Saquinavir/r (1000/100mg) levels reduced when taken fasted and should be taken with food

Simon Collins, HIV i-Base

Marta Boffito and colleagues from the Chelsea and Westminster Hospital, compared absorption of saquinavir 500mg (dosed at 1000mg SQV with 100mg RTV, twice daily) when taken with a high calorie fat-containing meal (~ 1070kcal; 46-66g of fat), to when taken under fasted conditions. [1] An interim analysis of 10/22 patients who completed this cross-over study, where three consecutive doses were taken in either fed/fasted or fasted/fed state, separated by one week.

Administration of SQV/r under fasted conditions resulted in an approximate 70% decrease in SQV

PK parameters, and are detailed in Table 1. There was no significant change in ritonavir PK. The researchers concluded that saquinavir/r should be taken with food in order to ensure maximum therapeutic exposure.

Table 1: Saquinavir levels (fed and fasted)

Fed Fasted
AUC ng.h/mL 38,927 11,478
Cmax ng/mL 6,399 1,587
Ctrough ng/mL 1,294 373


Boffito M et al. Effect of a fat-containing meal on the pharmacokinetic (PK) profile of saquinavir 500mg tablet/ritonavir (SQV/r) 1000/100 mg BID in HIV-infected individuals. 7th International Workshop on Clinical Pharmacology of HIV Therapy, 20-22 April 2006, Lisbon. Abstract 66.

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