Breast Cancer Resistance Protein Inhibitors

DrugDrug NameDrug Indication
DB08912DabrafenibTafinlar is a kinase inhibitor that was initially indicated as a single agent for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test [FDA label]. Tafinlar in combination with [DB08911] is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations as detected by an FDA-approved test. The use in combination is based on the demonstration of durable response rate. Improvement in disease-related symptoms or overall survival has not been demonstrated for Tafinlar in combination with trametinib [FDA label]. In May 2018, Tafinlar (dabrafenib) and Mekinist ([DB08911]) have been approved in combination to treat anaplastic thyroid cancer caused by an abnormal BRAF V600E gene [L2712].
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.
DB09048NetupitantNetupitant is an antiemitic drug approved by the FDA in October 2014 for use in combination with palonosetron for the prevention of acute and delayed vomiting and nausea associated with cancer chemotherapy including highly emetogenic chemotherapy.
DB06210EltrombopagThrombopoietin receptor agonists are pharmaceutical agents that stimulate platelet production in the bone marrow. In this, they differ from the previously discussed agents that act by attempting to curtail platelet destruction.
DB09183DasabuvirDasabuvir, in combination with [DB09296], [DB09297], and [DB00503] (as Viekira Pak) is indicated for the treatment of patients with HCV genotype 1a with [DB00811] or genotype 1b without [DB00811] including those with compensated cirrhosis [FDA Label].
DB09027LedipasvirWhen used in combination with the antiviral medication [DB08934] as the commercially available product Harvoni, ledipasvir is indicated for the treatment of HCV genotypes 1, 4, 5, and 6 with or without [DB00811] depending on the level of liver damage or cirrhosis [FDA Label]. Its use has also proven successful in the treatment of HCV in patients co-infected with HIV [A19627].
DB09291RolapitantThis drug is indicated in adults in combination with other antiemetics for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy.
DB09297ParitaprevirWhen used within the fixed-dose combination product with [DB09296], [DB09183], and [DB00503] as the FDA-approved product Viekira Pak, paritaprevir is indicated for the treatment of HCV genotype 1b without cirrhosis or with compensated cirrhosis, and when combined with [DB00811] for the treatment of HCV genotype 1a without cirrhosis or with compensated cirrhosis. When used within the fixed-dose combination product with [DB09296] and [DB00503] as the FDA- and Health Canada-approved product Technivie, paritaprevir is indicated in combination with [DB00811] for the treatment of patients with genotype 4 chronic hepatitis C virus (HCV) infection without cirrhosis or with compensated cirrhosis. When used within the fixed-dose combination product with [DB09296], [DB09183], and [DB00503] as the Health Canada-approved, commercially available product Holkira Pak, paritaprevir is indicated for the treatment of HCV genotype 1b with or without cirrhosis, and when combined with [DB00811] for the treatment of HCV genotype 1a with or without cirrhosis.
DB09102DaclatasvirIndicated for use with sofosbuvir, with or without ribavirin, for the treatment of chronic HCV genotype 1a/b or 3 infection. The dosing regimen of 60mg daclatasvir 60 mg with 400mg sofosbuvir once a day is recommended for both genontypes. Resistance: Reduced susceptibility to daclatasvir was associated with the polymorphisms at NS5A amino acid positions M28, Q30, L31, and Y93 in genotypes 1a, 1b, and 3a patients. NS5A Resistance Testing is recommended for HCV genotype 1a-infected patients with cirrhosis prior to the initiaition of the treatment, as the risk of resistance development is higher in genotype 1a patients.
DB09330OsimertinibOsimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy.
DB11575GrazoprevirGrazoprevir is indicated in combination with [DB11574] (as the fixed dose combination product Zepatier) with or without [DB00811] for treatment of chronic HCV genotypes 1a, 1b, or 4 infection in adults.
DB11574ElbasvirElbasvir, when used in combination with [DB11575] as the combination product Zepatier, is indicated for use with or without ribavirin for the treatment of chronic HCV genotypes 1 or 4 infection in adults [FDA Label].
