High Potent Antineoplastic Small Molecule Dasatinib Bulk Powder for Oncology Research CAS 302962-49-8

Dasatinib More Info

Dasatinib is a potent, next-generation, oral tyrosine kinase inhibitor that has become a cornerstone in the treatment of certain forms of leukemia. Chemically designated as N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide monohydrate, it has the molecular formula C₂₂H₂₆ClN₇O₂S (for the anhydrous form) and a molecular weight of approximately 488.01 g/mol . Marketed under the brand name Sprycel®, dasatinib was first approved by the U.S. Food and Drug Administration (FDA) in 2006 and is also known by the developmental code BMS-354825 . Unlike first-generation tyrosine kinase inhibitors, dasatinib was rationally designed to bind to multiple conformations of the BCR-ABL kinase domain, including the active and inactive states, which underlies its increased potency and broader activity against resistant mutants .

The primary mechanism of action of dasatinib involves the potent inhibition of several oncogenic tyrosine kinases, including BCR-ABL, SRC family kinases (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ . At the molecular level, dasatinib binds to the ATP-binding site of these kinases, forming critical hydrogen bonds with specific residues such as Thr315 in the BCR-ABL protein . By blocking kinase activity, dasatinib effectively inhibits the downstream signaling pathways that drive uncontrolled proliferation, survival, and resistance to apoptosis in malignant cells . A key clinical advantage of dasatinib over imatinib is its ability to inhibit most imatinib-resistant BCR-ABL mutants, with the notable exception of the T315I mutation, which confers resistance to both drugs . This broad inhibitory profile makes dasatinib approximately 325-fold more potent than imatinib against unmutated BCR-ABL in preclinical models .

Clinically, dasatinib is indicated for the treatment of adults with newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase, as well as for patients with CML who are resistant or intolerant to prior therapy including imatinib . It is also approved for the treatment of adults with Ph+ acute lymphoblastic leukemia (ALL) . The recommended dosage varies by indication and line of therapy, ranging from 100 mg once daily (for chronic phase CML) to 140 mg daily (for accelerated or blast phase CML and Ph+ ALL) . In pediatric populations, dosing is weight-based . Long-term follow-up studies have demonstrated deep and durable responses, including high rates of major molecular response and molecular remission, with some adult patients achieving treatment-free remission after sustained deep molecular response .

The pharmacokinetic profile of dasatinib supports oral once-daily administration. It is rapidly absorbed following oral intake, with peak plasma concentrations typically achieved within 0.5 to 1.5 hours . The absolute bioavailability of dasatinib is not fully established but is estimated to be approximately 25-34% . Food, particularly a high-fat meal, can reduce the rate and extent of absorption, decreasing the area under the concentration-time curve (AUC) by approximately 20-25%, which is why dasatinib is usually taken without food . Dasatinib is extensively metabolized in the liver, primarily by the cytochrome P450 enzyme CYP3A4, and to a lesser extent by flavin-containing monooxygenase 3 (FMO-3) and UGT enzymes . The drug has an elimination half-life of approximately 3 to 5 hours, and excretion occurs mainly via the feces (approximately 85%) and to a lesser extent in the urine (approximately 4%) .

The safety profile of dasatinib is well-characterized, though it differs from other tyrosine kinase inhibitors. The most common adverse effects include myelosuppression (neutropenia, thrombocytopenia, anemia), which is dose-related and typically manageable with dose reduction or temporary interruption . Fluid retention is a hallmark toxicity of dasatinib, with pleural effusion occurring in approximately 10-28% of patients, particularly in those receiving the 140 mg twice-daily dose . Other frequent side effects include diarrhea, headache, skin rash, and fatigue . Serious but less common complications include pulmonary arterial hypertension, QTc prolongation, and bleeding events, particularly in patients with severe thrombocytopenia . Notably, dasatinib has a higher risk of pleural effusion but lower rates of severe edema and rash compared to imatinib . Dasatinib carries a boxed warning for the risk of pulmonary arterial hypertension, which should be evaluated before and during treatment . As with all tyrosine kinase inhibitors, dasatinib is contraindicated during pregnancy due to teratogenic potential, and women of childbearing potential should use effective contraception during treatment .

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