Drug-Coated Balloons: Medications Used
Paclitaxel is the only clinically proven drug used on drug-coated balloons that effectively inhibits restenosis in both coronary and peripheral applications. 1, 2, 3
Primary Drug: Paclitaxel
Paclitaxel remains the sole medication with demonstrated clinical efficacy when delivered via drug-coated balloons. 3, 4 The drug works through several mechanisms:
Paclitaxel is a lipophilic, antiproliferative agent that exhibits rapid intracellular uptake and irreversible binding to microtubules, altering cell structure and reducing proliferation, migration, and signaling. 4
Standard paclitaxel doses on drug-coated balloons range from 2-3.5 μg/mm² balloon surface, though newer formulations use up to 6 μg/mm² to increase drug transfer to vessel walls. 5
The drug is typically mixed with iopromide (a hydrophilic X-ray contrast medium) as the coating matrix, which has proven highly effective in multiple randomized controlled trials. 4
Clinical Applications by Vascular Territory
Peripheral Artery Disease
Multiple prospective randomized trials demonstrate that paclitaxel-coated balloons significantly improve patency rates compared to conventional balloon angioplasty in peripheral applications. 1, 2
Primary patency rates at 6-12 months range from 38-63% for dialysis access maintenance when treated with paclitaxel drug-coated balloons. 1
Coronary Artery Disease
For coronary in-stent restenosis, paclitaxel drug-coated balloons are recommended as a reasonable alternative to drug-eluting stents, particularly when additional stent layers are undesirable. 2, 6
The European Society of Cardiology provides Class IIa, Level B recommendation for drug-eluting balloons specifically for in-stent restenosis after prior bare metal stent implantation. 1, 2
Failed Alternative Drugs
Despite extensive preclinical testing, no alternative drugs have proven effective as drug-coated balloon coatings. 3 The following drugs failed to reduce late lumen loss compared to uncoated balloons in porcine models:
- Arsenic trioxide (late lumen loss 0.87 ± 0.44 mm vs. 1.07 ± 0.60 mm for uncoated balloons) 3
- Betamethasone dipropionate (1.00 ± 0.54 mm) 3
- Bortezomib (1.74 ± 0.46 mm) 3
- Methotrexate (1.09 ± 0.72 mm) 3
- Thalidomide (1.59 ± 0.55 mm) 3
- Epothilones (0.86 ± 0.61 mm) 3
In contrast, paclitaxel-coated balloons reliably reduced in-stent stenosis with late lumen loss of only 0.36 ± 0.25 mm. 3
Limus Drugs Under Investigation
Limus drugs (sirolimus, everolimus) are currently being explored as potential alternatives to paclitaxel for balloon coating, though clinical proof of efficacy remains lacking. 3 These drugs have proven highly effective when delivered via drug-eluting stents with polymer carriers 1, but their utility on drug-coated balloons without sustained-release mechanisms has not been established.
Critical Safety Warning
The FDA issued a warning in January 2019 about possible increased long-term mortality rates among peripheral artery disease patients treated with paclitaxel-coated balloons compared to control devices. 1, 2
Continued use is permitted under current standard of care with mandatory patient discussion of risks and benefits, including possible increased risk of long-term mortality. 1, 2
This warning requires careful patient selection and informed consent before using paclitaxel-coated devices in peripheral applications. 2, 6
Practical Considerations
Drug transfer efficiency varies with coating formulation, with 5-29% of the initial paclitaxel dose successfully transferred to vessel walls during balloon inflation. 3
Dual antiplatelet therapy for 2-6 months is recommended after drug-coated balloon procedures for peripheral artery disease revascularization. 2