed after 7-8 days. Before the next dose of Tarceva, the serum trough level of the active ingredient is 1.238 ng/mL.
In cancer tissue samples, after 9 days of treatment, the active component level is found to be on average 1.185 ng/g. This is about 63% of the maximum level in serum at equilibrium. After 60 minutes of taking Tarceva, the maximum content of the drug in plasma can be 73%. Binding to plasma proteins is 95%.
Tarceva metabolism occurs in the liver, with the involvement of enzymes in the process. Extrahepatic metabolic processes are observed in the intestinal cavity, in the lungs, directly in tumor tissues.
The average clearance is close to 4.47 l/h. The half-life is 36.2 h. Metabolic products and unchanged drug residues are excreted mainly with feces (more than 90%), and to a lesser extent through the kidneys.
Concomitant treatment with Tarceva and Gemcitabine does not affect the serum clearance rates of erlotinib.
Dosing and administration
Tarceva is taken orally, once a day, 60 minutes before meals or two hours after meals.
- For non-small cell lung cancer, the recommended dose is 150 mg of Tarceva per day.
- In case of pancreatic cancer, it is recommended to take 100 mg of Tarceva per day, for a long time, in combination with Gemcitabine.
Use Tartsevs during pregnancy
The possibility of using Tarceva in pregnant patients has not been sufficiently studied. Preclinical testing of the toxic effects of the drug at standard doses indicated embryotoxicity.
Given the above, it is not recommended to use Tarceva for therapy of pregnant patients. Women of childbearing age should exclude pregnancy before starting therapy, and also use reliable methods of contraception.
The possibility of treatment with Tarceva during breastfeeding has not been studied, therefore, it is not recommended to use this type of drug.
Contraindications
Tarceva treatment should be avoided in the following situations:
- in case of severe liver and kidney damage;
- during pregnancy and breastfeeding;
- in pediatrics;
- if you are prone to allergies to Tarceva.
Relative contraindications are:
- patient smoking;
- galactose intolerance, lactase deficiency;
- peptic ulcer;
- concomitant chemotherapy with taxanes.
Side effects Tartsevs
Most often, specialists detect the following side effects while taking the medication Tarceva:
- diarrhea, nausea, mouth ulcers, abdominal pain, bloating, bleeding in the digestive tract (up to perforation);
- emaciation;
- development of liver failure;
- conjunctivitis, corneal ulcers (sometimes with perforation), keratitis;
- cough, difficulty breathing, bleeding from the nasal mucosa;
- skin rashes, baldness, deterioration of the skin and nails, changes in pigmentation;
- headaches, neuropathies;
- depressive states;
- feeling of fatigue, infection (pneumonia, phlegmon, septic complications).
Overdose
No special effects were observed when a single dose of Tarceva up to 1600 mg was taken orally.
When taking higher doses, the following symptoms may occur:
- severe diarrhea;
- skin rash;
- increased levels of liver transaminases.
In case of a possible overdose, Tarceva is discontinued and treatment with symptomatic medications is prescribed instead.
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Interactions with other drugs
Ketoconazole, Ciprofloxacin affect the metabolism of Tarceva and increase its concentration in the blood serum.
Rifampicin, drugs that induce the CYP3A4 isoenzyme, increase the metabolism of Tarceva and decrease the level of the drug in plasma.
Medicines that cause changes in pH in the upper gastrointestinal tract may affect the solubility of the active ingredient in Tarceva and its degree of bioavailability.
Omeprazole, proton pump inhibitors, ranitidine, histamine receptor blockers reduce the maximum concentration of Tarceva.
Warfarin and other coumarin drugs increase the risk of bleeding.
Statins in combination with Tarceva increase the risk of myopathy.
Smoking during treatment with Tarceva reduces the exposure to the active ingredient by approximately 2 times.
Tarceva increases serum platinum concentrations, which should be taken into account when taking Carboplatin or Paclitaxel concomitantly.
Capecitabine increases plasma levels of the active ingredient Tarceva.
Storage conditions
Tarceva is stored in rooms with a temperature regime from +15 to +30°C, completely inaccessible to children.
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Shelf life
Tarceva can be stored for 3 years from the date of manufacture of the medication.
Attention!
To simplify the perception of information, this instruction for use of the drug "Tartseva" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.