Cytochrome P-450 CYP3A4 Inhibitors (strong)

DrugDrug NameDrug Indication
DB00220NelfinavirUsed in combination with other antiviral drugs in the treatment of HIV in both adults and children.
DB00224IndinavirIndinavir is an antiretroviral drug for the treatment of HIV infection.
DB00582VoriconazoleFor the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp.
DB00976TelithromycinFor the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.
DB01026KetoconazoleFor the treatment of the following systemic fungal infections: candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.
DB01072AtazanavirUsed in combination with other antiretroviral agents for the treatment of HIV-1 infection, as well as postexposure prophylaxis of HIV infection in individuals who have had occupational or nonoccupational exposure to potentially infectious body fluids of a person known to be infected with HIV when that exposure represents a substantial risk for HIV transmission.
DB01149NefazodoneFor the treatment of depression.
DB01167ItraconazoleFor the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis.
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).
DB01232SaquinavirFor the treatment of HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues.
DB01264DarunavirDarunavir, co-administered with ritonavir, and with other antiretroviral agents, is indicated for the treatment of human immunodeficiency virus (HIV) infection in antiretroviral treatment-experienced adult patients, such as those with HIV-1 strains resistant to more than one protease inhibitor.
DB01263PosaconazoleFor prophylaxis of invasive Aspergillus and Candida infections in patients, 13 years of age and older, who are at high risk of developing these infections due to being severely immunocompromised as a result of procedures such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD), or due to hematologic malignancies with prolonged neutropenia from chemotherapy. Also for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Posaconazole is used as an alternative treatment for invasive aspergillosis, Fusarium infections, and zygomycosis in patients who are intolerant of, or whose disease is refractory to, other antifungals.
DB01601LopinavirIndicated in combination with other antiretroviral agents for the treatment of HIV-infection.
DB01118AmiodaroneIntravenously, for initiation of treatment and prophylaxis of frequently recurring ventricular fibrillation and hemodynamically unstable ventricular tachycardia in patients refractory to other therapy. Orally, for the treatment of life-threatening recurrent ventricular arrhythmias such as recurrent ventricular fibrillation and recurrent hemodynamically unstable ventricular tachycardia.
DB05521TelaprevirTelaprevir, 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].
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].
DB09054IdelalisibIdelalisib is indicated in the treatment of chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). For the treatment of relapsed CLL, it is currently indicated as a second-line agent in combination with rituximab in patients for whom rituximab alone would be considered appropriate therapy due to other co-morbidities, while in the treatment of FL and SLL it is intended to be used in patients who have received at least two prior systemic therapies.
DB09063CeritinibCeritinib is a kinase inhibitor indicated for the treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. This indication is approved under accelerated approval based on tumor response rate and duration of response. An improvement in survival or disease-related symptoms has not been established. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trials.
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.
DB09118StiripentolIndicated for use in conjunction with clobazam and valproate as adjunctive therapy of refractory generalized tonic-clonic seizures in patients with severe myoclonic epilepsy in infancy (SMEI, Dravet’s syndrome) whose seizures are not adequately controlled with clobazam and valproate.
