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Dasatinib

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Dasatinib is a kinase inhibitor used to treat certain types of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL). It works by targeting and blocking the action of abnormal proteins that signal cancer cells to multiply. This helps slow or stop the progression of the disease in adult patients.


Ingredient
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Dasatinib
Reference Brand
Sprycel
Manufacturer
Bristol-Myers Squibb
Product Form
Tablet
Regulatory Classification
Rx
Primary Category
Cancer Treatment
Product Category
Antineoplastic agents, Tyrosine kinase inhibitors
Pharmacological Class
Protein kinase inhibitors
Manufacturer Description
A targeted therapy used for specific types of blood cancer when other treatments have not worked.
Mechanism of Action
Dasatinib works by blocking specific proteins (tyrosine kinases) that tell cancer cells to multiply. By shutting down these signals, the medication helps stop the growth and spread of leukaemic cells.
Route of Administration
Oral
Onset Time
Varies by patient; monitored via blood tests
Duration
3-5 hours (half-life)
Contraindications
Hypersensitivity to dasatinib, Breastfeeding
Severe Adverse Events
Severe bleeding, Pleural effusion (fluid around lungs), Heart failure, Low white blood cell count
Common Side Effects
Headache, Diarrhoea, Skin rash
Uncommon Side Effects
Fluid retention (oedema), Fatigue, Muscle pain, Shortness of breath
Drug Interactions
Antacids, Ketoconazole, St John’s wort, Rifampicin
Pregnancy Safety Warnings
Do not use in pregnancy; highly effective contraception required.
Age Restrictions
Children and adults
Storage Guidelines
Store at room temperature.
Related Products
Imatinib, Nilotinib, Bosutinib

Dasatinib FAQ

What should I do if I develop a pleural effusion while taking dasatinib?

If you notice shortness of breath, chest pain, or a persistent cough, contact your oncology team promptly. They may order imaging studies and adjust the dasatinib dose or temporarily discontinue the drug.

Can dasatinib be taken with proton-pump inhibitors like omeprazole?

Proton-pump inhibitors can modestly reduce dasatinib absorption. If both are needed, your doctor may recommend taking dasatinib at a different time of day (e.g., with food and milk) and monitoring for reduced efficacy.

Is it safe to travel internationally with dasatinib?

Yes, but keep the medication in its original labeled bottle, carry a copy of the prescription, and ensure you have enough supply for the entire trip. Some countries may require a doctor’s note for controlled oncology medicines.

How does dasatinib differ from imatinib?

Dasatinib is a second-generation TKI that binds more tightly to BCR-ABL and also inhibits several additional kinases, providing activity against some imatinib-resistant leukaemias. It often achieves quicker molecular responses but may have a higher risk of fluid retention.

What laboratory tests are required before starting dasatinib?

Baseline CBC, liver and renal function tests, an ECG to assess QT interval, and confirmation of BCR-ABL positivity by molecular testing are standard prerequisites.

Can dasatinib be used in children with CML?

Dasatinib is approved for adult patients; its safety and dosing in paediatric CML are still being studied. Use in children should only occur within a clinical trial or specialist paediatric oncology setting.

Are there any lifestyle modifications that can reduce side effects?

Maintaining adequate hydration, eating a balanced diet, limiting alcohol, and avoiding grapefruit products can help minimise gastrointestinal upset and drug-interaction risks.

What happens if I miss a dose while I’m on a holiday?

Take the missed tablet as soon as you remember on the same day. Do not take a double dose the next day; follow the missed-dose guidance provided by your healthcare team.

How long will I need to stay on dasatinib therapy?

Chronic-phase CML usually requires lifelong treatment to maintain remission. Your oncologist will evaluate response regularly and discuss any potential therapy changes.

Is dasatinib covered by the NHS for eligible patients?

Dasatinib is listed on the NHS Cancer Drugs Fund for specific indications like chronic-phase CML after failure of first-line TKIs. Eligibility is determined by specialist assessment and local commissioning policies.

Dasatinib: Generic Medication Overview

Dasatinib is a prescription medicine classified under oncology support therapies. Its active ingredient is dasatinib, a targeted cancer drug that belongs to the tyrosine-kinase inhibitor (TKI) class. In the United Kingdom it is regulated by the Medicines and Healthcare products Regulatory Agency (MHRA) and is typically supplied in a bottle of tablets, most commonly in a 50 mg strength. Dasatinib is used under the supervision of a specialist oncologist or haematologist and is not available over the counter.

