Information about Temsirolimus
Liver safety of Temsirolimus
Temsirolimus therapy is frequently associated with mild serum enzyme elevations, but has yet to be linked to instances of clinically apparent liver injury with jaundice.
Mechanism of action of Temsirolimus
Temsirolimus (tem" sir oh' li mus) is an ester of sirolimus, both of which bind to the same intracellular receptor as tacrolimus and cyclosporine, but which block the "mammalian target of rapamycin" (mTOR) rather than calcineurin. mTOR is a serine/threonine kinase which plays an important role in signaling pathways of several cytokines and growth factors, which are involved in carcinogenesis and cancer progression. Inhibition of mTOR causes a decrease in protein synthesis and cell cycle arrest. Temsirolimus therapy has been shown to inhibit progression and prolong survival in patients with advanced and metastatic renal cell cancer.
FDA approval information for Temsirolimus
Temsirolimus was approved for use in the United States in 2007 and current indications are limited to therapy of advanced renal cell cancer.
Dosage and administration for Temsirolimus
Temsirolimus is being actively investigated as therapy of other solid tumors. Temsirolimus is available as liquid solution for injection in vials of 25 mg/mL under the brand name of Torisel. The recommended dose is 25 mg intravenously once weekly until disease progression or unacceptable toxicity.
Side effects of Temsirolimus
Temsirolimus has many, largely dose dependent, side effects including hypersensitivity reactions, oral ulcers, diarrhea, nausea, poor appetite, fatigue, peripheral edema, rash, anemia and interstitial pneumonitis.