BCRP/ABCG2 Inhibitors
- Name
- BCRP/ABCG2 Inhibitors
- Accession Number
- DBCAT002662 (DBCAT004102)
- Description
Not Available
- Drugs
Drug Drug Description Quercetin A natural flavonoid found in foods and natural supplement products. Naringenin Not Available Novobiocin For the treatment of infections due to staphylococci and other susceptible organisms Estrone An estrogen used to treat perimenopausal and postmenopausal symptoms. Saquinavir An HIV protease inhibitor used in combination with other antiretroviral agents for the treatment of HIV-1 with advanced immunodeficiency. Omeprazole A proton pump inhibitor used to treat GERD associated conditions such as heartburn and gastric acid hypersecretion, and to promote healing of tissue damage and ulcers caused by gastric acid and H. pylori infection. Hesperetin For lowering cholesterol and, possibly, otherwise favorably affecting lipids. In vitro research also suggests the possibility that hesperetin might have some anticancer effects and that it might have some anti-aromatase... Genistein Currently Genistein is being studied in clinical trials as a treatment for prostate cancer. Nelfinavir A viral protease inhibitor used in the treatment of HIV infection. Diethylstilbestrol Used in the treatment of prostate cancer. Previously used in the prevention of miscarriage or premature delivery in pregnant women prone to miscarriage or premature delivery. Ritonavir An HIV protease inhibitor used in combination with other antivirals in the treatment of HIV infection. Pantoprazole A proton pump inhibitor used to treat erosive esophagitis, gastric acid hypersecretion, and to promote healing of tissue damage caused by gastric acid. Cyclosporine A steroid-sparing immunosuppressant used in organ and bone marrow transplants as well as inflammatory conditions such as ulcerative colitis, rheumatoid arthritis, and atopic dermatitis. Taurocholic acid The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats... Imatinib A tyrosine kinase inhibitor used to treat a number of leukemias, myelodysplastic/myeloproliferative disease, systemic mastocytosis, hypereosinophilic syndrome, dermatofibrosarcoma protuberans, and gastrointestinal stromal tumors. Estradiol An estrogenic steroid used to treat vasomotor symptoms of vulvar and vaginal atrophy in menopause, hypoestrogenism, prevention of postmenopausal osteoporosis, treatment of breast cancer, and advanced androgen-dependent carcinoma of the prostate. Daidzin Not Available Sorafenib A kinase inhibitor used to treat unresectable liver carcinoma, advanced renal carcinoma, and differentiated thyroid carcinoma. Sunitinib A receptor tyrosine kinase inhibitor and chemotherapeutic agent used for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST). Dronabinol A synthetic delta-9-THC used in the treatment of anorexia and weight loss in HIV patients as well as nausea and vomiting in cancer chemotherapy. Buprenorphine A partial opioid agonist used for management of severe pain that is not responsive to alternative treatments. Also used for maintenance treatment of opioid addiction. Sulfasalazine A salicylate used to treat Crohn's disease, ulcerative colitis, and rheumatoid arthritis. Telmisartan An ARB used to treat hypertension, diabetic nephropathy, and congestive heart failure. Dexamethasone A glucocorticoid available in various modes of administration that is used for the treatment of various inflammatory conditions, including bronchial asthma, as well as endocrine and rheumatic disorders. Dasatinib A tyrosine kinase inhibitor used for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia or chronic myeloid leukemia. Rabeprazole A proton pump inhibitor used to help gastrointestinal ulcers heal, to treat symptoms of gastroesophageal reflux disease (GERD), to eradicate Helicobacter pylori, and to treat hypersecretory conditions such as Zollinger-Ellison Syndrome. Elacridar For the treatment of solid tumors. Nilotinib A kinase inhibitor used for the chronic phase treatment of Chronic Myeloid Leukemia (CML) that is Philadelphia chromosome positive and for the treatment of CML that is resistant to therapy containing imatinib. Erlotinib An EGFR tyrosine kinase inhibitor used to treat certain small cell lung cancers or advanced metastatic pancreatic cancers. Vandetanib An antineoplastic kinase inhibitor used to treat symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. Cabazitaxel An antineoplastic agent used for the treatment of hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing treatment regimen. Rilpivirine A non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with other antiretrovirals to specifically treat human immunodeficiency virus type 1 (HIV-1). Vismodegib A hedgehog pathway inhibitor used to treat patients with locally advanced or metastatic basal cell carcinoma. Regorafenib A kinase inhibitor used to treat patients with