Pharmacokinetic enhancer (booster) for antiretroviral therapy
Brand names: Tybost, Evotaz, Prezcobix
Updated · Methodology
First line
Cobicistat is a pharmacokinetic enhancer in first-line antiretroviral therapy for HIV. GeSIDA 2024 recommends cobicistat-based combinations (Symtuza, Genvoya, Evotaz) in patients who need darunavir- or elvitegravir-based regimens with preserved renal function (eGFR > 70 mL/min). Drug-interaction review is mandatory – cobicistat inhibits CYP3A4 and raises levels of most co-administered drugs.
Sources
ICD-10: B20 · ICD-11: 1C62
Strong reversible inhibitor of CYP3A4 and, to a lesser extent, CYP2D6, MATE1 and P-glycoprotein. Has no antiretroviral activity on its own – it is given only in fixed-dose combinations with darunavir, atazanavir or elvitegravir to raise and sustain their therapeutic concentrations. CYP3A4 inhibition is similar to ritonavir but with less impact on lipids and glycaemia.
Cobicistat levels fall by ~50% in the second and third trimesters, risking loss of antiretroviral effect. EMA advises against starting a cobicistat-based regimen in pregnancy; women who conceive on therapy are switched to a ritonavir-boosted regimen.
Breastfeeding by women with HIV is not recommended in Spain irrespective of the regimen, due to vertical transmission risk.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
8 pairs found. Sorted from critical to minor.
Mechanism
Cobicistat is a strong CYP3A4 inhibitor. Tybost Section 4.3 strict contraindication with ergot alkaloids.
Symptoms
Fatal ergotism.
Management
Combination contraindicated.
Mechanism
Cobicistat is a strong CYP3A4 inhibitor (similar to ritonavir). Everolimus rises 10+ fold.
Symptoms
Acute immunosuppression.
Management
Combination contraindicated.
Sources
Mechanism
Lovastatin is a CYP3A4 sensitive substrate (like simvastatin). Cobicistat causes 30-fold rise. Tybost Section 4.3.
Symptoms
Rhabdomyolysis within 5–10 days.
Management
Combination contraindicated. Pravastatin or rosuvastatin.
Sources
Mechanism
Cobicistat is a strong CYP3A4 inhibitor (potency similar to ritonavir). Tybost Section 4.3 strict contraindication with pimozide.
Symptoms
QT prolongation, syncope, torsades de pointes.
Management
Combination contraindicated. For HIV, switch to a regimen without cobicistat (dolutegravir + 2 NRTIs).
Mechanism
Cobicistat inhibits CYP3A4 (quinidine metabolism) and itself prolongs PR via MATE1 inhibition. Quinidine concentration rises, additive QT effect.
Symptoms
QT prolongation, torsades de pointes.
Management
Combination contraindicated.
Mechanism
Strong CYP3A4 inducer. Cobicistat falls 80% – ART failure.
Symptoms
Rising viral load, resistance risk.
Management
Combination contraindicated. TB in HIV patient – dolutegravir-based ARV (double dose with rifampicin).
Mechanism
Cobicistat is a strong CYP3A4 inhibitor. Simvastatin rises 30-fold with fatal rhabdomyolysis risk. Tybost Section 4.3.
Symptoms
Myalgia, weakness, dark urine within 5 days.
Management
Combination contraindicated. Alternative statin: pravastatin 20–40 mg or rosuvastatin 5–10 mg.
Sources
Mechanism
Sirolimus is a CYP3A4 sensitive substrate, P-gp substrate, NTI. Cobicistat raises concentration 10+ fold with severe toxicity: nephrotoxicity, hepatotoxicity, cytopenia.
Symptoms
Rising creatinine, thrombocytopenia, hepatitis within days.
Management
Combination contraindicated. For HIV in transplant patient – regimen without cobicistat.
