What specific information does the dasatinib package insert contain?

Dasatinib (Dasatinib) is a targeted anti-cancer drug belonging to the tyrosine kinase inhibitor (TKI) class. Its trade name is Sprycel, and its Chinese trade name is Shidasai. It is widely used in the treatment of BCR-ABL fusion gene Types of leukemia, especially Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL). The drug instructions for dasatinib are extremely important medical guidance documents in clinical use. They are usually formulated by regulatory agencies (such as FDA, EMA or NMPA) and reviewed and determined after submission by the drug marketing authorization holder. The instructions cover many aspects, from basic drug information to detailed instructions for use, pharmacokinetics, safety warnings, recommendations for special groups, etc., and are crucial for doctors and patients to use the drug safely and rationally.

First of all, the indications of dasatinib will be clearly listed in the drug instructions. In adults, it is indicated for patients with newly diagnosed Ph+ chronic-phase CML, as well as patients with Ph+ CML that is resistant or intolerant to imatinib or other treatment modalities, whether in chronic phase, accelerated phase or blast phase (including myeloid or lymphoblastic phase). Additionally, it is approved for use in adults with Ph+ ALL, particularly those who are resistant or intolerant to standard treatments. In the pediatric population, dasatinib is approved for use in patients 1 year old and older with chronic phase Ph+CML and children with newly diagnosed Ph+ALL who require combination chemotherapy. Its indications are wide and cover multiple disease stages, indicating that it has important therapeutic value in clinical practice.

Secondly, the instructions provide clear guidance on usage and dosage. In adults with CML in the chronic phase, the recommended starting dose is 100 mg orally daily; in patients with accelerated phase, blast phase CML or Ph+ ALL, the starting dose is increased to 140 mg once daily. Drugs must be swallowed whole and must not be crushed, cut or chewed to prevent changes in the drug release pattern from affecting efficacy or causing adverse reactions. The instructions also indicate that the drug can be taken with food or on an empty stomach, and is not subject to food restrictions, which increases the convenience of medication. For pediatric patients, the dose is adjusted according to weight. For example, the daily dose for children weighing between 10 and 20 kg is 40 mg, and so on. For children weighing more than 45 kg, the recommended dose is 100 mg once daily. Taking into account the growth of children, the instructions recommend re-evaluating the weight and adjusting the dosage every 3 months to ensure the safety and effectiveness of the medication.

The instructions also detail the pharmacokinetic characteristics of dasatinib, including its mode of absorption, bioavailability, and metabolic pathways (mainly through the liverCYP3A4 enzyme metabolism), half-life and excretion mode and other information. These contents are of key significance for evaluating the dynamic changes of drugs in the body and drug-drug interactions. In addition, dasatinib has strong blood-brain barrier permeability, so it has also been tried as an exploratory treatment in some studies of central nervous system leukemia.

Regarding adverse reactions, the drug instructions list common and serious adverse events and grade them according to their frequency of occurrence. Common side effects include bone marrow suppression (such as neutropenia, thrombocytopenia), gastrointestinal discomfort (such as nausea, diarrhea), rash, fatigue, fever, etc., while more serious adverse reactions involve pericardial effusion, pulmonary hypertension, QT interval prolongation, and serious infection. The instructions recommend that in the event of serious adverse reactions, the dose should be suspended or adjusted, and supportive treatment should be carried out under the guidance of a doctor.

In addition, the instructions specifically emphasize that dasatinib should be used with caution in special populations. For example, there is a potential risk of fetal toxicity when using dasatinib in pregnant and lactating women. There is relevant evidence in animal experiments. Therefore, the instructions recommend avoiding use during pregnancy and emphasize the importance of effective contraceptive measures. For patients with abnormal liver and kidney function, the instructions recommend evaluating organ function before initial use and closely monitoring physiological parameters during medication.

In terms of drug storage, expiry date and disposal, the instructions also give clear guidance. For example, the drug should be stored in a dry and light-proof environment to avoid exposure to children. Expired or unused medicines should be disposed of safely in accordance with relevant national regulations to avoid any impact on the environment due to random discarding.

In short, the dasatinib drug instructions provide a complete information system from indications, usage and dosage, adverse reactions to pharmacokinetics, safe medication warnings, etc., and are an indispensable reference for patients in the medication process. Before prescribing dasatinib, doctors should fully assess the patient's condition and comorbid diseases, and formulate an individualized treatment plan based on the instructions.

Reference materials:https://go.drugbank.com/drugs/DB01254