INSTRUCTION
FOR MEDICAL USE OF THE DRUG
RADACHLORIN®
Registration number: LP-№(000291)-(RG-RU)
Trade name: Radachlorin®
International Nonproprietary Name (INN): Sum of sodium salts of chlorin e6, chlorin p6, purpurin 5
Dosage form: Concentrate for solution preparation for infusion
Trade name: Radachlorin®
International Nonproprietary Name (INN): Sum of sodium salts of chlorin e6, chlorin p6, purpurin 5
Dosage form: Concentrate for solution preparation for infusion
Composition:
100 ml of concentrate contains:
Active ingredient:
Radachlorin® – 5 g
(sum of sodium salts of chlorin e6, chlorin p6, purpurin 5 – 0.35 g)
Excipients:
Meglumine – 0.2 g
Water for injection – up to 100 ml
Description:
A dark green solution with a yellowish tint and a faint characteristic odor.
Pharmacotherapeutic group: Photosensitizing agent.
ATC code: L01XD
Pharmacological Properties
Pharmacodynamics
Radachlorin® is a second-generation photosensitizer intended for fluorescent diagnostics (FD) and photodynamic therapy (PDT) of malignant tumors.
The PDT method is based on the ability of Radachlorin® to selectively accumulate in tumors after intravenous administration and generate singlet oxygen under light exposure, exerting a toxic effect on tumor cells and modifying their plasma membranes when exposed to light at a wavelength corresponding to one of the absorption peaks of the drug (402, 502, 532, 608, or 662 nm).
The development of the therapeutic effect after PDT with Radachlorin® occurs in three stages:
• Stage 1: A characteristic light response during PDT, manifested by edema and hyperemia of the irradiated area of varying severity.
• Stage 2: Tumor necrosis, forming 2-4 days after PDT.
• Stage 3: Necrotic mass rejection and epithelialization of the wound defect within 2-8 weeks, depending on tumor size.
Radachlorin® at doses of 0.5-2.4 mg/kg, when the tumor is irradiated with laser light 3 hours after drug administration, is non-mutagenic and does not damage the DNA of normal cells.
Pharmacokinetics
After a single intravenous administration of Radachlorin® at doses of 0.5-2.4 mg/kg, the drug distributes between the blood and tissues within 0.5-5 hours. The serum concentration peaks 15-30 minutes after administration and rapidly decreases, measuring 10 µg/L one hour after administration, 5 µg/L after 3 hours, and 1 µg/L after 24 hours (at a dose of 0.5 mg/kg).
Tumor concentrations peak within 1 hour (10-20 µg/mL). However, due to faster elimination from surrounding healthy tissues, the highest therapeutic index (contrast index) is observed 3 hours after administration. Tumor tissue concentrations exceed those in healthy tissues by 3-6 times on average, depending on tumor morphology, ranging from 2 to 10 µg/mL.
Rapid elimination of Radachlorin® from the blood, skin, and mucous membranes, along with a high contrast index, prevents damage to healthy organs and tissues and minimizes skin photosensitivity to daylight.
The highest levels of Radachlorin® are observed in the liver, kidneys, and tumor tissue 3 hours after administration. About 70-80% of Radachlorin® is metabolized in the liver to biladienes (linear tetrapyrroles, also products of heme metabolism). The drug is excreted unchanged in feces (15%) and urine (3%).
Cumulative excretion over 12 hours averages 15-20% of the administered dose. Approximately 98% is eliminated or metabolized within 48 hours. Trace amounts can persist in the skin for up to 6 days.
Indications for Use
• Fluorescent diagnostics of skin cancer.
• Photodynamic therapy for superficial skin tumors (excluding melanoma).
• Photodynamic therapy for precancerous (dysplasia grades I-III, erosion) and cancerous (carcinoma in situ) cervical lesions.
Contraindications
Hypersensitivity to any drug component.
Pregnancy and breastfeeding
Age under 18 (no clinical data for children).
