BCRP/ABCG2 Substrates
- Name
- BCRP/ABCG2 Substrates
- Accession Number
- DBCAT002663
- Description
Not Available
- Drugs
Drug Drug Description Gefitinib A tyrosine kinase inhibitor used as first-line therapy to treat non-small cell lung carcinoma (NSCLC) that meets certain genetic mutation criteria. Topotecan An antineoplastic agent used to treat ovarian cancer, small cell lung cancer, or cervical cancer. Glyburide A sulfonylurea used in the treatment of non insulin dependent diabetes mellitus. Pravastatin An HMG-CoA reductase inhibitor used to lower lipid levels and to reduce the risk of cardiovascular events, including myocardial infarction and stroke. Doxorubicin A medication used to treat various cancers, including AIDS-associated Kaposi's Sarcoma and metastatic cancers. Mitoxantrone A chemotherapeutic agent used for the treatment of secondary progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis. Sorafenib A kinase inhibitor used to treat unresectable liver carcinoma, advanced renal carcinoma, and differentiated thyroid carcinoma. Sulfasalazine A salicylate used to treat Crohn's disease, ulcerative colitis, and rheumatoid arthritis. Dasatinib A tyrosine kinase inhibitor used for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia or chronic myeloid leukemia. Prazosin An alpha-blocker that causes a decrease in total peripheral resistance and is used to treat hypertension. Lamivudine A reverse transcriptase inhibitor used to treat HIV and hepatitis B infections. Irinotecan A topoisomerase inhibitor used to treat metastatic carcinoma of the colon or rectum and pancreatic adenocarcinoma. Etoposide A podophyllotoxin derivative used to treat testicular and small cell lung tumors. Dactinomycin An actinomycin used to treat a wide variety of cancers. Conjugated estrogens A mixture of estrogens used in estrogen replacement therapy for menopause and hypoestrogenism, used in the treatment of various malignancies, and used in the treatment of postmenopausal osteoporosis. Cerivastatin A statin (or HMG CoA reductase inhibitor) used with dietary changes to decrease lipid levels and reduce the risk of cardiovascular events. Testosterone A hormone used to treat hypogonadism, breast carcinoma in women, or the vasomotor symptoms of menopause. Tamoxifen A selective estrogen receptor modulator used to treat estrogen receptor positive breast cancer, reduce the risk of invasive breast cancer following surgery, or reduce the risk of breast cancer in high risk women. Daunorubicin An anthracycline aminoglycoside used to induce remission of nonlymphocytic leukemia and acute lymphocytic leukemia. Methotrexate An antineoplastic agent used the treatment of a wide variety of cancers as well as severe psoriasis, severe rheumatoid arthritis, and juvenile rheumatoid arthritis. Folic acid A nutrient used to treat megaloblastic anemia and is found in many supplements. Alvocidib Investigated for use/treatment in esophageal cancer, leukemia (lymphoid), lung cancer, liver cancer, and lymphoma (unspecified). Teniposide A cytotoxic drug used as an adjunct for chemotherapy induction in the treatment of refractory childhood acute lymphoblastic leukemia. Nitrofurantoin An antibiotic used to treat urinary tract infections. Ivermectin An anti parasite medication used to treat head lice, onchocerciasis, strongyloidiasis, ascariasis, trichuriasis, and enterobiasis. Camptothecin Investigated for the treatment of cancer. Riluzole A glutamate antagonist used to treat amyotrophic lateral sclerosis. Cladribine A purine antimetabolite used to treat Multiple Sclerosis (MS) and hairy cell leukemia. Clofarabine A purine nucleoside used to treat relapsed or refractory acute lymphoblastic leukemia in patients 1 to 21 years old. Oxaliplatin A platinum based chemotherapy agent used to treat carcinoma of the colon or rectum or stage III colon cancer. Pitavastatin An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke. Pazopanib An antineoplastic agent used in the treatment of advanced renal cell cancer and advanced soft tissue sarcoma in patients with prior chemotherapy. Teriflunomide A pyrimidine synthesis inhibitor with anti-inflammatory and immunomodulatory properties used to treat patients with the relapsing-remitting form of multiple sclerosis. Leflunomide A pyrimidine synthesis inhibitor indicated to treat rheumatoid arthritis. 