Olverembatinib is a targeted therapy drug indicated for patients with specific types of leukemia, with olverembatinib as its primary active ingredient. Belonging to the class of small-molecule protein tyrosine kinase inhibitors, it exerts its therapeutic effect by precisely inhibiting the activity of Bcr-Abl tyrosine kinase.
Indications
This product is indicated for adult patients with chronic myeloid leukemia (CML) who are resistant to existing tyrosine kinase inhibitors (e.g., imatinib, dasatinib, etc.) and have been confirmed to harbor the T315I gene mutation by professional genetic testing. It can be used for both the chronic phase (relatively stable stage) and accelerated phase (disease progression stage) of the disease.
Specifications
Each tablet contains 10 mg of olverembatinib as the active ingredient. The dosage is usually marked on the surface of the tablet to facilitate patients in confirming the dosage to be taken.
Dosage and Administration
This is a prescription-only medicine and must be used under the full guidance of a physician experienced in the diagnosis and treatment of leukemia. The dosage regimen shall not be adjusted without medical supervision.
Administration method
Must be administered with meals (may be taken with breakfast, lunch, or dinner). The tablets should be swallowed whole and must not be split or crushed. It is recommended to take the medicine at a fixed time every day (e.g., early morning or evening) to maintain regular medication intake.
Recommended dosage
40 mg (4 tablets) once every other day until disease progression or intolerable adverse drug reactions occur.
Missed dose management
If a missed dose is remembered within 4 hours, take the dose immediately. If more than 4 hours have elapsed, skip the missed dose and resume the regular dosing schedule; do not take a double dose to make up for the missed one.
Vomiting management
In case of vomiting after administration, no supplementary dose is required.
Efficacy assessment
For patients in the chronic phase, if blood indicators fail to return to normal after 3 consecutive months of treatment; for patients in the accelerated phase, if there is no improvement in disease condition after 6 consecutive months of treatment, the attending physician shall evaluate whether to continue the medication.
Contraindications
This product is contraindicated in the following populations:
Patients hypersensitive to olverembatinib or any component of this product;
Patients with severe hepatic impairment.
Precautions
Special Populations Requiring Cautious Use
Pregnant women, lactating women, patients with moderate to severe hepatic and renal impairment, and individuals who need prolonged exposure to sunlight should use this product with caution.
Pre-treatment Preparation
The presence of the T315I gene mutation must be confirmed by professional testing before initiating treatment. Patients who are taking other medications (including traditional Chinese medicines and health supplements) or have underlying diseases should inform the physician in advance to avoid potential drug interactions.
Monitoring and Protection During Treatment
Regular monitoring of hepatic and renal function: Liver function should be tested once every 4 weeks during treatment. For patients with abnormal hepatic or renal function, the monitoring frequency shall be adjusted according to the physician’s instructions.
Sun protection: Effective sun protection measures should be taken during the treatment period to avoid prolonged exposure to direct sunlight, thereby reducing the risk of cutaneous adverse reactions.
Medication inspection: If there is any abnormality in the color, shape, or odor of the tablets, discontinue use immediately and contact the physician.
Combined Medication Instructions
Given its unique and targeted mechanism of action, this product must not be combined with other medications without medical approval. Clinicians will formulate personalized treatment plans based on the patient’s individual condition, combining chemotherapy, immunotherapy, supportive care, or other therapeutic modalities. When combination therapy is deemed necessary under special circumstances, it must be carried out under close monitoring to prevent drug interactions that may affect efficacy or increase the risk of adverse reactions.
Drug Interactions
Concomitant use with CYP3A4 inhibitors
May significantly increase the plasma concentration of this product, with a 76% increase in peak plasma concentration and a 159% increase in total exposure. Dose adjustment and close monitoring must be performed strictly in accordance with the physician’s instructions.
Concomitant use with CYP3A4 inducers
May lead to a significant decrease in the plasma concentration of this product, with a 61% reduction in peak plasma concentration and a 75% reduction in total exposure, which may compromise therapeutic efficacy. Concomitant use should be avoided or the treatment plan adjusted accordingly.
Concomitant use with drug transporter inhibitors
May affect the absorption of this product in the body; use under the guidance of a physician with appropriate monitoring is recommended.
Concomitant use with gastric acid inhibitors: This product dissolves more readily in an acidic environment. Concomitant use with gastric acid inhibitors may reduce its efficacy and should be avoided.
Adverse Reactions
Common Adverse Reactions (Incidence > 10%)
Including thrombocytopenia, skin hyperpigmentation, anemia, hypertriglyceridemia, leukopenia, proteinuria (increased urine foaming), hypocalcemia, neutropenia, elevated blood bilirubin (jaundice indicator), elevated γ-glutamyl transferase (liver enzyme abnormality), hyponatremia, fever, myalgia, hyperglycemia, hypokalemia, rash, limb soreness, tachycardia, etc.
Among these, 60.5% of patients may experience Grade 3 or higher moderate to severe adverse reactions. Moderate to severe adverse reactions with an incidence > 3% include thrombocytopenia, leukopenia, neutropenia, anemia, hypertriglyceridemia, hypertension, and fever.
Serious Adverse Reactions (Incidence 19.4%)
The most common serious adverse reactions include thrombocytopenia (8.5%), anemia (3.1%), and pulmonary infection (1.6%).
Management of Adverse Reactions
Approximately 22.9% of patients require dose reduction due to adverse reactions, primarily caused by thrombocytopenia (14.7%), neutropenia (3.4%), and leukopenia (2.2%). 38.6% of patients require treatment interruption, commonly due to thrombocytopenia (26.3%) and neutropenia (6.3%). In case of any discomfort, contact the physician immediately. Monitor basic indicators such as blood pressure, heart rate, and respiratory rate, and promptly report any abnormal manifestations such as skin ecchymosis, persistent fever, and marked fatigue.
Overdosage
Ingestion of a dose exceeding the recommended amount may affect the hematopoietic system, leading to abnormal blood cell counts. In such cases, close monitoring of blood indicators is required. The physician will adjust the frequency of examinations as appropriate and administer supportive care such as nutritional supplementation and electrolyte regulation.
Discontinuation Criteria
Treatment should be temporarily interrupted or discontinued under the following circumstances. All dosage adjustments must be determined by the physician; patients shall not discontinue or modify the dosage on their own:
Vascular occlusion symptoms
Sudden limb pain, swelling, or skin discoloration—discontinue the medication immediately for observation. After symptom relief, the physician will assess whether to resume treatment.
Significant cytopenia
Conduct regular blood tests. In case of abnormalities, first administer supportive care such as blood transfusion; treatment interruption may be necessary until indicators return to normal.
Hepatic dysfunction
If liver function indicators exceed 2.5 times the upper limit of normal before treatment, treatment should be postponed. If Grade 3 or higher severe abnormalities occur during treatment, discontinue the medication immediately and increase the monitoring frequency until indicators improve to mild abnormalities or return to normal.
Severe hypertension
In case of Grade 3 (systolic blood pressure ≥ 180 mmHg) or Grade 4 hypertension, discontinue treatment until blood pressure stabilizes. The physician will assess subsequent treatment plans.
Other special circumstances
If discomfort occurs after discontinuation, seek medical attention promptly to evaluate whether permanent discontinuation or treatment plan adjustment is required.
