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Interaction Report

Report ID: Date Produced: 12 July 2018

Antiretroviral Treatment Co-medications

Abacavir Rifapentine Bictegravir/FTC/TAF (with ATV or DRV) /Cobi/FTC/TAF Elvitegravir/Cobi/FTC/TDF (FTC) Emtricitabine/TAF -uiyk (3TC) Rilpivirine/FTC/TAF Tenofovir-DF (AZT/ZDV)

This report lists the summaries of potential interactions (i.e. "red", "amber" and “yellow” classifications) for the drugs in the table above. Interactions with a "green" or "grey" classification (i.e. no clinically significant interaction or no clear data) have been checked and are listed at the end of this report, but summaries are not shown. For full details of all interactions, see www.hiv-druginteractions.org . Description of the interactions

© Liverpool Drug Interactions Group, University of Liverpool, Pharmacology Research Labs, 1st Floor Block H, 70 Pembroke Place, LIVERPOOL, L69 3GF. This report is provided for information only. It is not intended to replace a consultation with an appropriately qualified health professional. Information presented relates only to known or suspected effects of interacting medications, and is based on relevant data in the public domain. No clinical advice is given or implied, clinicians must exercise their own judgement in relation to the risks and benefits of combining drugs, which depend on factors beyond pharmacokinetic interactions between two drugs. The University of Liverpool shall not be held responsible for the application or use of any information it gives and the user shall hold the University of Liverpool harmless against any consequences arising from the same. We aim to ensure that information is accurate and consistent with current knowledge and practice. However, the University of Liverpool and its servants or agents shall not be responsible or in any way liable for the continued currency of information in this publication whether arising from negligence or otherwise howsoever or for any consequences arising therefrom. The University of Liverpool expressly exclude liability for errors, omissions or inaccuracies to the fullest extent permitted by law. Interaction Report from www.hiv-druginteractions.org Page 2 of 4

Drugs that should not be coadministered (RED)

Etravirine + Rifapentine Rifapentine is a potent inducer of CYP450 enzymes. Etravirine should not be used with rifapentine as co-administration may cause significant decreases in etravirine plasma concentrations and loss of therapeutic effect of etravirine. Rilpivirine + Rifapentine Coadministration is contraindicated as significant decreases in rilpivirine plasma concentrations may occur. Cobicistat (with ATV or DRV) + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease cobicistat concentrations and consequently those of atazanavir or darunavir being boosted, leading to loss of therapeutic effect and possible development of resistance. Elvitegravir/Cobi/FTC/TAF + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease cobicistat concentrations and consequently those of elvitegravir being boosted, leading to loss of therapeutic effect and possible development of resistance. Elvitegravir/Cobi/FTC/TDF + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease cobicistat concentrations and consequently those of elvitegravir being boosted, leading to loss of therapeutic effect and possible development of resistance. Rilpivirine/FTC/TAF + Rifapentine Coadministration has not been studied and is contraindicated as significant decreases in rilpivirine plasma concentrations may occur. In addition, rifapentine is an inducer of P- glycoprotein and therefore is expected to decrease the absorption of and thereby its plasma concentrations which may result in loss of therapeutic effect and development of resistance. Bictegravir/FTC/TAF + Rifapentine Coadministration is not recommended. Rifapentine is an inducer of P-glycoprotein and therefore is expected to decrease both tenofovir alafenamide and bictegravir exposures. This may result in loss of therapeutic effect and development of resistance.

Potential clinically significant interaction - likely to require additional monitoring, alteration of drug dosage or timing of administration (AMBER)

Efavirenz + Rifapentine Coadministration has not been studied but may decrease efavirenz and rifapentine concentrations. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than rifampicin but higher than rifabutin. Perform therapeutic drug monitoring for efavirenz and adjust dosage if needed. Nevirapine + Rifapentine Coadministration has not been studied but may decrease nevirapine concentrations. Nevirapine is unlikely to significantly alter rifapentine pharmacokinetics. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than rifampicin but higher than rifabutin. Perform therapeutic drug monitoring for nevirapine and adjust dosage if needed.

© Liverpool Drug Interactions Group, University of Liverpool, Pharmacology Research Labs, 1st Floor Block H, 70 Pembroke Place, LIVERPOOL, L69 3GF. This report is provided for information only. It is not intended to replace a consultation with an appropriately qualified health professional. Information presented relates only to known or suspected effects of interacting medications, and is based on relevant data in the public domain. No clinical advice is given or implied, clinicians must exercise their own judgement in relation to the risks and benefits of combining drugs, which depend on factors beyond pharmacokinetic interactions between two drugs. The University of Liverpool shall not be held responsible for the application or use of any information it gives and the user shall hold the University of Liverpool harmless against any consequences arising from the same. We aim to ensure that information is accurate and consistent with current knowledge and practice. However, the University of Liverpool and its servants or agents shall not be responsible or in any way liable for the continued currency of information in this publication whether arising from negligence or otherwise howsoever or for any consequences arising therefrom. The University of Liverpool expressly exclude liability for errors, omissions or inaccuracies to the fullest extent permitted by law. Interaction Report from www.hiv-druginteractions.org Page 3 of 4

