Cytochrome P-450 CYP3A5 Inhibitors (strong)

DrugDrug NameDrug Indication
DB08873BoceprevirBoceprevir, when used in combination with [DB00811], [DB00008], and [DB00022] is indicated for use in the treatment of chronic HCV genotype 1 infection in adults [FDA Label].
DB09065CobicistatCobicistat is a CYP3A inhibitor indicated to increase systemic exposure of atazanavir or darunavir (once daily dosing regimen) in combination with other antiretroviral agents in the treatment of HIV-1 infection. It is not interchangeable with ritonavir to increase systemic exposure of darunavir 600 mg twice daily, fosamprenavir, saquinavir, or tipranavir due to lack of exposure data. The use of cobicistat is not recommended with darunavir 600 mg twice daily, fosamprenavir, saquinavir or tipranavir. Complex or unknown mechanisms of drug interactions preclude extrapolation of ritonavir drug interactions to certain cobicistat interactions. Cobicistat and ritonavir when administered with either atazanavir or darunavir may result in different drug interactions when used with concomitant medications.
DB01026KetoconazoleFor the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.
DB13179TroleandomycinFor the treatment of bacterial infection.
DB00220NelfinavirUsed in combination with other antiviral drugs in the treatment of HIV in both adults and children.
DB01211ClarithromycinAn alternative medication for the treatment of acute otitis media caused by H. influenzae, M. catarrhalis, or S. pneumoniae in patients with a history of type I penicillin hypersensitivity. Also for the treatment of pharyngitis and tonsillitis caused by susceptible Streptococcus pyogenes, as well as respiratory tract infections including acute maxillary sinusitis, acute bacterial exacerbations of chronic bronchitis, mild to moderate community-acquired pneuomia, Legionnaires' disease, and pertussis. Other indications include treatment of uncomplicated skin or skin structure infections, helicobacter pylori infection, duodenal ulcer disease, bartonella infections, early Lyme disease, and encephalitis caused by Toxoplasma gondii (in HIV infected patients in conjunction with pyrimethamine). Clarithromycin may also decrease the incidence of cryptosporidiosis, prevent the occurence of α-hemolytic (viridans group) streptococcal endocarditis, as well as serve as a primary prevention for Mycobacterium avium complex (MAC) bacteremia or disseminated infections (in adults, adolescents, and children with advanced HIV infection).
DB01167ItraconazoleFor the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis.
DB01149NefazodoneFor the treatment of depression.
DB00503RitonavirIndicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.
DrugDrug NameTargetType
DB08873BoceprevirCytochrome P450 3A4enzyme
DB08873BoceprevirCytochrome P450 3A5enzyme
DB08873BoceprevirMultidrug resistance protein 1transporter
DB08873BoceprevirNS3/4A proteintarget
DB09065CobicistatCytochrome P450 2D6enzyme
DB09065CobicistatMultidrug resistance protein 1transporter
DB09065CobicistatATP-binding cassette sub-family G member 2transporter
DB09065CobicistatCytochrome P450 3A4enzyme
DB09065CobicistatCytochrome P450 3A5enzyme
DB09065CobicistatCytochrome P450 3A7enzyme
DB09065CobicistatCytochrome P450 3A43enzyme
DB09065CobicistatSolute carrier organic anion transporter family member 1B1transporter
DB09065CobicistatSolute carrier organic anion transporter family member 1B3transporter
