Analysis of the pharmacological efficacy and main clinical effects of Pitobrutinib/Pitobrutinib (Zepali)

Pitobrutinib/Pirtobrutinib is an oral Bruton's tyrosine kinase (BTK) inhibitor and belongs to a new generation of targeted anti-tumor drugs. It reversibly binds to the BTK enzyme, effectively blocking the BCR (BCR) signaling pathway, thereby inhibiting the proliferation and survival of malignant B cells. This mechanism is different from traditional irreversible BTK inhibitors, giving pitubrutinib an advantage in providing sustained anti-tumor effects in patients with drug-resistant mutations or who are unable to tolerate traditional BTK inhibitors.

In clinical application, Pitobrutinib is mainly used to treat relapsed or refractory B cell malignancies, including chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), etc. It can effectively control disease progression by inhibiting BTK signaling, reducing the proliferation rate of tumor cells and inducing apoptosis. Compared with traditional BTK inhibitors, pitubrutinib shows higher selectivity and lower off-target effects, reduces the risk of common adverse reactions such as arrhythmia and bleeding, and improves patient tolerance.

Pitubrutinib also demonstrates significant efficacy advantages in patient management. Clinical studies have shown that long-term use of pitubrutinib can significantly extend progression-free survival (PFS), improve overall response rate (ORR), and is also effective in drug-resistant patients carrying C481S and other BTK mutations. This provides a new treatment option for patients who have failed previous BTK inhibitor treatment, making it occupy an important position in the personalized treatment of B-cell lymphoma.

In addition, the oral administration method of pitubrutinib provides patients with convenience while performing well in terms of drug safety. Common adverse reactions include mild to moderate fatigue, diarrhea, joint pain and mild decrease in platelets, most of which can be alleviated by adjusting the dose or symptomatic treatment. Doctors should pay attention to changes in the patient's blood routine and liver and kidney function during medication, and adjust the dosage according to the specific condition to ensure a balance between drug efficacy and safety and achieve the best clinical treatment effect.

Reference materials:https://pmc.ncbi.nlm.nih.gov/articles/PMC10841293/