Temsirolimus

DAE Class; Rx

Common Brand Names; Torisel

• Antineoplastics, mTOr Kinase Inhibitors

Inhibitor of mammalian target of rapamycin (mTOR)
Used for advanced renal cell cancer
Premedication with antihistamine is recommended due to risk of hypersensitivity / infusion reaction

Indicated for the treatment of advanced renal cell cancer.

For the treatment of heavily pretreated, relapsed or refractory mantle cell lymphoma (MCL). 

For the treatment of relapsed or refractory high-grade malignant glioma.

For the treatment of relapsed or refractory neuroblastoma in pediatric patients.

For the treatment of relapsed or refractory rhabdomyosarcoma.

For the treatment of recurrent glioblastoma multiforme.

Bilirubin > 1.5 times the upper limit of normal

>10%

Decreased hemoglobin (94%)

Hyperglycemia (89%)

Hypercholesterolemia (87%)

Hypertriglyceridemia (83%)

Increased alkaline phosphatase (68%)

Increased serum creatinine (57%)

Decreased lymphocyte count (53%)

Asthenia (51%)

Hypophosphatemia (49%)

Rash (47%)

Mucositis (41%)

Decreased platelet count (40%)

Increased AST/SGOT (38%)

Nausea (37%)

Edema (35%)

Leukopenia (32%)

Anorexia (32%)

Anemia (>30%)

Dyspnea (28%)

Pain (28%)

Hyperlipidemia (28%)

Diarrhea (27%)

Cough (26%)

Pyrexia (24%)

Abdominal pain (21%)

Decreased potassium levels (21%)

Back pain (20%)

Constipation (20%)

Dysguesia (20%)

Infections (20%)

Pruritus (19%)

Urinary tract infection (15%)

Vomiting (19%)

Weight loss (19%)

Decreased neutrophils (19%)

Arthralgia (18%)

Chest pain (16%)

Headache (15%)

Nail disorders (14%)

Epistaxis (12%)

Insomnia (12%))

Pharyngitis (12%)

Dry skin (11%)

1-10%

Rhinitis (10%)

Acne (10%)

Hypersensitivity reaction (9%)

Pneumonia (8%)

Increased total bilirubin (8%)

Interstitial lung disease (2%)

Bowel perforation (1%)

Chills

Depression

Myalgia

Post-marketing Reports

Pancreatitis

Cholecystitis

Cholelithiasis

May increase risks of hypersensitivity reactions; hyperglycemia; hyperlipidemia; intracerebral hemorrhage (CNS tumor and/or on anticoagulants)

To treat hypersensitivity reactions, stop therapy and treat with an antihistamine; therapy may be restarted at physician discretion at a slower rate

Monitor for symptoms or radiographic changes of interstitial lung disease (ILD); if ILD suspected, discontinue therapy, and consider use of corticosteroids and/or antibiotics

Infections may result from immunosuppression

Bowel perforation may occur; evaluate fever, abdominal pain, bloody stools, and/or acute abdomen promptly

Renal failure, sometimes fatal, has occurred; monitor renal function at baseline and while on therapy

Due to abnormal wound healing, use caution in perioperative period

Elderly patients may be more likely to experience certain adverse reactions, including diarrhea, edema and pneumonia

Monitor throughout the infusion and appropriate supportive care should be available; interrupt infusion in all patients with severe infusion reactions and administer medical therapy

Interstitial lung disease reported, some resulting in death; prescribing information recommends baseline radiographic assessment by lung CT or chest radiograph prior to initiation

Avoid pregnancy during and for 3 months post-treatment

Consider dose modification if used concurrently with CYP3A4 inhibitors or inducers

Proteinuria (including cases of nephrotic syndrome) has occurred; monitor urine protein prior to start of therapy and periodically thereafter; discontinue therapy in patients who develop nephrotic syndrome

Avoid grapefruit juice

May decrease effects of live vaccinations

Angioedema reported in patients taking mammalian target of rapamycin (mTOR) inhibitors in combination with ramipril and/or amlodipine; monitor patients for signs and symptoms of angioedema when temsirolimus is given concomitantly with an angiotensin converting enzyme (ACE) inhibitors (eg, ramipril) or calcium channel blockers (CCB; eg, amlodipine)

Pregnancy

Can cause fetal harm when administered to pregnant women based on animal studies and the mechanism of action

Lactation

Data are not available regarding the presence in human milk, the effects on breastfed infants, or the effects on milk production

Adults

25 mg IV once weekly.

Geriatric

25 mg IV once weekly.

Adolescents

Safety and efficacy have not been established.

Children

Safety and efficacy have not been established.

Temsirolimus