Organic Anion Transporting Polypeptide 1B1 Inhibitors

DrugDrug NameDrug Indication
DB06290SimeprevirIndicated for the treatment of adults with chronic hepatitis C virus (HCV) infection: typically in combination with sofosbuvir in patients with HCV genotype 1 without cirrhosis or with compensated cirrhosis and in combination with peginterferon alfa (Peg-IFN-alfa) and ribavirin (RBV) in patients with HCV genotype 1 or 4 without cirrhosis or with compensated cirrhosis. Resistance: Reduced susceptibility to simeprevir was most commonly associated with the viral NS3 Q80K polymorphism. Amino acid substitutions at NS3 positions S122, R155 and/or D168 are also shown to reduce susceptibility to simeprevir in genotype 1a/b patients.
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].
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.
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.
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.
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].
DB01601LopinavirIndicated in combination with other antiretroviral agents for the treatment of HIV-infection.
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].
DB12070LetermovirFor use in prophylaxis of cytomegalovirus (CMV) infection and disease in adult CMV-seropositive recipients of an allogeneic hematopoietic stem cell transplant (HSCT) [FDA Label].
DrugDrug NameTargetType
DB06290SimeprevirNS3 proteasetarget
DB06290SimeprevirSerum albumincarrier
DB06290SimeprevirCytochrome P450 1A2enzyme
DB06290SimeprevirMultidrug resistance protein 1transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 1B1transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 1B3transporter
DB06290SimeprevirCytochrome P450 3A4enzyme
DB06290SimeprevirCanalicular multispecific organic anion transporter 1transporter
DB06290SimeprevirATP-binding cassette sub-family G member 2transporter
DB06290SimeprevirSolute carrier organic anion transporter family member 2B1transporter
DB06290SimeprevirSodium/bile acid cotransportertransporter
DB06290SimeprevirBile salt export pumptransporter
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
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
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
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
DB09297ParitaprevirUDP-glucuronosyltransferase 1-1enzyme
DB09102DaclatasvirNonstructural protein 5Atarget
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
DB11613VelpatasvirCytochrome P450 2B6enzyme
DB11613VelpatasvirCytochrome P450 2C8enzyme
DB11613VelpatasvirCytochrome P450 3A4enzyme
DB11613VelpatasvirNonstructural protein 5Atarget
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
DB01601LopinavirHuman immunodeficiency virus type 1 proteasetarget
DB01601LopinavirCytochrome P450 3A4enzyme
DB01601LopinavirCytochrome P450 2D6enzyme
DB01601LopinavirCytochrome P450 2C19enzyme
DB01601LopinavirMultidrug resistance protein 1transporter
DB01601LopinavirCytochrome P450 2B6enzyme
DB01601LopinavirCytochrome P450 2C9enzyme
DB01601LopinavirCytochrome P450 2C8enzyme
DB01601LopinavirCYP3Aenzyme
DB01601LopinavirSolute carrier organic anion transporter family member 1B1transporter
DB01601LopinavirSolute carrier organic anion transporter family member 1B3transporter
DB01601LopinavirBile salt export pumptransporter
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 5Atarget
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
DB12070LetermovirUDP-glucuronosyltransferase 1-1enzyme
DB12070LetermovirUDP-glucuronosyltransferase 1-3enzyme
DB12070LetermovirSolute carrier organic anion transporter family member 1B1transporter
DB12070LetermovirSolute carrier organic anion transporter family member 1B3transporter
DB12070LetermovirTripartite terminase subunit 1target
DB12070LetermovirTripartite terminase subunit 2target
DB12070LetermovirTripartite terminase subunit 3target
DB12070LetermovirCytochrome P450 2D6enzyme
DB12070LetermovirCytochrome P450 2C8enzyme
DB12070LetermovirCytochrome P450 2C19enzyme
DB12070LetermovirCytochrome P450 2C9enzyme
DB12070LetermovirCytochrome P450 2B6enzyme
DB12070LetermovirMultidrug resistance protein 1transporter
DB12070LetermovirATP-binding cassette sub-family G member 2transporter
DB12070LetermovirBile salt export pumptransporter
DB12070LetermovirSolute carrier family 22 member 8transporter
DB12070LetermovirCanalicular multispecific organic anion transporter 1transporter
DB12070LetermovirCytochrome P450 3A4enzyme
DB12070LetermovirCytochrome P450 3A5enzyme
DB12070LetermovirCytochrome P450 3A7enzyme
DB12070LetermovirCytochrome P450 3A43enzyme