Caution
Use with caution in patients with hypertension or diabetes.
Dosage and Administration
The drug is administered as a single intravenous infusion over 30 minutes. Light exposure at 662 ± 3 nm begins 3 hours after infusion. The optimal regimen is 1.0-1.2 mg/kg and light exposure of 300 J/cm² at 662 ± 3 nm.
For partial response or stabilization, repeat therapy can use 0.5-0.6 mg/kg – 300 J/cm² or 1.0-1.2 mg/kg – 200 J/cm², tailored to tumor characteristics.
Light is applied using a quartz fiber laser for surface irradiation with or without microlenses for skin tumors, or macrolenses (spot diameter 2.5-3 cm) for cervical lesions. Diode lasers emitting at 662 ± 3 nm are used.
Preparation for Infusion
The required dose is diluted in 200 ml of one of the following solutions:
• 0.9% sodium chloride
• 5% or 10% dextrose
• 10% mannitol
• Ringer’s solution
• 4% or 8% potassium chloride
Do not use acidic infusion solutions.
Precautions
• During laser exposure, both doctor and patient must wear protective glasses.
• Patients should avoid bright light for one week post-infusion.
Side effects
• Local pain at the irradiation site during and up to 1 hour after PDT.
• Swelling lasting 2-7 days.
• Rarely, skin itching and leukocytosis.
Storage
Store at 2-8°C, protected from light. Avoid freezing. Keep out of reach of children.
Shelf life
2.5 years. Do not use after expiration.
Prescription only.
Manufacturer:
1 Federal State Budgetary Institution “National Medical Research Center of Cardiology” of the Ministry of Health of Russia, 121552, Moscow, 3rd Cherepkovskaya St., 15A, buildings 24, 25, 48
2 LLC “COMPANY “DEKO”, legal address: 129344, Moscow, Eniseyskaya St., 3, building 4
Production address: 171130, Tver Region, Vyshnevolotsk Urban District, Zelenogorsky Settlement, Sovetskaya St., 6a.
Marketing Authorization Holder/Consumer Claims Address:
LLC “RADA-PHARMA”, 109316, Moscow, Volgogradsky Prospect, 42, building 5, tel. +7 (495) 980-13-05.
100 ml of concentrate contains:
Active ingredient:
Radachlorin® – 5 g
(sum of sodium salts of chlorin e6, chlorin p6, purpurin 5 – 0.35 g)
Excipients:
Meglumine – 0.2 g
Water for injection – up to 100 ml
Description:
A dark green solution with a yellowish tint and a faint characteristic odor.
Pharmacotherapeutic group: Photosensitizing agent.
ATC code: L01XD
Pharmacological Properties
Pharmacodynamics
Radachlorin® is a second-generation photosensitizer intended for fluorescent diagnostics (FD) and photodynamic therapy (PDT) of malignant tumors.
The PDT method is based on the ability of Radachlorin® to selectively accumulate in tumors after intravenous administration and generate singlet oxygen under light exposure, exerting a toxic effect on tumor cells and modifying their plasma membranes when exposed to light at a wavelength corresponding to one of the absorption peaks of the drug (402, 502, 532, 608, or 662 nm).
The development of the therapeutic effect after PDT with Radachlorin® occurs in three stages:
• Stage 1: A characteristic light response during PDT, manifested by edema and hyperemia of the irradiated area of varying severity.
• Stage 2: Tumor necrosis, forming 2-4 days after PDT.
• Stage 3: Necrotic mass rejection and epithelialization of the wound defect within 2-8 weeks, depending on tumor size.
Radachlorin® at doses of 0.5-2.4 mg/kg, when the tumor is irradiated with laser light 3 hours after drug administration, is non-mutagenic and does not damage the DNA of normal cells.