How Dasatinib Works in the Body

Dasatinib blocks the activity of several tyrosine kinases that drive the growth of certain cancer cells. The most important target is the BCR-ABL protein, an abnormal enzyme created by the Philadelphia chromosome-a genetic abnormality found in chronic myeloid leukaemia (CML) and some cases of acute lymphoblastic leukaemia (ALL). By binding to the ATP-binding site of BCR-ABL and other kinases (such as SRC family kinases), dasatinib prevents the enzyme from transferring phosphate groups that would otherwise trigger uncontrolled cell division.

Key pharmacologic points:

  • Rapid onset: Blood levels rise within a few hours after oral ingestion.
  • Peak effect: Typically reached 2-4 hours post-dose.
  • Duration: The drug’s activity persists for about 24 hours, allowing once-daily dosing.
  • Metabolism: Primarily processed in the liver by the enzyme CYP3A4; metabolites are excreted in the feces and urine.

By inhibiting BCR-ABL signalling, dasatinib reduces the proliferation of malignant leukaemic cells and encourages their programmed death.

Conditions Treated by Dasatinib

Dasatinib is approved in the UK for the following indications, all based on assessments by the MHRA and clinical guidelines from NICE:

  • Chronic myeloid leukaemia (CML) in the chronic phase - typically after failure or intolerance to first-line therapy such as imatinib.
  • Ph+ acute lymphoblastic leukaemia (ALL) - in adult patients, either as part of front-line therapy or in relapse.

These approvals are supported by large randomised trials that demonstrated improved cytogenetic and molecular response rates compared with earlier TKIs. Dasatinib is prescribed only after a thorough diagnostic work-up confirming the presence of the BCR-ABL fusion gene.

Evidence-Based Off-Label Uses

Research studies have explored dasatinib in a limited number of solid tumours and rare haematologic conditions. While some early-phase trials reported activity in:

  • Systemic mastocytosis
  • Certain forms of melanoma
  • Some advanced sarcomas

these uses remain investigational and are not approved by the MHRA. Off-label prescribing requires careful risk-benefit assessment by a specialist and informed consent from the patient.

Evaluating Dasatinib for Your Health Profile

Who Might Benefit

  • Adults diagnosed with BCR-ABL-positive leukaemia who are eligible for TKI therapy.
  • Patients who have not achieved adequate response with first-generation TKIs or who have intolerance to those agents.

Absolute Contraindications

  • Known hypersensitivity to dasatinib or any of its excipients.
  • Concurrent use of strong CYP3A4 inducers (e.g., rifampicin, carbamazepine) that could markedly lower drug exposure.
  • Pregnant women - dasatinib is classified as contraindicated in pregnancy due to fetal toxicity.

Relative Contraindications and Cautions

  • Severe hepatic impairment (Child-Pugh C): dose adjustment may be required; use only if clearly indicated.
  • Moderate renal impairment: monitor renal function; no formal dose reduction is required but caution is advised.
  • Concurrent anticoagulation (e.g., warfarin, DOACs): increased risk of bleeding; close monitoring of coagulation parameters is recommended.

Special Populations

  • Pregnancy & lactation: Dasatinib can cause teratogenic effects; women of child-bearing potential should use effective contraception during treatment and for at least 3 months after cessation. Breast-feeding is not recommended.
  • Elderly patients: May experience higher rates of cytopenias; dose titration based on tolerability is common.

If any of these conditions apply, a detailed discussion with the treating oncologist is essential before starting therapy.

Safety Profile and Interactions

Common Side Effects

  • Fluid retention / pleural effusion - often mild but can progress; monitor for shortness of breath.
  • Myelosuppression (low blood counts) - includes neutropenia, thrombocytopenia, and anemia.
  • Gastro-intestinal upset - nausea, diarrhoea, or abdominal pain.
  • Headache and fatigue - usually transient.
  • Rash or skin irritation - may require topical treatment.

Most of these effects are manageable with dose adjustments or supportive care.

