Tezacaftor-d6

Tezacaftor-d6 (VX-661-d6) is deuterium labeled Tezacaftor. Tezacaftor (VX-661) is a F508del CFTR corrector. It helps CFTR protein reach the cell surface. However, Ivacaftor (VX-770, HY-13017), a CFTR potentiator, helps to prolong the opening time of cell surface CFTR protein channels. Tezacaftor combining with Ivacaftor, shows potent efficacy against cystic fibrosis and diseases with homozygous for the CFTR Phe508del mutation. Moreover, Elexacaftor (VX-445, HY-111772) is also a CFTR corrector. Elexacaftor-Tezacaftor-Ivacaftor aims at with cystic fibrosis (CF) with at least one Phe508del mutation, often avoids the indication for lung transplantation[1][2][3][4].

Product Specifications

CAS Number

[1961280-94-3]

Product Name Alternative

VX-661-d6

UNSPSC

12352005

Target

CFTR; Isotope-Labeled Compounds

Related Pathways

Membrane Transporter/Ion Channel; Others

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

FC1=C(NC(C2(CC2)C3=CC=C4OC(OC4=C3)(F)F)=O)C=C5C(N(C[C@H](CO)O)C(C(C([2H])([2H])[2H])(CO)C([2H])([2H])[2H])=C5)=C1

Molecular Formula

C26H21D6F3N2O6

Molecular Weight

526.53

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Treatment with VX-661 and Ivacaftor in a Phase 2 Study Resulted in Statistically Significant Improvements in Lung Function in People with Cystic Fibrosis Who Have Two Copies of the F508del Mutation. April 18, 2013|[3]Taylor-Cousar JL, et al. Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del. N Engl J Med. 2017 Nov 23;377 (21) :2013-2023. |[4]Burgel PR, et al. Rapid Improvement after Starting Elexacaftor-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and Advanced Pulmonary Disease. Am J Respir Crit Care Med. 2021 Jul 1;204 (1) :64-73. |[5]Huang Y, et al. Elexacaftor/Tezacaftor/Ivacaftor Improved Clinical Outcomes in a Patient with N1303K-CFTR Based on In Vitro Experimental Evidence. Am J Respir Crit Care Med. 2021 Nov 15;204 (10) :1231-1235.