Lopinavir + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease lopinavir/ritonavir concentrations which may reduce the therapeutic effect. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than with rifampicin but higher than with rifabutin. Consider using rifabutin. Ritonavir + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease ritonavir concentrations which may reduce the therapeutic effect. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than with rifampicin but higher than with rifabutin. Consider using rifabutin. Saquinavir + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease saquinavir/ritonavir concentrations which may reduce the therapeutic effect. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than with rifampicin but higher than with rifabutin. Consider using rifabutin. Atazanavir + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease atazanavir or atazanavir/ritonavir concentrations which may reduce the therapeutic effect. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than with rifampicin but higher than with rifabutin. Consider using rifabutin. Darunavir + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease darunavir/ritonavir concentrations which may reduce the therapeutic effect. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than with rifampicin but higher than with rifabutin. Consider using rifabutin. Fosamprenavir + Rifapentine Coadministration has not been studied and is not recommended as it may significantly decrease fosamprenavir/ritonavir concentrations which may reduce the therapeutic effect. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than with rifampicin but higher than with rifabutin. Consider using rifabutin. Raltegravir + Rifapentine Coadministration of raltegravir (400 mg twice daily) alone or with rifapentine (900 mg once weekly or 600 mg once daily) was studied in 16 HIV-negative subjects. Coadministration with weekly rifapentine increased raltegravir AUC and Cmax by 71% and 89%, but Cmin decreased by 12%. Coadministration with daily rifapentine did not change raltegravir AUC or Cmax but decreased Cmin by 41%. The increase in raltegravir observed with once weekly rifapentine was safe. Once weekly rifapentine (for treatment of latent TB) can be used with raltegravir without dose adjustment. However, the proper dosing strategy of daily rifapentine (for treatment of active TB) is still under clinical investigation. Maraviroc + Rifapentine Coadministration has not been studied but may decrease maraviroc concentrations as in vitro data suggest that rifapentine is an inducer of CYP3A4. The magnitude of induction is lower than observed for rifampicin but higher than rifabutin. Consider increasing maraviroc to 600 mg twice daily when coadministered with rifapentine in the absence of a protease inhibitor or other potent CYP3A4 inhibitors. Dolutegravir + Rifapentine Coadministration may decrease dolutegravir concentrations due to CYP3A4 induction. The magnitude of rifapentine-mediated CYP3A4 induction is predicted to be lower than with rifampicin but higher than with rifabutin. In healthy volunteers receiving weekly rifapentine and isoniazid, the addition of dolutegravir resulted in flu-like symptoms and LFT elevations

© Liverpool Drug Interactions Group, University of Liverpool, Pharmacology Research Labs, 1st Floor Block H, 70 Pembroke Place, LIVERPOOL, L69 3GF. This report is provided for information only. It is not intended to replace a consultation with an appropriately qualified health professional. Information presented relates only to known or suspected effects of interacting medications, and is based on relevant data in the public domain. No clinical advice is given or implied, clinicians must exercise their own judgement in relation to the risks and benefits of combining drugs, which depend on factors beyond pharmacokinetic interactions between two drugs. The University of Liverpool shall not be held responsible for the application or use of any information it gives and the user shall hold the University of Liverpool harmless against any consequences arising from the same. We aim to ensure that information is accurate and consistent with current knowledge and practice. However, the University of Liverpool and its servants or agents shall not be responsible or in any way liable for the continued currency of information in this publication whether arising from negligence or otherwise howsoever or for any consequences arising therefrom. The University of Liverpool expressly exclude liability for errors, omissions or inaccuracies to the fullest extent permitted by law. Interaction Report from www.hiv-druginteractions.org Page 4 of 4 in 2 out of 4 patients, leading to study termination. Limited pharmacokinetic data suggested lower dolutegravir exposure. Intolerance is likely to be related to rifapentine (+/- healthy volunteer status) rather than isoniazid, since in the INSPIRING study the addition of dolutegravir to daily rifampicin and isoniazid was well tolerated in HIV-TB co-infected adults. The combination of dolutegravir and rifapentine should be used with caution until further data are available.

Emtricitabine/TAF + Rifapentine Coadministration is not recommended. Rifapentine is an inducer and therefore is expected to decrease the exposure of tenofovir alafenamide which may result in loss of therapeutic effect and development of resistance. Based on a drug-drug interaction study with rifampicin, if coadministration is required consider using tenofovir 25 mg twice daily. Coadministration of tenofovir alafenamide 25 mg twice daily with rifampicin 600 mg once daily in healthy volunteers gave comparable plasma tenofovir alafenamide and intracellular tenofovir-DP exposures to those observed with tenofovir alafenamide 25 mg once daily in the absence of rifampicin.

No clinically significant interaction expected (GREEN)

Zidovudine (AZT/ZDV) + Rifapentine

Tenofovir-DF + Rifapentine Lamivudine (3TC) + Rifapentine

Emtricitabine (FTC) + Rifapentine + Rifapentine

Ibalizumab-uiyk + Rifapentine

© Liverpool Drug Interactions Group, University of Liverpool, Pharmacology Research Labs, 1st Floor Block H, 70 Pembroke Place, LIVERPOOL, L69 3GF. This report is provided for information only. It is not intended to replace a consultation with an appropriately qualified health professional. Information presented relates only to known or suspected effects of interacting medications, and is based on relevant data in the public domain. No clinical advice is given or implied, clinicians must exercise their own judgement in relation to the risks and benefits of combining drugs, which depend on factors beyond pharmacokinetic interactions between two drugs. The University of Liverpool shall not be held responsible for the application or use of any information it gives and the user shall hold the University of Liverpool harmless against any consequences arising from the same. We aim to ensure that information is accurate and consistent with current knowledge and practice. However, the University of Liverpool and its servants or agents shall not be responsible or in any way liable for the continued currency of information in this publication whether arising from negligence or otherwise howsoever or for any consequences arising therefrom. The University of Liverpool expressly exclude liability for errors, omissions or inaccuracies to the fullest extent permitted by law.