Temsirolimus

What it is and how it works

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.

Indications

Temsirolimus injection is indicated for the treatment of advanced renal cell carcinoma. Temsirolimus injection is a kinase inhibitor indicated for the treatment of advanced renal cell carcinoma.

Dosage and administration (summary)

The recommended dose of Temsirolimus injection is 25 mg administered as an intravenous infusion over a 30-60 minute period once a week. Treat until disease progression or unacceptable toxicity. Antihistamine pre-treatment is recommended. Dose reduction is required in patients with mild hepatic impairment. Temsirolimus injection vial contents must first be diluted with the enclosed diluent before diluting the resultant solution with 250 mL of 0.9% Sodium Chloride Injection. Advanced Renal Cell Carcinoma The recommended dose of Temsirolimus injection for advanced renal cell carcinoma is 25 mg administered as an intravenous infusion over a 30 – 60 minute period once a week.

Contraindications

Temsirolimus injection is contraindicated in patients with bilirubin >1.5×ULN . Temsirolimus injection is contraindicated in patients with bilirubin > 1.5×ULN.

Warnings and precautions

Hypersensitivity/Infusion Reactions (including some life-threatening and rare fatal reactions) can occur early in the first infusion of Temsirolimus injection. Patients should be monitored throughout the infusion. To treat hypersensitivity reactions, stop Temsirolimus injection and treat with an antihistamine. Temsirolimus injection may be restarted at physician discretion at a slower rate. Hepatic Impairment: Use caution when treating patients with mild hepatic impairment and reduce dose. ( 2.4 , 5.2 ) Hyperglycemia and hyperlipidemia are likely and may require treatment.

Pregnancy

Pregnancy Risk Summary Based on findings in animal studies and its mechanism of action, temsirolimus can cause fetal harm when administered to a pregnant woman . Although there are no data on the use of Temsirolimus injection in pregnant women, there are limited data on the use of sirolimus, the active metabolite of temsirolimus, during pregnancy.

Storage and supply

Temsirolimus injection Kit contains one vial of Temsirolimus injection and one vial of DILUENT which includes a deliverable volume of 1.8 mL and is supplied as follows: Presentation NDC Strength Description Temsirolimus injection Kit 65219-200-05 25 mg/mL per vial Temsirolimus injection 25 mg/mL is a “clear, colorless to light yellow viscous soluti…

Source: Temsirolimus (Temsirolimus) — US FDA prescribing information, 2020-03-30, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.