Dasatab 100 mg (Dasatinib) Tablets

Dasatab 100 mg (Dasatinib): Premium Treatment for Philadelphia Chromosome-Positive Leukemia

Product Overview

Dasatab 100 mg is a high-potency formulation of Dasatinib, a groundbreaking tyrosine kinase inhibitor developed specifically for patients with Philadelphia chromosome-positive (Ph+) leukemias. As the standard adult dose for chronic phase chronic myeloid leukemia (CML), this 100 mg tablet represents a critical therapeutic option for patients worldwide. Manufactured by Eskayef Pharmaceuticals Ltd. and distributed globally by Saif Pharma, Dasatab 100 mg delivers consistent, reliable results in the management of these challenging hematologic malignancies.

Therapeutic Indications

Dasatab 100 mg is specifically indicated for:

In Adult Patients:

• First-line treatment of newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase
• Treatment of chronic, accelerated, or blast phase (myeloid or lymphoid) Ph+ CML in patients who have developed resistance or intolerance to prior therapy, including Imatinib
• Management of Ph+ acute lymphoblastic leukemia (ALL) with resistance or intolerance to prior therapy

In Pediatric Patients:

• Treatment of Ph+ CML in chronic phase for children 1 year and older
• Treatment of newly diagnosed Ph+ ALL when used in combination with appropriate chemotherapy regimens

Advanced Mechanism of Action

Dasatinib operates as a potent multi-kinase inhibitor, targeting several key enzymes involved in the progression of leukemia. At nanomolar concentrations, it effectively inhibits:

• BCR-ABL kinase (the product of the Philadelphia chromosome)
• SRC family kinases (SRC, LCK, YES, FYN)
• c-KIT
• EPHA2
• PDGFRβ

What distinguishes Dasatinib from first-generation tyrosine kinase inhibitors is its ability to bind to multiple conformations of the ABL kinase. This unique property enables it to overcome resistance mechanisms that develop against treatments like Imatinib, including BCR-ABL kinase domain mutations, activation of alternate signaling pathways through SRC family kinases, and multi-drug resistance gene overexpression.

Pharmacokinetic Properties

Dasatab 100 mg demonstrates favorable pharmacokinetic characteristics that make it suitable for convenient once-daily dosing:

Absorption and Food Effects

The medication reaches maximum plasma concentrations between 0.5-6 hours after oral administration. While a high-fat meal can increase the mean AUC by approximately 14%, Dasatinib can be taken with or without food, providing flexibility for patients.

Distribution

With an apparent volume of distribution of 2505 L (CV% 93%), Dasatinib achieves extensive tissue distribution. It binds substantially to plasma proteins (approximately 96%), while its active metabolite demonstrates similar binding characteristics (93%).

Metabolism

Dasatinib undergoes metabolism primarily through the CYP3A4 enzyme pathway. While an active metabolite is formed (representing about 5% of the AUC of Dasatinib), it typically plays a minimal role in the overall therapeutic effect. Additional enzymes involved in metabolism include FMO-3 and UGT.

Elimination

With a terminal half-life of 3-5 hours and mean oral clearance of 363.8 L/hr, Dasatinib is primarily eliminated through fecal excretion (85% of administered dose), with only 4% recovered in urine. Only 19% of the fecal elimination represents unchanged Dasatinib.

Dosage and Administration

Dasatab 100 mg represents the standard adult dose for chronic phase CML and is administered as follows:

Adult Dosing:

• Chronic Phase CML: 100 mg once daily (standard dose)
• Accelerated Phase CML, Blast Phase CML, or Ph+ ALL: 140 mg once daily (requiring combination of tablets)

Tablets should always be swallowed whole, not crushed, cut, or chewed, as tablet manipulation reduces bioavailability. Dasatab can be taken flexibly with or without food, either morning or evening.

Pediatric Dosing:

For pediatric patients, dosing is based on body weight:

• 10 to <20 kg: 40 mg daily
• 20 to <30 kg: 60 mg daily
• 30 to <45 kg: 70 mg daily
• ≥45 kg: 100 mg daily (standard adult dose)

Regular weight assessment and dose adjustment every 3 months are essential for pediatric patients to ensure appropriate dosing as they grow.

