Temsirolimus


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Advanced renal cell carcinoma
Adult: 25 mg once a week via infusion over 30-60 minutes. Continue until disease progression or unacceptable toxicity. Treatment interruption and/or dose reduction may be required if toxicity occurs. Premedication with antihistamine is recommended to prevent hypersensitivity reactions.

Intravenous
Mantle cell lymphoma
Adult: Relapsed or refractory type: 175 mg once a week for 3 weeks, then 75 mg once a week thereafter, given via infusion over 30-60 minutes. Treatment interruption and/or dose reduction may be required if absolute neutrophil count (ANC) falls below 1,000 cells/mm3 and platelet count is below 50,000 cells/mm3. Restart treatment with reduced dose as follows: if last dose is 175 mg, reduce to 75 mg; if last dose is 75 mg, reduce to 50 mg; if last dose is 50 mg, reduce to 25 mg. If neutrophil and platelet counts are not maintained at or above these levels on the new dose, treatment should be withheld and the next lower dose given once the counts have recovered. Premedication with antihistamine is recommended to prevent hypersensitivity reactions.
Special Patient Group
Advanced renal cell carcinoma:
Patients taking strong CYP3A4 inhibitors: 12.5 mg once a week. If concomitant strong CYP3A4 inhibitor is discontinued, allow at least 1 week to elapse before increasing to the dose used prior to initiation of CYP3A4 inhibitor.
Patients taking strong CYP3A4 inducers: 50 mg once a week. If concomitant strong CYP3A4 inducer is discontinued, reduce to the dose used prior to initiation of CYP3A4 inducer.
Hepatic Impairment
Advanced renal cell carcinoma: Mild (bilirubin >1-1.5 x ULN or AST >ULN with bilirubin ≤ULN): Reduce dose to 15 mg once a week. Moderate to severe (bilirubin >1.5 x ULN): Contraindicated.

Mantle cell lymphoma:
Moderate to severe: Contraindicated.
Hướng dẫn pha thuốc
Add 1.8 mL of provided diluent to prepare a concentration of 10 mg/mL. Withdraw the required dose and further dilute in 250 mL of NaCl 0.9% solution.
Chống chỉ định
Hypersensitivity to temsirolimus and sirolimus. Moderate to severe hepatic impairment. Pregnancy and lactation. Concomitant administration of live vaccines.
Thận trọng
Patient with diabetes, hyperlipidaemia, CNS metastases/tumour, risk factors for skin cancer. Patients taking strong CYP3A4 inhibitors or inducers. Perioperative period. Mild hepatic and severe renal impairment.
Phản ứng phụ
Significant: Hyperglycaemia, anaemia, neutropenia, thrombocytopenia, impaired wound healing, cataracts, increased cholesterol and triglycerides.
Blood and lymphatic system disorders: Leucopenia, lymphopenia.
Eye disorders: Conjunctivitis.
Gastrointestinal disorders: Abdominal distension or pain, constipation, diarrhoeoa, nausea, vomiting, stomatitis, gastritis, gastrointestinal haemorrhage, dysphagia, gingivitis.
General disorders and administration site conditions: Asthenia, fatigue, pain, pyrexia, chills, oedema.
Infections and infestations: Bacterial and viral infections.
Investigations: Increased creatinine, AST/ALT.
Metabolism and nutrition disorders: Decreased appetite, dehydration, diabetes mellitus, hypokalaemia, hypocalcaemia, hypophosphataemia.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia, back pain.
Nervous system disorders: Headache, dizziness, paraesthesia, dysgeusia, ageusia.
Psychiatric disorders: Insomnia, anxiety, depression, somnolence.
Renal and urinary disorders: Candidiasis, UTI.
Respiratory, thoracic and mediastinal disorders: Pharyngitis, rhinitis, sinusitis, epistaxis, cough.
Skin and subcutaneous tissue disorders: Folliculitis, rash, dermatitis, acne, nail disorder, ecchymosis, petechiae, pruritus.
Vascular disorders: Hypertension, thrombophlebitis, venous thromboembolism.
Potentially Fatal: Hypersensitivity/infusion reactions (including anaphylaxis, chest pain, dyspnoea, flushing), bowel perforation, opportunistic infections (e.g. Pneumocystis jiroveci pneumonia) or sepsis, interstitial lung disease, intracerebral bleeding, acute renal failure.
IV/Parenteral: D
Thông tin tư vấn bệnh nhân
Avoid exposure to sunlight or UV light.
MonitoringParameters
Monitor CBC with differential and platelets weekly; serum glucose, cholesterol and triglycerides, renal and hepatic functions at baseline and during treatment; symptoms or radiographic changes of interstitial lung disease.
Tương tác
Decreased exposure with CYP3A4 inducers (e.g. rifampicin, carbamazepine, phenytoin). Increased exposure with CYP3A4 inhibitors (e.g. clarithromycin, ritonavir, ketoconazole). May increase the risk of intracerebral bleeding when given with anticoagulants. Concomitant use with sunitinib may result in dose-limiting toxicities. Increased risk of angioneurotic oedema with ACE inhibitors or Ca channel blockers.
Potentially Fatal: May diminish the therapeutic effect of live vaccines.
Food Interaction
Increased plasma levels with grapefruit and grapefruit juice. Decreased plasma levels with St John’s wort.
Tác dụng
Description: Temsirolimus is an inhibitor of mammalian target of rapamycin (mTOR) kinase, a protein which controls cell division. It binds to the intracellular protein FKBP-12 to form a complex that inhibits the activation of mTOR, thus inhibiting angiogenesis and tumour cell proliferation, growth and survival.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: At end of infusion (temsirolimus); 0.5-2 hours after infusion (sirolimus).
Metabolism: Metabolised by CYP3A4 to sirolimus (major active metabolite) and 4 minor metabolites.
Excretion: Mainly via faeces (78%); via urine (approx 5%). Elimination half-life: Approx 17 hours (temsirolimus); approx 55 hours (sirolimus).
Đặc tính

Chemical Structure Image
Temsirolimus

Source: National Center for Biotechnology Information. PubChem Database. Temsirolimus, CID=6918289, https://pubchem.ncbi.nlm.nih.gov/compound/Temsirolimus (accessed on Jan. 23, 2020)

Bảo quản
Store between 2-8°C. Protect from light. Do not freeze.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
Phân loại MIMS
Phân loại ATC
L01XE09 - temsirolimus ; Belongs to the class of protein kinase inhibitors, other antineoplastic agents. Used in the treatment of cancer.
References
Anon. Temsirolimus. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/04/2018.

Anon. Temsirolimus. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/04/2018.

Buckingham R (ed). Temsirolimus. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2018.

Joint Formulary Committee. Temsirolimus. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2018.

Torisel (Wyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/04/2018.

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