The Need for Anthracyclines Grows

The latest headline is daunting, with the World Health Organization’s International Agency for Research on Cancer announcing a 75 percent increase in cancer cases worldwide by 2030. Cancer to Increase 75 Percent by 2030This astounding prediction, published in Reuters on June 1, 2012 offered an unfortunate reality, based on data from GLOBOCAN. Causes are thought to be poor lifestyle choices worldwide, such as obesity and smoking. Statistics show that sub-Saharan Africa continues to show rising numbers of cancers linked to infections, particularly cervical cancer, liver cancer and Kaposi’s sarcoma. Wealthier countries like Britain and Australia are plagued with high rates of cancers associated with smoking, such as lung cancer. This foreboding data creates an urgent need for research and development of cancer treatments, such as the drugs in the anthracycline category.

Anthracyclines are anti-tumor antibiotics that disrupt DNA replication by interfering with enzymes. Classified as antineoplastic antibiotics, anthracyclines are produced by Streptomyces peucetius and coeruleorubidus. Initially isolated as red substances found from microorganisms in 1939, these chemotherapy drugs were not used for human treatment until the 1960’s, which is when the antitumor properties were discovered. Also indicated for the treatment of many childhood cancers, anthracyclines offer a double-edged sword in terms of treatment for patients. The good news is that this efficacious group of drugs has significantly increased survival rates. Unfortunately there is a risk of cardiotoxicity for patients who receive anthracyclines, and this risk is present for 10 to 15 years after treatment. However, with current knowledge regarding these potential adverse effects, comprehensive monitoring of patients can be done, with a special focus on the patient’s left ventricle in the heart. As anthracyclines are documented to possibly weaken the left ventricle, which is responsible for pumping oxygen-rich blood back into the body after exercise, patients should be informed of these risks and monitored effectively for up to two decades following treatment. There are several anthracyclines in both the antibiotic and antineoplastic classified groups, including Daunorubicin Hydrochloride, Doxorubicin Hydrochloride, Epirubicin Hydrochloride, Idarubicin Hydrochloride, Valrubicin, and Pirarubicin Hydrochloride.

