Table 2.
Pharmacokinetic properties of mavacamtem, tirzepatide, and vutrisiran
| Drug (route of administration) | F (%) | T max (h) | PPB (%) | Vd (L/kg) | Drug metabolism | t ½ (h) | Renal excretion (%) | Dose (mg) |
|---|---|---|---|---|---|---|---|---|
| Mavacamten (oral) | 80 | 1 | 98 | 9.5 | CYP2C19 (74%), CYP3A4 (18%), and CYP2C9 (8%) | 6–9 days* | 85 | 2.5–15 QD |
| Tirzepatide (s.c.) | 80 | 8–72 | 99 | 0.14 | Proteolytic cleavage of the peptide backbone, β-oxidation of the C20 fatty acid moiety, and amide hydrolysis | 5 days | 0* | 2.5–15 qWeek |
| Vutrisiran (s.c) | 4 (1–12) | 80 | 0.14 | Endonucleases and exonucleases to short nucleotide fragments | 2–6 | 20* | 25 mg once every 3 months |
CYP, cytochrome P450; F, oral bioavailability; H, hours; i.v., intravenous; PPB, plasma protein binding; s.c., subcutaneous; t1/2, drug half-life; Tmax, time to peak plasma levels; Vd, volume of distribution; *, renal excretion without biotransformation (up to 23 days in CYP2C19 poor metabolizers).