Vocabria Drug Interactions

Vocabria tablets/injection, in combination with rilpivirine tablets/injection, are indicated for the treatment of HIV-1, therefore, the prescribing information for rilpivirine tablets/injection should be consulted for associated interactions.
Effect of other medicinal products/agents on the pharmacokinetics of cabotegravir: Cabotegravir is primarily metabolised by uridine diphosphate glucuronosyl transferase (UGT) 1A1 and to a lesser extent by UGT1A9. Medicinal products which are strong inducers of UGT1A1 or UGT1A9 are expected to decrease cabotegravir plasma concentrations leading to lack of efficacy (see Contraindications and Table 16 as follows). In poor metabolizers of UGT1A1, representing a maximum clinical UGT1A1 inhibition, the mean AUC, C_max and C_tau of oral cabotegravir increased by up to 1.5-fold. The impact of a UGT1A1 inhibitor may be slightly more pronounced, however, considering the safety margins of cabotegravir, this increase is not expected to be clinically relevant. No dosing adjustments for Vocabria are, therefore, recommended in the presence of UGT1A1 inhibitors (e.g. atazanavir, erlotinib, sorafenib).
Cabotegravir is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), however, because of its high permeability, no alteration in absorption is expected when co-administered with either P-gp or BCRP inhibitors.
Effect of cabotegravir on the pharmacokinetics of other medicinal products: In vivo, cabotegravir did not have an effect on midazolam, a cytochrome P450 (CYP) 3A4 probe. In vitro, cabotegravir did not induce CYP1A2, CYP2B6, or CYP3A4.
In vitro, cabotegravir inhibited the organic anion transporters (OAT) 1 (IC₅₀=0.81 μM) and OAT3 (IC₅₀=0.41 μM). Therefore, caution is advised when co-dosing with narrow therapeutic index OAT1/3 substrate drugs (e.g. methotrexate).
Based on the in vitro and clinical drug interaction profile, cabotegravir is not expected to alter concentrations of other anti-retroviral medications including protease inhibitors, nucleoside reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, integrase inhibitors, entry inhibitors and/or ibalizumab.
The drug interaction data provided in Table 16 is obtained from studies with oral cabotegravir (increase is indicated as "↑", decrease as "↓", no change as "↔", area under the concentration versus time curve as "AUC", maximum observed concentration as "C_max", concentration at end of dosing interval as "Cτ").
Suspension for injection: Vocabria and rilpivirine injections are intended for use as a complete regimen for the treatment of HIV-1 infection and should not be administered with other antiretroviral medicinal products for the treatment of HIV. The following information regarding drug-drug interactions with other antiretroviral medicinal products is provided in the event that Vocabria and rilpivirine injections are stopped and initiation of an alternative antiviral therapy is necessary (see Precautions).
No drug interaction studies have been performed with cabotegravir injection. (See Table 16.)

Click on icon to see table/diagram/image