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. Apixaban An anticoagulant used for the prophylaxis of stroke and systemic embolism in nonvalvular atrial fibrillation, and deep vein thrombosis(DVT) leading to pulmonary embolism(PE), including in patients after a hip or knee replacement surgery. 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. Zidovudine A dideoxynucleoside used in the treatment of HIV infection. 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. Fluorouracil A pyrimidine analog used to treat basal cell carcinomas, and as an injection in palliative cancer treatment. Mycophenolate mofetil An inosine monophosphate dehydrogenase inhibitor used to prevent the rejection of kidney, heart, or liver transplants. Rosuvastatin An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke. Sofosbuvir A direct-acting antiviral agent used to treat specific hepatitis C virus (HCV) infections in combination with other antiviral agents. Lenvatinib A receptor tyrosine kinase inhibitor used for the treatment of metastatic thyroid cancer, advanced renal cell carcinoma in combination with everolimus, and unresectable hepatocellular carcinoma. Idelalisib An antineoplastic kinase inhibitor used to treat chronic lymphocytic leukemia (CLL), relapsed follicular B-cell non-Hodgkin lymphoma (FL), and relapsed small lymphocytic lymphoma (SLL). Osimertinib A tyrosine kinase inhibitor used in the treatment of certain types of non-small cell lung carcinoma. Riociguat A stimulator of soluble guanylate cyclase indicated for the management of persistent or recurrent chronic thromboembolic pulmonary hypertension and pulmonary arterial hypertension. Venetoclax A BCL-2 inhibitor used to treat chronic lymphocytic leukemia, small lymphocytic lymphoma, or acute myeloid leukemia. 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. Ombitasvir A direct acting antiviral agent used in combination with other antiviral agents for the treatment of Hepatitis C Virus (HCV) infections. Delafloxacin A fluoroquinolone antibiotic used to treat skin and skin structure infections. 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. Copanlisib A PI3K inhibitor used to treat relapsed follicular lymphoma in adults. Abemaciclib A medication used to treat HR+ HER2- advanced or metastatic breast cancer. Brigatinib An anaplastic lymphoma kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Dolutegravir An antiviral agent used for the treatment of HIV-1 infections in combination with other antiretroviral agents. 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. Ertugliflozin An SGLT2 inhibitor used to treat type 2 diabetes mellitus alone or in combination with other antidiabetic drugs. Testosterone cypionate An androgen used to treat low or absent testosterone. Testosterone enanthate An androgen used to treat low or absent testosterone. Testosterone undecanoate An androgen indicated for testosterone replacement therapy in adult males with primary hypogonadism and hypogonadotropic hypogonadism. 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. 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. Ritonavir An HIV protease inhibitor used in combination with other antivirals in the treatment of HIV infection. Lusutrombopag A medication used to treat thrombocytopenia in patients with chronic liver disease scheduled to have a procedure. Duvelisib An inhibitor of phosphatidylinositol 3-kinase delta and gamma used to treat relapsed or refractory chronic lymphocytic leukemia or small lymphocytic lymphoma. Sumatriptan A serotonin receptor agonist used to treat migraines and cluster headaches. Vincristine A vinca alkaloid used to treat acute leukemia, malignant lymphoma, Hodgkin's disease, acute erythraemia, and acute panmyelosis. Ezetimibe A cholesterol absorption inhibitor used to lower total cholesterol, LDL-C, Apo-B, and non-HDL-C in primary hyperlipidemia and familial cholesterolemia. Docetaxel A taxoid antineoplastic agent used in the treatment of various cancers, such as locally advanced or metastatic