MATE inhibitors

Includes Multidrug and toxin extrusion protein 1 and Multidrug and toxin extrusion protein 2 inhibitors
DrugDrug NameDrug Indication
DB01137LevofloxacinFor the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms: Corynebacterium species, Staphylococus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus (Groups C/F/G), Viridans group streptococci, Acinetobacter lwoffii, Haemophilus influenzae, Serratia marcescens.
DB00537CiprofloxacinCiprofloxacin is only indicated in infections caused by susceptible bacteria.[L6469,L6472,L6475,L6478,L6481,L6484,L6487,L6490,L6493] Ciprofloxacin immediate release tablets, oral suspensions, and intravenous injections are indicated for the treatment of skin and skin structure infections, bone and joint infections, complicated intra-abdominal infections, nosocomial pneumonia, febrile neutropenia, adults who have inhaled anthrax, plague, chronic bacterial prostatitis, lower respiratory tract infections including acute exacerbations of chronic bronchitis, urinary tract infections, complicated urinary tract infections in pediatrics, complicated pyelonephritis in pediatrics, and acute sinusitis.[L6481,L6478] A ciprofloxacin otic solution and otic suspension with hydrocortisone are indicated for acute otitis externa.[L6469,L6484] Ciprofloxacin suspension with dexamethasone is indicated for acute otitis media in pediatric patients with tympanostomy tubes or acute otitis externa.[L6490] A ciprofloxacin intratympanic injection is indicated for pediatric patients with bilateral otitis media with effusion who are having tympanostomy tubes placed or pediatric patients 6 months or older with acute otitis externa.[L6493] A ciprofloxacin eye drop is indicated for bacterial corneal ulcers and conjunctivitis.[L6472] A ciprofloxacin eye ointment is indicated for bacterial conjunctivitis.[L6475] A ciprofloxacin extended release tablet is indicated for uncomplicated urinary tract infections, complicated urinary tract infections, and acute uncomplicated pyelonephritis.[L6487]
DB00501CimetidineFor the treatment and the management of acid-reflux disorders (GERD), peptic ulcer disease, heartburn, and acid indigestion.
DB12001Abemaciclib* Indicated in combination with fulvestrant for the treatment of women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer with disease progression following endocrine therapy. * Inidicated as monotherapy for the treatment of adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting.
DB12267BrigatinibThe anaplastic lymphoma kinase positive, metastatic non-small cell lung cancer (ALK+ NSCLC), represents only 3-5% of the NSCLC cancer cases, but the ALK mutation, overexpression and presence in several oncogenic fusion proteins in solid and hematologic tumors have pointed out the importance as well as its potential as a cancer therapy target.[A31311] The ALK-related cases of NSCLC are associated with the presence of the fusion gene EML4-ALK which fused the ALK protein with the echinoderm microtubule-associated protein like-4 whose original function is the correct formation of microtubules.[A31313] The presence of the aberrant fusion protein results in abnormal signaling that provokes increased cell growth, proliferation and survival.[A31316] Crizotinib is indicated for the treatment of such cases but the presence of ALK kinase domain mutations confer resistance to the treatment. Thus, brigatinib is indicated for the treatment of patients with ALK+ NSCLC with intolerance to Crizotinib.[A31314]
DB11799BictegravirBictegravir is indicated in the management of HIV-1 infection in patients not previously treated with antiretroviral therapy. Additionally, Bictegravir is indicated in the management of HIV-1 infection in patients who are virologically suppressed (HIV-1 RNA <50 c/mL) on a regular antiretroviral regimen for a minimum of three months without a history of failure in treatment and no known factors associated with the resistance to the individual components of the medication. It is used in combination with tenofovir and emtricitabine [L1219, L1220].
DB04948LofexidineLofexidine is indicated for mitigation of symptoms associated with acute withdrawal from opioids and for facilitation of the completion of opioid discontinuation treatment. It is the first non-opioid medication for the symptomatic management of opioid discontinuation.[L2801] Opioid withdrawal syndrome is a debilitating manifestation of opioid dependence.[A33085] This condition is extremely unpleasant lasting several days with some of the main features being abdominal pain, nausea, diarrhea, mydriasis, lacrimation, and piloerection. These symptoms are often observed after abrupt reductions in the opioid dose and can be resolved by re-administration of the opioid.[A33088]
DB12483CopanlisibIndicated for the treatment of adult patients with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies.
DB12332RucaparibIndicated as monotherapy for the treatment of patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer who have been treated with two or more chemotherapies. Select patients for therapy based on an FDA-approved companion diagnostic for rucaparib.