DrugDrug NameTargetType
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
DB00224IndinavirHuman immunodeficiency virus type 1 proteasetarget
DB00224IndinavirCytochrome P450 3A4enzyme
DB00224IndinavirCytochrome P450 3A5enzyme
DB00224IndinavirCytochrome P450 3A7enzyme
DB00224IndinavirMultidrug resistance protein 1transporter
DB00224IndinavirSolute carrier family 22 member 1transporter
DB00224IndinavirMultidrug resistance-associated protein 1transporter
DB00224IndinavirSolute carrier organic anion transporter family member 1A2transporter
DB00224IndinavirSolute carrier organic anion transporter family member 1B1transporter
DB00224IndinavirCanalicular multispecific organic anion transporter 1transporter
DB00224IndinavirCytochrome P450 2C19enzyme
DB00224IndinavirCytochrome P450 2C9enzyme
DB00224IndinavirCytochrome P450 2D6enzyme
DB00582VoriconazoleCytochrome P450 2C19enzyme
DB00582VoriconazoleCytochrome P450 3A4enzyme
DB00582VoriconazoleCytochrome P450 2C9enzyme
DB00582VoriconazoleDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00582VoriconazoleDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00582VoriconazoleCytochrome P450 3A5enzyme
DB00582VoriconazoleCytochrome P450 3A7enzyme
DB00582VoriconazoleProstaglandin G/H synthase 1enzyme
DB00582VoriconazoleLanosterol 14-alpha demethylasetarget
DB00976Telithromycin23S rRNAtarget
DB00976TelithromycinCytochrome P450 3A4enzyme
DB00976TelithromycinCytochrome P450 1A2enzyme
DB00976TelithromycinCytochrome P450 3A5enzyme
DB00976TelithromycinCytochrome P450 3A7enzyme
DB00976TelithromycinCytochrome P450 2D6enzyme
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
DB01026KetoconazoleSteroid 21-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
DB01072AtazanavirHuman immunodeficiency virus type 1 proteasetarget
DB01072AtazanavirCytochrome P450 3A4enzyme
DB01072AtazanavirCytochrome P450 2C9enzyme
DB01072AtazanavirMultidrug resistance protein 1transporter
DB01072AtazanavirMultidrug resistance-associated protein 1transporter
DB01072AtazanavirCytochrome P450 1A2enzyme
DB01072AtazanavirSerum albumincarrier
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
DB01149NefazodoneCytochrome P450 3A7enzyme
DB01149NefazodoneMultidrug resistance protein 1transporter
DB01149Nefazodone5-hydroxytryptamine receptor 2Ctarget
DB01149NefazodoneCytochrome P450 1A2enzyme
DB01149NefazodonePotassium voltage-gated channel subfamily H member 2target
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
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
DB01232SaquinavirHuman immunodeficiency virus type 1 proteasetarget
DB01232SaquinavirCytochrome P450 3A4enzyme
DB01232SaquinavirCytochrome P450 3A5enzyme
DB01232SaquinavirAlpha-1-acid glycoprotein 1carrier
DB01232SaquinavirSerum albumincarrier
DB01232SaquinavirCytochrome P450 3A7enzyme
DB01232SaquinavirMultidrug resistance protein 1transporter
DB01232SaquinavirSolute carrier family 22 member 1transporter
DB01232SaquinavirSolute carrier organic anion transporter family member 1A2transporter
DB01232SaquinavirATP-binding cassette sub-family G member 2transporter
DB01232SaquinavirSolute carrier organic anion transporter family member 1B1transporter
DB01232SaquinavirMultidrug resistance-associated protein 1transporter
DB01232SaquinavirCanalicular multispecific organic anion transporter 1transporter
DB01232SaquinavirCholesterol side-chain cleavage enzyme, mitochondrialenzyme
DB01232SaquinavirCytochrome P450 2C19enzyme
DB01232SaquinavirCytochrome P450 2C8enzyme
DB01232SaquinavirCytochrome P450 2C9enzyme
DB01232SaquinavirCytochrome P450 2D6enzyme
DB01264DarunavirHuman immunodeficiency virus type 1 proteasetarget
