OATP1B1/SLCO1B1 Inhibitors
- Name
- OATP1B1/SLCO1B1 Inhibitors
- Accession Number
- DBCAT003931
- Description
Not Available
- Drugs
Drug Drug Description 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... Cholic Acid A bile acid used for the treatment of bile acid synthesis disorders due to single enzyme defects and as an adjunctive treatment of peroxisomal disorders with disrupted liver function. Rifampin An antibiotic used alone or in combination with other antimicrobial drugs to treat tuberculosis and asymptomatic carriers of Neisseria meningitidis. 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. Estrone An estrogen used to treat perimenopausal and postmenopausal symptoms. 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. Saquinavir An HIV protease inhibitor used in combination with other antiretroviral agents for the treatment of HIV-1 with advanced immunodeficiency. Ritonavir An HIV protease inhibitor used in combination with other antivirals in the treatment of HIV infection. Nelfinavir A viral protease inhibitor used in the treatment of HIV infection. Indinavir A protease inhibitor used to treat HIV infection. Hyperforin Hyperforin is a phytochemical generated by the plants of the Hypericum family. One of the most important members of this family, due to its medical properties, is Hypericum perforatum, also... 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. Quinidine A medication used to restore normal sinus rhythm, treat atrial fibrillation and flutter, and treat ventricular arrhythmias. Levocarnitine A quaternary ammonium compound used to treat carnitine deficiency or to stimulate gastric and pancreatic secretions in hyperlipoproteinemia. Sirolimus An mTOR inhibitor immunosuppressant used to prevent organ transplant rejections, treat lymphangioleiomyomatosis, and treat adults with perivascular epithelioid cell tumors. Simvastatin An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular events including myocardial infarction and stroke. Lovastatin An HMG-CoA reductase inhibitor used to lower LDL cholesterol and reduce the risk of cardiovascular disease and associated conditions, including myocardial infarction and stroke. Atorvastatin An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke. Troglitazone For the treatment of Type II diabetes mellitus. It is used alone or in combination with a sulfonylurea, metformin, or insulin as an adjunct to diet and exercise. Rosiglitazone A thiazolidinedione indicated as an adjunct to diet and exercise to maintain glycemic control in type 2 diabetes. Pioglitazone A thiazolidinedione used adjunctively with diet and exercise to normalize glycemic levels in adults with type 2 diabetes mellitus. Irinotecan A topoisomerase inhibitor used to treat metastatic carcinoma of the colon or rectum and pancreatic adenocarcinoma. Caspofungin An echinocandin used to treat a variety of fungal infections. Bezafibrate A lipid-lowering fibrate used in the management of primary and secondary hyperlipidaemia, when there is a lack of clinical improvement following lifestyle modifications or correction of the underlying disorder. Gemfibrozil A lipid regulator that is used in the reduction of serum triglyceride levels in high-risk patients with hyperlipidemia. Acetylcysteine A medication that can be used as a mucolytic in patients with certain lung conditions and as an antidote for acetaminophen overdose. Verapamil A non-dihydropyridine calcium channel blocker used in the treatment of angina, arrhythmia, and hypertension. Pantoprazole A proton pump inhibitor used to treat erosive esophagitis, gastric acid hypersecretion, and to promote healing of tissue damage caused by gastric acid. Digoxin A cardiac glycoside used in the treatment of mild to moderate heart failure and for ventricular response rate control in chronic atrial fibrillation. Eltrombopag A thrombopoietin receptor agonist used to treat thrombocytopenia or aplastic anemia associated with various etiologies. Pazopanib An antineoplastic agent used in the treatment of advanced renal cell cancer and advanced soft tissue sarcoma in patients with prior chemotherapy. Cabazitaxel An antineoplastic agent used in combination with corticosteroids to treat metastatic castration-resistant prostate cancer in patients 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). Dabrafenib A kinase inhibitor used to treat patients with specific types of melanoma, non-small cell lung cancer, and thyroid cancer. 