Avatrombopag (Doptelet) is an oral small-molecule thrombopoietin receptor agonist (TPO-RA) that effectively increases preoperative platelet levels in patients with chronic liver disease (CLD) and improves persistent thrombocytopenic purpura (ITP).
Avatrombopag (Doptelet) Indications
Chronic Liver Disease-Related Thrombocytopenia
The FDA has approved it for the treatment of thrombocytopenia in patients with chronic liver disease scheduled for invasive procedures.
Avatrombopag (Doptelet) Dosage and Administration
1. Patient Monitoring
Platelet counts should be measured before starting treatment, and the measurement should be performed no more than 2 days before the planned procedure.
2. Administration Method
(1) Oral Administration
Start 8-14 days before the scheduled procedure, take once daily for 7 consecutive days; the patient should undergo the procedure 2-8 days after the last dose.
(2) Not Affected by Meals
The medication is not affected by food intake (can be taken on an empty stomach or with food).
3. Regular Dosage
Take 3 mg orally once daily for 7 consecutive days.
4. Missed Dosage Management
If a dose is missed, take it immediately upon remembering it on the same day; take the next dose at the scheduled time the following day (do not take double the dose at once).
Common Adverse Reactions of Avatrombopag (Doptelet)
Headache.
Precautions for Avatrombopag (Doptelet)
Thrombosis/Thromboembolic Complications
Thrombopoietin receptor agonists (TPO-RAs), including avatrombopag (Doptelet), have been observed in patients with chronic liver disease as associated with thrombosis and thromboembolic complications.
(1) For patients with known thromboembolic risk factors (such as hereditary thrombotic predisposition, including factor VLeiden mutation, prothrombin 20210A mutation, antithrombin deficiency, protein C or protein S deficiency, etc.), the potential for increased risk should be assessed.
(2) Avatrombopag (Doptelet) should only be used in patients with active thrombosis, a history of thrombosis, or no hepatic blood flow if the potential benefit outweighs the potential risk.
Special Populations for Avatrombopag (Doptelet)
1. Pregnant Women
There are currently insufficient human study data; pregnant women should be informed of the potential risks of avatrombopag (Doptelet) to the fetus.
2. Lactating Women
Avatrombopag (Doptelet) is distributed in rat milk, but it is unclear whether it is distributed in human milk. Women are advised to avoid breastfeeding during treatment and for at least 28 days after the last dose.
3. Pediatric Patients
The safety and efficacy of avatrombopag (Doptelet) in pediatric patients have not been established.
4. Elderly Patients
There is currently a lack of sufficient research data on patients aged 65 years and older, making it impossible to determine whether there are differences in response between elderly patients and younger adults. However, existing data do not show any clinically significant differences in response between the two groups.
5. Patients with Hepatic Impairment
(1) Pharmacokinetics were not significantly altered in patients with mild to moderate hepatic impairment (Child-Pugh A or B).
(2) Peak plasma concentrations and systemic exposures were reduced by 20%-30% in patients with severe hepatic impairment (Child-Pugh C) compared to patients with mild to moderate hepatic impairment.
6. Patients with Renal Impairment
(1) Pharmacokinetics were not significantly altered in patients with mild to moderate renal impairment (creatinine clearance ≥30 mL/min).
(2) Pharmacokinetics in patients with severe renal impairment (creatinine clearance <30 mL/min) have not been established.
Avatrombopag (Doptelet) Drug Interactions
1. Drugs Containing Polyvalent Cations
Antacids and mineral supplements, such as antacids and mineral supplements, have no clinically significant effect on avatrombopag (Doptelet) exposure.
2. Specific Drugs
When used in combination with avatrombopag (Doptelet), such as calcium carbonate, cyclosporine, and midazolam, there were no significant changes in mutual exposure.
Avatrombopag (Doptelet) Pharmacokinetics
Absorption
Bioavailability
The pharmacokinetics of avatrombopag (Doptelet) are dose-dependent within the single-dose range of 1-50 mg.
After multiple doses, steady-state plasma concentrations were reached on day 5, with a systemic accumulation ratio of approximately 2.
Peak plasma concentrations of avatrombopag (Doptelet) occur within 6-8 hours after oral administration.
Onset of Action
The average time to peak platelet count is 12 days.
Food Effects
A high-fat diet has no effect on the pharmacokinetics of avatrombopag (Doptelet).
Avatrombopag (Doptelet) Storage Conditions
Oral tablets
Storage temperature: 20-25℃ (permissible fluctuations within the range of 15-30℃).
Storage requirements: Store in the original packaging to avoid damage that could affect drug stability.
