cobicistat + darunavir ethanolate + emtricitabine + tenofovir alafenamide fumarate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
cobicistat + darunavir ethanolate + emtricitabine + tenofovir alafenamide fumarate: clinical details
Prescribing considerations
- Initiation should be supervised by a clinician experienced in HIV-1 management.
- Review genotype and darunavir resistance-associated mutations before selection, especially in treatment-experienced patients.
- Assess renal and hepatic function, hepatitis B and C status, pregnancy status and the complete interaction profile.
- Stopping in HIV/HBV co-infection can precipitate severe hepatitis exacerbation and requires prolonged clinical and laboratory follow-up.
Contraindications and cautions
- Hypersensitivity to an active substance or excipient.
- Severe hepatic impairment.
- Strong CYP3A inducers, including carbamazepine, phenobarbital, phenytoin, rifampicin and St John’s wort.
- Contraindicated interacting medicines include oral midazolam, triazolam, simvastatin, lovastatin, ticagrelor, domperidone and specified antiarrhythmics, antipsychotics and ergot derivatives.
- Do not initiate if creatinine-clearance-based eGFR is below 30 mL/min; discontinue if it falls below this threshold.
Monitoring
- HIV viral load, clinical response and adherence.
- Baseline and ongoing renal function.
- Liver tests, with closer AST and ALT monitoring in hepatitis, cirrhosis or pre-existing transaminase elevation.
- Weight, blood glucose and lipid profile where clinically appropriate.
- New inflammatory or autoimmune symptoms after starting treatment.
- Medication reconciliation for CYP3A, P-gp and transporter interactions.
Clinical pharmacology
Darunavir inhibits HIV-1 protease. Cobicistat inhibits CYP3A and transporters to enhance darunavir exposure. Emtricitabine and intracellularly activated tenofovir inhibit reverse transcriptase through viral DNA chain termination. Cobicistat may raise serum creatinine by inhibiting tubular creatinine secretion without reducing glomerular filtration.
Formulation and product differences
- The selected product is a yellow to yellowish-brown, capsule-shaped film-coated tablet.
- The tablet should not be crushed and must be administered with food.
- The selected product information does not describe a liquid or dispersible formulation.
cobicistat + darunavir ethanolate + emtricitabine + tenofovir alafenamide fumarate preparations and strengths
Tablet
Route: Oral
Strengths: 800 mg + 150 mg + 200 mg + 10 mg
cobicistat + darunavir ethanolate + emtricitabine + tenofovir alafenamide fumarate interactions
Cobicistat and darunavir strongly affect CYP3A and several transporters, creating clinically important interactions. This list is not exhaustive.
Carbamazepine, phenobarbital, phenytoin or rifampicin
Can lower antiretroviral exposure and cause loss of HIV control; the combination is contraindicated.
St John’s wort
Can substantially reduce antiretroviral exposure; the combination is contraindicated.
Simvastatin, lovastatin or lomitapide
Concentrations may rise markedly, increasing serious toxicity including muscle injury; the combination is contraindicated.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.