Pitobrutinib/Pitobrutinib (Zepali) drug basic information and main parameter description

Pirtobrutinib is a new generation of non-covalent (reversible) Bruton's tyrosine kinase (BTK) inhibitor, mainly used to treat a variety of hematological malignancies derived from B cells. Unlike traditional covalent BTK inhibitors, pitubrutinib does not rely on binding to the C481 site, so it still has potential therapeutic value in patients who have failed previous BTK inhibitor treatments or developed drug-resistant mutations. This property has attracted great attention in the field of relapsed or refractory Bcell lymphoma.

From the perspective of the basic properties of the drug, pitubrutinib is an oral small molecule targeted drug. The administration method is once a day, which is convenient for patients to maintain long-term treatment. The drug inhibits the proliferation and survival of tumor cells by highly selectively inhibiting the BTK signaling pathway and blocking B cell receptor signaling. It has high target selectivity and relatively little impact on other kinases, helping to reduce some non-specific adverse reactions.

In terms of main parameters, pitubrutinib has good oral bioavailability and relatively stable plasma concentration, and is suitable for continuous administration mode. Drugs are mainly metabolized by the liver in the body, involving the CYP enzyme system. Therefore, special attention needs to be paid to potential drug interactions when using potent enzyme inducers or inhibitors together. In clinical studies, its common dosage regimen is fixed dosage for long-term use. The specific dosage needs to be determined by the doctor based on the patient's condition and tolerance.

From the perspective of applicable population and clinical positioning, pitubrutinib is mainly used for patients with B cell tumors, such as mantle cell lymphoma, who have received BTK inhibitor treatment in the past and have poor efficacy or resistance. Overall, this drug takes into account drug resistance management and safety requirements while maintaining the effectiveness of targeted therapy. It is an important supplementary option in the current field of BTK inhibitors, but it still needs to be used and followed up under the guidance of professional doctors.

Keyword tags: Pitobrutinib, BTK inhibitor, oral administration, drug interaction, relapsed lymphoma

Reference materials:https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/216059s002lbl.pdf