Sources
Verbatim lines from the interaction sections, in the language of the label
«CONTRAINDICATIONS: Anticonvulsants: carbamazepine, phenobarbital, phenytoin»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Anti-gout: colchicine»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Ergot Derivatives: dihydroergotamine, ergotamine, methylergonovine»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Antiarrhythmic: dronedarone»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Ergot Derivatives: dihydroergotamine, ergotamine, methylergonovine»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Herbal Products: St. John's wort ( Hypericum perforatum )»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Lipid-modifying Agents: lomitapide, lovastatin, simvastatin»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Anticonvulsants: carbamazepine, phenobarbital, phenytoin»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Anticonvulsants: carbamazepine, phenobarbital, phenytoin»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Antipsychotics: lurasidone, pimozide»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Antianginal: ranolazine»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Phosphodiesterase-5 (PDE-5) Inhibitor: sildenafil when administered as Revatio ® for the treatment of pulmonary arterial hypertension»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Lipid-modifying Agents: lomitapide, lovastatin, simvastatin»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Antiarrhythmic: dronedarone»FDA, section 4 · Open on DailyMed
«CONTRAINDICATIONS: Anticonvulsants: carbamazepine, phenobarbital, phenytoin»FDA, section 4 · Open on DailyMed
«Established and Other Potentially Significant Interactions: midazolam (oral), triazolam ↑ midazolam ↑ triazolam Coadministration with triazolam or oral administered midazolam is contraindicated due…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Corticosteroids: e.g., betamethasone budesonide ciclesonide dexamethasone fluticasone methylprednisolone mometasone triamcinolone ↓…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Corticosteroids: e.g., betamethasone budesonide ciclesonide dexamethasone fluticasone methylprednisolone mometasone triamcinolone ↓…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Antibacterials (macrolide or ketolide antibiotics): clarithromycin erythromycin telithromycin ↑ clarithromycin ↑ erythromycin ↑…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: clopidogrel ↓ clopidogrel active metabolite Coadministration with clopidogrel is not recommended due to potential reduction of the…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Corticosteroids: e.g., betamethasone budesonide ciclesonide dexamethasone fluticasone methylprednisolone mometasone triamcinolone ↓…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Corticosteroids: e.g., betamethasone budesonide ciclesonide dexamethasone fluticasone methylprednisolone mometasone triamcinolone ↓…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: efavirenz ↓ cobicistat ↓ darunavir ↓ atazanavir TYBOST coadministered with darunavir: Coadministration of darunavir and TYBOST with…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Antibacterials (macrolide or ketolide antibiotics): clarithromycin erythromycin telithromycin ↑ clarithromycin ↑ erythromycin ↑…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Corticosteroids: e.g., betamethasone budesonide ciclesonide dexamethasone fluticasone methylprednisolone mometasone triamcinolone ↓…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Antibacterials (macrolide or ketolide antibiotics): clarithromycin erythromycin telithromycin ↑ clarithromycin ↑ erythromycin ↑…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Corticosteroids: e.g., betamethasone budesonide ciclesonide dexamethasone fluticasone methylprednisolone mometasone triamcinolone ↓…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: Corticosteroids: e.g., betamethasone budesonide ciclesonide dexamethasone fluticasone methylprednisolone mometasone triamcinolone ↓…»FDA, section 7 · Open on DailyMed
