Table 6.
Drug | Study description | Sample size and genotype distributions | PK results in relation to CYP2C8 genotype | Covariates | Ref. |
---|---|---|---|---|---|
Ibuprofen | 400 mg single-dose PK |
CYP2C8*1/*1, n = 9 CYP2C8*1/*3, n = 10 CYP2C8*3/*3, n = 6 |
↓R-ibuprofen CL ↑ in *1/*3 and *3/*3 vs *1/*1 | CYP2C9 genotype was also determined for each subject | [68] |
Ibuprofen | 400 mg single-dose PK |
CYP2C8*1/*1, n = 93 CYP2C8*1/*3, n = 35 CYP2C8*3/*3, n = 2 |
↓Ibuprofen CL in *1/*3 and *3/*3 vs *1/*1 ↓R- and S-ibuprofen CL with *3 allele vs *1/*1 | CYP2C9 genotype was also determined for each subject | [69] |
Ibuprofen | 600 mg single-dose PK (cross-over bioequivalence study |
CYP2C8*1/*1, n = 43 CYP2C8*1/*2, n = 3 CYP2C8*1/*3, n = 11 CYP2C8*1/*4, n = 10 CYP2C8*3/*3, n = 2 |
↑R-ibuprofen CL in *1/*3 vs *1/*1 | CYP2C9 genotype was also determined for each subject Weight-adjusted clearance was also assessed | [70] |
Diclofenac | 50 mg single-dose PK |
CYP2C8*1/*1, n = 71 CYP2C8*1/*3, n = 19 CYP2C8*1/*4, n = 7 CYP2C8*3/*3, n = 5 |
↑Urinary ratio of parent to metabolite in *3 and *4 carriers vs *1/*1 | None reported | [73] |
Tenoxicam | 20 mg single-dose PK (cross-over bioequivalence study) |
CYP2C8*1/*1, n = 10 CYP2C8*1/*3, n = 5 CYP2C8*1/*4, n = 2 CYP2C8*3/*3, n = 1 |
No association between CYP2C8 polymorphisms and PK | Analysis of variance which included confounders such as age, sex, menstrual cycle phase, body weight and formulation of drug CYP2C9 genotype was also determined for all subjects | [77] |
CL: Oral clearance; PK: Pharmacokinetics.