• Advanced renal cell carcinoma.

Contraindicated in:

• OB: Pregnancy (may cause fetal harm)
• Lactation: Lactation.

Use Cautiously in:

• Hypersensitivity to temsirolimus, sirolimus or polysorbate 80
• Perioperative patients (may impair wound healing)
• Rep: Women of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children
• Geri: ↑ risk for adverse reactions in older adults (especially diarrhea, edema, and pneumonia).

CV: edema, hypertension, venous thromboembolism.

Derm: rash, abnormal wound healing.

EENT: conjunctivitis.

Endo: hyperglycemia.

F and E: edema, hypophosphatemia.

GI: ↑ liver enzymes, anorexia, diarrhea, mucositis, nausea, BOWEL PERFORATION .

GU: nephrotic syndrome, proteinuria, RENAL FAILURE.

Hemat: anemia, leukopenia, lymphopenia, thrombocytopenia.

Metab: hyperlipidemia, hypertriglyceridemia.

Neuro: weakness.

Resp: INTERSTITIAL LUNG DISEASE.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), INFECTION.

Drug-Drug:

• Concurrent use of strong CYP3A4 inhibitors, including ketoconazole, itraconazole, voriconazole, clarithromycin, atazanavir, nelfinavir, ritonavir, ↑ levels and risk of toxicity; avoid concurrent use; if need to use CYP3A4 inhibitor, consider ↓ dose of temsirolimus.
• Concurrent use of strong strong CYP3A4 inducers , including dexamethasone, phenytoin, phenobarbital, carbamazepine, rifampin or rifabutin may ↓ levels and effectiveness; avoid concurrent use; if need to use CYP3A4 inducer, consider ↑ dose of temsirolimus.
• Concurrent use with sunitinib↑ risk of toxicity (rash, gout, cellulitis).
• May ↓ antibody response to and ↑ risk of adverse reactions from live virus vaccines; avoid current use.
• ↑ risk of angioedema when used with ACE inhibitors or calcium channel blockers.

Drug-Natural Products:

• St. John's wort may ↓ blood levels; avoid concurrent use.

Drug-Food:

• Grapefruit juice may ↑ blood levels and ↑ risk of toxicity.

(Generic available)

• Solution for injection: 25 mg/mL (comes with a diluent containing polysorbate 80, polyethylene glycol 400 and dehydrated alcohol);

• IV (Adults): 25 mg once weekly. Concurrent use of strong CYP3A4 inhibitor: 12.5 mg once weekly. Concurrent use of strong CYP3A4 inducer: 50 mg once weekly.

Torisel

• Binds to an intracellular protein. The resultant complex inhibits an enzyme, mTOR (mammalian target of rapamycin). Inhibition of this enzyme arrests cell growth in the G1 phase.

• Decreased spread of renal cell carcinoma.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: enzyme inhibitors, kinase inhibitors

Absorption: IV administration results in complete bioavailability.

Distribution: Temsirolimus and sirolimus partition extensively in formed blood elements.

Metabolism/Excretion: Mostly metabolized by the liver to sirolimus, an active metabolite Primarily eliminated in feces.

Half-life: Temsirolimus: 17.3 hr; sirolimus: 54.6 hr.

• Explain purpose of temsirolimus to patient.
• Advise patient to notify health care professional immediately if any new or worsening abdominal pain or blood in stools occur or if signs of bowel perforation (fever, abdominal pain, metabolic acidosis, bloody stools, diarrhea), or signs and symptoms of hypersensitivity reactions or infection occur.
• Advise patient to avoid drinking grapefruit juice while taking temsirolimus.
• Advise patients to notify health care professional if excessive thirst or volume or frequency of urination and diabetic patients to closely monitor glucose.
• Inform patient of the increased risk for intracerebral bleeding with temsirolimus.
• Advise patient to consult health care professional prior to taking any Rx, OTC, or herbal products, especially St. John's Wort.
• Instruct patient not to receive any vaccinations without advice of health care professional and to avoid contact with persons who have received live vaccines during therapy.
• Rep: May be teratogenic. Advise female patients of reproductive potential and male patient with partners of reproductive potential to use effective contraception during and for 3 mo after last dose of therapy. Advise females to avoid breastfeeding during and for 3 wks after last dose. May cause male and female infertility.

tem-si-RO-li-mus

NDC Code^*

• 0008- Wyeth Pharmaceuticals LLC, a subsidiary of Pfizer Inc.
  • 0008-1179- Torisel
    • 0008-1179-01- 1 KIT in 1 CARTON (0008-1179-01) * 1.8 mL in 1 VIAL, SINGLE-USE (0008-1125-01) * 25 mL in 1 VIAL, SINGLE-USE (0008-1279-01)

• 16729- Accord Healthcare Inc.
  • 16729-223- Temsirolimus
    • 16729-223-61- 1 KIT in 1 KIT (16729-223-61) * 1.8 mL in 1 VIAL, SINGLE-DOSE (16729-222-30) * 1 mL in 1 VIAL, SINGLE-DOSE (16729-221-30)