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. Posizolid For the treatment of gram-positive infections, including multiresistant strains. 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). Eluxadoline A mixed mu-opioid receptor agonist used to treat irritable bowel syndrome with diarrhea. Sacubitril A neprilysin inhibitor used in combination with valsartan as an adjunct to reduce the risk of cardiovascular death and hospitalization for heart failure in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction. Daclatasvir 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. Telaprevir An NS3/4A viral protease inhibitor used in combination with other antivirals for the curative treatment of chronic Hepatitis C Virus infections. Lobeglitazone Lobeglitazone was approved by the Ministry of Food and Drug Safety (South Korea) in 2013, and is being monitored by postmarketing surveillance until 2019. Lobeglitazone is not approved for use... 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. Rucaparib A poly (ADP-ribose) polymerase (PARP) inhibitor used to treat recurrent ovarian and prostate cancers in previously treated adults. 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. Atazanavir An antiviral protease inhibitor used in combination with other antiretrovirals for the treatment of HIV. Erythromycin A macrolide antibiotic used to treat and prevent a variety of bacterial infections. Cerivastatin A statin (or HMG CoA reductase inhibitor) used with dietary changes to decrease lipid levels and reduce the risk of cardiovascular events. Ouabain For the treatment of atrial fibrillation and flutter and heart failure Valsartan An angiotensin-receptor blocker used to manage hypertension alone or in combination with other antihypertensive agents and to manage heart failure in patients who are intolerant to ACE inhibitors. Fluvastatin An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke. Pitavastatin An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke. Axitinib An oral VEGFR and kinase inhibitor used for the treatment of advanced renal cell carcinoma after failure of one prior systemic therapy. Rosuvastatin An HMG-CoA reductase inhibitor used to lower lipid levels and reduce the risk of cardiovascular disease including myocardial infarction and stroke. Paritaprevir A direct acting antiviral agent used in combination with other antiviral agents for the treatment of Hepatitis C Virus (HCV) infections. Dipyridamole A phosphodiesterase inhibitor used to prevent postoperative thromboembolic events. Vincristine A vinca alkaloid used to treat acute leukemia, malignant lymphoma, Hodgkin's disease, acute erythraemia, and acute panmyelosis. Benzbromarone A uricosuric agent which is taken daily for the prevention of gout flares. Cholecystokinin For use as a diagnostic aid for evaluation of gallbladder disorders. It is also used in conjunction with secretin in pancreatic insufficiency . 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. Genistein Currently Genistein is being studied in clinical trials as a treatment for prostate cancer. Ivermectin An anti parasite medication used to treat head lice, onchocerciasis, strongyloidiasis, ascariasis, trichuriasis, and enterobiasis. Nifedipine A dihydropyridine calcium channel blocker indicated for the management of several subtypes of angina pectoris, and hypertension. Novobiocin For the treatment of infections due to staphylococci and other susceptible organisms Nystatin A polyene ionophore antifungal used to treat cutaneous, mucocutaneous, and gastrointestinal mycotic infections, particularly those caused by Candida species. Valspodar Valspodar has been used in trials studying the treatment of Cancer, Sarcoma, Leukemia, Lymphoma, and Breast Cancer, among others. Reserpine For the treatment of hypertension Silibinin A flavonolignan with hepatoprotective effects used to treat toxic liver damage and as an adjunct in the management of chronic conditions such as cirrhosis and hepatitis. Sulfasalazine A salicylate used to treat Crohn's disease, ulcerative colitis, and rheumatoid arthritis. Tipranavir A protease inhibitor used to treat HIV-1 resistant to more than 1 protease