Temsirolimus

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.

• 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.

• Temsirolimus injection is contraindicated in patients with bilirubin >1.5×ULN [see Warnings and Precautions ( 5.2 )]. Temsirolimus injection is contraindicated in patients with bilirubin > 1.5×ULN.contraindicated

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. ( 2.1 ) Antihistamine pre-treatment is recommended. ( 2.2 ) Dose reduction is required in patients with mild hepatic impairment. ( 2.4 ) 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. ( 2.5 ) 2.1 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. Treatment should continue until disease progression or unacceptable toxicity occurs. 2.2 Premedication Patients should receive prophylactic intravenous diphenhydramine 25 to 50 mg (or similar antihistamine) approximately 30 minutes before the start of each dose of Temsirolimus injection [see Warnings and Precautions ( 5.1 )] . 2.3 Dosage Interruption/Adjustment Temsirolimus injection should be held for absolute neutrophil count (ANC) <1,000/mm 3 , platelet count <75,000/mm 3 , or NCI CTCAE grade 3 or greater adverse reactions. Once toxicities have resolved to grade 2 or less, Temsirolimus injection may be restarted with the dose reduced by 5 mg/week to a dose no lower than 15 mg/week. 2.4 Dose Modification Guidelines Hepatic Impairment : Use caution when treating patients with hepatic impairment.

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. ( 5.1 ) To treat hypersensitivity reactions, stop Temsirolimus injection and treat with an antihistamine. Temsirolimus injection may be restarted at physician discretion at a slower rate. ( 5.1 ) 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. Monitor glucose and lipid profiles. ( 5.3 , 5.6 ) Infections may result from immunosuppression. ( 5.4 ) Monitor for symptoms or radiographic changes of interstitial lung disease (ILD). If ILD is suspected, discontinue Temsirolimus injection, and consider use of corticosteroids and/or antibiotics. ( 5.5 ) Bowel perforation may occur. Evaluate fever, abdominal pain, bloody stools, and/or acute abdomen promptly. ( 5.7 ) Renal failure, sometimes fatal, has occurred. Monitor renal function at baseline and while on Temsirolimus injection. ( 5.8 ) Due to abnormal wound healing, use Temsirolimus injection with caution in the perioperative period. ( 5.9 ) Proteinuria and nephrotic syndrome may occur. Monitor urine protein prior to the start of Temsirolimus injection therapy and periodically thereafter. Discontinue Temsirolimus injection in patients with who develop nephrotic syndrome. ( 5.11 ) Live vaccinations and close contact with those who received live vaccines should be avoided.

The following serious adverse reactions have been associated with Temsirolimus injection in clinical trials and are discussed in greater detail in other sections of the label [see Warnings and Precautions ( 5 )] . Hypersensitivity/Infusion Reactions [see Warnings and Precautions ( 5.1 )] Hepatic Impairment [see Warnings and Precautions ( 5.2 )] Hyperglycemia/Glucose Intolerance [see Warnings and Precautions ( 5.3 )] Infections [see Warnings and Precautions ( 5.4 )] Interstitial Lung Disease [see Warnings and Precautions ( 5.5 )] Hyperlipidemia [see Warnings and Precautions ( 5.6 )] Bowel Perforation [see Warnings and Precautions ( 5.7 )] Renal Failure [see Warnings and Precautions ( 5.8 )] Wound Healing Complications [see Warnings and Precautions ( 5.9 )] Intracerebral Hemorrhage [see Warnings and Precautions ( 5.10 )] The most common (≥ 30%) adverse reactions observed with Temsirolimus injection are rash, asthenia, mucositis, nausea, edema, and anorexia. The most common (≥30%) laboratory abnormalities observed with Temsirolimus injection are anemia, hyperglycemia, hyperlipidemia, hypertriglyceridemia, lymphopenia, elevated alkaline phosphatase, elevated serum creatinine, hypophosphatemia, thrombocytopenia, elevated AST, and leukopenia. The most common adverse reactions (incidence ≥ 30%) are rash, asthenia, mucositis, nausea, edema, and anorexia.

Lactation: Do not breastfeed. ( 8.2 ) 8.1 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 [see Clinical Pharmacology ( 12.1 )] . 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; however, these data are insufficient to inform a drug-associated risk of adverse developmental outcomes. In animal reproductive studies, oral daily administration of temsirolimus to pregnant rats and rabbits during organogenesis caused adverse embryo-fetal effects at approximately 0.04 and 0.12 times the AUC in patients at the recommended dose, respectively (see Data ) . Advise pregnant women of the potential hazard to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2–4% and 15–20%, respectively.

Metabolism

Absorption Following administration of a single 25 mg dose of Temsirolimus injection in patients with cancer, mean temsirolimus C max in whole blood was 585 ng/mL (coefficient of variation, CV =14%), and mean AUC in blood was 1627 ng•h/mL (CV=26%). Typically C max occurred at the end of infusion.

