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Дазатиниб

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Дазатиниб

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Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

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Overview of Дазатиниб

What is Dasatinib?

Property Description
Active Ingredient (INN) Dasatinib
Pharmacological Class Protein-Tyrosine Kinase Inhibitor (PTKI)
Type Synthetic, Second-Generation Small Molecule
Form Film-coated tablets
Rx/OTC Status Prescription-only medicine (Rx)

1. What Type of Medicine is Dasatinib and What Class Does it Belong To?

Dasatinib (INN, International Nonproprietary Name) is a synthetic, small-molecule medication that functions as a highly targeted Protein-Tyrosine Kinase Inhibitor (PTKI), classifying it as a modern antineoplastic agent. The drug is clinically recognized as a second-generation TKI, a significant distinguishing factor, often utilized in settings where older, first-generation inhibitors may be less effective or poorly tolerated. This compound is chemically synthesized and is used as a single active ingredient product.


2. Principle of Action and Core Purpose

Dasatinib’s core purpose is to stop the uncontrolled growth and survival of specific cancer cells by interrupting their disease-driving signals. The medication achieves this by selectively binding to and inhibiting multiple overactive enzymes, including the BCR-ABL fusion protein and the Src family kinases, which are implicated in promoting cancerous growth. Dasatinib specifically blocks enzymes like the BCR-ABL protein kinase, leading to the reduction of leukemia cells in the body. This precision allows for systematic management of the underlying molecular disorder.


3. Dosage Form and Administration Characteristics

Dasatinib is formulated for long-term therapeutic management and is supplied as a film-coated tablet intended for oral administration. This feature is central to its patient positioning, supporting a convenient, consistent, and long-term treatment plan. This oral route is essential for maintaining therapeutic levels of the synthetic compound, which is necessary for sustained inhibition of the target kinases.

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What side effects are possible with Дазатиниб?

Possible Side Effects and Safety Information

Dasatinib's safety profile is defined by adverse reactions classified according to their frequency in clinical use, as documented by regulatory agencies (e.g., FDA and EMA). These effects are organized by the System-Organ Classes (SOCs) they affect, with significant risk concentrated in hematologic, cardiovascular, and fluid management systems.

Very Common Adverse Reactions (ge 1/10) include Myelosuppression (anemia, neutropenia, thrombocytopenia), Fluid Retention (peripheral edema, pleural effusion), diarrhea, fatigue, and headache.

Common Adverse Reactions (ge 1/100 to < 1/10) include hypertension, cardiac failure, and various forms of hemorrhage (bleeding).


Serious Adverse Reactions and Safety Considerations

The label officially documents several Serious Adverse Reactions (SARs). These include Severe Myelosuppression (Grade 3/4 blood count abnormalities), Severe Fluid Retention (Grade 3/4 pleural effusion or pulmonary edema), and Pulmonary Arterial Hypertension (PAH). PAH is a serious, potentially irreversible risk associated with long-term exposure to the medication.

Safety notes for specific populations are also documented: Older adults (ge 65 years) may experience a higher incidence of fluid retention events. For pediatric patients, effects on growth and bone development are noted in official prescribing information. Patients must be assessed for conditions such as pre-existing cardiac risks and Hepatitis B infection prior to initiating treatment, as documented in regulatory safety guidelines. The incidence of pleural effusion is often highest during the first year of treatment.

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Overdose and Emergency Response

Dasatinib Overdose and When to Seek Help

The official regulatory documentation for Dasatinib defines the overdose profile primarily by its severe, dose-dependent toxicity, which necessitates immediate medical intervention.


Documented Manifestations and Severe Outcomes

Overdose is documented to result in severe myelosuppression, a condition involving profound reductions in blood cell counts. This includes thrombocytopenia, neutropenia, and anemia. Due to the severely low platelet count, a key life-threatening outcome associated with overdose is the risk of major hemorrhage, including potential central nervous system or gastrointestinal bleeding. Other severe manifestations documented in regulatory labeling include fluid retention such as pleural effusion and pericardial effusion.