«CONTRAINDICATIONS: Concomitant administration with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors, boceprevir, telaprevir…»FDA, section 4 · Open on DailyMed
«telaprevir, eritromicina, claritromicina, telitromicina y nefazodona y medicamentos que contienen cobicistat ) (ver secciones 4.4 y 4.5).»AEMPS, section 4.3 · Open on CIMA
«En caso de tratamiento con corticoides a largo plazo: Se espera que el tratamiento concomitante con inhibidores de CYP3A, incluyendo medicamentos que contienen cobicistat, aumente el riesgo de…»AEMPS, section 4.4 · Open on CIMA
«El metabolismo de budesónida está mediado principalmente por CYP3 A4. Se espera que el tratamiento concomitante con inhibidores del CYP3A, por ejemplo itraconazol, ketoconazol, inhibidores de la…»AEMPS, section 4.5 · Open on CIMA
«Se espera que el tratamiento concomitante con inhibidores del CYP3A, incluidos los productos que contienen cobicistat, aumenten el riesgo efectos sistémicos adversos. La combinación se debe evitar a…»AEMPS, section 4.4 · Open on CIMA
«Se ha demostrado una reducción significativa de la inhibición plaquetaria en pacientes infectados con VIH tratados con TARV potenciadas con ritonavir o con cobicistat. Aunque la relevancia clínica de…»AEMPS, section 4.5 · Open on CIMA
«Se espera que el tratamiento concomitante con inhibidores de CYP3A, incluyendo medicamentos que contienen cobicistat, aumente el riesgo de reacciones adversas sistémicas. Se debe evitar esa…»AEMPS, section 4.5 · Open on CIMA
«Se espera que el tratamiento concomitante con inhibidores de CYP3A, incluyendo medicamentos que contienen cobicistat, aumente el riesgo de reacciones adversas sistémicas . Se debe evitar esa…»AEMPS, section 4.5 · Open on CIMA
«Se espera que el tratamiento concomitante con inhibidores de CYP3A, incluyendo medicamentos que contienen cobicistat, aumente el riesgo de reacciones adversas sistémicas. Se debe evitar esa…»AEMPS, section 4.5 · Open on CIMA
«Advertencias especiales: Se espera que el tratamiento conjunto con inhibidores de CYP3A, incluidos los productos que contienen cobicistat, aumente el riesgo de efectos secundarios sistémicos. Se debe…»AEMPS, section 4.4 · Open on CIMA
«- Inhibidores de CYP3A: se espera que el tratamiento concomitante con inhibidores de CYP3A, incluyendo medicamentos que contienen cobicistat, aumente el riesgo de reacciones adversas sistémicas. Se…»AEMPS, section 4.5 · Open on CIMA
«Se espera que el tratamiento concomitante con inhibidores de CYP3A, incluyendo medicamentos que contienen cobicistat, aumente el riesgo de reacciones adversas sistémicas. Se debe evitar esa…»AEMPS, section 4.5 · Open on CIMA
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Cobicistat is evaluated for the following indications with varying evidence strength: HIV infection (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Cobicistat (≥ 1 in 100): Nausea, Diarrhoea, Headache, Rash, Creatinine rise of 0.1–0.15 mg/dL (artefactual, not nephrotoxicity). See the Safety section for uncommon and serious reactions.
Cobicistat levels fall by ~50% in the second and third trimesters, risking loss of antiretroviral effect. EMA advises against starting a cobicistat-based regimen in pregnancy; women who conceive on therapy are switched to a ritonavir-boosted regimen.
Breastfeeding by women with HIV is not recommended in Spain irrespective of the regimen, due to vertical transmission risk.
Cobicistat is contraindicated in: Co-administration with CYP3A4-sensitive drugs (simvastatin, lovastatin, dronedarone, amiodarone at start, cisapride, oral midazolam, pimozide, ergotamine and other ergot alkaloids, sildenafil for pulmonary hypertension); Strong CYP3A4 inducers (rifampicin, phenytoin, phenobarbital, carbamazepine, St John's wort); Severe renal impairment (eGFR < 50 mL/min) for tenofovir disoproxil regimens. Full list in the Safety section.
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Deferasirox, Ergoferon (antibodies to γ-interferon, CD4, and histamine in homeopathic dilutions), Methylthioninium chloride (methylene blue), Ethylmethylhydroxypyridine succinate, Anas Barbariae Hepatis et Cordis Extractum (homeopathic), Deproteinized hemoderivative from calf blood, Naloxone, Antibodies to S-100 brain-specific protein (homeopathic)