VELEXBRU TIRABRUTINIB HYDROCHLORIDE盐酸替拉布鲁替尼

Velexbru indications
For the treatment of relapsed or refractory primary central nervous system lymphoma (PCNSL).

Disease background:
Primary central nervous system lymphoma is a malignant lymphoma that is confined to the brain and spinal cord (including the eyes) at the onset. Clinical manifestations vary depending on the location of the lesion and include local neuropathy, neuropsychiatric symptoms, symptoms related to increased intracranial pressure, epileptic seizures, eye symptoms, headache, movement disorders, cranial neuropathy and radiculopathy.

Velexbru ingredients and specifications
Active ingredient: tirabrutinib hydrochloride
Dosage form: 80 mg/tablet (oral tablet)
Velexbru mechanism of action
Target action: As a highly selective oral BTK inhibitor, it inhibits the survival and proliferation of malignant B cells by blocking BTK, a key mediator in the B cell receptor (BCR) signaling pathway.
Therapeutic basis: The BCR signaling pathway is continuously activated in B cell non-Hodgkin’s lymphoma, and inhibition of BTK can exert an anti-tumor effect.
Velexbru global approval status
Japan PMDA: On March 25, 2020, the world’s first BTK inhibitor approved for relapsed/refractory PCNSL (there is no standard treatment for this indication).
Velexbru Usage and Dosage
Standard dose: 480 mg (6 tablets) once a day, taken on an empty stomach.
Dose adjustment: needs to be adjusted individually according to the patient’s tolerance.
Medication requirements: swallow the whole tablet, do not break, crush or chew.
Velexbru adverse reactions
Common adverse reactions (≥10%):

Rash
Vomiting
Neutropenia
Anemia
Leukopenia
Serious adverse reactions:

Infection (such as pneumonia)
Bleeding
High fever
Serious skin reactions
Velexbru contraindications and people who should use with caution
Absolute contraindications: those who are allergic to this product.
Careful evaluation is required:

Patients with active infection

Bone marrow suppression

Hepatitis B virus carriers or past infections (HBsAg negative but HBcAb/HBsAb positive)

Abnormal liver function

Pregnant/lactating women (contraceptive measures are required)

Velexbru clinical research data

Based on the ONO-4059-02 trial (a multicenter phase I/II study in Japan, 44 patients with relapsed/refractory PCNSL):

Overall response rate (ORR): 52.9% (9/17 cases) in the 480 mg fasting group.

Grade 3-4 adverse events: neutropenia, leukopenia, and hypertriglyceridemia (11.8% each).

Velexbru drug interactions

CYP enzyme-affecting drugs: dose adjustment is required for combined use with strong CYP3A inhibitors/inducers.

Anticoagulants/antiplatelets: increased risk of bleeding.

Velexbru precautions

Dietary restrictions: avoid grapefruit and its products, and take the drug on an empty stomach (1 hour before or 2 hours after a meal).
Infection monitoring: See a doctor immediately if you have symptoms such as fever and cough.
Vaccination: Live vaccines are prohibited, and the effectiveness of inactivated vaccines may be reduced.
Fertility risks: Contraception is required during treatment and for at least 1 week after the last dose.
Laboratory monitoring: Regularly check blood routine, liver function and hepatitis B virus markers.
Velexbru missed dose treatment
If you remember to miss a dose on the same day, you should take it immediately; if it is close to the next dose, skip it, and double dose compensation is prohibited.
Velexbru storage conditions
Store at room temperature (15-30°C), protect from light and moisture, and keep out of reach of children.