2014•Expert Opinion on PharmacotherapyRequires access

Cobicistat: a new opportunity in the treatment of HIV disease?

Amedeo Ferdinando Capetti, Giuliano Rizzardini

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Abstract

INTRODUCTION: Cobicistat (Cobi), a selective novel CYP3A4 inhibitor, is an orally administered, non-antiretroviral pharmacokinetic enhancer which boosts the plasma levels of several drugs, including HIV-1 protease inhibitors and the integrase strand transfer inhibitor elvitegravir (ELV). AREAS COVERED: PubMed and www.clinicaltrials.gov were searched with the term 'cobicistat' for all clinical trials conducted up to date, as well as for those ongoing and to be opened in the near future as well as for pharmacology data. A review of abstracts from major HIV, infectious diseases and pharmacology conferences from 2010 to 2014 was also conducted. EXPERT OPINION: Cobi has shown good efficacy in HIV-infected treatment-naïve subjects, either in combination with ELV, within a quadruple drug, single tablet regimen, and in combination with atazanavir and darunavir. Coformulations containing cobi will mark the near future of antiretroviral therapy, therefore it will be necessary for physicians to become familiar with their management. In particular, the inhibition of creatinine secretion by the proximal renal tubule will require the acquisition of competences in estimating the real glomerular filtration rate, since studies with iohexol clearance have shown that the eGFR reduction is cosmetic. The long-term metabolic advantages of cobi versus ritonavir can be hypothesized, given the initial data from current trials.

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What this paper is about

INTRODUCTION: Cobicistat (Cobi), a selective novel CYP3A4 inhibitor, is an orally administered, non-antiretroviral pharmacokinetic enhancer which boosts the plasma levels of several drugs, including HIV-1 protease inhibitors and the integrase strand transfer inhibitor elvitegravir (ELV). AREAS COVERED: PubMed and www.clinicaltrials.gov were searched with the term 'cobicistat' for all clinical trials conducted up to date, as well as for those ongoing and to be opened in the near future as well as for pharmacology data. A review of abstracts from major HIV, infectious diseases and pharmacology conferences from 2010 to 2014 was also conducted. EXPERT OPINION: Cobi has shown good efficacy in HIV-infected treatment-naïve subjects, either in combination with ELV, within a quadruple drug, single tablet regimen, and in combination with atazanavir and darunavir. Coformulations containing cobi will mark the near future of antiretroviral therapy, therefore it will be necessary for physicians to become familiar with their management. In particular, the inhibition of creatinine secretion by the proximal renal tubule will require the acquisition of competences in estimating the real glomerular filtration rate, since studies with iohexol clearance have shown that the eGFR reduction is cosmetic. The long-term metabolic advantages of cobi versus ritonavir can be hypothesized, given the initial data from current trials.

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Available abstract

INTRODUCTION: Cobicistat (Cobi), a selective novel CYP3A4 inhibitor, is an orally administered, non-antiretroviral pharmacokinetic enhancer which boosts the plasma levels of several drugs, including HIV-1 protease inhibitors and the integrase strand transfer inhibitor elvitegravir (ELV). AREAS COVERED: PubMed and www.clinicaltrials.gov were searched with the term 'cobicistat' for all clinical trials conducted up to date, as well as for those ongoing and to be opened in the near future as well as for pharmacology data. A review of abstracts from major HIV, infectious diseases and pharmacology conferences from 2010 to 2014 was also conducted. EXPERT OPINION: Cobi has shown good efficacy in HIV-infected treatment-naïve subjects, either in combination with ELV, within a quadruple drug, single tablet regimen, and in combination with atazanavir and darunavir. Coformulations containing cobi will mark the near future of antiretroviral therapy, therefore it will be necessary for physicians to become familiar with their management. In particular, the inhibition of creatinine secretion by the proximal renal tubule will require the acquisition of competences in estimating the real glomerular filtration rate, since studies with iohexol clearance have shown that the eGFR reduction is cosmetic. The long-term metabolic advantages of cobi versus ritonavir can be hypothesized, given the initial data from current trials.

Key concepts: Medicine, Cobicistat, Human immunodeficiency virus (HIV), Disease, Intensive care medicine, Virology, Antiretroviral therapy, Internal medicine

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