Is Capecitabine a Tablet?
Yes, capecitabine is administered orally as a tablet, not by injection. 1
Formulation Details
Capecitabine is supplied as film-coated tablets for oral administration in two strengths 1:
- 150 mg tablets (light peach-colored, biconvex, oblong)
- 500 mg tablets (peach-colored, biconvex, oblong)
The tablets contain inactive ingredients including anhydrous lactose, croscarmellose sodium, hydroxypropyl methylcellulose, microcrystalline cellulose, magnesium stearate, and purified water, with a film coating containing hydroxypropyl methylcellulose, talc, titanium dioxide, and synthetic yellow and red iron oxides. 1
Clinical Significance of Oral Administration
Capecitabine was specifically designed as an oral fluoropyrimidine prodrug to replace intravenous 5-fluorouracil (5-FU) administration. 2 This design offers several practical advantages:
- Eliminates need for continuous infusion devices that are required for 5-FU, reducing complications associated with central venous catheters 3, 4
- Provides greater patient convenience with home administration rather than hospital-based infusion 5, 4
- Reduces hospitalization time compared to bolus fluorouracil and leucovorin therapy 5
Standard Dosing Regimens
The typical oral dosing schedule across multiple cancer types is 2:
- 1,250 mg/m² orally twice daily for days 1-14
- Followed by a 7-day rest period
- Repeated every 3 weeks
In combination regimens (such as CAPEOX), the dose is typically reduced to 1,000 mg/m² orally twice daily for days 1-14. 2
Mechanism Supporting Oral Route
Capecitabine achieves nearly 100% bioavailability after oral administration, making the oral route highly effective. 3, 4 The drug is converted to 5-FU through a three-step enzymatic pathway, with the final conversion occurring preferentially in tumor tissue via thymidine phosphorylase, which is present at higher concentrations in malignant compared to normal tissue. 3, 5
Common Pitfall to Avoid
Do not confuse capecitabine with 5-FU/leucovorin, which requires continuous intravenous infusion. 2 While both are fluoropyrimidines with similar mechanisms of action, capecitabine's oral formulation and tumor-preferential activation distinguish it from its intravenous predecessor. 2, 3