Terarutinib hydrochloride is a new generation of Bruton tyrosine kinase inhibitor developed by Ono Pharmaceutical Co., Ltd. in Japan.

1、 Drug name

1. Common name: Tirabrutinib Hydrochloride

2. Product Name: Velerbru

3. Drug type: Bruton type tyrosine kinase (BTK) inhibitor

2、 Indications

1. Recurrent or refractory primary lymphoma of the central nervous system.

2. Primary macroglobulinemia and lymphoplasmacytic lymphoma.

3、 Specifications and characteristics

1. Specification: Each tablet contains 80mg of telacitinib.

2. Dosage form: Yellow film coated tablets, with a length of approximately 12.3mm, a short diameter of approximately 5.3mm, a thickness of approximately 3.9mm, and a weight of approximately 250mg.

4、 Main components

1. Active ingredient: Tirabrutinib.

2. Main additives: crystalline cellulose, lactose hydrate, polyvinylpyrrolidone, light anhydrous silicic acid, magnesium stearate, polyvinyl alcohol (partially saponified), titanium oxide, polyethylene glycol 4000, talcum powder, yellow ferric oxide.

5、 Usage and dosage

1. Adult standard dose: 480mg once daily, taken orally on an empty stomach.

2. It should be taken at least 1 hour before meals or 2 hours after meals to avoid food affecting blood drug concentration.

6、 Dose adjustment

1. Reduction stage:

Conventional dose: 480mg.

Level 1 reduction: 320mg.

Level 2 reduction: 160mg.

2. Principles for handling side effects (refer to NCI-CTCAEv4.0):

Grade 4 neutropenia: medication can be resumed after recovery to grade 3 or below, and dosage can be reduced if recurrence occurs.

Grade 3 thrombocytopenia with accompanying bleeding: resume medication after recovering to grade 2 or below.

Grade 4 thrombocytopenia, Grade 3 or above non hematological toxicity (excluding interstitial lung disease and skin disorders): Discontinue medication and restart after recovery.

Skin disorders above level 3: Discontinue medication and restart after recovering to level 2 or below.

Interstitial lung disease grade 2 or 3: Discontinue medication and restart after recovery.

Grade 4 interstitial lung disease or Stevens Johnson syndrome, toxic epidermal necrolysis (TEN): discontinue medication.

7、 Medication precautions

1. Before and after meals: Take on an empty stomach and avoid taking within 1 hour before meals to 2 hours after meals.

2. Omission: It is recommended that if missed, it should be skipped near the next medication time and should not be taken twice (refer to similar medications).

8、 Medication for special populations

1. Co infected individuals: may worsen the infection, caution is required.

2. Individuals with low bone marrow function: may exacerbate the decrease in blood cells.

3. Hepatitis B virus carrier or former infected person: may cause reactivation of the virus, and liver function and viral markers need to be monitored.

4. Patients with liver dysfunction: mainly metabolized by the liver, blood drug concentration may increase, and clinical data is lacking.

5. Women with fertility: contraception is required during medication and within 2 days after discontinuation.

6. Pregnant women: Use only when the benefits of treatment outweigh the risks; Animal experiments have shown risks of fetal death, deformities, and low birth survival rates.

7. Breastfeeding women: Avoid breastfeeding, animal tests have shown that drugs can enter breast milk.

8. Children: No clinical trials have been conducted.

9、 Adverse reactions

1. Common side effects (incidence ≥ 5%): rash (36.4%), neutropenia (22.7%), leukopenia (15.9%), lymphopenia (9.1%), thrombocytopenia (9.1%), nausea, stomatitis, constipation, etc.

2. Major side effects:

Bleeding (frequency unknown).

Infection (pneumonia 4.5%, aspergillus infection 2.3%, etc.), including reactivation of hepatitis B and herpes zoster.

Severe skin disorders (TEN, Stevens Johnson syndrome, erythema multiforme 2.3%, etc.).

Bone marrow suppression (febrile neutropenia, various blood cell reductions).

Allergic reactions (including anaphylactic shock).

Interstitial lung diseases (interstitial pneumonia, pulmonary inflammation, etc.).

Liver dysfunction (AST, ALT, γ - GTP, Al-P, bilirubin elevation, etc.).

10、 Contraindications

1. Patients with a history of allergies to the ingredients of this medication.

11、 Drug interactions

1. Strong or moderate CYP3A inhibitors (such as itraconazole, clarithromycin, posaconazole, etc.) may increase the blood concentration of the drug and enhance side effects.

2. Strong or moderate CYP3A inducers (such as rifampicin, carbamazepine, phenytoin, etc.): may reduce the blood concentration of the drug and weaken its efficacy.

3. Anticoagulants and antiplatelet drugs: may increase the risk of bleeding.

12、 Storage method

1. Store at room temperature.

2. Validity period: 5 years.

3. Aluminum plastic packaging should be stored away from moisture after opening.

13、 Manufacturer

Manufacturing and sales: Ono Pharmaceutical Co., Ltd.

Velexbruinformation