DB01264DarunavirCytochrome P450 3A4enzyme
DB01263PosaconazoleCytochrome P450 3A4enzyme
DB01263PosaconazoleMultidrug resistance protein 1transporter
DB01263PosaconazoleLanosterol 14-alpha demethylasetarget
DB01601LopinavirHuman immunodeficiency virus type 1 proteasetarget
DB01601LopinavirCytochrome P450 3A4enzyme
DB01601LopinavirCytochrome P450 2D6enzyme
DB01601LopinavirCytochrome P450 2C19enzyme
DB01601LopinavirMultidrug resistance protein 1transporter
DB01601LopinavirCytochrome P450 1A2enzyme
DB01601LopinavirCytochrome P450 2B6enzyme
DB01601LopinavirCytochrome P450 2C9enzyme
DB01601LopinavirCytochrome P450 2C8enzyme
DB01118AmiodaroneBeta-1 adrenergic receptortarget
DB01118AmiodaronePotassium voltage-gated channel subfamily H member 2target
DB01118AmiodaroneCytochrome P450 2C8enzyme
DB01118AmiodaroneCytochrome P450 2C9enzyme
DB01118AmiodaroneCytochrome P450 2D6enzyme
DB01118AmiodaroneVoltage-dependent T-type calcium channel subunit alpha-1Htarget
DB01118AmiodaroneVoltage-dependent calcium channel subunit alpha-2/delta-2target
DB01118AmiodaroneCytochrome P450 3A4enzyme
DB01118AmiodaroneCytochrome P450 1A2enzyme
DB01118AmiodaroneCytochrome P450 3A5enzyme
DB01118AmiodaroneCytochrome P450 3A7enzyme
DB01118AmiodaroneCytochrome P450 1A1enzyme
DB01118AmiodaroneMultidrug resistance protein 1transporter
DB01118AmiodaroneCytochrome P450 2C19enzyme
DB01118AmiodaroneCytochrome P450 2A6enzyme
DB01118AmiodaroneThyroid hormone receptor alphatarget
DB01118AmiodaroneThyroid hormone receptor betatarget
DB01118AmiodaronePeroxisome proliferator-activated receptor gammatarget
DB05521TelaprevirCytochrome P450 3A4enzyme
DB05521TelaprevirNS3/4A proteintarget
DB05521TelaprevirMultidrug resistance protein 1transporter
DB05521TelaprevirSerum albumincarrier
DB05521TelaprevirAlpha-1-acid glycoprotein 1carrier
DB05521TelaprevirSolute carrier organic anion transporter family member 1B1target
DB05521TelaprevirSolute carrier organic anion transporter family member 2B1target
DB08873BoceprevirCytochrome P450 3A4enzyme
DB08873BoceprevirCytochrome P450 3A5enzyme
DB08873BoceprevirMultidrug resistance protein 1transporter
DB08873BoceprevirNS3/4A proteintarget
DB09054IdelalisibPhosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta isoform (P110δ)target
DB09054IdelalisibATP-binding cassette sub-family G member 2transporter
DB09054IdelalisibMultidrug resistance protein 1transporter
DB09054IdelalisibAldehyde oxidaseenzyme
DB09054IdelalisibUDP-glucuronosyltransferase 1A4enzyme
DB09054IdelalisibUDP-glucuronosyltransferase 1A1enzyme
DB09054IdelalisibCytochrome P450 2C8enzyme
DB09054IdelalisibCytochrome P450 2C19enzyme
DB09054IdelalisibCytochrome P450 2B6enzyme
DB09054IdelalisibCytochrome P450 3A4enzyme
DB09054IdelalisibSolute carrier organic anion transporter family member 1B1transporter
DB09054IdelalisibSolute carrier organic anion transporter family member 1B3transporter
DB09054IdelalisibCytochrome P450 3A5enzyme
DB09054IdelalisibCytochrome P450 3A43enzyme
DB09054IdelalisibCytochrome P450 3A7enzyme
DB09063CeritinibALK tyrosine kinase receptortarget
DB09063CeritinibMultidrug resistance protein 1transporter
DB09063CeritinibCytochrome P450 3A4enzyme
DB09063CeritinibCytochrome P450 2C9enzyme
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
DB09118StiripentolCytochrome P450 2C19enzyme
DB09118StiripentolCytochrome P450 2D6enzyme
DB09118StiripentolCytochrome P450 3A4enzyme
DB09118StiripentolCytochrome P450 1A2enzyme
DB09118StiripentolCytochrome P450 2C9enzyme
DB09118StiripentolGABA-A receptor (anion channel)target
DB09118StiripentolL-lactate dehydrogenase A chaintarget
DB09118StiripentolL-lactate dehydrogenase B chaintarget