metastatic colorectal cancer, unresectable, locally advanced, or metastatic gastrointestinal stromal tumors, and hepatocellular carcinoma. Ponatinib A kinase inhibitor used to treat patients with various types of chronic myeloid leukemia (CML). Dabrafenib A kinase inhibitor used to treat patients with specific types of melanoma, non-small cell lung cancer, and thyroid cancer. Afatinib An antineoplastic agent used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with non-resistant EGFR mutations or resistance to platinum-based chemotherapy. Cobicistat A CYP3A inhibitor used to increase the systemic exposure of atazanavir or darunavir in combination with other antiretroviral agents in the treatment of HIV-1 infection. Rolapitant A neurokinin-1 (NK-1) receptor antagonist used in combination with other antiemetics for the prevention of delayed nausea and vomiting associated with emetogenic chemotherapy. Daclatasvir A direct-acting antiviral agent used to treat specific hepatitis C virus (HCV) infections in combination with other antiviral agents. Alectinib A kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Dasabuvir A direct-acting antiviral agent used to treat specific hepatitis C virus (HCV) infections in combination with other antiviral agents. Velpatasvir A NS5A inhibitor used to treat chronic hepatitis C infections in patients without cirrhosis or with compensated cirrhosis. Simeprevir A direct-acting antiviral agent that inhibits HCV NS3/4A protease to treat chronic hepatitis C virus (HCV) infection in adults with HCV genotype 1 or 4. Topiroxostat Indicated for the treatment of gout and hyperurcemia in Japan. Voxilaprevir A nonstructural protein 3 and 4a protease inhibitor used to treat Hepatitis C infections. Enasidenib An isocitrate dehydrogenase-2 inhibitor used to treat relapsed or refractory acute myeloid leukemia with an isocitrate dehydrogenase-2 mutation. Pibrentasvir A Hepatitis C NS5A inhibitor used to treat Hepatitis C. Glecaprevir A Hepatitis C NS3/4A protease inhibitor used to treat Hepatitis C. Abemaciclib A medication used to treat HR+ HER2- advanced or metastatic breast cancer. Letermovir An antiviral medication used to treat CMV infections and disease in adult CMV-seropositive recipients of an allogeneic hematopoietic stem cell transplant (HSCT). Brigatinib An anaplastic lymphoma kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Rucaparib A poly (ADP-ribose) polymerase (PARP) inhibitor used to treat recurrent ovarian and prostate cancers in previously treated adults. Baricitinib A Janus kinase inhibitor used to treat moderate to severe rheumatoid arthritis that has responded poorly to at least one TNF antagonist. Cannabidiol An active cannabinoid used as an adjunctive treatment for the management of seizures associated with Lennox-Gastaut syndrome or Dravet syndrome and symptomatic relief of moderate to severe neuropathic pain or other painful conditions, like cancer. Estradiol acetate An estrogen used to treat vasomotor symptoms and moderate to severe vulvar and vaginal atrophy from menopause. Estradiol benzoate An estrogen indicated in combination with progesterone for the treatment of irregular menstruation. Estradiol cypionate An estradiol prodrug used to treat vasomotor symptoms and hypoestrogenisms from hypogonadism. Estradiol dienanthate An estrogen used in some combined hormonal oral contraceptives. Estradiol valerate An estradiol prodrug used to treat some effects of menopause, hypoestrogenism, androgen dependant carcinoma of the prostate, and in combination products for endometriosis and contraception. Isavuconazole Indicated for patients 18 years of age and older for the treatment of invasive aspergillosis [FDA Label]. Indicated for patients 18 years of age and older for the treatment of... Nabiximols In Canada, Sativex has received a Notice of Compliance (NOC) for use as an as adjunctive treatment for symptomatic relief of spasticity in patients with multiple sclerosis (MS) who have... Medical Cannabis The use of the plant species Cannabis sativa and Cannabis indica, popularly known as marijuana, has gained popularity in recent years for the management of a wide variety of medical... Avatrombopag A thrombopoietin receptor agonist used to treat thrombocytopenia in patients with chronic liver disease who are scheduled to undergo a procedure. Gefitinib A tyrosine kinase inhibitor used as first-line therapy to treat non-small cell lung carcinoma (NSCLC) that meets certain genetic mutation criteria. Safinamide A MAO-B inhibitor used as an add-on treatment to levodopa/carbidopa for Parkinson's disease during "off" episodes. Paritaprevir A direct acting antiviral agent used in combination with other antiviral agents for the treatment of Hepatitis C Virus (HCV) infections. Fostamatinib A spleen tyrosine kinase inhibitor used to treat chronic immune thrombocytopenia after attempting