DB11613VelpatasvirVelpatasvir is used in combination therapy with other antiviral medications to treat chronic hepatitis C virus (HCV) infected patients with HCV genoptypes 1-6, and to treat HCV and HIV co-infected patients. Depending on the level of cirrhosis or decompensation, combination therapy can also include therapy with [DB00811]. When used in combination with [DB08934] as the combination product Epclusa, Velpatasvir is indicated for the treatment of adult patients with chronic hepatitis C virus (HCV) genotype 1, 2, 3, 4, 5, or 6 infection without cirrhosis or with compensated cirrhosis, or in combination with [DB00811] if associated with decompensated cirrhosis [FDA Label].
DB00360SapropterinFor the treatment of tetrahydrobiopterin (BH4) deficiency.
DB14569TedizolidNot Available
DB00503RitonavirIndicated in combination with other antiretroviral agents for the treatment of HIV-1 infection.
DB06654SafinamideSafinamide is indicated as an add-on treatment to levodopa with or without other medicines for Parkinson’s disease
DB13879GlecaprevirIndicated for the treatment of adult patients with chronic hepatitis C virus (HCV) genotype 1, 2, 3, 4, 5 or 6 infection without cirrhosis or with compensated cirrhosis (Child-Pugh A). MAVYRET is also indicated for the treatment of adult patients with HCV genotype 1 infection, who previously have been treated with a regimen containing an HCV NS5A inhibitor or an NS3/4A protease inhibitor (PI), but not both [FDA Label].
DB13878PibrentasvirIndicated for the treatment of adult patients with chronic hepatitis C virus (HCV) genotype 1, 2, 3, 4, 5 or 6 infection without cirrhosis or with compensated cirrhosis (Child-Pugh A). MAVYRET is also indicated for the treatment of adult patients with HCV genotype 1 infection, who previously have been treated with a regimen containing an HCV NS5A inhibitor or an NS3/4A protease inhibitor (PI), but not both [FDA Label].
DB12026VoxilaprevirVosevi (Voxilaprevir/[DB08934]/[DB11613]) is approved for use in patients with genotypes 1-6 who have been previously treated with an NS5A inhibitor, or patients with genotypes 1a or 3 infection who have previously been treated with an HCV regimen containing [DB08934] without an NS5A inhibitor [L935].
DB01167ItraconazoleFor the treatment of the following fungal infections in immunocompromised and non-immunocompromised patients: pulmonary and extrapulmonary blastomycosis, histoplasmosis, aspergillosis, and onychomycosis.
DB12015AlpelisibAlpelisib is indicated in combination with fulvestrant to treat postmenopausal women, and men, with advanced or metastatic breast cancer.[Label] This cancer must be hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and PIK3CA­ mutated.[Label] The cancer must be detected by an FDA-approved test following progression on or after an endocrine-based regimen.[Label]
DrugDrug NameTargetType
DB08912DabrafenibCytochrome P450 3A4enzyme
DB08912DabrafenibCytochrome P450 2C8enzyme
DB08912DabrafenibMultidrug resistance protein 1transporter
DB08912DabrafenibATP-binding cassette sub-family G member 2transporter
DB08912DabrafenibSolute carrier organic anion transporter family member 1B1transporter
DB08912DabrafenibSolute carrier organic anion transporter family member 1B3transporter
DB08912DabrafenibSolute carrier family 22 member 6transporter
DB08912DabrafenibSolute carrier family 22 member 8transporter
DB08912DabrafenibSerine/threonine-protein kinase B-raftarget
DB08912DabrafenibRAF proto-oncogene serine/threonine-protein kinasetarget
DB08912DabrafenibSerine/threonine-protein kinase SIK1target
DB08912DabrafenibSerine/threonine-protein kinase Nek11target