Required Emergency Actions

Suspected overdose requires that an individual seek immediate medical attention. Regulatory guidance mandates to call emergency services immediately if the exposed individual exhibits signs of a life-threatening scenario, such as collapse, seizure, trouble breathing, or inability to be awakened.


Management and Monitoring

Management procedures described in official labeling emphasize general supportive care and symptomatic treatment for the manifestations that occur. No specific antidote is known for Dasatinib overdose. Due to the high risk of hematological toxicity, the individual will require close hospital observation and frequent monitoring of blood cell counts (Complete Blood Counts). Treatment interruption or permanent discontinuation of therapy is also a mandated management step.

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Therapeutic Uses of Дазатиниб

What Дазатиниб Treats: Main Uses and Benefits

Дазатиниб is a prescription medication utilized in the treatment of specific blood and bone marrow cancers, collectively known as leukemias. Its primary therapeutic domain involves managing diseases that are Philadelphia chromosome-positive (Ph+), a condition marked by an abnormal chromosome that causes cancer cell proliferation.

The medication is used to address:

  • Chronic Myeloid Leukemia (CML): It is indicated for newly diagnosed adult patients in the chronic phase of Ph+ CML. It is also utilized in adult patients with CML (chronic, accelerated, or blast phase) who have developed resistance or intolerance to prior therapies, including imatinib.
  • Acute Lymphoblastic Leukemia (ALL): Дазатиниб is used in adult patients with Ph+ ALL who have demonstrated resistance or intolerance to previous treatment regimens.

Furthermore, the drug is used in pediatric patients (ages 1 year and older) for Ph+ CML in the chronic phase, and in combination with chemotherapy for newly diagnosed Ph+ ALL. The administration of this agent contributes to the therapeutic management of these hematologic malignancies.

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Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Dasatinib

This section outlines the official population eligibility and non-eligibility rules for Dasatinib as defined by governmental regulatory documents.

Category Official Regulatory Status / Rule
Contraindicated Populations Patients with known hypersensitivity to the medicine or any of its excipients. Pregnant women and breastfeeding women are contraindicated.
Age-Related Eligibility Use is allowed for adults and pediatric patients 1 year of age and older. Use is not recommended for children younger than 1 year.
Conditional Use Restrictions Females of reproductive potential must use effective contraception during and for 30 days after treatment. Caution is required for patients with risk factors for QT prolongation or pre-existing hepatic impairment. Permanent discontinuation is required if Pulmonary Arterial Hypertension (PAH) is confirmed.

The official eligibility profile is defined by these strict contraindications and conditional use requirements. Eligibility is established for adults and children one year and older. The most stringent restrictions apply to reproductive status and pre-existing conditions that pose known risks, such as confirmed PAH, which dictates mandatory permanent discontinuation of the medicine.

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What should I know about interactions with other medicines?

Interactions with other medicines and products

Dasatinib's official interaction profile is defined by its metabolic pathway and pH-dependent solubility, as documented by regulatory agencies.

Pharmacokinetic Interactions and Restrictions

Interaction Entity/Category Effect on Dasatinib Plasma Levels Regulatory Restriction
Strong CYP3A4 Inhibitors (e.g., ketoconazole) Increase (significant) Avoid if possible; if necessary, dose reduction is considered.
Strong CYP3A4 Inducers (e.g., rifampin, St. John's Wort) Decrease (significant) Avoid co-administration due to reduced efficacy risk.
PPIs (e.g., omeprazole) / H2-RAs (e.g., famotidine) Decrease (substantial) Avoid co-administration (use is not recommended).
Antacids Decrease (when simultaneous) Administer at least 2 hours prior to or 2 hours after Dasatinib.
Grapefruit Juice Increase Avoid consumption.

