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Levofolinate Calcium: A Comprehensive Review of its Research and Development

Updated: Jul 18, 2023

Levofolinate Calcium is a chemotherapy drug used to treat various types of cancer. It has been the subject of extensive research and development, and in this article, we will explore the history, mechanism of action, clinical trials, and future prospects of Levofolinate Calcium.

History of Levofolinate Calcium

Levofolinate Calcium is a derivative of folic acid, which was first isolated in 1941. The discovery of folic acid led to the development of methotrexate, a chemotherapy drug that inhibits the metabolism of folic acid. Levofolinate Calcium was developed as a more potent inhibitor of folic acid metabolism.

Mechanism of Action

Levofolinate Calcium is a folate analogue that competes with folic acid for binding to the enzyme dihydrofolate reductase (DHFR). By inhibiting DHFR, Levofolinate Calcium prevents the synthesis of thymidylate, an essential component of DNA. This leads to DNA damage and cell death, which is particularly effective against rapidly dividing cancer cells.

Clinical Trials

Numerous clinical trials have been conducted to test the efficacy and safety of Levofolinate Calcium. In a phase III trial, Levofolinate Calcium was compared to 5-fluorouracil (5-FU) in the treatment of colorectal cancer. The trial showed that Levofolinate Calcium was non-inferior to 5-FU in terms of overall survival and progression-free survival.

In another phase III trial, Levofolinate Calcium was combined with oxaliplatin and 5-FU in the treatment of advanced colorectal cancer. The trial showed that the combination therapy significantly improved overall survival, progression-free survival, and response rates compared to 5-FU alone.

Future Prospects

Levofolinate Calcium continues to be studied for its potential in treating various types of cancer. One area of research is the combination of Levofolinate Calcium with other chemotherapy drugs, such as oxaliplatin and irinotecan. Another area of research is the use of Levofolinate Calcium in combination with targeted therapy, such as anti-EGFR and anti-VEGF agents.


In conclusion, Levofolinate Calcium is a chemotherapy drug that has been extensively studied for its efficacy and safety in the treatment of various types of cancer. Its mechanism of action is based on inhibiting folic acid metabolism, which leads to DNA damage and cell death. Clinical trials have shown that Levofolinate Calcium is effective in the treatment of colorectal cancer, both alone and in combination with other chemotherapy drugs. Future research will focus on combining Levofolinate Calcium with targeted therapy to improve its efficacy and reduce its side effects.


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