Pharmacokinetics
After a single intravenous administration of Radachlorin® at doses of 0.5-2.4 mg/kg, the drug distributes between the blood and tissues within 0.5-5 hours. The serum concentration peaks 15-30 minutes after administration and rapidly decreases, measuring 10 µg/L one hour after administration, 5 µg/L after 3 hours, and 1 µg/L after 24 hours (at a dose of 0.5 mg/kg).
Tumor concentrations peak within 1 hour (10-20 µg/mL). However, due to faster elimination from surrounding healthy tissues, the highest therapeutic index (contrast index) is observed 3 hours after administration. Tumor tissue concentrations exceed those in healthy tissues by 3-6 times on average, depending on tumor morphology, ranging from 2 to 10 µg/mL.
Rapid elimination of Radachlorin® from the blood, skin, and mucous membranes, along with a high contrast index, prevents damage to healthy organs and tissues and minimizes skin photosensitivity to daylight.
The highest levels of Radachlorin® are observed in the liver, kidneys, and tumor tissue 3 hours after administration. About 70-80% of Radachlorin® is metabolized in the liver to biladienes (linear tetrapyrroles, also products of heme metabolism). The drug is excreted unchanged in feces (15%) and urine (3%).
Cumulative excretion over 12 hours averages 15-20% of the administered dose. Approximately 98% is eliminated or metabolized within 48 hours. Trace amounts can persist in the skin for up to 6 days.
Indications for Use
• Fluorescent diagnostics of skin cancer.
• Photodynamic therapy for superficial skin tumors (excluding melanoma).
• Photodynamic therapy for precancerous (dysplasia grades I-III, erosion) and cancerous (carcinoma in situ) cervical lesions.
Contraindications
Hypersensitivity to any drug component.
Pregnancy and breastfeeding
Age under 18 (no clinical data for children).
Caution
Use with caution in patients with hypertension or diabetes.
Dosage and Administration
The drug is administered as a single intravenous infusion over 30 minutes. Light exposure at 662 ± 3 nm begins 3 hours after infusion. The optimal regimen is 1.0-1.2 mg/kg and light exposure of 300 J/cm² at 662 ± 3 nm.
For partial response or stabilization, repeat therapy can use 0.5-0.6 mg/kg – 300 J/cm² or 1.0-1.2 mg/kg – 200 J/cm², tailored to tumor characteristics.
Light is applied using a quartz fiber laser for surface irradiation with or without microlenses for skin tumors, or macrolenses (spot diameter 2.5-3 cm) for cervical lesions. Diode lasers emitting at 662 ± 3 nm are used.
Preparation for Infusion
The required dose is diluted in 200 ml of one of the following solutions:
• 0.9% sodium chloride
• 5% or 10% dextrose
• 10% mannitol
• Ringer’s solution
• 4% or 8% potassium chloride
Do not use acidic infusion solutions.
Precautions
• During laser exposure, both doctor and patient must wear protective glasses.
• Patients should avoid bright light for one week post-infusion.
Side effects
• Local pain at the irradiation site during and up to 1 hour after PDT.
• Swelling lasting 2-7 days.
• Rarely, skin itching and leukocytosis.
Storage
Store at 2-8°C, protected from light. Avoid freezing. Keep out of reach of children.
Shelf life
2.5 years. Do not use after expiration.
Prescription only.
Manufacturer:
1 Federal State Budgetary Institution “National Medical Research Center of Cardiology” of the Ministry of Health of Russia, 121552, Moscow, 3rd Cherepkovskaya St., 15A, buildings 24, 25, 48
2 LLC “COMPANY “DEKO”, legal address: 129344, Moscow, Eniseyskaya St., 3, building 4
Production address: 171130, Tver Region, Vyshnevolotsk Urban District, Zelenogorsky Settlement, Sovetskaya St., 6a.
Marketing Authorization Holder/Consumer Claims Address:
LLC “RADA-PHARMA”, 109316, Moscow, Volgogradsky Prospect, 42, building 5, tel. +7 (495) 980-13-05.
Contacts
+7 (495) 980-13-05
office@radapharma.ru
office@radapharma.ru