Apixaban (brand name Eliquis®)
Key facts as of 2025
| Item | Information |
|------|-------------|
| Approved dosage forms (oral) | 2.5 mg and 5 mg tablets (immediate‑release). No liquid, IV, or other formulation has been approved for routine clinical use as of 2025. |
| Typical dosing schedule | • 5 mg twice daily (BID) for most indications (stroke prevention in atrial fibrillation, treatment & secondary prevention of DVT/PE, prophylaxis after hip/knee arthroplasty).
• 2.5 mg BID for patients who have at least two of the following: age ≥ 80 yrs, body weight ≤ 60 kg, creatinine clearance ≤ 50 mL/min. |
| Oral bioavailability | • ≈ 50 % when taken orally. (Clinical pharmacology data report an absolute oral bioavailability of 50 ± 7 %.)
• Food effect: No clinically relevant alteration in absorption. Peak plasma concentration (Tmax) occurs 3–5 h after a dose, regardless of food. |
| Half‑life | ~12 h (range 9–15 h, depending on age, weight, and renal function). |
| Protein binding | 87–92 % (predominantly albumin). |
| Metabolism | CYP3A4, CYP3A5, CYP2J2 (minor). Not a major CYP3A4 inducer or inhibitor, but caution with strong inducers or inhibitors. |
| Elimination | ~25 % renal (glomerular filtration), ~75 % non‑renal (mainly hepatic via CYP enzymes). |
Why 50 %?
Apixaban’s oral bioavailability is determined by its limited first‑pass metabolism and relatively low solubility at low plasma concentrations. The FDA labeling (2024–2025) confirms this value:
“Apixaban has an oral bioavailability of approximately 50 %. Absorption is not affected by food. Peak plasma concentration occurs 3–5 h after dosing.”
Because the drug is highly protein‑bound and has a moderate volume of distribution, the 50 % figure is stable across most patient populations and has not changed in the 2024–2025 literature.
What’s new in 2025?
* Generics: Generic versions (2.5 mg and 5 mg tablets) have entered the market, offering similar pharmacokinetic profiles.
* Formulation stability: No new extended‑release or liquid formulations have been approved; the immediate‑release tablets remain the standard.
* Clinical guidance: Updated prescribing information reiterates the same dosage regimens and bioavailability data; no major pharmacokinetic changes have been reported.
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Bottom line
- Dosage form: 2.5 mg and 5 mg oral tablets only.
- Bioavailability: ~50 % orally, unaffected by food.
- No change in 2025 – the pharmacokinetic profile remains the same as earlier years.
If you’re planning therapy or dosing adjustments, always consult the most recent prescribing information or a qualified pharmacist—especially if the patient has renal impairment, is on interacting medications, or is on the edge of the dose‑adjustment criteria.