Clinical Considerations and Monitoring

Drug Interactions

Several important drug interactions require clinical attention:

• Strong CYP3A4 Inhibitors (ketoconazole, itraconazole, clarithromycin, etc.): May increase Dasatab concentrations, potentially enhancing toxicity risk. Avoid when possible; consider dose reduction if coadministration is necessary.
• Strong CYP3A4 Inducers (rifampin, phenytoin, carbamazepine, etc.): May decrease Dasatab concentrations, potentially reducing efficacy. Consider alternative medications or Dasatab dose increases when coadministration is unavoidable.
• Gastric Acid Reducing Agents: H2 antagonists and proton pump inhibitors should be avoided. If acid-reducing therapy is necessary, antacids should be administered at least 2 hours before or after Dasatab.

Safety Profile and Monitoring

Patients receiving Dasatab 100 mg require monitoring for several potential adverse effects:

• Myelosuppression: Regular complete blood counts are essential – every 2 weeks for 12 weeks, then every 3 months for chronic phase CML; weekly for 2 months, then monthly for advanced phase disease. Temporary discontinuation or dose reduction may be necessary.
• Bleeding Risk: Caution is warranted, particularly with concurrent antiplatelet or anticoagulant medications.
• Fluid Retention: Monitor for signs of pleural effusion, pulmonary edema, or peripheral edema. Management may include diuretics, short courses of steroids, or in severe cases, thoracentesis.
• Cardiac Effects: Patients should be evaluated for cardiac dysfunction and QT prolongation risks, particularly those with pre-existing cardiac conditions or electrolyte abnormalities.
• Pulmonary Arterial Hypertension: Though rare, this serious complication requires assessment for symptoms like dyspnea, fatigue, hypoxia, and fluid retention. If confirmed, permanent discontinuation is recommended.
• Dermatologic Reactions: Severe cases including Stevens-Johnson syndrome require immediate medical attention and drug discontinuation.
• Tumor Lysis Syndrome: More common in advanced disease; requires prophylactic hydration, uric acid control, and electrolyte monitoring.

Special Population Considerations

Pregnancy and Lactation

Dasatinib may cause fetal harm when administered during pregnancy. Women of reproductive potential should use effective contraception during treatment and for 30 days following the final dose. Breastfeeding is not recommended during treatment and for 2 weeks after the final dose.

Pediatric Use

While effective for pediatric patients, careful monitoring of bone growth and development is essential, as Dasatinib may affect these processes.

Hepatic Impairment

Due to its primary hepatic metabolism, caution is advised in patients with liver dysfunction.

Product Quality and Manufacturing

Eskayef Pharmaceuticals Ltd., with over three decades of pharmaceutical manufacturing excellence, produces Dasatab 100 mg under stringent quality control protocols. Since 1990, when Transcom Group acquired the Bangladesh operations of SK&F USA, Eskayef has established itself as a premium manufacturer of critical medications, including specialized oncology products like Dasatab.

Global Availability and Access

Through Saif Pharma’s extensive distribution network spanning 60+ countries including the United States, Canada, Saudi Arabia, UAE, China, India, and Pakistan, Dasatab 100 mg is available to patients worldwide. Established in 2014, Saif Pharma has built its reputation on providing high-quality, affordable oncology medications, helping improve treatment access for patients with challenging hematologic malignancies.

Storage and Handling

To maintain potency and stability, Dasatab 100 mg should be stored below 30°C in a dry place, protected from light, and kept out of reach of children.

Conclusion

Dasatab 100 mg (Dasatinib) represents a significant advancement in the treatment of Philadelphia chromosome-positive leukemias. As the standard adult dose for chronic phase CML, it provides powerful inhibition of multiple cancer-promoting pathways while overcoming common resistance mechanisms. When prescribed and monitored appropriately, this medication offers hope and improved outcomes for patients with these challenging hematologic malignancies.

For more information about Dasatab 100 mg and other oncology treatments, please visit www.saifpharma.com or consult with your healthcare professional. Trust in Eskayef’s manufacturing excellence and Saif Pharma’s global distribution expertise to deliver this critical medication to patients worldwide.