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Lomustine Capsules

Function and Efficacy

This product is a non-specific drug for the cell cycle. It is most sensitive to cells at the G2-S boundary or in the early S phase, and also has an inhibitory effect on the G2 phase. Animal experiments have shown that its mechanism is similar to that of BCNU. After entering the human body, its molecule breaks into two parts from the carbamide bond: one is the chloroethylamine part, which dissociates chlorine to form ethylene carbon cations, exerts a hydrocarbonization effect, causing DNA chain breaks, RNA and proteins to be hydrocarbonized, which are mainly related to anti-tumor effects; the other is the carbamyl part that becomes isocyanate, or is converted into carbamic acid to exert a carbamylation effect, which mainly reacts with proteins, especially with the terminal amino group of lysine. It is believed that this is mainly related to bone marrow toxicity. Carbamylation can also destroy some enzyme proteins, making it more difficult to repair DNA after being damaged by hydrocarbonization, which helps anti-cancer effects. Although this product has an alkylating agent effect, it has no cross-resistance with general alkylating agents, vincristine, methyl procarbazine and anti-metabolism drugs. Tests on mice and rabbits have shown that this drug is carcinogenic.

Ingredients

Main ingredient: Lomustine. Molecular formula: C9H16ClN3O2 Molecular weight: 233.7

Name Description Content CAS NO. Manufacturer
LomustineIngredients

This product is a non-specific drug for the cell cycle. It is most sensitive to cells at the G2-S boundary or in the early S phase, and also has an inhibitory effect on the G2 phase. Its molecule breaks into two parts from the carbamide bond: one is the chloroethylamine part, which dissociates chlorine to form ethylene carbon cations, exerts a hydrocarbonization effect, causes DNA chain breakage, and RNA and proteins are hydrocarbonized, which are mainly related to anti-tumor effects; the other is the carbamyl part that becomes isocyanate, or is converted into carbamic acid to exert a carbamylation effect, mainly reacting with proteins, especially with the terminal amino group of lysine. This is mainly related to bone marrow toxicity, and can also destroy some enzyme proteins, making it more difficult to repair DNA after being damaged by hydrocarbonization, which helps anti-cancer effects. Although this product has an alkylating agent effect, it has no cross-resistance with general alkylating agents, nor with vincristine, methyl procarbazine and antimetabolites. Tests on mice and rabbits have shown that the drug is carcinogenic.

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13010-47-4 4

Appearance

This product is in the form of capsules.

Indication

This product is highly lipid-soluble and can pass through the blood-brain barrier and enter the cerebrospinal fluid. It is often used for primary brain tumors (such as glioblastoma) and secondary tumors; for the treatment of solid tumors, such as combination therapy for gastric cancer, colorectal cancer, bronchial lung cancer, malignant lymphoma, etc.

Usage and Dosage

100-130 mg/m2, taken at once, once every 6-8 weeks, 3 times as a course of treatment.

Adverse Reactions

Nausea and vomiting may occur within 6 hours after oral administration and may last for 2 to 3 days. Pre-treatment with sedatives or metoclopramide and taking the drug on an empty stomach can alleviate the symptoms. A small number of patients experience gastrointestinal bleeding and liver damage. Bone marrow suppression: thrombocytopenia can be seen 3 to 5 weeks after taking the drug. White blood cell reduction can occur twice, in the first and fourth weeks after taking the drug, and will not recover until the sixth to eighth week. However, bone marrow suppression is cumulative. Occasionally, systemic rash may occur, which may cause teratogenesis and may also suppress testicular or ovarian function, causing amenorrhea or azoospermia.

Precautions

It is contraindicated for patients with liver damage, white blood cell count below 4x109/L, and platelet count below 80x109/L. If there is concurrent infection, the infection should be treated first.

Special Population Medication

Precautions for children: 100-130mg/m2, taken at once, repeated every 6-8 weeks. Precautions for pregnancy and lactation: This drug has carcinogenic and teratogenic effects, so it is contraindicated for pregnant and lactating women. Precautions for the elderly: This experiment has not been conducted and there is no reliable reference literature.

Drug Interactions

When this product is used in combination chemotherapy, anticancer drugs that can severely reduce leukocytes and platelets should be avoided.

Storage

Sealed storage

Packaging Specification

40mg

Validity Period

24 months

Manufacturer

ZHONGFU Pharmaceutical Co., Ltd.

  • Founded in:

    2000-04-22
  • Address:

    No. 2709, Yuwang North Street, Hanting District, Weifang City, Shandong Province
  • Tax NO.:

    913707037232674976
  • Registered Funds:

    78.364 million yuan
  • Website:

  • Email:

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