DB12615PlazomicinPlazomicin is indicated for the treatment of patients 18 years of age or older with Complicated Urinary Tract Infections (cUTI) including Pyelonephritis, who have limited or no alternative treatment options. It should only be used to treat infections that are proven or strongly suspected to be caused by susceptible microorganisms [FDA Label].
DB06608TafenoquineTafenoquine is used for the treatment and prevention of relapse of Vivax malaria in patients 16 years and older. Tafenoquine is not indicated to treat acute vivax malaria.[A35671] Malaria is a disease that remains to occur in many tropical countries. Vivax malaria, caused by _Plasmodium vivax_, is known to be less virulent and seldom causes death. However, it causes a substantive illness-related burden in endemic areas and it is known to present dormant forms in the hepatocytes named hypnozoites which can remain dormant for weeks or even months. This dormant form produces ongoing relapses.[A35671]
DB11901ApalutamideIndicated for the treatment of patients with non-metastatic, castration-resistant prostate cancer (NM-CRPC) [FDA Label].
DB01030TopotecanFor the treatment of advanced ovarian cancer in patients with disease that has recurred or progressed following therapy with platinum-based regimens. Also used as a second-line therapy for treatment-sensitive small cell lung cancer, as well as in combination with cisplatin for the treatment of stage IV-B, recurrent, or persistent cervical cancer not amenable to curative treatment with surgery and/or radiation therapy.
DB11817BaricitinibIndicated for the treatment of moderate to severe active rheumatoid arthritis in adult patients who have responded inadequately to, or who are intolerant to one or more disease-modifying anti-rheumatic drugs as monotherapy or in combination with methotrexate.
DB00205PyrimethamineFor the treatment of toxoplasmosis and acute malaria; For the prevention of malaria in areas non-resistant to pyrimethamine
DB11753RifamycinRifamycin is indicated for the treatment of adult patients with travelers' diarrhea caused by noninvasive strains of _E. coli_. The status of the disease should not be complicated by fever or blood in the stool. To prevent drug-resistant bacteria, it is important to mention that the use of rifamycin for this indication should be only done in cases where the infection is proven or strongly suspected to be caused by bacteria.[L4802] Travallers' diarrhea is very common problem affecting 20-60% of the travellers and it is defined as an increase in frequency of bowel movements to three or more loose stools per day during a trip abroad. This condition is rarely life threatening but in severe cases it can produce dehydration and sepsis. The most common cause of travellers' diarrhea is a pathogen and from the pathogens identified, bacteria is the most common cause followed by norovirus, rotavirus and similar viruses.[A39995]
DB12141GilteritinibGilteritinib is indicated for the treatment of adult patients who have relapsed or refractory acute myeloid leukemia with an FLT3 mutation detected by an FDA-approved test. This indication was expanded for a companion diagnostic to include use with gilteritinib such as the LeukoStrat CDx FLT3 Mutation Assay.[L4830] Acute myeloid leukemia is cancer that impacts the blood and bone marrow with a rapid progression. This condition produces low numbers of normal blood cells and the requirement of continuous need for transfusions.[L4832]
DB11978GlasdegibGlasdegib, in combination with cytarabine, is indicated for the treatment of newly diagnosed acute myeloid leukemia in adult patients who are over 75 years old or that have co-morbidities that preclude intensive induction chemotherapy.[L5080] Acute myeloid leukemia is characterized by abnormal production of myeloblasts, red cells, or platelets. It is considered a cancer of blood and bone marrow and it is the most common type of acute leukemia in adults.[L4832]
DrugDrug NameTargetType
DB01137LevofloxacinDNA gyrase subunit Atarget
