99% Ruxolitinib phosphate CAS 1092939-17-7 Pharmaceutical Grade API Raw Power

Ruxolitinib Phosphate More Info

Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable, potent, and selective Janus kinase inhibitor, assigned the CAS Registry Number 1092939-17-7. Its molecular structure incorporates a pyrrolo[2,3-d]pyrimidine core engineered to bind specifically and reversibly to the ATP-binding site of JAK1 and JAK2. The formation of the phosphate salt is a pharmaceutical strategy to optimize the physicochemical properties of the active compound, such as its solubility and formulation stability, thereby ensuring reliable drug delivery and consistent bioavailability in the body.

The primary mechanism of action for this drug is the selective inhibition of Janus kinases 1 and 2. By blocking these intracellular tyrosine kinases, it potently interrupts the JAK-STAT signaling pathway, which is critical for the signal transduction of numerous cytokines and growth factors, particularly those utilizing the common gamma chain receptor, such as interleukin-6 and erythropoietin. This inhibition reduces downstream pro-inflammatory and proliferative signaling, thereby directly addressing the dysregulated cytokine signaling and immune activation that drives disease activity in certain myeloproliferative neoplasms.

The main clinical applications of ruxolitinib phosphate are in the treatment of myeloproliferative neoplasms. It is approved for intermediate or high-risk myelofibrosis, whether primary or secondary to polycythemia vera or essential thrombocythemia. It is also indicated for the treatment of polycythemia vera in patients who have had an inadequate response to or are intolerant of hydroxyurea. Through its targeted action, it achieves significant reductions in spleen volume, alleviates debilitating disease-related symptoms such as night sweats and bone pain, and improves overall quality of life.

This medication is administered orally in tablet form, typically twice daily. Its pharmacokinetic profile shows rapid absorption, with peak plasma concentrations reached within one to two hours post-dose. It is metabolized primarily in the liver by the cytochrome P450 3A4 enzyme system, necessitating dose adjustments when co-administered with potent CYP3A4 inhibitors or inducers. Regular monitoring of blood counts is essential, as myelosuppression—manifesting as anemia, thrombocytopenia, and neutropenia—is its primary dose-limiting toxicity and is commonly observed during therapy.

The safety profile of ruxolitinib is characterized by its immunosuppressive and myelosuppressive effects. Common adverse reactions include anemia and thrombocytopenia, infections (including herpes zoster reactivation), bruising, dizziness, and headache. Due to its mechanism, it carries warnings for increased risk of serious infections, tuberculosis reactivation, and potential for secondary malignancies. Its benefit in controlling debilitating symptoms must be carefully weighed against these risks, with treatment requiring ongoing clinical and laboratory monitoring by a specialist.

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