inhibitor. Lopinavir An HIV-1 protease inhibitor used in combination with ritonavir to treat human immunodeficiency virus (HIV) infection. Darunavir A HIV protease inhibitor used in the treatment of human immunodeficiency virus (HIV) infection in patients with history of prior antiretroviral therapies. Indomethacin A nonsteroidal anti-inflammatory (NSAID) used for symptomatic management of chronic musculoskeletal pain conditions and to induce closure of a hemodynamically significant patent ductus arteriosus in premature infants. Amprenavir A protease inhibitor used to treat HIV infection. Diclofenac An NSAID used to treat the signs and symptoms of osteoarthritis and rheumatoid arthritis. Quercetin A natural flavonoid found in foods and natural supplement products. Nicardipine A calcium channel blocker used for the short-term treatment of hypertension and chronic stable angina. Progesterone A hormone used for a variety of functions, including contraception, control of abnormal uterine bleeding, maintenance of pregnancy, and prevention of endometrial hyperplasia. Vinblastine A vinca alkaloid used to treat breast cancer, testicular cancer, neuroblastoma, Hodgkin's and non-Hodgkins lymphoma, mycosis fungoides, histiocytosis, and Kaposi's sarcoma. Quinine An alkaloid used to treat uncomplicated Plasmodium falciparum malaria. Ketoconazole A broad spectrum antifungal used to treat seborrheic dermatitis and fungal skin infections. Candesartan An angiotensin-receptor blocker indicated in the treatment of hypertension. 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. Telithromycin An ketolide used to treat community acquired pneumonia of mild to moderate severity. Everolimus A mammalian target of rapamycin (mTOR) kinase inhibitor used to treat various types of malignancies. Sildenafil A phosphodiesterase inhibitor used for the treatment of erectile dysfunction. Tacrolimus A calcineurin inhibitor used to prevent organ transplant rejection and to treat moderate to severe atopic dermatitis. Sorafenib A kinase inhibitor used to treat unresectable liver carcinoma, advanced renal carcinoma, and differentiated thyroid carcinoma. 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. Asunaprevir An NS3 protease inhibitor used to treat hepatitis C genotype 1b. Fluticasone A corticosteroid indicated in the treatment of corticosteroid responsive dermatoses, asthma, and COPD. Fluticasone furoate An inhaled corticosteroid that can be used as maintenance treatment of asthma and/or chronic obstructive pulmonary disease (COPD) depending on the product. Also available as a nasal spray to manage symptoms of allergic rhinitis. Fluticasone propionate A glucocorticoid used to treat asthma, inflammatory pruritic dermatoses, and nonallergic rhinitis. 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. Dovitinib Investigated for use/treatment in multiple myeloma and solid tumors. Teriflunomide A pyrimidine synthesis inhibitor with anti-inflammatory and immunomodulatory properties used to treat patients with the relapsing-remitting form of multiple sclerosis. Fusidic acid A topical antibacterial agent used to prevent and treat mild to moderate skin infections caused by susceptible bacteria. Roxithromycin An antibiotic used to treat a variety of susceptible bacterial infections. Rifamycin An antibacterial used to treat traveler's diarrhea. Venetoclax A BCL-2 inhibitor used to treat chronic lymphocytic leukemia, small lymphocytic lymphoma, or acute myeloid leukemia. Mifepristone A cortisol receptor blocker used to treat Cushing's syndrome, and to terminate pregnancies up to 70 days gestation. Clotrimazole A topical broad-spectrum antifungal agent used for the treatment of a wide variety of dermatophyte infections and candidiasis. Beclomethasone dipropionate An inhaled corticosteroid used as maintenance treatment in the prophylaxis of asthma attacks. Pexidartinib An antitumor agent that is used for the treatment of rare disease tenosynovial giant cell tumors (TGCT) by inhibiting colony-stimulating factor 1 and its receptor. Fedratinib Fedratinib is indicated for the treatment of adult patients with intermediate-2 or high-risk primary or secondary (post-polycythemia vera or post-essential thrombocythemia) myelofibrosis.