Herceptin

Herceptin contains the active component trastuzumab, which is able to interact with the terminal apparatus of type 2 cutaneous growth factor, suppress the multiplication of tumor cells with overexpression of the HER2 type and weaken the process of HER2 overexpression.

Trastuzumab is also capable of exhibiting selective cytotoxicity against tumor cells. In addition, it should be noted that it is precisely the overexpression of HER2 that is considered the main cause of most cases of the development of breast carcinoma and the common form of gastric cancer. [1]

Indications Herceptin

It is used for the treatment of oncological diseases (as a monopreparation and in combination with other oncological substances), including metastatic breast carcinoma (against the background of HER2 overexpression by tumor cells), early stages of breast carcinoma (with overexpression), as well as adenocarcinoma affecting the esophageal-gastric tract and stomach (with the development of HER2 overexpression).

Release form

The release of the medication is realized in the form of a powder for the manufacture of infusion liquid: inside 0.15 g bottles (1 bottle inside a pack), as well as 0.44 g (inside the box - 1 powder bottle and 1 20 ml solvent bottle).

Pharmacodynamics

Trastuzumab is a recombinant DNA derivative of monoclonal humanized antibodies that selectively interacts with the extracellular domain of the endings of type 2 cutaneous growth factor (HER2). These antibodies are IgG1 comprising the human regions (heavy chain constant regions), as well as determining the complementarity of the murine regions of the HER2 antibody p185 in relation to HER2. [2]

The element trastuzumab prevents the multiplication of tumor cells with the development of HER2 overexpression during in vivo and in vitro processes. In in vitro tests, the antibody-dependent cytotoxicity of trastuzumab cells mainly affects tumor cells with the development of HER2 overexpression. [3]

Pharmacokinetics

Breast carcinoma.

After the introduction of drugs in the form of short intravenous infusions in portions of 0.01, 0.05, as well as 0.1, 0.25, 0.5 g once a week, the pharmacokinetic parameters were nonlinear. Increasing the dosage led to a decrease in drug clearance.

The half-life term is 28-38 days, therefore the excretion period after the cessation of the use of Herceptin is up to 27 weeks (190 days and 5 half-life terms).

A common form of gastric carcinoma.

With high drug rates, the systemic clearance is generally linear, and the half-life is approximately 26 days.

The median of the expected AUC values (equilibrium level over 3 weeks) is 1213 mg / L per day, the median of the equilibrium Cmax is 132 mg / L, and the median of the Cmin is 27.6 mg / L.

Dosing and administration

Prescribing Herceptin is only allowed after a HER2 tumor expression test has been performed.

The medication is administered through a dropper. During the manufacture of the liquid, the container must not be vigorously shaken (only shake it). When foam appears, leave the medicine bag for 5 minutes.

It is necessary to select a therapeutic regimen exclusively personally, taking into account the phase of the pathology and the peculiarities of its course, the patient's condition, his weight, height, age, etc., in accordance with the treatment regimens described in the literature.

During the process of administering the drug and for 6 hours after the 1st infusion, as well as 2 hours after further procedures (only at the hospital), constant monitoring of the patient's condition is performed in order to respond in a timely manner to the development of negative signs. When they appear, it is necessary to suspend the infusion, which is resumed only after the elimination of negative symptoms and the restoration of body functions. It is necessary to discontinue therapy completely if life-threatening signs develop.

• Application for children

You can not use the medication in children under the age of 18, since its therapeutic efficacy and safety have not been studied.

Use Herceptin during pregnancy

It is forbidden to prescribe Herceptin for HB and pregnancy. After the end of therapy, a woman who is at a fertile age needs to use reliable contraception for another six months, since the drug can provoke fatal pulmonary and renal hypoplasia in the fetus, as well as oligohydramnios.

Contraindications

It is contraindicated to prescribe with severe intolerance to trastuzumab, and in addition, with severe dyspnea associated with lung metastases, or with dyspnea in a phase requiring oxygen therapy.

It is used with caution in case of angina pectoris, myocardial insufficiency and increased blood pressure, or in cases when treatment with the introduction of karyotoxic drugs was carried out before the use of drugs.

Side effects Herceptin

Side symptoms may occur, including exacerbation / development of infections (pneumonia, herpes, flu, urea and epidermal lesions). The growth of tumors (benign and malignant) is possible. There may also be manifestations associated with the pancreas, kidneys, liver, CVS, NS and the hematopoietic system.

Signs of allergy associated with the respiratory system (tracheitis or bronchitis) and the epidermis (urticaria or itching) may develop, as well as anaphylaxis, angioedema and cardiogenic shock.

Interactions with other drugs

The drug is not compatible with 5% dextrose, as this can provoke protein aggregation.

Herceptin must not be mixed or dissolved in combination with other medicines.

Storage conditions

Herceptin must be kept out of the reach of children. Temperature indicators are within 2-8 ° С.

Shelf life

Herceptin can be used for 36 months from the date of manufacture of the medicinal product. The finished solution, when stored under aseptic conditions, has a shelf life of 1 month.

Analogs

Analogs of the medication are Vektibeks, Mabthera with Avastin, Gazyva and Arzerra with Mabkampat, as well as Erbitux and Trastumab.