DB01137LevofloxacinDNA topoisomerase 4 subunit Atarget
DB01137LevofloxacinDNA topoisomerase 2-alphatarget
DB01137LevofloxacinCytochrome P450 1A2enzyme
DB01137LevofloxacinSolute carrier family 22 member 2transporter
DB01137LevofloxacinMultidrug resistance protein 1transporter
DB01137LevofloxacinSolute carrier family 22 member 4transporter
DB01137LevofloxacinSolute carrier family 22 member 6transporter
DB01137LevofloxacinCytochrome P450 3A4enzyme
DB01137LevofloxacinMultidrug and toxin extrusion protein 1transporter
DB01137LevofloxacinMultidrug and toxin extrusion protein 2transporter
DB00537CiprofloxacinDNA gyrase subunit Atarget
DB00537CiprofloxacinDNA topoisomerase 4 subunit Atarget
DB00537CiprofloxacinDNA topoisomerase 2-alphatarget
DB00537CiprofloxacinCytochrome P450 1A2enzyme
DB00537CiprofloxacinCytochrome P450 3A4enzyme
DB00537CiprofloxacinCytochrome P450 3A5enzyme
DB00537CiprofloxacinCytochrome P450 3A7enzyme
DB00537CiprofloxacinMultidrug resistance protein 1transporter
DB00537CiprofloxacinPotassium voltage-gated channel subfamily H member 2target
DB00537CiprofloxacinDNA gyrase subunit Atarget
DB00537CiprofloxacinDNA topoisomerase 4 subunit Atarget
DB00537CiprofloxacinDNA topoisomerase 4 subunit Btarget
DB00537CiprofloxacinDNA gyrase subunit Atarget
DB00537CiprofloxacinMultidrug resistance protein MdtKtarget
DB00537CiprofloxacinGyrase Atarget
DB00537CiprofloxacinDNA gyrase subunit Atarget
DB00537CiprofloxacinMultidrug and toxin extrusion protein 1transporter
DB00537CiprofloxacinMultidrug and toxin extrusion protein 2transporter
DB00537CiprofloxacinSerum albumincarrier
DB00501CimetidineHistamine H2 receptortarget
DB00501CimetidineCytochrome P450 1A2enzyme
DB00501CimetidineCytochrome P450 2D6enzyme
DB00501CimetidineCytochrome P450 2C19enzyme
DB00501CimetidineCytochrome P450 3A4enzyme
DB00501CimetidineCytochrome P450 3A5enzyme
DB00501CimetidineCytochrome P450 3A7enzyme
DB00501CimetidineMultidrug resistance protein 1transporter
DB00501CimetidineSolute carrier family 22 member 2transporter
DB00501CimetidineSolute carrier family 22 member 1transporter
DB00501CimetidineSolute carrier family 22 member 3transporter
DB00501CimetidineSolute carrier family 22 member 5transporter
DB00501CimetidineSolute carrier family 22 member 6transporter
DB00501CimetidineSolute carrier family 22 member 8transporter
DB00501CimetidineMultidrug and toxin extrusion protein 1transporter
DB00501CimetidineSolute carrier family 22 member 4transporter
DB00501CimetidineSolute carrier family 22 member 11transporter
DB00501CimetidineSolute carrier family 22 member 7transporter
DB00501CimetidineCytochrome P450 11B1, mitochondrialenzyme
DB00501CimetidineCytochrome P450 2C8enzyme
DB00501CimetidineCytochrome P450 2C9enzyme
DB00501CimetidineCytochrome P450 2E1enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 3enzyme
DB00501CimetidineDimethylaniline monooxygenase [N-oxide-forming] 1enzyme
DB00501CimetidineBile salt export pumptransporter
DB00501CimetidineMultidrug and toxin extrusion protein 2transporter
DB12001AbemaciclibMultidrug and toxin extrusion protein 1transporter
DB12001AbemaciclibMultidrug and toxin extrusion protein 2transporter
DB12001AbemaciclibCyclin-dependent kinase 4target
DB12001AbemaciclibCyclin-dependent kinase 6target
DB12001AbemaciclibSerum albumincarrier
DB12001Abemaciclibalpha1-acid glycoproteincarrier
DB12001AbemaciclibCytochrome P450 3A4enzyme
DB12001AbemaciclibOrnithine carbamoyltransferase, mitochondrialtransporter
DB12001AbemaciclibMultidrug resistance protein 1transporter
DB12001AbemaciclibATP-binding cassette sub-family G member 2transporter
DB12267BrigatinibALK tyrosine kinase receptortarget
DB12267BrigatinibEpidermal growth factor receptortarget
DB12267BrigatinibTyrosine-protein kinase ABL1target
DB12267BrigatinibInsulin-like growth factor 1 receptortarget
DB12267BrigatinibReceptor-type tyrosine-protein kinase FLT3target
DB12267BrigatinibCytochrome P450 2C8enzyme
DB12267BrigatinibCytochrome P450 3A4enzyme
DB12267BrigatinibInsulin receptortarget
DB12267BrigatinibHepatocyte growth factor receptortarget