one other treatment. Lansoprazole A proton pump inhibitor used to help gastrointestinal ulcers heal, to treat symptoms of gastroesophageal reflux disease (GERD), to eradicate Helicobacter pylori, and to treat hypersecretory conditions such as Zollinger-Ellison Syndrome. Pravastatin An HMG-CoA reductase inhibitor used to lower lipid levels and to reduce the risk of cardiovascular events, including myocardial infarction and stroke. Dovitinib Investigated for use/treatment in multiple myeloma and solid tumors. Eltrombopag A thrombopoietin receptor agonist used to treat thrombocytopenia or aplastic anemia associated with various etiologies. Teriflunomide A pyrimidine synthesis inhibitor with anti-inflammatory and immunomodulatory properties used to treat patients with the relapsing-remitting form of multiple sclerosis. Vemurafenib A kinase inhibitor used to treat patients with Erdheim-Chester Disease who have the BRAF V600 mutation, and melanoma in patients who have the BRAF V600E mutation. Progesterone A hormone used for a variety of functions, including contraception, control of abnormal uterine bleeding, maintenance of pregnancy, and prevention of endometrial hyperplasia. Fusidic acid A topical antibacterial agent used to prevent and treat mild to moderate skin infections caused by susceptible bacteria. Netupitant An antiemetic agent used in combination with palonosetron to prevent acute and delayed vomiting and nausea caused by chemotherapy. Ledipasvir A direct-acting antiviral agent used to treat specific hepatitis C virus (HCV) infections in combination with other antiviral agents. Osimertinib A tyrosine kinase inhibitor used in the treatment of certain types of non-small cell lung carcinoma. Grazoprevir An antiviral and NS3/4A protease inhibitor used to treat hepatitis C infections. Elbasvir An antiviral and NS5A inhibitor used to treat hepatitis C infections. Sapropterin A cofactor used as an adjunct to phenylalanine restriction in the treatment of phenylketonuria (PKU). Tedizolid An oxazolidinone class antibiotic that inhibits bacterial protein synthesis and is proven to be effective in the treatment of certain Gram-positive bacterial infections. Dacomitinib A medication used to treat non small cell lung cancer with EGFR exon 19 deletion of exon 21 L858R substitution. Venetoclax A BCL-2 inhibitor used to treat chronic lymphocytic leukemia, small lymphocytic lymphoma, or acute myeloid leukemia. Gilteritinib An AXL receptor tyrosine kinase inhibitor used to treat relapsed or refractory acute myeloid leukemia. Glasdegib A sonic hedgehog receptor inhibitor used to treat newly diagnosed acute myeloid leukemia in patients over 75 years who cannot receive intense chemotherapy. Olaparib A poly (ADP-ribose) polymerase (PARP) inhibitor used to treat ovarian cancer, breast cancer, pancreatic cancer, and prostate cancer. Itraconazole An antifungal agent used for the treatment of various fungal infections in immunocompromised and non-immunocompromised patients, such as pulmonary and extrapulmonary blastomycosis, histoplasmosis, and onychomycosis. Palbociclib An endocrine-based chemotherapeutic agent used in combination with other antineoplastic agents to treat HER2-negative and HR-positive advanced or metastatic breast cancer. Alpelisib Alpelisib is indicated in combination with fulvestrant to treat postmenopausal women, and men, with advanced or metastatic breast cancer. This cancer must be hormone receptor (HR)-positive, human epidermal growth factor... Beclomethasone dipropionate An inhaled corticosteroid used as maintenance treatment in the prophylaxis of asthma attacks. Fedratinib Fedratinib is indicated to treat adults with primary or secondary myelofibrosis that is either intermediate-2 or high risk. Istradefylline A selective adenoside A2A receptor antagonist indicated in adjunct to levodopa and carbidopa for the treatment of Parkinson's Disease. Caffeine A stimulant present in tea, coffee, cola beverages, analgesic drugs, and agents used to increase alertness. It is also used in to prevent and treat pulmonary complications of premature birth. Lasmiditan An oral 5HT1F agonist used for the acute treatment of migraine headache with or without aura. Darolutamide An androgen receptor antagonist used for castration-resistant, non-metastatic prostate cancer and metastatic hormone-sensitive prostate cancer. Upadacitinib An oral Janus kinase (JAK)1-selective inhibitor used in the treatment of moderate to severe rheumatoid arthritis, active psoriatic arthritis, ankylosing spondylitis, and severe atopic dermatitis, including in patients who did not respond well to other therapies. Tafamidis A medication used to treat transthyretin-mediated amyloidosis. Capmatinib A kinase inhibitor targeting c-Met receptor tyrosine kinase in the treatment of non-small cell lung cancer with MET exon 14 skipping. Selpercatinib A RET receptor tyrosine kinase inhibitor for the treatment of RET-driven non-small cell lung cancer, medullary thyroid cancer, and thyroid cancer in appropriate patient populations. Ripretinib A kinase inhibitor used to treat advanced gastrointestinal stromal tumor (GIST). Clofazimine A riminophenazine antimycobacterial used to treat leprosy. Dexamethasone acetate Commonly known as decadron, dexamethasone acetate is a glucocorticosteroid previously marketed in the USA for the treatment of inflammatory respiratory, allergic, autoimmune, and other conditions.