Pharmacodynamic Interactions

Co-administration with other agents may increase the risk of specific labeled adverse events: co-administration with anticoagulants or medicines that inhibit platelet function requires caution due to an increased potential for bleeding/hemorrhage. Similarly, caution is advised with medicinal products known to prolong the QT interval due to the possibility of additive cardiac risk. The regulatory profile strictly governs co-administration and timing rules based on documented pharmacokinetic and pharmacodynamic outcomes.

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Mechanism of Action

Targeted Inhibition of Key Tyrosine Kinases

The drug functions as a multi-targeted Protein-Tyrosine Kinase Inhibitor (PTKI), engaging mechanisms that regulate overactive cellular processes. It exerts its primary effect by binding competitively to the ATP-binding pocket of multiple enzymes, notably the BCR-ABL fusion protein kinase and the Src family kinases (SFK). This action disrupts the constant, unregulated signaling required for cell proliferation and survival signaling.

Forcing Cell Cycle Arrest and Programmed Cell Death

By suppressing the pro-survival signals originating from the inhibited kinases, the drug initiates or suppresses signaling sequences that lead to specific downstream effects. This molecular action forces the targeted cell population into G0/G1 cell cycle arrest (suppressing division) and simultaneously activates the apoptotic cascade (programmed cell death). The physiological consequence is the induction of apoptosis and suppression of proliferation in the cell population expressing the target kinases.

Modulating Cellular Adhesion and Mobility

The multi-targeted inhibitory profile, specifically against the Src family kinases, engages mechanisms that regulate cell-to-cell signaling and movement. This indirectly modifies early molecular steps that shape systemic physiological outcomes related to cellular integrity and invasive signaling patterns.

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Dosage and Administration Information

How Dasatinib is Used

Dasatinib is an antineoplastic agent that is administered according to standardized regimens. The general principle of its use is continuous, daily oral administration. The medicine is formulated as film-coated tablets that must be swallowed whole to ensure proper dosing; they must not be crushed, cut, or chewed.


Dosing Regimens and Frequency

Standard regimens require Dasatinib to be taken once daily (QD) at a consistent time each day. The dosing schedule varies based on the specific indication:

Indication Standard Starting Dose (Adult)
Newly Diagnosed Chronic Phase CML 100 mg once daily
Advanced Phase CML (Accelerated/Blast) 140 mg once daily
Ph+ Acute Lymphoblastic Leukemia (ALL) 140 mg once daily

Administration Conditions and Management

Dasatinib tablets can be taken with or without food. The treatment is generally considered long-term and is continued unless specific toxicity or disease progression occurs. If a dose is missed, the standard protocol is to not take an extra dose to compensate. Instead, the next scheduled dose should be taken at the usual time. For pediatric patients (1 year and older), the starting dose is determined based on body weight or body surface area. Furthermore, administration requires specific timing if used concurrently with antacids, which must be taken at least two hours before or two hours after the Dasatinib dose.

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Recent Clinical Evidence

Research evidence / Overview of studies for Dasatinib

Evidence for Use in Newly Diagnosed Ph+ Chronic Myeloid Leukemia (CML), Chronic Phase

Research exploring this use involves major, multi-year Randomized Controlled Trials (RCTs) that compared the measured outcomes of Dasatinib against Imatinib, the previous standard initial therapy. These studies included adults with newly diagnosed chronic-phase CML who had not received prior targeted therapy. Researchers examined the status of patients' disease over time by monitoring key molecular markers, specifically Complete Cytogenetic Response (CCyR) and Major Molecular Response (MMR).

These trials provided data describing the measured rates and timing of achieving these specific molecular and cytogenetic response milestones. Researchers continuously monitored metrics, including Progression-Free Survival (PFS) and Overall Survival (OS), over many years to describe the course of the disease in the study groups. What remains uncertain is the final, long-term survival comparison against older therapies, as this observation continues over extended durations (more than 10 years).