DB12267BrigatinibReceptor tyrosine-protein kinase erbB-4target
DB12267BrigatinibReceptor tyrosine-protein kinase erbB-2target
DB12267BrigatinibATP-binding cassette sub-family B member 5transporter
DB12267BrigatinibATP-binding cassette sub-family G member 2transporter
DB12267BrigatinibSolute carrier family 22 member 1transporter
DB12267BrigatinibMultidrug and toxin extrusion protein 1transporter
DB12267BrigatinibMultidrug and toxin extrusion protein 2transporter
DB12267BrigatinibCYP3Aenzyme
DB11799BictegravirReverse transcriptase/RNaseHtarget
DB11799BictegravirIntegrasetarget
DB11799BictegravirCytochrome P450 3A4enzyme
DB11799BictegravirUDP-glucuronosyltransferase 1-1enzyme
DB11799BictegravirPOU domain, class 2, transcription factor 2enzyme
DB11799BictegravirMultidrug and toxin extrusion protein 1enzyme
DB04948LofexidineAlpha-2A adrenergic receptortarget
DB04948LofexidineAlpha-1A adrenergic receptortarget
DB04948Lofexidine5-hydroxytryptamine receptor 1Atarget
DB04948Lofexidine5-hydroxytryptamine receptor 7target
DB04948Lofexidine5-hydroxytryptamine receptor 2Ctarget
DB04948Lofexidine5-hydroxytryptamine receptor 1Dtarget
DB04948LofexidineCytochrome P450 2D6enzyme
DB04948LofexidineCytochrome P450 1A2enzyme
DB04948LofexidineCytochrome P450 2C19enzyme
DB04948LofexidineATP-binding cassette sub-family B member 5transporter
DB04948LofexidineMultidrug and toxin extrusion protein 1transporter
DB12483CopanlisibPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformtarget
DB12483CopanlisibPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoformtarget
DB12483CopanlisibCytochrome P450 3A4enzyme
DB12483CopanlisibCytochrome P450 3A5enzyme
DB12483CopanlisibCytochrome P450 3A7enzyme
DB12483CopanlisibCytochrome P450 3A43enzyme
DB12483CopanlisibMultidrug resistance protein 1transporter
DB12483CopanlisibATP-binding cassette sub-family G member 2transporter
DB12483CopanlisibMultidrug and toxin extrusion protein 2transporter
DB12483CopanlisibSerum albumincarrier
DB12332RucaparibPoly [ADP-ribose] polymerase 1target
DB12332RucaparibPoly [ADP-ribose] polymerase 2target
DB12332RucaparibPoly [ADP-ribose] polymerase 3target
DB12332RucaparibCytochrome P450 2D6enzyme
DB12332RucaparibCytochrome P450 1A2enzyme
DB12332RucaparibCytochrome P450 3A4enzyme
DB12332RucaparibMultidrug resistance protein 1transporter
DB12332RucaparibATP-binding cassette sub-family G member 2transporter
DB12332RucaparibMultidrug and toxin extrusion protein 1transporter
DB12332RucaparibMultidrug and toxin extrusion protein 2transporter
DB12332RucaparibSolute carrier family 22 member 1transporter
DB12332RucaparibMultidrug resistance-associated protein 4transporter
DB12332RucaparibSolute carrier organic anion transporter family member 1B1transporter
DB12332RucaparibSolute carrier organic anion transporter family member 1B3transporter
DB12332RucaparibSolute carrier family 22 member 6transporter
DB12332RucaparibSolute carrier family 22 member 8transporter
DB12332RucaparibCytochrome P450 3A5enzyme
DB12332RucaparibCytochrome P450 3A7enzyme
DB12332RucaparibCytochrome P450 3A43enzyme
DB12332RucaparibCytochrome P450 2C19enzyme
DB12332RucaparibCytochrome P450 2C9enzyme
DB12332RucaparibCytochrome P450 2C8enzyme
DB12332RucaparibUDP-glucuronosyltransferase 1-1enzyme
DB12615PlazomicinMultidrug and toxin extrusion protein 1transporter
DB12615PlazomicinMultidrug and toxin extrusion protein 2transporter
DB12615Plazomicin30S ribosomal protein S14target
DB12615Plazomicin30S ribosomal protein S11target
DB06608TafenoquineCytochrome P450 2D6enzyme
DB06608TafenoquineFerredoxin--NADP reductase, apicoplastenzyme
DB06608TafenoquineSolute carrier family 22 member 2transporter
DB06608TafenoquineMultidrug and toxin extrusion protein 1transporter
DB06608TafenoquineMultidrug and toxin extrusion protein 2transporter
DB11901ApalutamideAndrogen receptortarget
DB11901ApalutamideCytochrome P450 3A4enzyme
DB11901ApalutamideCytochrome P450 2C8enzyme
DB11901ApalutamideCytochrome P450 2C19enzyme
DB11901ApalutamideCytochrome P450 2C9enzyme
DB11901ApalutamideMultidrug resistance protein 1transporter
