Elexacaftor and tezacaftor are CFTR correctors that bind to different sites on the CFTR protein and have an additive effect in facilitating the cellular processing and trafficking of F508del-CFTR to increase the amount of CFTR protein delivered to the cell surface compared to either molecule alone. Ivacaftor potentiates the channel open probability (or gating) of the CFTR protein at the cell surface. The combined effect of elexacaftor, tezacaftor and ivacaftor is increased quantity and function of F508del-CFTR at the cell surface, resulting in increased CFTR activity as measured by CFTR mediated chloride transport.
This medicinal substance has been classified in the anatomical therapeutic chemical (ATC) classification according to its main therapeutic use as follows:
| ATC code | Group title | Classification |
|---|---|---|
| R07AX32 | Ivacaftor, tezacaftor and elexacaftor | R Respiratory system → R07 Other respiratory system products → R07A Other respiratory system products → R07AX Other respiratory system products |
Competent medicine agencies globally have authorized commercialization of this active ingredient according to these medication package inserts (MPIs):
| Title | Information Source | Document Type | |
|---|---|---|---|
| KAFTRIO Granules | European Medicines Agency (EU) | MPI, EU: SmPC | |
| KAFTRIO Film-coated tablet | European Medicines Agency (EU) | MPI, EU: SmPC |
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