tafamidis meglumine + tafamidis

Tafamidis is a first-in-class small molecule developed by Pfizer (initially by FoldRx) for the treatment of transthyretin-mediated amyloidosis (ATTR). It acts as a kinetic stabilizer of the transthyretin (TTR) tetramer. ATTR is a progressive, fatal disease characterized by the dissociation of the TTR tetramer into unstable monomers, which subsequently misfold and aggregate into amyloid fibrils that deposit in various organs, primarily the heart (cardiomyopathy) and peripheral nerves (polyneuropathy). Tafamidis binds with high affinity and selectivity to the two thyroxine-binding sites on the TTR tetramer, preventing its dissociation and thereby inhibiting the amyloidogenic process. The drug is marketed in two orally administered formulations: **tafamidis meglumine (Vyndaqel)**, a salt form, and **tafamidis (Vyndamax)**, the free acid form. Vyndamax (61 mg) was developed as a more convenient, single-capsule alternative to the Vyndaqel (80 mg, administered as four 20 mg capsules) regimen, offering bioequivalent exposure of the active moiety.

Brand names

VyndaqelVyndamax

Other names

2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acidtafamidis free acidtafamidis meglumine salt