breast cancer, metastatic prostate cancer, gastric adenocarcinoma, and head and neck cancer. Talazoparib A poly-ADP ribose polymerase inhibitor used to treat HER2-, BRCA mutated locally advanced or metastatic breast cancer and HRR gene-mutated metastatic castration-resistant prostate cancer. Dacomitinib A medication used to treat non small cell lung cancer with EGFR exon 19 deletion of exon 21 L858R substitution. Larotrectinib A kinase inhibitor used to treat solid tumors with neurotrophic receptor tyrosine kinase gene fusion, are metastatic, high risk for surgery, or have no alternative treatments. Revefenacin An anticholinergic agent used to treat COPD. Rivaroxaban A factor Xa inhibitor used to treat deep vein thrombosis (DVT) and pulmonary embolism (PE). May also be used as thrombosis prophylaxis in specific situations. Fimasartan An angiotensin II receptor antagonist (ARB) used to treat hypertension and heart failure. Glasdegib A sonic hedgehog receptor inhibitor used to treat newly diagnosed acute myeloid leukemia in patients over 75 years who cannot receive intense chemotherapy. Pantoprazole A proton pump inhibitor used to treat erosive esophagitis, gastric acid hypersecretion, and to promote healing of tissue damage caused by gastric acid. Allopurinol A xanthine oxidase inhibitor used to reduce urinary and serum uric acid concentrations in patients with gout, recurrent calcium oxalate calculi, and various malignancies. 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. Tegaserod A serotonin-4 (5-HT4) receptor agonist indicated for the treatment of constipation predominant irritable bowel syndrome (IBS-C) specifically in women under the age of 65. There is currently no safety or efficacy data for use of tegaserol in men. Tenofovir alafenamide A nucleoside analog reverse transcriptase inhibitor used for the treatment of chronic hepatitis B virus infection in adults with compensated liver disease. Raloxifene A selective estrogen receptor modulator that is used to prevent and treat osteoporosis and reduce the risk of invasive breast cancer in high-risk postmenopausal women. 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... Cisplatin A platinum based chemotherapy agent used to treat various sarcomas, carcinomas, lymphomas, and germ cell tumors. Carboplatin A alkylating agent used to treat advanced ovarian cancer. Celecoxib An NSAID used to treat osteoarthritis, rheumatoid arthritis, acute pain, menstrual symptoms, and to reduce polyps is familial adenomatous polyposis. Donepezil An acetylcholinesterase inhibitor used to treat the behavioral and cognitive effects of Alzheimer's Disease and other types of dementia. Trastuzumab deruxtecan An antibody used to treat certain types of unresectable or metastatic HER2 positive breast cancer. 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. Ubrogepant An oral CGRP antagonist used in the acute treatment of migraine with or without aura. Tazemetostat A methyltransferase inhibitor indicated to treat patients 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection. Tezacaftor A medication used to treat homozygous or heterozygous F508del mutation cystic fibrosis. Rimegepant An oral CGRP receptor antagonist used for the acute treatment of migraines with or without aura in adults. Ozanimod A sphingosine 1-phosphate receptor modulator being studied to treat Multiple Sclerosis (MS) and inflammatory bowel disease (IBD). Prasterone A steroid formulated as a vaginal insert indicated for the treatment of moderate to severe dyspareunia associated with menopausal vulvar and vaginal atrophy. Selumetinib A MEK 1/2 inhibitor used in pediatric patients to treat neurofibromatosis type 1 (NF1) accompanied by symptomatic, inoperable plexiform neurofibromas (PN). Tucatinib A kinase inhibitor used to treat certain types of unresectable/metastatic HER-2 positive breast cancer. Pemigatinib A kinase inhibitor used to treat locally advanced or metastatic, unresectable cholangiocarcinoma in previously treated adult patients. Pralatrexate An antineoplastic agent used for the treatment of relapsed or refractory peripheral T-cell lymphoma. 