Dasatinib


Concise Prescribing Info
Indications/Uses
Chronic myeloid leukaemia.
Dosage/Direction for Use
Adult : PO Chronic phase CML: Initial: 100 mg once daily, up to 140 mg once daily. Accelerated, myeloid or lymphoid blast phase CML or Philadelphia chromosome-positive ALL: Initial: 140 mg once daily, up to 180 mg once daily.
Dosage Details
Oral
Chronic myeloid leukaemia
Adult: Chronic phase CML: Initially, 100 mg once daily, may increase up to 140 mg once daily. Accelerated, myeloid or lymphoid blast phase CML or Philadelphia chromosome-positive ALL: Initially, 140 mg once daily, may increase up to 180 mg once daily.
Hepatic Impairment
No dosage adjustment needed.
Administration
May be taken with or without food. Swallow whole, do not break/crush/cut.
Contraindications
Concomitant use w/ CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin,  voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
Special Precautions
Patients w/ predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
Adverse Reactions
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
Potentially Fatal: Severe bleeding events, including fatal CNS and GI haemorrhages; MI. Uncommon: Sepsis.
MonitoringParameters
Evaluate patients for manifestations of underlying cardiopulmonary disease prior to and during therapy. Measure full blood counts wkly for the 1st 2 mth and then mthly thereafter.
Overdosage
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
Drug Interactions
Concomitant use w/ drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia w/ antiplatelet drugs, anticoagulants, and NSAIDs.
Potentially Fatal: May reduce plasma levels w/ antacids, administer antacid 2 hr apart from the admin of dasatinib. May increase plasma levels w/ CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin or voriconazole). May reduce plasma levels w/ CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital or rifampicin).
Food Interaction
Avoid St John's wort as it may decrease dasatinib levels. Avoid grapefruit juice as it may increase dasatinib levels.
Action
Description: Dasatinib is an inhibitor of multiple tyrosine kinases. It is used for the treatment of all phases of chronic myeloid leukaemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukaemia (ALL) in adults who have resistance or intolerance to previous therapy, including imatinib.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 0.5-6 hr.
Distribution: Volume of distribution: 2505 L. Plasma protein binding: Approx 96% (dasatinib); approx 93% (active metabolite).
Metabolism: Extensively hepatic via CYP3A4 isoenzyme to form its active metabolite.
Excretion: Via faeces (approx 85%, 19% as unchanged drug); urine (approx 4%, 0.1% as unchanged drug).
Storage
Store at 25°C.
References
Anon. Dasatinib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 30/10/2013.

Anon. Dasatinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/10/2013.

Buckingham R (ed). Dasatinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/10/2013.

Joint Formulary Committee. Dasatinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/10/2013.

Sprycel (Dasatinib): Drug Safety Communication - Risk of Pulmonary Arterial Hypertension. U.S. FDA. https://www.fda.gov/. Accessed 30/10/2013.

Disclaimer: This information is independently developed by MIMS based on Dasatinib from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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