[T797,L10695,L14348] Developed in 1957, dexamethasone is... Fostemsavir An antiretroviral HIV-1 attachment inhibitor targeted against the gp120 subunit within the HIV-1 gp160 envelope glycoprotein. Pralsetinib A RET receptor tyrosine kinase inhibitor for the treatment of metastatic RET-driven non-small cell lung cancer. Lonafarnib A potent farnesyl transferase inhibitor used to reduce mortality associated with Hutchinson-Gilford progeria syndrome (HGPS) and other progeroid laminopathies. Relugolix An oral GnRH receptor antagonist for androgen deprivation therapy in the treatment of advanced prostate cancer. Tepotinib An oral tyrosine kinase inhibitor targeted against MET for the treatment of metastatic non-small cell lung cancer in patients exhibiting MET exon 14 skipping mutations. Febuxostat A xanthine oxidase inhibitor used for the management of chronic hyperuricemia in adults with gout who have an inadequate response or intolerance to allopurinol. Avanafil A phosphodiesterase-5 (PDE5) inhibitor used to treat erectile dysfunction. Tivozanib A kinase inhibitor to treat adult patients with renal cell carcinoma (RCC) who have failed prior systemic therapies or experienced relapsed disease. Infigratinib An FGFR inhibitor used to treat locally advanced or metastatic cholangiocarcinoma in adults with a fibroblast growth factor receptor 2 (FGFR2) rearrangement. Sotorasib An experimental KRAS inhibitor being investigated for the treatment of KRAS G12C mutant non small cell lung cancer, colorectal cancer, and appendix cancer. Tecovirimat An antiviral medication used to treat smallpox, monkeypox, and cowpox. Avapritinib A selective tyrosine kinase inhibitor being investigated for the treatment of multidrug resistant gastrointestinal tumors. Brincidofovir An oral lipid prodrug of cidofovir used in the treatment of human smallpox disease. Belumosudil An oral inhibitor of rho-associated coiled-coil-containing protein kinases (ROCK) used in the treatment of chronic graft-versus-host disease (GVHD). Lorlatinib An anaplastic lymphoma kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Mobocertinib An oral kinase inhibitor targeted against EGFR and used in the treatment of NSCLC with EGFR exon 20 insertion mutations. Asciminib An inhibitor of ABL/BCR-ABL1 tyrosine kinase for the treatment of patients with Philadelphia chromosome-positive CML, including those with the T315I mutation. Maribavir A cytomegalovirus (CMV) pUL97 kinase inhibitor used for the treatment of refractory post-transplant CMV infection. Sotagliflozin An orally administered dual SGLT1/2 inhibitor used alongside insulin to improve glycemic control in patients with type 1 diabetes mellitus. Roxadustat A hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor used to treat symptomatic anemia associated with chronic kidney disease. Cannabinol Cannabinol (CBN) is a physiologically inactive constituent of Cannabis sativa. Pacritinib A kinase inhibitor used for the treatment of primary and secondary myelofibrosis in adult patients with significantly reduced platelet counts. Oteseconazole An azole antifungal used to prevent recurrent vulvovaginal candidiasis in females who are not of reproductive potential. Stiripentol An antiepileptic agent used in combination with other anticonvulsants to treat seizures associated with Dravet syndrome. Baloxavir marboxil A polymerase acidic endonuclease inhibitor used to treat uncomplicated influenza. Deucravacitinib A TYK2 inhibitor being investigated as a treatment for psoriasis. Niraparib A poly-ADP ribose polymerase inhibitor used to treat recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer responding to platinum based chemotherapy. Olutasidenib An isocitrate dehydrogenase-1 (IDH1) inhibitor indicated for the treatment of patients with relapsed or refractory acute myeloid leukemia with a susceptible IDH1 mutation as detected by an FDA-approved test. Elacestrant An estrogen receptor antagonist used to treat ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy. Pirtobrutinib A kinase inhibitor used to treat relapsed or refractory mantle cell lymphoma (MCL) after at least two lines of systemic therapy. Sparsentan An endothelin and angiotensin II receptor antagonist indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy at risk of rapid disease progression. - Drugs & Drug Targets