Tesetaxel: Novel Oral Targeted Tubulin Inhibitor
Tesetaxel is an investigational anticancer agent undergoing testing to evaluate its safety and efficacy in various forms of cancer. Studies are currently underway to examine the potential role of tesetaxel in a variety of clinical indications.
Tesetaxel is a novel oral semi-synthetic taxane and is the leading taxane in clinical development. Taxanes, such as paclitaxel (Taxol®) and docetaxel (Taxotere®), are mainstays of modern anticancer therapy. These drugs are believed to kill cancer cells by disrupting critical proteins that maintain the structure of cancer cells. More recent research suggests that they may also disrupt the blood supply to malignant tumors (i.e., an “antiangiogenic” effect).
Certain taxanes have been approved by FDA for the treatment of breast, lung, ovarian, gastric, and prostate cancers. However, all currently approved taxanes require intravenous (IV) infusion under close medical supervision due to a high level of toxicity. Both paclitaxel and docetaxel can cause severe, occasionally fatal, infusion reactions, which require pre-medication with steroids and antihistamines. Other serious reactions associated with taxanes include long-lasting damage to peripheral nerves (neuropathy).
With tesetaxel, Genta hopes to provide patients with an oral taxane that retains the broad anticancer activity of the IV drugs, while providing substantially improved safety. Tesetaxel is administered orally which obviates the risk of taxane-related infusion reactions and the need for associated premedications. Oral dosing provides a high level of convenience for patients, physicians and nurses, and increases dosing flexibility.
The safety and efficacy of tesetaxel have not been established for any use.
