Dasatinib (Dasakast) 50 mg, 60 tablets: profile, composition and research
Reference page for Dasatinib (Dasakast) 50 mg, 60 tablets. Active substance: Дазатиниб / Dasatinib.
- What it is: dasatinib, an oral tyrosine kinase inhibitor used in leukaemias.
- Presentation: film-coated tablets, 50 mg, 60 tablets per pack.
- Status: prescription antineoplastic medicine.
- Research: studies in chronic myeloid leukaemia, links below.
- Where to buy: APV Pharmacy (price and availability there).
Key facts
| Active substance | Dasatinib |
|---|---|
| Form | Film-coated tablets |
| Strength | 50 mg per tablet |
| Pack size | 60 tablets |
| Category | Prescription medicine |
| Article (SKU) | 5476 |
What dasatinib is
Dasatinib is an oral antineoplastic medicine from the tyrosine kinase inhibitor group. It is a small molecule that suppresses the activity of several enzymes sustaining the division of tumour cells in certain types of leukaemia.
It is supplied as film-coated tablets; this listing is the 50 mg strength, with 60 tablets to a pack. The 50 mg tablets are oval and biconvex, with an orange film coating.
The medicine is a prescription antineoplastic product. It is used under the supervision of a haematologist, because it concerns diseases of the blood that require constant monitoring.
How dasatinib works
The target is the BCR-ABL protein
In chronic myeloid leukaemia the cells form an abnormal BCR-ABL protein, a constantly active tyrosine kinase that drives the cell towards uncontrolled division. Dasatinib binds both the active and the inactive form of this enzyme and inhibits it at very low concentrations.
Additional targets
Beyond BCR-ABL the medicine inhibits SRC-family kinases, as well as c-KIT, the ephrin receptor kinase and the platelet-derived growth factor receptor. This widens the range of signalling pathways it affects.
Overcoming resistance
In cell-model experiments dasatinib acted on imatinib-resistant cells as well, with the exception of the T315I mutation. With certain mutations the medicine can therefore lose activity, which is taken into account when therapy is chosen.
Approved uses
The prescribing information names chronic myeloid leukaemia in the chronic phase in newly diagnosed patients, and also the chronic phase, the accelerated phase and myeloid or lymphoid blast crisis in resistance or intolerance to prior therapy, including imatinib.
A separate indication is Philadelphia chromosome-positive acute lymphoblastic leukaemia in resistance or intolerance to previous treatment. Contraindications include pregnancy, breastfeeding and age below 18 years.
Use calls for laboratory monitoring: the medicine affects the blood count and can prolong the QT interval on an ECG. Prescribing and follow-up are the task of a haematologist.
What the research shows
An early study in patients with imatinib-resistant Philadelphia chromosome-positive leukaemias showed a high rate of haematological and cytogenetic response; the work was published in the New England Journal of Medicine in 2006.
The DASISION study compared dasatinib with imatinib in newly diagnosed patients in the chronic phase; the five-year results confirmed a higher rate of deep molecular response with dasatinib.
In Philadelphia chromosome-positive acute lymphoblastic leukaemia, dasatinib was studied as first-line therapy in adults. The data continue to be refined, and the choice of medicine remains an individual decision for the specialist.
Published research
Primary sources, verified against PubMed:
- Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias., PubMed 16775234 (The New England journal of medicine, 2006).
- Dasatinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia., PubMed 20525995 (The New England journal of medicine, 2010).
- Dasatinib as first-line treatment for adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia., PubMed 21931113 (Blood, 2011).
- Final 5-Year Study Results of DASISION: The Dasatinib Versus Imatinib Study in Treatment-Naive Chronic Myeloid Leukemia Patients Trial., PubMed 27217448 (Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2016).
Listed for reference. Publication of a study is not a claim about this particular product.
Precautions
- This is a prescription medicine. Prescribing, dosing and monitoring belong to a haematologist.
- Treatment affects the blood count: low blood-cell counts and a greater tendency to bleed are possible. Regular tests are needed.
- The medicine can prolong the QT interval. A physician assesses the risk, particularly with heart disease and electrolyte disturbances.
- In liver impairment the dose is adjusted by a physician, and liver function is monitored during treatment.
- Fluid retention, oedema, rash and digestive upset are possible. Marked symptoms should be reported to a doctor.
- The medicine is contraindicated in pregnancy; reliable contraception is needed during treatment and breastfeeding is stopped.
Frequently asked
Is dasatinib a prescription medicine?
Yes. It is a prescription antineoplastic medicine and is not intended for self-medication.
Why does this page not give a dosing schedule?
The dose and the length of the course are set by a haematologist from the test results. A reference page does not prescribe treatment.
What matters about the T315I mutation?
Cell-model experiments indicate that dasatinib does not act on cells carrying this mutation. Mutation testing helps a physician choose therapy.
Where does the order ship from?
Shipping and customs handling are described on the APV Pharmacy delivery page.