Tarceva

The category of antineoplastic agents is Tarceva - an antitumor drug, a representative of tyrosine kinase inhibitors.

Indications of the tarcevs

The main indications for the appointment of Tarceva are as follows:

• Supportive treatment of localized or metastatic non-small cell lung cancer, if there is no increase in the development of the disease after 4 chemotherapy courses.
• Cancerous tumors in the lungs, localized or metastatic spread, if one or more chemotherapy courses did not have the expected effect.
• Localized or metastatic inoperable cancer in the pancreas (as a first-line drug, in combination with Gemcitabine).

[1]

Release form

Tarceva is produced in tablet form, with a protective shell coating. The active ingredient is the antitumor substance erlotinib.

The tablets are rounded, with smooth edges, covered with a film of a light-yellowish hue. 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 pack of cardboard contains three blister plates and a paper instruction.

[2]

Pharmacodynamics

Tarceva on the basis of erlotinib is the strongest drug that inhibits tyrosine kinase of EGF receptors (epidermal growth factor of a person).

The tyrosine kinase is responsible for the internal processes of the phosphorylation of EGF, which are expressed on top of healthy and tumor cell structures. The inhibition of phosphotyrosine activity of the growth factor inhibits the development of cancer cells and / or causes their death. 

[3], [4], [5]

Pharmacokinetics

The active component of Tarcev is well absorbed after oral administration. The limiting content in the serum is observed after four hours. Biological availability in a healthy person is estimated at 59%. The presence of food masses in the stomach can increase the bioavailability of the drug.

The limiting content in the serum is 1.995 ng / ml. Concentration equilibrium is observed after 7-8 days. Before using the subsequent dose of Tarcev, the minimum level of the active ingredient in the serum is 1.238 ng / ml.

In samples of cancer tissues after 9 days of treatment, the level of the active ingredient is found to average 1.158 ng / g. This is about 63% of the limit level in the serum in a state of equilibrium. After 60 minutes after taking Tarcev, the limiting content of the drug in the plasma can reach 73%. Binding to plasma proteins is 95%.

Metabolism of Tarceva 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 hours. Metabolism products and unchanged drug residues are excreted mainly with calves (more than 90%), and to a lesser extent - through the kidneys.

The combined treatment of Tarceva and Gemcitabine has no effect on the clearance of the substance erlotinib in the serum.

[6], [7], [8], [9], [10], [11]

Use of the tarcevs during pregnancy

The possibility of treating Tarceva with pregnant women was insufficiently investigated. Preclinical testing of the toxic effect of the drug in standard dosages indicated the presence of embryotoxicity.

Given the above, it is not recommended to use Tarceva for the therapy of pregnant patients. Women of childbearing age before starting therapy should exclude the presence of pregnancy, and also use reliable methods of contraception.

The possibility of Tarceva medicament treatment during breastfeeding has not been investigated, therefore it is not recommended to use this type of drug.

Contraindications

Tarcev's treatment should be avoided in such situations:

• with severe liver and kidney damage;
• with gestation and lactation;
• in pediatrics;
• with a tendency to allergies to Tarceva.

 Relative contraindications are:

• smoking patient;
• intolerance to galactose, insufficiency of lactase;
• peptic ulcer;
• simultaneous chemotherapy with taxanes.

[12]

Side effects of the tarcevs

Most often, specialists detect such side effects when taking Tarceva's medication:

• diarrhea, nausea, oral ulcers, abdominal pain, bloating, bleeding in the digestive tract (up to the perforation);
• emaciation;
• development of hepatic insufficiency;
• conjunctivitis, corneal ulcers (sometimes with perforations), keratitis;
• cough, shortness of breath, bleeding of the nasal mucosa;
• skin rashes, baldness, deterioration of skin and nails, changes in pigmentation;
• pain in the head, neuropathy;
• depressive conditions;
• sensation of fatigue, attachment of infection (pneumonia, phlegmon, septic complications).

[13], [14], [15]

Dosing and administration

Take Tarceva orally, once a day, 60 minutes before a meal, or two hours after a meal.

• When a non-small cell cancer process in the lungs, 150 mg of Tarceva per day is recommended.
• When the cancer process in the pancreas is recommended to take 100 mg of Tarceva per day, for a long time, in conjunction with Gemcitabine.

[16], [17]

Overdose

With oral administration of a single dose of Tartz to 1600 mg, no special effects were observed.

When taking higher doses, the following symptoms may occur:

• severe diarrhea;
• skin rash;
• an increase in the level of hepatic transaminases.

With a possible overdose Tarceva abolished, in exchange prescribe treatment with symptomatic medicines.

[18], [19]

Interactions with other drugs

Ketoconazole, Ciprofloxacin affect the metabolism of Tarceva and increase its concentration in serum.

Rifampicin, inductors of the isoenzyme CYP3A4 increase the metabolism of Tarceva and lower the level of the drug in the plasma.

Medications that cause a change in pH in the upper segment of the digestive tract can affect the solubility of the active ingredient Tarceva and the degree of its bioavailability.

Omeprazole, proton pump inhibitor drugs, ranitidine, histamine receptor blocking drugs lower the level of the limiting concentration of the drug Tarceva.

Warfarin and other coumarin preparations increase the risk of bleeding.

Statins combined with Tarceva increase the risk of myopathy.

Smoking during treatment Tarceva reduces the exposure of the active ingredient by about 2 times.

Tarceva increases the concentration of platinum in the blood serum, which should be taken into account when taking carboplatin or Paclitaxel.

Capecitabine increases the plasma content of the active ingredient Tarceva.

[20], [21], [22]

Storage conditions

Keep Tarceva in rooms with a temperature regime of +15 to +30 ° C, in the total inaccessibility of children.

[23], [24], [25]

Shelf life

Tarceva can be stored for 3 years from the moment of production of the medicament.

[26], [27]