by Dasatinib drugs are an inhibitor of multiple tyrosine kinases. It is active against Philadelphia-chromosome positive (Ph+) acute lymphocytic leukemia (ALL), in patients who have received prior therapy including imatinib. It is being studied in the treatment of other types of cancer.
A low dose of aspirin is sometimes prescribed along with this drug to prevent heart attacks and strokes. This medicine can increase the risk of bleeding when used with aspirin.
This medication has caused liver problems in some people. In case of any symptoms such as tired feeling, loss of appetite, stomach or back pain, yellowing eyes or skin, or dark urine, contact a doctor.
In vitro, dasatinib inhibited the BCR-ABL kinase at nanomolar concentrations and also inhibited other tyrosine kinases associated with leukemia such as breakpoint cluster region-ABL, EPHA2 receptor tyrosine kinases and Abelson murine leukemia. It also potently inhibited imatinib mesylate-resistant leukemia cell lines exhibiting BCR-ABL kinase domain mutations, activation of alternate signaling pathways, and multi-drug resistance gene overexpression.
The Dasatinib drugs market is a dynamic and rapidly evolving segment of the pharmaceutical industry. Dasatinib, a tyrosine kinase inhibitor, has shown remarkable efficacy in the treatment of Chronic Myeloid Leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), leading to its widespread adoption in the field of oncology.
Dasatinib is well absorbed from the gastrointestinal tract. Its solubility is pH dependent and its absorption increases with increasing acidity. It is extensively metabolized by CYP3A4 and its active metabolite has equipotent activity. Both the parent compound and its metabolites are excreted via feces.
The major interindividual variation in the PK of dasatinib is due to gut microbiome variation, which alters enzymatic metabolism and the excretion of drug. The resulting metabolic and pharmacokinetic profiles influence the exposure-response relationship of dasatinib.
Dasatinib and its metabolites are excreted in the feces. It is mainly eliminated by urination, whereas first-pass metabolism and other enzymes contribute to the total clearance of the drug. The pharmacodynamic effects of dasatinib are altered by these metabolic interactions and the presence of other drugs in the body.
The gut microbiome is increasingly recognized as the second genome of a person. It can directly impact a patient’s response to drugs by affecting their bioavailability, efficacy, and toxicity. Its impact is most prominent on a subset of drugs with a narrow therapeutic window, such as dasatinib. Therefore, understanding the mechanisms by which gut microbiome can modify a patient’s PK profile is crucial to personalized medicine.
Alembic Pharmaceuticals declared that they gained approval from the US health regulator in June 2022, for marketing Dasatinib tablets. These tablets are used for treating various types of cancer.
