Active Ingredient: Fruquintinib
Fruquintinib as monotherapy is indicated for the treatment of adult patients with metastatic colorectal cancer (mCRC) who have been previously treated with available standard therapies, including fluoropyrimidine-, oxaliplatin-, and irinotecan-based chemotherapies, anti-VEGF agents, and anti-EGFR agents, and who have progressed on or are intolerant to treatment with either trifluridine-tipiracil or regorafenib.
For this indication, competent medicine agencies globally authorize below treatments:
For:
Oral, 5 milligrams fruquintinib, once daily, 21 doses in total, over the duration of 28 days.
The recommended dose of fruquintinib is 5 mg once daily at approximately the same time each day for 21 consecutive days, followed by a 7-day rest period to comprise a complete cycle of 28 days.
Treatment with fruquintinib should be continued until disease progression or unacceptable toxicity occurs.
If a dose is missed by less than 12 hours, it should be taken, and the next dose should be taken as scheduled.
If a dose is missed by more than 12 hours, it should be skipped, and the next dose should be taken as scheduled.
If a patient vomits after taking a dose, the patient should not repeat the dose on the same day but resume the usual dosing as prescribed on the following day.
The dose should be modified based on safety and tolerability. Fruquintinib should be permanently discontinued in patients unable to tolerate a dose of 3 mg once daily. The recommended dose reduction schedule for adverse reactions is provided in Table 1.
Table 1. Recommended fruquintinib dose reduction schedule:
| Dose reduction schedule | Dose and schedule |
|---|---|
| First dose reduction | 4 mg once daily |
| Second dose reduction | 3 mg once daily |
The recommended dose modifications for adverse reactions are provided in Table 2.
Table 2. Recommended dose modification for fruquintinib for adverse reactions:
| Adverse reaction | Severity1 | Dose modification |
|---|---|---|
| Hypertension | Grade 3 | • Withhold if Grade 3 hypertension persists despite initiation or modification of antihypertensive treatment. • If hypertension recovers to Grade 1 or baseline, resume at a reduced dose as per Table 1. If the patient still experiences Grade 3 hypertension after taking 3 mg daily, permanently discontinue. |
| Grade 4 | Permanently discontinue. | |
| Haemorrhagic events | Grade 2 | • Withhold until bleeding fully resolves or recovers to Grade 1. • Resume at a reduced dose as per Table 1. If the patient still experiences Grade 2 haemorrhagic events after taking 3 mg daily, permanently discontinue. |
| Grade ≥ 3 | Permanently discontinue. | |
| Proteinuria | ≥ 2 g/24 hours | • Withhold until proteinuria fully resolves or is < 1 g / 24 hours (Grade 1). • Resume at a reduced dose as per Table 1. If the patient still experiences ≥ 2 g/24 hours proteinuria after taking 3 mg daily, permanently discontinue. Permanently discontinue for nephrotic syndrome. |
| Liver function test abnormalities | Grade 2 or 3 liver function test abnormalities | • Withhold until liver function test abnormality recovers to Grade 1 or baseline. • Resume at a reduced dose as per Table 1. If the patient still experiences Grade 2 or Grade 3 liver function test abnormalities after taking 3 mg daily, permanently discontinue. |
| Grade ≥ 2 elevation (> 3 x ULN) of either alanine aminotransferase (ALT) or aspartate aminotransferase (AST) with concurrent total bilirubin elevation > 2 x ULN in the absence of cholestasis; Grade 4 liver function test abnormalities | Permanently discontinue. | |
| Palmar-plantar erythrodysaesthesia syndrome (PPES) | Grade 2 | • Administer supportive treatment. • Withhold until PPES recovers to Grade 1 or baseline. • Resume at the same dose level. |
| Grade 3 | • Administer supportive treatment. • Withhold until PPES recovers to Grade 1 or baseline. • Resume at a reduced dose as per Table 1. If the patient still experiences Grade 3 PPES after taking 3 mg daily, permanently discontinue. | |
| Other adverse reactions | Grade 3 | • Withhold until the reaction recovers to Grade 1 or baseline. • Resume at a reduced dose as per Table 1. If the patient still experiences Grade 3 other adverse reactions after taking 3 mg daily, permanently discontinue. |
| Grade 4 | Discontinue. Consider resuming at a reduced dose as per Table 1 if the toxicity recovers to Grade 1 or baseline and the potential benefit outweighs the risks. |
1 Graded per national cancer institute common terminology criteria for adverse events, version 5.0 (NCI CTCAE v5).
Fruquintinib can be taken with or without food.
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