DB08912DabrafenibLIM domain kinase 1target
DB08912DabrafenibCytochrome P450 2B6enzyme
DB08912DabrafenibCytochrome 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
DB09065CobicistatSolute carrier organic anion transporter family member 1B1transporter
DB09065CobicistatSolute carrier organic anion transporter family member 1B3transporter
DB09048NetupitantSubstance-P receptortarget
DB09048NetupitantCytochrome P450 3A43enzyme
DB09048NetupitantCytochrome P450 2C9enzyme
DB09048NetupitantCytochrome P450 2D6enzyme
DB09048NetupitantCytochrome P450 3A4enzyme
DB06210EltrombopagThrombopoietin receptortarget
DB06210EltrombopagCytochrome P450 2C8enzyme
DB06210EltrombopagCytochrome P450 1A2enzyme
DB06210EltrombopagUDP-glucuronosyltransferase 1-1enzyme
DB06210EltrombopagUDP-glucuronosyltransferase 1-3enzyme
DB06210EltrombopagSolute carrier organic anion transporter family member 1B1transporter
DB06210EltrombopagATP-binding cassette sub-family G member 2transporter
DB06210EltrombopagUDP-glucuronosyltransferase 1-9enzyme
DB09183DasabuvirNonstructural protein 5B (NS5B)target
DB09183DasabuvirCytochrome P450 2C8enzyme
DB09183DasabuvirCytochrome P450 3A4enzyme
DB09183DasabuvirCytochrome P450 2D6enzyme
DB09183DasabuvirUDP-glucuronosyltransferase 1A1enzyme
DB09183DasabuvirATP-binding cassette sub-family G member 2transporter
DB09183DasabuvirATP-binding cassette sub-family B member 5transporter
DB09183DasabuvirMultidrug resistance protein 1transporter
DB09027LedipasvirNonstructural protein 5Atarget
DB09027LedipasvirMultidrug resistance protein 1transporter
DB09027LedipasvirATP-binding cassette sub-family G member 2transporter
DB09291RolapitantNeurokinin-1 Receptor (NK1R)target
DB09291RolapitantCytochrome P450 2D6enzyme
DB09291RolapitantCytochrome P450 3A4enzyme
DB09291RolapitantATP-binding cassette sub-family G member 2transporter
DB09291RolapitantMultidrug resistance protein 1transporter
DB09297ParitaprevirNS3/4A proteintarget
DB09297ParitaprevirCytochrome P450 3A4enzyme
DB09297ParitaprevirCytochrome P450 3A5enzyme
DB09297ParitaprevirATP-binding cassette sub-family G member 2transporter
DB09297ParitaprevirMultidrug resistance protein 1transporter
DB09297ParitaprevirSolute carrier organic anion transporter family member 1B1transporter
DB09297ParitaprevirSolute carrier organic anion transporter family member 1B3transporter
DB09102DaclatasvirNonstructural Protein 5A (NS5A)target
DB09102DaclatasvirCytochrome P450 3A5enzyme
DB09102DaclatasvirCytochrome P450 3A4enzyme
DB09102DaclatasvirCytochrome P450 3A43enzyme
DB09102DaclatasvirCytochrome P450 3A7enzyme
DB09102DaclatasvirMultidrug resistance protein 1transporter
DB09102DaclatasvirSolute carrier organic anion transporter family member 1B1transporter
DB09102DaclatasvirSolute carrier organic anion transporter family member 1B3transporter
DB09102DaclatasvirATP-binding cassette sub-family G member 2transporter
DB09330OsimertinibEpidermal growth factor receptortarget
DB09330OsimertinibMultidrug resistance protein 1transporter
DB09330OsimertinibATP-binding cassette sub-family G member 2transporter
DB09330OsimertinibCytochrome P450 3A4enzyme
DB09330OsimertinibCytochrome P450 1A2enzyme
DB11575GrazoprevirMultidrug resistance protein 1transporter
DB11575GrazoprevirSolute carrier organic anion transporter family member 1B1transporter
DB11575GrazoprevirSolute carrier organic anion transporter family member 1B3transporter
DB11575GrazoprevirCytochrome P450 3A4enzyme
DB11575GrazoprevirNS3/4A proteintarget
DB11575GrazoprevirSerum albumincarrier
DB11575GrazoprevirAlpha-1-acid glycoprotein 1carrier
DB11574ElbasvirNonstructural Protein 5A (NS5A)target