DB01026KetoconazoleCytochrome P450 3A4enzyme
DB01026KetoconazoleCytochrome P450 2C9enzyme
DB01026KetoconazoleCytochrome P450 2C19enzyme
DB01026KetoconazoleCytochrome P450 3A5enzyme
DB01026KetoconazoleCytochrome P450 1A2enzyme
DB01026KetoconazoleCytochrome P450 2C8enzyme
DB01026KetoconazoleCytochrome P450 1A1enzyme
DB01026KetoconazoleCytochrome P450 2D6enzyme
DB01026KetoconazoleCytochrome P450 3A7enzyme
DB01026KetoconazoleBile salt export pumptransporter
DB01026KetoconazoleMultidrug resistance protein 1transporter
DB01026KetoconazoleSolute carrier organic anion transporter family member 1A2transporter
DB01026KetoconazoleCholesterol side-chain cleavage enzyme, mitochondrialenzyme
DB01026KetoconazoleCytochrome P450 11B1, mitochondrialenzyme
DB01026KetoconazoleCytochrome P450 1B1enzyme
DB01026KetoconazoleCytochrome P450 26A1enzyme
DB01026KetoconazoleCytochrome P450 2A6enzyme
DB01026KetoconazoleCytochrome P450 2B6enzyme
DB01026KetoconazoleLanosterol 14-alpha demethylaseenzyme
DB01026KetoconazoleLanosterol 14-alpha demethylasetarget
DB01026KetoconazoleAndrogen receptortarget
DB01026Ketoconazole17-hydroxylasetarget
DB01026KetoconazoleSteroid 21-hydroxylasetarget
DB01026Ketoconazole11-hydroxylasetarget
DB01026KetoconazoleCytochrome P450 19A1target
DB01026KetoconazolePotassium voltage-gated channel subfamily H member 2target
DB01026KetoconazoleNuclear receptor subfamily 1 group I member 2target
DB01026KetoconazoleNuclear receptor subfamily 1 group I member 3target
DB01026KetoconazoleUDP-glucuronosyltransferase 1-1enzyme
DB01026KetoconazoleUDP-glucuronosyltransferase 2B7enzyme
DB01026KetoconazoleSolute carrier organic anion transporter family member 1B1transporter
DB13179TroleandomycinCytochrome P450 2C9enzyme
DB13179TroleandomycinCytochrome P450 2C19enzyme
DB13179TroleandomycinCytochrome P450 3A5enzyme
DB13179TroleandomycinCytochrome P450 3A43enzyme
DB13179Troleandomycin50S ribosomal protein L4target
DB13179Troleandomycin50S ribosomal protein L32target
DB13179TroleandomycinMultidrug resistance protein 1transporter
DB13179TroleandomycinCytochrome P450 2A6enzyme
DB13179TroleandomycinCytochrome P450 2C18enzyme
DB13179TroleandomycinCytochrome P450 2C8enzyme
DB13179TroleandomycinCytochrome P450 3A4enzyme
DB13179TroleandomycinNuclear receptor subfamily 1 group I member 2target
DB13179TroleandomycinCytochrome P450 3A7enzyme
DB00220NelfinavirHIV-1 proteasetarget
DB00220NelfinavirCytochrome P450 2C19enzyme
DB00220NelfinavirCytochrome P450 3A4enzyme
DB00220NelfinavirCytochrome P450 2B6enzyme
DB00220NelfinavirCytochrome P450 3A5enzyme
DB00220NelfinavirCytochrome P450 3A7enzyme
DB00220NelfinavirMultidrug resistance protein 1transporter
DB00220NelfinavirSolute carrier family 22 member 1transporter
DB00220NelfinavirSolute carrier organic anion transporter family member 1A2transporter
DB00220NelfinavirATP-binding cassette sub-family G member 2transporter
DB00220NelfinavirSolute carrier organic anion transporter family member 1B1transporter
DB00220NelfinavirCytochrome P450 1A2enzyme
DB00220NelfinavirCytochrome P450 2C9enzyme
DB00220NelfinavirCytochrome P450 2D6enzyme
DB00220NelfinavirSerum albumincarrier
DB00220NelfinavirUDP-glucuronosyltransferase 1-1enzyme
DB00220NelfinavirSolute carrier organic anion transporter family member 1B3transporter
DB00220NelfinavirSolute carrier organic anion transporter family member 2B1transporter
DB01211Clarithromycin50S ribosomal protein L10target
DB01211ClarithromycinCytochrome P450 3A4enzyme
