Category: pharmacological
Aliases: Ketek, HMR-3647
First-in-class ketolide antibiotic — semi-synthetic erythromycin derivative for community-acquired respiratory infections. Strong CYP3A4 inhibitor (more potent than clarithromycin) with predictable QT prolongation. Withdrawn from the US market 2007 after post-marketing reports of severe hepatotoxicity (including fulminant hepatic failure), transient visual disturbances (cycloplegia / diplopia), syncope, and myasthenia gravis exacerbation. Retained in the registry for historical reference and as the textbook example of "post-market signal forced withdrawal" alongside cerivastatin and rofecoxib. PK (Ketek label rev 12/2010, SS 800 mg PO qd × 7d in healthy adults, n=18): Cmax 2.27 ± 0.71 µg/mL, AUC(0-24) 12.5 ± 5.4 µg·h/mL, Tmax 1.0 h (range 0.5-3.0), t½ 9.81 ± 1.9 h, F 57%, Vd 2.9 L/kg IV (V/F derived ≈ 905 L; true V ≈ 516 L with F 0.57), protein binding 60-70%.
PO: 9.81h