Temsirolimus

What is Temsirolimus?

• Temsirolimus (Torisel) is a kinase inhibitor used for the treatment of advanced renal cell carcinoma.

Temsirolimus

Temsirolimus2DACS

What are the uses of this medicine?

Temsirolimus (Torisel) is approved to treat:

• Renal cell carcinoma (a type of kidney cancer) that is advanced.

How does this medicine work?

• 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.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• bilirubin >1.5×ULN.

What drug interactions can this medicine cause?

Tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following:

• anticoagulants ('blood thinners') such as warfarin (Coumadin)
• certain antifungal medications such as itraconazole (Sporanox)
• ketoconazole (Nizoral)
• voriconazole (Vfen)
• clarithromycin (Biaxin)
• dexamethasone (Decadron)
• certain medications used to treat HIV/AIDS such as atazanavir (Reyataz), indinavir (Crixivan), nelfinavir (Viracept), nevirapine (Viramune), ritonavir (Norvir), and saquinavir (Invirase)
• certain medications for seizures such as carbamazepine (Equetro, Tegretol), phenobarbital (Luminal),and phenytoin (Dilantin, Phenytek)
• medications to lower cholesterol and lipids
• nefazodone
• rifabutin (Mycobutin)
• rifampin (Rifadin, Rifamate, Rifiter)
• selective serotonin re-uptake inhibitors such as citalopram (Celexa), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem), fluvoxamine (Luvox), paroxetine (Paxil), and sertraline (Zoloft)
• sirolimus (Rapamune, Rapamycin)
• sunitinib (Sutent)
• telithromycin (Ketek)
• tell your doctor what herbal products you are taking, especially St. John's Wort.

Is this medicine FDA approved?

• Temsirolimus was approved for use in the United States in 2007 and current indications are limited to therapy of advanced renal cell cancer.

How should this medicine be used?

• Patients should receive prophylactic intravenous diphenhydramine 25 to 50 mg (or similar antihistamine) approximately 30 minutes before the start of each dose of Torisel.

Recommended dosage:

• The recommended dose of Torisel is 25 mg administered as an intravenous infusion over a 30–60 minute period once a week.
• Treat until disease progression or unacceptable toxicity.
• Dose reduction is required in patients with mild hepatic impairment.

Administration:

• Temsirolimus comes as a solution (liquid) to be given by infusion.
• Torisel is administered as an intravenous infusion over a 30- to 60-minute period once weekly.
• It is usually given by a doctor or nurse in a doctor's office or infusion center.
• Temsirolimus is usually given once every week.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• Torisel injection, 25 mg/mL supplied with DILUENT for Torisel.

This medicine is available in fallowing brand namesː

• Torisel

What side effects can this medication cause?

The most common side effects of this medicine include:

• rash
• asthenia
• mucositis
• nausea
• edema
• anorexia

The most common laboratory abnormalities may include:

• anemia
• hyperglycemia
• hyperlipidemia
• hypertriglyceridemia
• elevated alkaline phosphatase
• elevated serum creatinine
• lymphopenia
• hypophosphatemia
• thrombocytopenia
• elevated AST
• leukopenia

What special precautions should I follow?

• Hypersensitivity/Infusion Reactions (including some life-threatening and rare fatal reactions) can occur early in the first infusion of Torisel. Patients should be monitored throughout the infusion. To treat hypersensitivity reactions, stop Torisel and treat with an antihistamine. Torisel may be restarted at physician discretion at a slower rate.
• Use caution when treating patients with mild hepatic impairment and reduce dose.
• Hyperglycemia and hyperlipidemia are likely and may require treatment. Monitor glucose and lipid profiles.
• The use of Torisel may result in immunosuppression. Patients should be carefully observed for the occurrence of infections, including opportunistic infections.
• Cases of interstitial lung disease, some resulting in death, occurred in patients who received Torisel. Monitor for symptoms or radiographic changes of interstitial lung disease (ILD). If ILD is suspected, discontinue Torisel, and consider use of corticosteroids and/or antibiotics.
• The use of Torisel is likely to result in increases in serum triglycerides and cholesterol. Serum cholesterol and triglycerides should be tested before and during treatment with Torisel.
• Cases of fatal bowel perforation occurred in patients who received Torisel. Patients should be advised to report promptly any new or worsening abdominal pain or blood in their stools.
• Renal failure, sometimes fatal, has occurred. Monitor renal function at baseline and while on Torisel
• Use of Torisel has been associated with abnormal wound healing. Therefore, caution should be exercised with the use of Torisel in the perioperative period.
• Proteinuria and nephrotic syndrome may occur. Monitor urine protein prior to the start of Torisel therapy and periodically thereafter. Discontinue Torisel in patients with who develop nephrotic syndrome.
• The combination of Torisel and sunitinib resulted in dose-limiting toxicity.
• The use of live vaccines and close contact with those who have received live vaccines should be avoided during treatment with Torisel.
• Based on findings in animal studies and its mechanism of action, Torisel can cause fetal harm when administered to a pregnant woman. Advise patients of the potential hazard to the fetus and to use effective contraception.
• Elderly patients may be more likely to experience certain adverse reactions, including diarrhea, edema and pneumonia.
• Advise lactating women not to breastfeed during treatment with Torisel and for 3 weeks after the last dose.
• 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.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• thrombosis
• bowel perforation
• interstitial lung disease (ILD)
• seizure
• psychosis

Treatment of overdosage: In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on findings in animal studies and its mechanism of action, temsirolimus can cause fetal harm when administered to a pregnant woman.
• Advise pregnant women of the potential hazard to a fetus.

Can this medicine be used in children?

• Limited data are available on the use of temsirolimus in pediatric patients.
• The effectiveness of temsirolimus in pediatric patients with advanced recurrent/refractory solid tumors has not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• TEMSIROLIMUS

Inactive ingredients:

• ANHYDROUS CITRIC ACID
• ALCOHOL
• PROPYLENE GLYCOL
• ALPHA.-TOCOPHEROL

Who manufactures and distributes this medicine?

• Wyeth Pharmaceuticals LLC, a subsidiary of Pfizer Inc.

What should I know about storage and disposal of this medication?

• Torisel must be stored at 2º–8º C (36º–46º F).
• Protect from light.
• Torisel is a cytotoxic drug.
• Follow applicable special handling and disposal procedures.

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• Dailymed label info on Temsirolimus
• FDA Temsirolimus