TEMSIROLIMUS

Other

Brand names: Temsirolimus

Intravenous

Mechanism of Action

12.1 Mechanism of Action Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor.

Indications

See full prescribing information

FDA Warnings

5 WARNINGS AND PRECAUTIONS Hypersensitivity/Infusion Reactions (including some life-threatening and rare fatal reactions) can occur early in the first infusion of Temsirolimus injection
7 ) Renal failure, sometimes fatal, has occurred
A benefit-risk assessment should be done prior to the continuation of temsirolimus therapy in patients with severe or life-threatening reactions
The overall frequency of ≥ grade 3 adverse reactions and deaths, including deaths due to progressive disease, were greater in patients with baseline bilirubin >1

Known Side Effects

7 documented side effects by frequency

Shortness of Breath

1-10%

Fatigue

1-10%

Diarrhea

1-10%

Nausea

1-10%

Fever

1-10%

Vomiting

1-10%

Rash

0.1-1%

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Formulations

Dosage Forms

Tablet

Route

Intravenous