Herceptin

Herceptin contains the active component trastuzumab, which is capable of interacting with the cutaneous growth factor type 2 terminal apparatus, suppressing the proliferation of tumor cells with HER2 overexpression and weakening the process of HER2 overexpression.

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

Indications Herceptin

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

Release form

The drug is released in the form of powder for the manufacture of infusion fluid: inside vials of 0.15 g (1 vial inside a pack), as well as 0.44 g (inside a box - 1 vial of powder and 1 vial of solvent with a volume of 20 ml).

Pharmacodynamics

Trastuzumab is a recombinant DNA derivative of humanized monoclonal antibodies that selectively interact with the extracellular domain of the human herpes simplex receptor 2 (HER2). These antibodies are IgG1, including human regions (heavy chain constant regions), and also determine the complementarity of the mouse regions of the p185 HER2 antibody to HER2. [ 2 ]

The trastuzumab element prevents the proliferation of tumor cells with the development of HER2 overexpression in both in vivo and in vitro processes. 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 administration of the drug in the form of short-term 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 is 28-38 days, so the excretion period after discontinuation of Herceptin is up to 27 weeks (190 days and 5 half-lives).

A common form of gastric carcinoma.

At high drug levels, systemic clearance is largely linear and the half-life is approximately 26 days.

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

Dosing and administration

Herceptin can only be prescribed after testing for HER2 tumor expression.

The medicine is administered through a dropper. During the preparation of the liquid, the container must not be shaken vigorously (only rocked). If foam appears, the bag with the medicine must be left for 5 minutes.

The therapeutic regimen must be selected exclusively individually, taking into account the phase of the pathology and the characteristics of its progression, the patient’s condition, his weight, height, age, etc., in accordance with the treatment regimens described in the literature.

During the administration of the drug and for 6 hours after the first infusion, as well as 2 hours after further procedures (only in hospital), the patient's condition is constantly monitored in order to promptly respond to the development of negative signs. If they appear, the infusion should be suspended and resumed only after the elimination of negative symptoms and restoration of body functions. Therapy should be completely discontinued if life-threatening signs develop.

• Application for children

The medication should not be used in children under 18 years of age, as its therapeutic efficacy and safety have not been studied.

Use Herceptin during pregnancy

It is prohibited to prescribe Herceptin during breastfeeding and pregnancy. After the end of therapy, a woman of fertile age must 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

Contraindicated in cases of severe intolerance to trastuzumab, as well as in cases of severe dyspnea associated with lung metastases, or in cases of dyspnea in the phase requiring oxygen therapy.

It should be used with caution in cases of angina pectoris, myocardial insufficiency and elevated blood pressure, or in cases where treatment with karyotoxic drugs was carried out before using the drug.

Side effects Herceptin

Side effects may be observed, including exacerbation/development of infections (pneumonia, herpes, flu, lesions of the bladder and epidermis). Growth of tumors (benign and malignant) is possible. Manifestations associated with the pancreas, kidneys, liver, cardiovascular system, nervous system and hematopoietic system may also be observed.

It is possible that signs of allergy associated with the respiratory system (tracheitis or bronchitis) and epidermis (urticaria or itching), as well as anaphylaxis, Quincke's edema and cardiogenic shock may develop.

Interactions with other drugs

The drug is not compatible with 5% dextrose, as it may provoke protein aggregation.

Herceptin must not be mixed or diluted in combination with other medications.

Storage conditions

Herceptin should be stored in a place out of reach of children. Temperature indicators are within the range of 2-8°C.

Shelf life

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

Analogues

The drug's analogues include Vectibex, MabThera with Avastin, Gazyva and Arzerra with Mabcampat, as well as Erbitux and Trastumab.