Immunosuppressants & ARVs

Legend
↑     Potential elevated exposure of the immunosuppressant
↓     Potential decreased exposure of the immunosuppressant
↔   No significant effect
D     Potential decreased exposure of ARV drug
E     Potential elevated exposure of ARV drug

Numbers refer to increased or decreased AUC as observed in drug-drug interaction studies

ATV/c:
ATV co-formulated with COBI (300/150 mg qd)

DRV/c:
DRV co-formulated with COBI (800/150 mg qd)

CAB/RPV:
CAB and RPV im long acting injections

* available as prolonged release formulation

AM (antimetabolite)
CNI (calcineurin inhibitors)
CS (corticosteroids)
mTOR (mTOR inhibitors)

Interactions with ABC, FTC, 3TC, ZDV
ABC:
Potential decrease in mycophenolate exposure

ZDV:
- Potential risk of additive haematoxicity with azathioprine;
- Potential alteration in mycophenolate exposure, monitor plasma concentrations

Interactions with cabotegravir (oral)
None

Interactions with ibalizumab
None

Comments

1. TDM of immunosuppressant is recommended.
2. Monitor renal function.
3. Both drugs can potentially prolong the QT interval, ECG monitoring recommended.

♥ EFV prolonged the QT interval above the regulatory threshold of concern in homozygous carriers of the CYP2B6*6/*6 allele (516T variant). Coadministration with a drug with a known risk of TdP is contraindicated in the EFV European label.

^ LEN causes moderate inhibition of CYP3A4 and, when discontinued, remains in the circulation for prolonged periods. Residual concentrations of LEN may affect the exposure of sensitive CYP3A4 substrates and/or narrow therapeutic index drugs that are initiated within 9 months after the last subcutaneous dose of LEN.

Further Information
For additional drug-drug interactions and for more detailed pharmacokinetic interaction data and dosage adjustments, please refer to: http://www.hiv-druginteractions.org (University of Liverpool)