Arglabine (Lyophilisate) Instructions for Use

ATC Code

L01X (Other antineoplastic drugs)

Clinical-Pharmacological Group

Radiosensitizing drug

Pharmacotherapeutic Group

Antineoplastic agent

Pharmacological Action

Arglabin is a biologically active sesquiterpene lactone isolated from the smooth wormwood Artemisia glabella.

It possesses antineoplastic and radiosensitizing action. Being an inhibitor of farnesyl transferase, the drug prevents the attachment of a farnesyl group to cellular proteins, which leads to disruption of the prenylation of the product of the Ras oncogene.

The defarnesylation of the Ras oncogene leads to apoptosis of the tumor cell, inhibits the growth of tumor cells by interrupting the mitotic signal for cell division, and simultaneously reduces the influence of factors that adversely affect the immune system, which leads to normalization of the body’s immune status.

Arglabin has a radiosensitizing effect, significantly increasing the frequency of objective tumor regressions and the frequency of pronounced therapeutic pathomorphosis of III-IV degree both in the primary tumor and in metastatically altered lymph nodes.

Pharmacokinetics

With intravenous administration of the drug, the maximum peak concentrations in the blood, amounting to 31.6±0.6 µg/ml, are established immediately after its administration.

Distribution of the drug through tissues and organs during the first two hours after administration is due to the high value of the rate constant. After the second hour of drug administration, the distribution rate slows down by 25 times.

The drug is capable of accumulating in most body tissues, passes into the interstitial fluid and enters the body’s cells. During the distribution of the drug in tissues, the transition from blood to tissues occurs at a rate 3.75 times greater than the reverse process of exit from tissues, which confirms the fact of drug deposition in tissues.

Metabolic elimination and biodegradation of the drug is due to the destruction of the lactone ring. In percentage terms of the entire administered dose, up to 27-32% is metabolized in tissues, the remaining amount is excreted unchanged.

Indications

• As a radiosensitizing agent during radiation and chemoradiation therapy for cancer of the breast, liver, lungs, and ovaries.

ICD codes

Dosage Regimen

Lyophilisate

For the purpose of radiosensitization against the background of radiation or chemoradiation therapy Arglabin is administered 15 minutes before the radiation therapy session every other day at a dose of 5 mg/kg, intravenously as a bolus in the form of a 2% solution, for a total of 15 administrations.

Before administration, the required calculated dose of Arglabine is diluted in 0.9% sodium chloride solution to a concentration of 20 mg/1 ml.

Adverse Reactions

A bitter taste in the mouth and dizziness during drug administration are possible, which stop on their own within the next 5-10 minutes.

Contraindications

• Pregnancy and the period of breastfeeding;
• Cachexia;
• Hypersensitivity to wormwood.

Use in Pregnancy and Lactation

The use of the drug is contraindicated during pregnancy and breastfeeding.

Special Precautions

Influence on the ability to drive vehicles and mechanisms

During the treatment period, caution must be exercised when driving motor vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

When using high doses (600-800 mg), a burning sensation in the oral cavity, nausea, and skin itching may appear, which disappear after reducing the drug dose.

Drug Interactions

Arglabin potentiates the effect of standard antineoplastic chemotherapeutic drugs (fluorouracil, cyclophosphamide, methotrexate).

Storage Conditions

In a place protected from light, at a temperature from -5°C (23°F) to 0°C (32°F). Keep out of reach of children.

Shelf Life

Shelf life – 2 years.

Dispensing Status

By prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.