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). Empagliflozin An SGLT2 inhibitor used to manage type 2 diabetes mellitus. Artesunate Artesunate is an artemesinin derivative indicated for the initial treatment of severe malaria. Fostemsavir An antiretroviral HIV-1 attachment inhibitor targeted against the gp120 subunit within the HIV-1 gp160 envelope glycoprotein. Risdiplam An oral mRNA splicing modifier used in the treatment of spinal muscular atrophy (SMA). Nifurtimox An antiparasitic drug used for the treatment of Chagas disease (Trypanosoma cruzi infection). Pralsetinib A RET receptor tyrosine kinase inhibitor for the treatment of metastatic RET-driven non-small cell lung cancer. Berotralstat An inhibitor of plasma kallikrein used for prophylaxis of angioedema attacks in patients with hereditary angioedema. Opicapone A catechol-O-methyltransferase inhibitor used as an adjunct treatment for Parkinson's Disease in adults currently receiving levodopa and a dopa decarboxylase inhibitor. Vericiguat A soluble guanylate cyclase stimulator used to reduce heart failure-related hospitalization and cardiovascular death in patients with chronic systolic heart failure. Cabotegravir An HIV-1 integrase inhibitor used for treatment and pre-exposure prophylaxis of HIV-1 infection. Trilaciclib A CDK4 and CDK6 inhibitor to reduce the risk of chemotherapy induced myelosuppression. Sulpiride A selective D2 dopamine receptor antagonist indicated to treat chronic and acute schizophrenia. Temozolomide An alkylating agent used to treat glioblastoma multiforme and refractory anaplastic astrocytoma. Amisulpride A dopamine D2 receptor antagonist used in the treatment of acute and chronic schizophrenia, and in the prevention and treatment of postoperative nausea and vomiting in adults. Infigratinib An FGFR inhibitor used to treat locally advanced or metastatic cholangiocarcinoma in adults with a fibroblast growth factor receptor 2 (FGFR2) rearrangement. Atogepant An oral CGRP antagonist used for the preventative therapy of episodic migraine headaches. 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. Deucravacitinib A TYK2 inhibitor being investigated as a treatment for psoriasis. Futibatinib A kinase inhibitor used to treat intrahepatic cholangiocarcinoma in previously treated adults. Linzagolix A selective gonadotropin-releasing hormone (GnRH) receptor antagonist used for the symptomatic treatment of uterine fibroids. Niraparib A poly-ADP ribose polymerase inhibitor used to treat recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer responding to platinum based chemotherapy. Pirtobrutinib A kinase inhibitor used to treat relapsed or refractory mantle cell lymphoma (MCL) after at least two lines of systemic therapy. Daprodustat A small-molecule hypoxia-inducible factor prolyl hydroxylase inhibitor used for the treatment of anemia in patients with chronic kidney disease. 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. Leniolisib A phosphoinositide 3-kinase-delta inhibitor that is used to treat activated phosphoinositide 3-kinase delta syndrome. Momelotinib A Janus Kinase inhibitor used to treat intermediate or high-risk myelofibrosis. Gefapixant A P2X3 receptor antagonist that reduces the cough reflex in patients with refractory or unexplained chronic cough. Binimetinib A medication used to treat metastatic melanoma with specific mutations. Aprocitentan An endothelin receptor antagonist used for the treatment of uncontrolled hypertension in patients inadequately controlled on other treatments. Resmetirom A thyroid hormone receptor-beta agonist used to treat noncirrhotic nonalcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis in adults. Elafibranor A peroxisome proliferator-activated receptor agonist used to treat primary biliary cholangitis in adults with intolerance of inadequate response to ursodeoxycholic acid. Ensifentrine A phosphodiesterase inhibitor used for the maintenance treatment of chronic obstructive pulmonary disease (COPD) in adults. Deuruxolitinib A Janus Kinase inhibitor used to treat severe alopecia areata in adults. Seladelpar A PPAR-delta agonist used to treat primary biliary cholangitis alone or in combination with ursodeoxycholic acid in adults. - Drugs & Drug Targets