DB01211ClarithromycinCytochrome P450 2C19enzyme
DB01211ClarithromycinCytochrome P450 3A5enzyme
DB01211ClarithromycinCytochrome P450 3A7enzyme
DB01211ClarithromycinMultidrug resistance protein 1transporter
DB01211ClarithromycinSolute carrier family 22 member 7transporter
DB01211ClarithromycinCytochrome P450 1A2enzyme
DB01211ClarithromycinPotassium voltage-gated channel subfamily H member 2target
DB01211ClarithromycinSolute carrier organic anion transporter family member 1B1target
DB01211ClarithromycinSolute carrier organic anion transporter family member 1B3target
DB01167ItraconazoleLanosterol 14-alpha demethylasetarget
DB01167ItraconazoleLanosterol 14-alpha demethylasetarget
DB01167ItraconazoleCytochrome P450 3A4enzyme
DB01167ItraconazoleCytochrome P450 2D6enzyme
DB01167ItraconazoleCytochrome P450 3A5enzyme
DB01167ItraconazoleCytochrome P450 3A7enzyme
DB01167ItraconazoleCytochrome P450 2B6enzyme
DB01167ItraconazoleMultidrug resistance protein 1transporter
DB01167ItraconazoleCytochrome P450 1A1enzyme
DB01167ItraconazoleCytochrome P450 2E1enzyme
DB01167ItraconazoleSolute carrier organic anion transporter family member 2B1transporter
DB01149Nefazodone5-hydroxytryptamine receptor 2Atarget
DB01149NefazodoneSodium-dependent serotonin transportertarget
DB01149NefazodoneSodium-dependent noradrenaline transportertarget
DB01149NefazodoneAlpha-1A adrenergic receptortarget
DB01149NefazodoneAlpha-1B adrenergic receptortarget
DB01149NefazodoneCytochrome P450 3A4enzyme
DB01149NefazodoneCytochrome P450 2D6enzyme
DB01149NefazodoneSodium-dependent dopamine transportertarget
DB01149NefazodoneAlpha-2A adrenergic receptortarget
DB01149Nefazodone5-hydroxytryptamine receptor 1Atarget
DB01149NefazodoneCYP2B proteinenzyme
DB01149NefazodoneCytochrome P450 3A5enzyme
DB01149NefazodoneMultidrug resistance protein 1transporter
DB01149Nefazodone5-hydroxytryptamine receptor 2Ctarget
DB01149NefazodoneCytochrome P450 1A2enzyme
DB01149NefazodonePotassium voltage-gated channel subfamily H member 2target
DB01149NefazodoneCYP3Aenzyme
DB01149NefazodoneSolute carrier organic anion transporter family member 1B3transporter
DB01149NefazodoneSolute carrier organic anion transporter family member 2B1transporter
DB00503RitonavirHuman immunodeficiency virus type 1 proteasetarget
DB00503RitonavirCytochrome P450 2D6enzyme
DB00503RitonavirCytochrome P450 2C9enzyme
DB00503RitonavirCytochrome P450 2C19enzyme
DB00503RitonavirCytochrome P450 2B6enzyme
DB00503RitonavirCytochrome P450 2C8enzyme
DB00503RitonavirMultidrug resistance protein 1transporter
DB00503RitonavirMultidrug resistance-associated protein 1transporter
DB00503RitonavirCanalicular multispecific organic anion transporter 1transporter
DB00503RitonavirSolute carrier organic anion transporter family member 1A2transporter
DB00503RitonavirATP-binding cassette sub-family G member 2transporter
DB00503RitonavirSolute carrier organic anion transporter family member 1B1transporter
DB00503RitonavirCytochrome P450 1A2enzyme
DB00503RitonavirCytochrome P450 2E1enzyme
DB00503RitonavirNuclear receptor subfamily 1 group I member 2target
DB00503RitonavirSerum albumincarrier
DB00503RitonavirCytochrome P450 3A4enzyme
DB00503RitonavirCytochrome P450 3A5enzyme
DB00503RitonavirCytochrome P450 3A7enzyme
DB00503RitonavirCytochrome P450 3A43enzyme
DB00503RitonavirUDP-glucuronosyltransferase 1-1enzyme
DB00503RitonavirSolute carrier organic anion transporter family member 2B1transporter