Evidence for Use in Ph+ CML Resistant or Intolerant to Prior Therapy

Research exploring this specific situation, involving patients who showed resistance or intolerance to a prior therapy (such as Imatinib), included Phase 2 multicenter studies and subsequent comparative trials. These studies monitored the achievement of Major Cytogenetic Response (MCyR), Complete Cytogenetic Response (CCyR), and Major Molecular Response (MMR) in adults who had switched therapies.

Findings from these initial single-arm studies described the measured patterns of molecular response in this heterogeneous group. Long-term follow-up reports from these trials provide context on the persistence of the molecular changes measured over multiple years. A key limitation here is that a significant part of the initial supporting data came from non-randomized Phase 2 studies, limiting the ability to fully contextualize the findings.

Long-Term Studies and Durability of Response

For the key CML indications, the initial clinical trials were designed to continue monitoring patients for many years. Follow-up research reports regularly describe the sustained durability of the measured molecular changes, focusing on whether patients maintain their molecular and cytogenetic response milestones over time. What remains uncertain is the need for continuous monitoring to establish the full, final long-term picture, as the studies are designed to track patients for the rest of their lives.

Key Studies & References

  1. Dasatinib or imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: 2-year follow-up from a randomized phase 3 trial (DASISION) (NCT00481247)
  2. Five-year results of the DASISION trial: Dasatinib vs imatinib in newly diagnosed chronic-phase CML
  3. Dasatinib in imatinib-resistant or -intolerant chronic-phase, chronic myeloid leukemia patients: 7-year follow-up of study CA180-034 (NCT00123474)
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Frequently Asked Questions (FAQ)

Common questions about Дазатиниб (FAQ)


Q: Can I stop taking Dasatinib if my test results are good?

Official prescribing information indicates that stopping Dasatinib (known as Treatment-Free Remission, or TFR) is an option only for specific patients with chronic phase CML who have achieved a long-lasting, deep molecular response. This decision is based on a doctor’s assessment and confirmation of strict remission criteria, followed by careful, regular molecular monitoring as defined in official protocols.


Q: Can I take vitamins or supplements with Dasatinib?

The use of any non-prescription medicines, vitamins, or dietary supplements is typically reviewed by a healthcare professional before starting treatment. Official safety notes describe that certain products, particularly strong herbal supplements, can interact with how the body processes Dasatinib, potentially altering its concentration in the blood.


Q: How long after starting Dasatinib can I expect improvement?

Clinical trial data describes that Dasatinib can induce rapid responses in adult patients with newly diagnosed chronic phase CML. For example, the measured time to achieve a Complete Cytogenetic Response (CCyR)—a key molecular measure—was typically between 3.1 and 5.5 months in these studies. This timeframe relates to objective molecular changes rather than immediate physical symptoms.


Q: How do I know if Dasatinib is working?

Treatment effectiveness is generally assessed by healthcare professionals using regular blood and bone marrow tests. These tests measure key response markers, which include Complete Hematologic Response (CHR), Complete Cytogenetic Response (CCyR), and Major Molecular Response (MMR). The specific goal is to see a reduction in the abnormal cancer-related cells.


Q: How often should a blood test be done when taking Dasatinib?

Official regulatory guidelines indicate that a complete blood count (CBC) is typically performed weekly for the first two months of treatment. After this initial phase, the monitoring frequency is usually reduced to monthly, or as directed by the treating physician. This frequent monitoring is necessary to ensure proper surveillance for myelosuppression (low blood counts).


Q: Can Dasatinib cause sleep problems?

Yes, according to official prescribing information, insomnia (difficulty sleeping) is listed as a common adverse reaction. This means it has been reported in between 1% and 10% of patients in clinical trials.


Q: Is there a link between Dasatinib and sunlight exposure?

Regulatory documents have noted severe skin reactions, including photosensitivity, associated with Dasatinib use. In relation to photosensitivity, official safety information highlights the importance of protective measures, such as protective clothing and sunscreen, and suggests limiting prolonged exposure to direct sunlight.


Q: What are the registered trade names for Dasatinib?