Serious Adverse Events

  • Severe myelosuppression leading to infection or bleeding.
  • Pulmonary hypertension - rare but potentially life-threatening; monitor for worsening dyspnoea.
  • QT-interval prolongation - risk for cardiac arrhythmia; baseline ECG recommended.
  • Bleeding complications - especially when combined with anticoagulants.

Patients experiencing fever, persistent cough, sudden swelling, or unexplained bruising should seek urgent medical attention.

Drug Interactions

  • CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, grapefruit juice) can increase dasatinib levels → higher toxicity risk.
  • CYP3A4 inducers (e.g., St John’s wort, phenytoin) may lower exposure → reduced efficacy.
  • Antacids containing aluminium or magnesium - reduce absorption; separate administration by at least 2 hours.
  • Proton-pump inhibitors (omeprazole, esomeprazole) - may modestly decrease bioavailability; dose timing should be considered.

A complete medication review, including over-the-counter products and herbal supplements, is recommended before initiation.

Food and Lifestyle Interactions

  • Take with food or a full glass of milk - improves absorption and reduces gastrointestinal irritation.
  • Alcohol - do not consume in excess; it may exacerbate liver toxicity.
  • Driving or operating machinery: Most patients tolerate daily activities, but severe fatigue or dizziness warrants caution.
  • Sun exposure: No direct photosensitivity reported, but patients with rash should protect skin from excessive UV light.

How to Take Dasatinib

  • Standard dosing: The usual adult dose for chronic-phase CML is 100 mg once daily; however, many clinicians initiate therapy with a 50 mg tablet in patients at risk of fluid retention or with comorbidities. The exact dose must be prescribed by the treating specialist.
  • Administration: Swallow the 50 mg tablet whole with food or milk; do not crush, chew, or split the tablet.
  • Missed dose: If a dose is missed, take it as soon as remembered on the same day; do not double the next dose.
  • Dose modifications: Based on blood count trends, liver function tests, and tolerance, the physician may reduce the dose to 50 mg or increase to 100 mg.
  • Overdose: Symptoms may include severe nausea, vomiting, diarrhoea, and profound myelosuppression. Seek emergency care; supportive measures are the mainstay of treatment.
  • Discontinuation: Dasatinib should not be stopped abruptly without medical guidance. Tapering is usually not required, but monitoring for disease recurrence is essential.

Monitoring and Follow-Up

Regular clinical and laboratory monitoring is integral to safe dasatinib therapy:

  • Complete blood count (CBC): weekly for the first month, then every 2-4 weeks, to detect cytopenias early.
  • Liver function tests (LFTs): at baseline and periodically; adjust dose if transaminases rise markedly.
  • Renal function: serum creatinine and eGFR at baseline; repeat as clinically indicated.
  • Electrocardiogram (ECG): baseline and periodically to assess QT interval, especially in patients with cardiac risk factors.
  • Chest imaging: If pleural effusion is suspected, a chest X-ray or ultrasound is recommended.
  • Molecular monitoring: Quantitative PCR for BCR-ABL transcripts every 3 months to gauge treatment efficacy.

Any abnormal result should be discussed with the oncology team promptly.

Storage and Handling

  • Keep the bottle of 50 mg tablets at room temperature (20-25 °C), away from direct sunlight and moisture.
  • Store out of reach of children and pets.
  • Do not use the medication after the expiration date printed on the label.
  • If a tablet becomes discolored or crumbly, discard it and obtain a new supply.
  • Follow local pharmacy guidelines for safe disposal of unused tablets (e.g., return-to-pharmacy programmes).

Medication-Specific Glossary

Tyrosine-Kinase Inhibitor (TKI)
A class of drugs that block enzymes (tyrosine kinases) involved in signalling pathways that promote cancer cell growth.
Pleural Effusion
Accumulation of fluid in the space surrounding the lungs, which can cause shortness of breath and chest discomfort.
Myelosuppression
Decrease in the production of blood cells by the bone marrow, leading to low counts of red cells, white cells, or platelets.
QT-Interval Prolongation
Extension of the heart’s electrical reset phase on an ECG, which can increase the risk of abnormal heart rhythms.

Medical Disclaimer

This article provides educational information about dasatinib and is not a substitute for professional medical advice. Treatment decisions, including the use of dasatinib for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Dasatinib is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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