DB11901ApalutamideATP-binding cassette sub-family G member 2transporter
DB11901ApalutamideSolute carrier organic anion transporter family member 1B1transporter
DB11901ApalutamideSolute carrier family 22 member 2transporter
DB11901ApalutamideSolute carrier family 22 member 8transporter
DB11901ApalutamideMultidrug and toxin extrusion protein 2transporter
DB11901ApalutamideGABA-A receptor (anion channel)target
DB01030TopotecanDNA topoisomerase I, mitochondrialtarget
DB01030TopotecanDNA topoisomerase 1target
DB01030TopotecanATP-binding cassette sub-family G member 2transporter
DB01030TopotecanMultidrug resistance protein 1transporter
DB01030TopotecanCytochrome P450 3A4enzyme
DB01030TopotecanDNAtarget
DB01030TopotecanMultidrug and toxin extrusion protein 1transporter
DB01030TopotecanMultidrug and toxin extrusion protein 2transporter
DB11817BaricitinibSolute carrier family 22 member 8transporter
DB11817BaricitinibATP-binding cassette sub-family G member 2transporter
DB11817BaricitinibMultidrug and toxin extrusion protein 2transporter
DB11817BaricitinibCytochrome P450 3A4enzyme
DB11817BaricitinibTyrosine-protein kinase JAK1target
DB11817BaricitinibTyrosine-protein kinase JAK2target
DB11817BaricitinibSolute carrier family 22 member 6transporter
DB11817BaricitinibSolute carrier family 22 member 2transporter
DB11817BaricitinibSolute carrier organic anion transporter family member 1B3transporter
DB11817BaricitinibProtein-tyrosine kinase 2-betatarget
DB11817BaricitinibTyrosine-protein kinase JAK3target
DB00205PyrimethamineBifunctional dihydrofolate reductase-thymidylate synthasetarget
DB00205PyrimethamineDihydrofolate reductasetarget
DB00205PyrimethamineCytochrome P450 2C8enzyme
DB00205PyrimethamineBeta-hexosaminidase subunit betatarget
DB00205PyrimethamineMultidrug and toxin extrusion protein 1transporter
DB00205PyrimethamineMultidrug and toxin extrusion protein 2transporter
DB11753RifamycinCytochrome P450 3A4enzyme
DB11753RifamycinCytochrome P450 2C19enzyme
DB11753RifamycinCytochrome P450 2B6enzyme
DB11753RifamycinCytochrome P450 2C8enzyme
DB11753RifamycinCytochrome P450 2C9enzyme
DB11753RifamycinCytochrome P450 2D6enzyme
DB11753RifamycinSolute carrier organic anion transporter family member 1A2transporter
DB11753RifamycinSolute carrier organic anion transporter family member 1B1transporter
DB11753RifamycinSolute carrier organic anion transporter family member 1B3transporter
DB11753RifamycinSolute carrier organic anion transporter family member 2A1transporter
DB11753RifamycinSolute carrier organic anion transporter family member 2B1transporter
DB11753RifamycinSerum albumincarrier
DB11753RifamycinDNA-directed RNA polymerase subunit betatarget
DB11753RifamycinDNA-directed RNA polymerase subunit alphatarget
DB11753RifamycinDNA-directed RNA polymerase subunit beta'target
DB11753RifamycinMultidrug and toxin extrusion protein 1transporter
DB11753RifamycinCytochrome P450 1A2enzyme
DB11753RifamycinMultidrug resistance protein 1transporter
DB12141GilteritinibSerum albumincarrier
DB12141GilteritinibCytochrome P450 3A4enzyme
DB12141GilteritinibReceptor-type tyrosine-protein kinase FLT3target
DB12141GilteritinibSerotonin Receptorstarget
DB12141GilteritinibMultidrug resistance protein 1transporter
DB12141GilteritinibMultidrug and toxin extrusion protein 1transporter
DB12141GilteritinibATP-binding cassette sub-family G member 2transporter
DB12141GilteritinibSolute carrier family 22 member 1transporter
DB12141GilteritinibTyrosine-protein kinase receptor UFOtarget
DB12141GilteritinibALK tyrosine kinase receptortarget
DB11978GlasdegibCytochrome P450 3A4enzyme
DB11978GlasdegibSmoothened homologtarget
DB11978GlasdegibCytochrome P450 2C8enzyme
DB11978GlasdegibUDP-glucuronosyltransferase 1-9enzyme
DB11978GlasdegibSerum albumincarrier
DB11978GlasdegibMultidrug resistance protein 1transporter
DB11978GlasdegibATP-binding cassette sub-family G member 2transporter
DB11978GlasdegibMultidrug and toxin extrusion protein 1transporter
DB11978GlasdegibMultidrug and toxin extrusion protein 2transporter