There is no specific treatment for Temsirolimus injection intravenous overdose. Temsirolimus injection has been administered to patients with cancer in phase 1 and 2 trials with repeated intravenous doses as high as 220 mg/m 2 . The risk of several serious adverse events, including thrombosis, bowel perforation, interstitial lung disease (ILD), seizure, and psychosis, is increased with doses of Temsirolimus injection greater than 25 mg.

• May 30, 2007NDANDA022088Pf Prism Cv
• Jul 30, 2018ANDAANDA203153Accord Hlthcare
• Aug 16, 2019ANDAANDA207383Gland

1. 1Disease Progression47911%
2. 2Death2876.4%
3. 3Dyspnoea2154.8%
4. 4Fatigue2064.6%
5. 5Pneumonia1904.2%
6. 6Diarrhoea1894.2%
7. 7Nausea1894.2%
8. 8Anaemia1874.2%
9. 9Pyrexia1794.0%
10. 10Vomiting1763.9%
11. 11Thrombocytopenia1643.6%
12. 12Dehydration1623.6%
13. 13Stomatitis1563.5%
14. 14Rash1433.2%
15. 15Renal Cell Carcinoma1363.0%

The 10 most recently updated of 1,017 ClinicalTrials.gov registrations naming Temsirolimus as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Immunotherapy in Combination With Prednisone and Sirolimus for Kidney Transplant Recipients With Unresectable or Metastatic Skin Cancer
  Recruiting · Phase 1 · Phase 2 · Interventional · 16 enrolled · National Cancer Institute (NCI)
  NCT05896839updated 2026-06-12
• EVERST- Everolimus After Alpelisib in Women With Hormone Receptor-positive (HR+) Metastatic Breast Cancer (MBC)
  Recruiting · Observational · 19 enrolled · Tel-Aviv Sourasky Medical Center
  NCT07646171updated 2026-06-12
• Everolimus Aging Study
  Active not recruiting · Phase 2 · Interventional · 106 enrolled · University of Wisconsin, Madison
  NCT05835999updated 2026-06-11
• VTP-1000 in Adults With Celiac Disease
  Recruiting · Early phase 1 · Interventional · 45 enrolled · Barinthus Biotherapeutics
  NCT06310291updated 2026-06-11
• Testing Lutetium Lu 177 Dotatate in Patients With Somatostatin Receptor Positive Advanced Bronchial Neuroendocrine Tumors
  Recruiting · Phase 2 · Interventional · 70 enrolled · National Cancer Institute (NCI)
  NCT04665739updated 2026-06-11
• 131I-apamistamab-based Conditioning for Hematopoietic Stem Cell Transplant (HSCT) in Advanced Sickle Cell Disease (SCD)
  Recruiting · Phase 1 · Interventional · 24 enrolled · Columbia University
  NCT07015684updated 2026-06-10
• Siplizumab for Sickle Cell Disease Transplant
  Terminated · Phase 1 · Phase 2 · Interventional · 1 enrolled · Columbia University
  NCT06078696updated 2026-06-10
• Rapamycin - Effects on Alzheimer's and Cognitive Health
  Active not recruiting · Phase 2 · Interventional · 40 enrolled · The University of Texas Health Science Center at San Antonio
  NCT04629495updated 2026-06-09
• Elacestrant With Everolimus for the Treatment of Recurrent Advanced or Metastatic ER-Positive Endometrial Cancer
  Not yet recruiting · Phase 2 · Interventional · 50 enrolled · Jonsson Comprehensive Cancer Center
  NCT07634601updated 2026-06-09
• Human Lysozyme Goat Milk for the Prevention of Graft Versus Host Disease in Patients With Blood Cancer Undergoing a Donor Stem Cell Transplant
  Active not recruiting · Phase 1 · Interventional · 52 enrolled · City of Hope Medical Center
  NCT04177004updated 2026-06-08

Frequently asked questions

How does Temsirolimus work?

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.

What is Temsirolimus used for?

According to FDA labeling, Temsirolimus carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Temsirolimus?

Temsirolimus is classified as Mammalian target of rapamycin (mTOR) kinase inhibitors, Kinase Inhibitor, mTOR Inhibitors, Protein Kinase Inhibitors, Cellular Proliferation Alteration.

What are the brand names for Temsirolimus?

Temsirolimus is marketed under brand names including Torisel.

What are the contraindications for Temsirolimus?

Temsirolimus labeling lists contraindications including: Temsirolimus injection is contraindicated in patients with bilirubin >1.5×ULN [see Warnings and Precautions ( 5.2 )]. Temsirolimus injection is contraindicated in patients with bilirubin > 1.5×ULN.. Always consult the full prescribing information and a clinician.