  • Daunorubicin HydrochlorideDaunorubicin Hydrochloride, CAS# 23541-50-6, is an effectual treatment for ALL or acute lymphocytic leukemia. Daunorubicin works to prevent cell growth by preventing DNA replication, and has shown to be better suited for treating leukemia cells versus solid tumors. Administered intravenously, daunorubicin is an orange colored solution. Side effects that usually do not require medical attention include a darkening or redness of the skin and urine, due to the coloring of the solution. Other side effects may include nausea and vomiting, diarrhea and hair loss. Injections of 5 mg/ml are available, and Bedford Laboratories markets daunorubicin hydrochloride under the name daunorubicin. Recent clinical research indicates a possible novel use for daunorubicin as a potential therapeutic drug for the treatment of pulmonary hypertension.  Ruchika Nijhara, PhD, MBA, CLP at Georgetown University has published current research regarding this new use for anthracyclines, like daunorubicin, to treat pulmonary hypertension through the induction of cell death and suppression of pulmonary artery constriction. In combination with cardioprotectants, daunorubicin is being tested in animals to determine it’s healing effects for both blood pressure and hypertrophy.
  • Doxorubicin HydrochlorideDoxorubicin Hydrochloride, CAS# 25316-40-9, is administered as a chemotherapeutic agent. Doxorubicin is known as the brand name Adriamycin, which is marketed by Pharmacia, or as the brand name Rubex, which is marketed by Bristol-Myers Squibb. When used in combination with other chemotherapy drugs, the most commonly used dosage of doxorubicin is 40 to 60 mg/m2 via IV every 21 to 28 days. This is a standard dose for patients with several types of cancer including neuroblastoma, ovarian, Hodgkin’s disease, Wilms’ Tumor, Osteosarcoma and others. Side effects may include nausea, hair loss, indigestion, and fatigue.
  • Epirubicin HydrochlorideEpirubicin Hydrochloride, CAS# 56390-09-1, is also known as the brand Ellence, which is manufactured by Pfizer. As an anticancer drug derived from a specific strain of bacteria, epirubicin is a formidable opponent against a wide range of cancer types. Data published in the January 2008 Journal of Cancer Institute documented results from eight randomized clinical trials, which compared epirubicin and other anticancer agents in the market today. The Journal of Cancer Institute stated their support for the use of epirubicin over the use of other anticancer drugs not in the anthracycline category. Possible side effects include mouth sores, nausea and vomiting.
  • Idarubicin HydrochlorideIdarubicin Hydrochloride, CAS# 57852-57-0 is also recognized as the brand name Idamycin, which is marketed by Pfizer.  As a sterile lyophilized powder for reconstitution and intravenous administration, idarubicin, CAS# 57852-57-0, is available in a 20 mg single use only vial. Patients suffering from acute myeloid leukemia, or AML, benefit greatly from treatment with idarubicin. Adverse effects are similar to other anthracyclines, but specifically include a possibility of dermatologic effects and rashes.
  • ValrubicinValrubicin, CAS# 56124-62-0, is used to treat bladder cancer. Known as the brand Valstar, marketed by Endo Pharmaceuticals Solutions Inc., valrubicin can be found in doses of 40 mg/ ml. Side effects include bladder irritation, an increased frequency in urination, painful urination, urinary incontinence and urinary tract infections.
  • Pirarubicin HydrochloridePirarubicin Hydrochloride, CAS# 72496-41-4, is known by it’s brand names in countries other then the United States, like Théprubicine, marketed by Sanofi-Aventis in France and Pinorubin, marketed by Mercian Coperation in Japan. Therarubicin is indicated only for the treatment of metastatic breast cancer in France.  Pirarubicin should be used as an IV infusion only, and the typical dose for breast cancer is 50 mg/m2 every 21 or 28 days. Adverse effects may include tachycardia and arrhythmia.
  • Aclarubicin HydrochlorideAclarubicin Hydrochloride, CAS# 75443-99-1, has been marketed under the names Aclacin, Aclacinomycine, Aclacinon, Aclaplastin, and Jaclacin. Aclarubicin Hydrochloride is produced from the Soil bacteria Streptomyces galilaeus. It belongs to the 2nd generation of anthracyclines, and is antagonistic to other agents that inhibit topoisomerase II, like amsacrine, teniposide and etoposide. This product differs from doxorubicin and daunorubicin in its structure, mechanisms of action and toxicity profile, and it is less cardiotoxic. Aclarubicin Hydrochloride has been used as an effective therapy in patients with metastatic cancers with minor side effects reported.  Recently there has been research conducted on its positive effects on patients with lung cancers, and elderly patients with acute myelomonocytic leukaemia (AMMoL).
  • AmrubicinAmrubicin, CAS# 110267-81-7, is also known as the brand Calsed that is manufactured by Sumitomo Pharmaceuticals. Amrubicin is a 3rd-generation synthetic anthracycline analogue, and is a potent topoisomerase II inhibitor. It has shown promising activity in Small Cell Lung Cancer (SCLC). In a recent study, patients were given amrubicin as a second-line therapy. Results of the study showed a significantly improved response rate and longer, progression-free survival than patients treated with topotecan. This promising drug is being studied further as a single agent and in combination with anti-cancer therapies for a variety of solid tumors, including lung and breast cancers.
  • ZorubicinZorubicin, CAS# 54083-22-6, is a semisynthetic derivative of daunorubicin, similar to doxorubicin, and is an aminoglycoside anti-tumor drug used to treat various types of cancers with high toxicity. It is produced by Streptomyces peucetius and inhibits the progression of the enzyme topoisomerase II. Zorubicin is injected via IV and is usually given once every 21–28 days.

LGM Pharma provides complete technical and regulatory support for research and development projects. The above products are top quality API products available from LGM Pharma, along with assistance for the entire R&D process. Anthracyclines are expected to be not only clinically necessary products, but also drugs to aid in the future onslaught of cancer cases worldwide.


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