DB11574ElbasvirMultidrug resistance protein 1transporter
DB11574ElbasvirCytochrome P450 3A4enzyme
DB11574ElbasvirCytochrome P450 3A5enzyme
DB11574ElbasvirCytochrome P450 3A7enzyme
DB11574ElbasvirCytochrome P450 3A43enzyme
DB11613VelpatasvirCytochrome P450 2B6enzyme
DB11613VelpatasvirCytochrome P450 2C8enzyme
DB11613VelpatasvirCytochrome P450 3A4enzyme
DB11613VelpatasvirNonstructural Protein 5A (NS5A)target
DB11613VelpatasvirMultidrug resistance protein 1transporter
DB11613VelpatasvirATP-binding cassette sub-family G member 2transporter
DB11613VelpatasvirSolute carrier organic anion transporter family member 1B1transporter
DB11613VelpatasvirSolute carrier organic anion transporter family member 1B3transporter
DB11613VelpatasvirSolute carrier organic anion transporter family member 2B1transporter
DB00360SapropterinPhenylalanine-4-hydroxylasetarget
DB00360SapropterinNitric oxide synthase, endothelialtarget
DB00360SapropterinTyrosine 3-monooxygenasetarget
DB00360SapropterinTryptophan 5-hydroxylase 1target
DB00360SapropterinProstaglandin G/H synthase 2enzyme
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
DB00503RitonavirBile salt export pumptransporter
DB06654SafinamideAmine oxidase [flavin-containing] Btarget
DB06654SafinamideAmine oxidase [flavin-containing] Aenzyme
DB06654SafinamideATP-binding cassette sub-family G member 2transporter
DB06654SafinamideSolute carrier organic anion transporter family member 3A1transporter
DB06654SafinamideCytochrome P450 3A4enzyme
DB06654SafinamideCytochrome P450 1A1enzyme
DB06654SafinamideCytochrome P450 1A2enzyme
DB06654SafinamideCytochrome P450 2B6enzyme
DB06654SafinamideCytochrome P450 2C9enzyme
DB06654SafinamideCytochrome P450 2D6enzyme
DB06654SafinamideCytochrome P450 2C19enzyme
DB06654SafinamideCytochrome P450 2E1enzyme
DB06654SafinamideCytochrome P450 3A5enzyme
DB13879GlecaprevirCYP3Aenzyme
DB13879GlecaprevirUDP-glucuronosyltransferase 1-1enzyme
DB13879GlecaprevirMultidrug resistance protein 1transporter
DB13879GlecaprevirATP-binding cassette sub-family G member 2transporter
DB13879GlecaprevirSolute carrier organic anion transporter family member 1B1transporter
DB13879GlecaprevirSolute carrier organic anion transporter family member 1B3transporter
DB13879GlecaprevirNS3 proteasetarget
DB13878PibrentasvirNonstructural Protein 5A (NS5A)target
DB13878PibrentasvirCYP3Aenzyme
DB13878PibrentasvirUDP-glucuronosyltransferase 1-1enzyme
DB13878PibrentasvirMultidrug resistance protein 1transporter
DB13878PibrentasvirATP-binding cassette sub-family G member 2transporter
DB13878PibrentasvirSolute carrier organic anion transporter family member 1B1transporter
DB13878PibrentasvirSolute carrier organic anion transporter family member 1B3transporter
DB12026VoxilaprevirCytochrome P450 3A4enzyme
DB12026VoxilaprevirCytochrome P450 1A2enzyme
DB12026VoxilaprevirCytochrome P450 2C8enzyme
DB12026VoxilaprevirNS3/4A proteintarget
DB12026VoxilaprevirMultidrug resistance protein 1transporter
DB12026VoxilaprevirATP-binding cassette sub-family G member 2transporter
DB12026VoxilaprevirSolute carrier organic anion transporter family member 1B1transporter
DB12026VoxilaprevirSolute carrier organic anion transporter family member 1B3transporter
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
DB12015AlpelisibPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformtarget
DB12015AlpelisibCytochrome P450 3A4enzyme
DB12015AlpelisibCytochrome P450 2C9enzyme
DB12015AlpelisibCytochrome P450 2C8enzyme
DB12015AlpelisibCytochrome P450 2C19enzyme
DB12015AlpelisibATP-binding cassette sub-family G member 2transporter
DB12015AlpelisibMultidrug resistance protein 1transporter