Sunitinib


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Metastatic renal cell carcinoma, Unresectable, metastatic malignant gastrointestinal stromal tumours
Adult: 50 mg once daily for 4 wk followed by a 2-wk rest period to comprise a complete 6-wk cycle. May be adjusted in increments or decrements of 12.5 mg based on individual tolerability. Min: 25 mg daily. Max: 75 mg daily.

Oral
Malignant tumour of endocrine pancreas, advanced
Adult: 37.5 mg once daily, given continuously. May be adjusted in increments or decrements of 12.5 mg, based on individual tolerability. Max: 50 mg daily.
Special Patient Group
Patients taking strong CYP3A4 inhibitors:
Unresectable, metastatic malignant gastrointestinal stromal tumours; Metastatic renal cell carcinoma: Reduce dose to a Min of 37.5 mg daily.
Advanced pancreatic neuroendocrine tumour Reduce dose to a Min of 25 mg daily.

Patients taking CYP3A4 inducers:
Unresectable, metastatic malignant gastrointestinal stromal tumours; Metastatic renal cell carcinoma: May increase in increments of 12.5 mg to a max of 87.5 mg daily.
Advanced pancreatic neuroendocrine tumour: May increase in increments of 12.5 mg to a max of 62.5 mg daily.
Hepatic Impairment
Severe: (Child-Pugh class C): Contraindicated.
Cách dùng
May be taken with or without food.
Chống chỉ định
Hypersensitivity to sunitinib. Severe hepatic (Child-Pugh class C) impairment. Lactation.
Thận trọng
Patients w/ history of CV events (e.g. heart failure, cardiomyopathy, MI, myocardial ischaemia); history of QT interval prolongation; bradycardia, electrolyte imbalance, thyroid dysfunction, underlying or poorly controlled HTN. Patient undergoing major surgery. Hepatic and renal impairment. Pregnancy. Concomitant use w/ potent CYP3A4 enzyme inhibitors and inducers should be avoided, if not possible, consider dosage adjustment.
Phản ứng phụ
Significant: QT prolongation, torsade de pointes, HTN, thyroid dysfunction (e.g. hypo- and hyperthyroidism, thyroiditis), hypoglycaemia, osteonecrosis of the jaw (ONJ), hepatobiliary disorder (e.g. acalculous cholecystitis, emphysematous cholecystitis), adrenal toxicity, hand-foot skin reaction, impaired wound healing or bleeding.
Nervous: Fatigue, asthenia, dizziness, paraesthesia, headache.
CV: Decreased LVEF, peripheral oedema.
GI: GI disturbance, nausea, vomiting, abdominal pain, dyspepsia, diarrhoea, anorexia, taste disturbance, stomatitis, oral mucositis, mouth irritation, pain, or dryness.
Resp: Dyspnoea, cough.
Hepatic: Increased ALT, AST, alkaline phosphatase, and bilirubin.
Genitourinary: Chromaturia, increased creatinine.
Endocrine: Increased amylase and lipase.
Haematologic: Neutropenia, thrombocytopenia, lymphopenia, anaemia.
Musculoskeletal: Arthralgia, myalgia, back and extremity pain.
Dermatologic: Yellow skin discolouration, skin and hair depigmentation, alopecia, dryness, rash, exfoliative dermatitis.
Immunologic: Myelosuppresion.
Others: Electrolyte disturbance (e.g. hypokalemia, hypernatremia), fever.
Potentially Fatal: Heart failure, cardiomyopathy, MI, myocardial ischaemia, tumour lysis syndrome (TLS), thrombotic microangiopathy (i.e. thrombocytopenic purpura, haemolytic uremic syndrome), proteinuria, renal failure, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, haemorrhagic events (e.g. epistaxis, hemoptysis/pulmonary haemorrhage, tumour haemorrhage), infection (e.g. resp infection, UTI, sepsis). Rarely, hepatic failure, GI perforation, pulmonary embolism, pancreatitis, nephrotic syndrome, necrotizing fasciitis, reversible posterior leukoencephalopathy syndrome (RPLS).
MonitoringParameters
Monitor LVEF, BP, ECG, adrenal function, CBC w/ differential and platelet, LFTs (prior to and during each cycle of treatment), blood glucose levels, urinalysis, serum chemistries (e.g. Mg, phosphate, K); signs/symptoms of hypoglycaemia, hypothyroidism, hyperthyroidism, or thyroiditis.
Quá liều
Symptoms: Impaired muscle coordination, head shakes, hypoactivity, piloerection, ocular discharge, GI distress. Management: General supportive treatment. Emesis or gastric lavage may be considered to eliminate unabsorbed drug.
Tương tác
Increased plasma concentration w/ potent CYP3A4 enzyme inhibitors (e.g. ketoconazole, erythromycin, ritonavir). Decreased plasma concentration w/ potent CYP3A4 enzyme inducers (e.g. rifampicin, dexamethasone, phenytoin, phenobarbital, carbamazepine).
Food Interaction
Increased plasma concentration w/ grapefruit juice. Decrease plasma concentration w/ St John’s wort.
Tác dụng
Description: Sunitinib inhibits signal transduction pathways involving multiple receptor tyrosine kinases which are implicated in tumour growth, pathologic angiogenesis and metastatic progression of cancer, including platelet-derived growth factor receptors (i.e. PDGFR-α, PDGFR-β), vascular endothelial growth factor receptors (i.e. VEGFR-1, VEGFR-2, VEGFR-3), stem cell factor receptor (i.e. c-Kit), fms-like tyrosine kinase-3 (Flt-3), colony-stimulating factor receptor type 1 (CSF-1R), and the glial cell-line-derived neurotrophic factor receptor (RET).
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 6-12 hr.
Distribution: Volume of distribution: 2,230 L. Plasma protein binding: Approx 95% (sunitinib); approx 90% (N-desmethyl metabolite).
Metabolism: Metabolised mainly by CYP3A4 enzyme to the primary active N-desmethyl metabolite.
Excretion: Mainly via faeces (approx 61%); urine (approx 16%, as unchanged drug and as N-desmethyl metabolite). Terminal elimination half-life: 40-60 hr (sunitinib); 80-110 hr (N-desmethyl metabolite).
Đặc tính

Chemical Structure Image
Sunitinib

Source: National Center for Biotechnology Information. PubChem Database. Sunitinib, CID=5329102, https://pubchem.ncbi.nlm.nih.gov/compound/Sunitinib (accessed on Jan. 23, 2020)

Bảo quản
Store at 25°C. Any unused portions should be disposed of in accordance w/ local requirements. Avoid contact w/ skin or mucous membranes by wearing gloves and protective equipment.
Phân loại MIMS
Phân loại ATC
L01EX01 - sunitinib ; Belongs to the class of other protein kinase inhibitors. Used in the treatment of cancer.
References
Anon. Sunitinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/03/2016.

Buckingham R (ed). Sunitinib Malate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/03/2016.

Joint Formulary Committee. Sunitinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/05/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Sunitinib Malate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 04/03/2016.

Sutent Capsule (Pfizer Laboratories Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/03/2016.

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