The original brand-name medication containing Dasatinib as the active ingredient is known as Sprycel. Additionally, various registered generic versions of the medicine may be available depending on the regulatory region.


Q: Is Dasatinib associated with muscle or joint pain?

Yes, musculoskeletal symptoms are noted in the official safety profile. Both joint pain (arthralgia) and muscle pain (myalgia) are listed as very common adverse reactions, meaning they are reported in 10% or more of patients.


Q: What is known about resistance to Dasatinib?

Dasatinib was designed to be active against most of the BCR-ABL gene mutations that cause resistance to the older drug Imatinib. However, official information notes that certain specific gene mutations, such as the T315I mutation, are not sensitive to Dasatinib.


Q: What is Dasatinib used for besides Chronic Myeloid Leukemia?

Regulatory indications specify that Dasatinib is also used to treat adult patients with Philadelphia chromosome-positive ( Ph+) Acute Lymphoblastic Leukemia ( ALL). This use is typically reserved for those who have not responded to, or are intolerant of, prior therapies.


Q: What are the signs that a side effect from Dasatinib might be serious?

Serious adverse reactions described in the official label include signs of severe fluid retention, such as shortness of breath, dry cough, or chest pain. Other serious signs include symptoms of bleeding (like unusual bruising or black stools) or cardiac issues (such as a fast or irregular heartbeat). These or any other severe symptoms described in the label warrant prompt notification of a healthcare provider.


Q: What is the main difference between first- and second-line CML therapy?

In the context of regulatory approval and clinical trials, first-line therapy is the treatment given initially to newly diagnosed patients. Second-line therapy is designated for patients whose disease has progressed or who have developed resistance or intolerance to the previous primary treatment.


Q: Can Dasatinib affect driving a car?

Official regulatory documents include safety notes that describe the need for caution regarding driving and operating machinery. This is because Dasatinib may cause side effects, such as dizziness or fatigue, which could potentially impair attention or motor skills.


Q: Are there genetic tests that can predict if Dasatinib will work?

The response to Dasatinib therapy is not determined by a single predictive genetic test. However, monitoring the presence of specific BCR-ABL mutations, such as T315I, is a critical part of official guidance used to guide treatment decisions, as certain mutations are known to make the drug ineffective.


Q: What is the chance of the disease recurring after stopping Dasatinib?

Clinical studies of treatment discontinuation (TFR) show that a portion of patients who stop taking the medicine will experience a molecular recurrence. Official data indicates that most of these recurrences happen within the first 6 to 12 months after stopping treatment, and patients usually regain their response when the therapy is resumed.


Q: Can men use Dasatinib if they plan to conceive a child?

Studies in animals have indicated a potential effect of Dasatinib on male reproductive organs. Official prescribing information notes that men undergoing treatment typically discuss appropriate contraceptive methods with their healthcare provider.


Q: Why is it important to know about liver and kidney function before starting Dasatinib?

Dasatinib is primarily processed by the liver, and official documents note that dose adjustment may be necessary if a patient has impaired liver function. While kidney (renal) impairment does not significantly alter the drug's clearance, careful monitoring is still required for patients with pre-existing kidney conditions.

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How should Дазатиниб be stored and disposed of?

Official Storage and Disposal Requirements

Dasatinib (e.g., Sprycel) must be stored according to strict regulatory guidelines to maintain its stability and prevent accidental exposure, as documented by governmental health authorities.

Requirement Area Official Instructions
Storage Temperature Store at Controlled Room Temperature (20 C to 25 C, 68 F to 77 F).
Container & Moisture Keep the medication in the original, tightly closed container, away from excess heat and moisture.
Child Safety Store the medication out of the sight and reach of children and pets.
Special Handling Tablets must not be crushed or cut. Wear gloves if handling broken tablets to prevent skin contact.
Disposal Dispose of unused or expired tablets through an authorized drug take-back program or as directed by a healthcare provider or local waste management. Do not discard in household trash or down a drain.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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