Doxorubicin Hydrochloride 25316-40-9

��发布时间：2025-03-27 ��浏览次数：388次

 Chemical Name: Doxorubicin Hydrochloride

CAS Number: 25316-40-9

Molecular Formula: C27H30ClNO11

Molecular Weight: 579.98 g/mol

Appearance: Orange-red crystalline powder

Solubility: Easily soluble in water and saline solution, insoluble in most organic solvents

Storage Conditions: Store at low temperatures (2-8°C), away from light, in a sealed container

 

What is Doxorubicin Hydrochloride?

Doxorubicin Hydrochloride (Doxorubicin) is an anthracycline antibiotic chemotherapy drug extracted from the bacterium Streptomyces peucetius and chemically modified. It is a broad-spectrum anti-tumor drug widely used in the treatment of various solid tumors and hematological malignancies, including breast cancer, lung cancer, stomach cancer, leukemia, and lymphoma. Doxorubicin inhibits cancer cell proliferation by interfering with DNA synthesis and replication and induces apoptosis, making it especially effective against highly proliferative tumors.

 

Mechanism of Action of Doxorubicin Hydrochloride

DNA Intercalation: Doxorubicin inserts itself into the DNA double helix, preventing DNA replication and transcription, thereby inhibiting cancer cell growth.

Topoisomerase II Inhibition: This enzyme is responsible for DNA unwinding during replication. Doxorubicin inhibits this enzyme, causing DNA breaks, which prevents cells from completing division, ultimately leading to apoptosis.

Generation of Oxygen Free Radicals: The drug generates reactive oxygen species (ROS) through oxidative stress, damaging cell membranes, proteins, and DNA structures, accelerating cancer cell death.

 

Main Uses of Doxorubicin Hydrochloride

Treatment of Various Malignant Tumors 

Doxorubicin is a broad-spectrum anti-cancer drug used to treat the following cancers:

Hematological tumors: Acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML), Hodgkin lymphoma, and non-Hodgkin lymphoma.

Breast cancer: Often used in HER2-positive breast cancer patients, especially for advanced or metastatic breast cancer.

Lung cancer: Including small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC).

Stomach and pancreatic cancers: Used in combination with other chemotherapy drugs to improve treatment efficacy.

Ovarian cancer, endometrial cancer, and bladder cancer: As first-line or adjuvant therapy.

 

Combination with Other Chemotherapy Drugs 

Doxorubicin is often combined with other chemotherapy drugs, such as:

CHOP regimen (for lymphoma treatment): Cyclophosphamide + Doxorubicin + Vincristine + Prednisone.

AC regimen (for breast cancer): Doxorubicin + Cyclophosphamide.

 

Consolidation Therapy Post-Chemotherapy 

For high-risk relapsed patients, Doxorubicin can be used as a consolidation therapy drug to reduce the survival of cancer cells and improve long-term survival rates.

 

Side Effects of Doxorubicin Hydrochloride

Despite its strong anti-tumor effects, Doxorubicin may cause severe side effects, including:

Cardiotoxicity (most severe side effect): Long-term use can lead to myocardial damage and congestive heart failure (CHF), so cumulative doses must be strictly controlled (generally not exceeding 450-550 mg/m²). Dexrazoxane can be used to reduce cardiotoxicity.

Bone marrow suppression (causing leukopenia and immune suppression): Can cause leukopenia, anemia, and thrombocytopenia, increasing infection risk.

Gastrointestinal reactions: Nausea, vomiting, diarrhea, and oral mucositis (mouth ulcers), affecting the patient's quality of life.

Hair loss: Due to the impact on rapidly dividing cells, hair loss is a common side effect, but it usually regrows after treatment.

Skin and vein inflammation: Extravasation of the drug can lead to skin ulceration and tissue necrosis, so intravenous administration should strictly avoid extravasation.

 

How to Reduce Doxorubicin's Side Effects?

Cardiac Protection: Use Dexrazoxane to reduce cardiotoxicity.

Reduce Bone Marrow Suppression: Administer granulocyte colony-stimulating factor (G-CSF) to reduce the risk of leukopenia.

Relieve Gastrointestinal Discomfort: Use antiemetics (such as Ondansetron and Metoclopramide).

Monitor Doses: Avoid cumulative doses exceeding 550 mg/m² to reduce long-term heart damage risks.

 

Applications of Doxorubicin Hydrochloride

Clinical Oncology Treatment: Standard chemotherapy regimen for both solid and hematological cancers.

Targeted Drug Development: As a core component of some nanomedicines or antibody-drug conjugates (ADC) to improve efficacy and reduce toxicity.

Experimental Research: Used in studies on cytotoxicity, DNA replication inhibition, and tumor resistance mechanisms.

 

Summary

Doxorubicin Hydrochloride is a broad-spectrum anti-cancer drug widely used in the treatment of various malignancies such as breast cancer, leukemia, lymphoma, lung cancer, and stomach cancer. Its primary mechanism of action includes DNA intercalation, topoisomerase II inhibition, and the generation of free radicals, which prevent cancer cell proliferation and induce apoptosis.

However, its cardiotoxicity is a major limiting factor, requiring strict dose control and potential use of cardiac protective agents (Dexrazoxane). Doxorubicin is often used in combination with other chemotherapy drugs to enhance anti-cancer effects while minimizing side effects.