[L8090,L47016] Istradefylline A selective adenoside A2A receptor antagonist indicated in adjunct to levodopa and carbidopa for the treatment of Parkinson's Disease. Dronedarone An antiarrhythmic agent used in the reduce the risk of hospitalization in patients with paroxysmal or persistent atrial fibrillation. Elexacaftor A small molecule CFTR corrector used in combination with tezacaftor and ivacaftor for the treatment of cystic fibrosis patients with one F508del-CFTR mutation. 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. Clarithromycin A macrolide antibiotic used for the treatment of a wide variety of bacterial infections such as acute otitis, pharyngitis, tonsillitis, respiratory tract infections, uncomplicated skin infections, and helicobacter pylori infection. Darolutamide An androgen receptor antagonist used for castration-resistant, non-metastatic prostate cancer and metastatic hormone-sensitive prostate cancer. Rimegepant An oral CGRP receptor antagonist used for the acute treatment of migraines with or without aura in adults. Osilodrostat An oral inhibitor of cortisol synthesis used to treat Cushing's disease by normalizing hypercortisolism. Bempedoic acid A drug used in conjunction with lifestyle modification and/or other agents for the treatment of refractory hypercholesterolemia. Remdesivir A nucleoside analog used to treat RNA virus infections including COVID-19. Artesunate Artesunate is an artemesinin derivative indicated for the initial treatment of severe malaria. Lurbinectedin A chemotherapeutic DNA alkylating agent used in the treatment of metastatic small-cell lung cancer. 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. Tirbanibulin A tyrosine kinase and tubulin inhibitor used to treat actinic keratosis on the face or scalp. 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. Diosmin A citrus flavonoid medication used to support vascular health. Infigratinib An FGFR inhibitor used to treat locally advanced or metastatic cholangiocarcinoma in adults with a fibroblast growth factor receptor 2 (FGFR2) rearrangement. 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). Fexinidazole An orally bioavailable 2-substituted 5-nitroimidazole used to treat early- and late-stage human African trypanosomiasis caused by Trypanosoma brucei gambiense. Atogepant An oral CGRP antagonist used for the preventative therapy of episodic migraine headaches. Romidepsin A histone deacetylase (HDAC) inhibitor used to treat cutaneous T-cell lymphoma. 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. Sotagliflozin An orally administered dual SGLT1/2 inhibitor used alongside insulin to improve glycemic control in patients with type 1 diabetes mellitus. Padeliporfin A vascular-acting photosensitizer used to treat low-risk prostate cancer in adults. Roxadustat A hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor used to treat symptomatic anemia associated with chronic kidney disease. Olaparib A poly (ADP-ribose) polymerase (PARP) inhibitor used to treat ovarian cancer, breast cancer, pancreatic cancer, and prostate cancer. Linzagolix A selective gonadotropin-releasing hormone (GnRH) receptor antagonist used for the symptomatic treatment of uterine fibroids. 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. Daprodustat A small-molecule hypoxia-inducible factor prolyl hydroxylase inhibitor used for the treatment of anemia in patients with chronic kidney disease. Trofinetide A drug used to treat Rett syndrome in children and adults. Leniolisib A phosphoinositide 3-kinase-delta inhibitor that is used to treat activated phosphoinositide 3-kinase delta syndrome. Tezacaftor A medication used to treat homozygous or heterozygous F508del mutation cystic fibrosis. Letermovir An antiviral medication used for prophylaxis in adult transplant recipients at risk of cytomegalovirus (CMV) infection and disease. Abiraterone An antiandrogen used in the treatment of metastatic castration-resistant prostate cancer and metastatic high-risk castration-sensitive prostate cancer. Palovarotene A selective agonist of retinoic acid receptor gamma (RARγ) used to reduce heterotopic ossification in patients with Fibrodysplasia Ossificans Progressiva (FOP). Encorafenib A kinase inhibitor used to treat unresectable or metastatic melanoma with specific mutations. Capivasertib A serine/threonine kinase inhibitor used to treat hormone receptor-positive, HER2-negative, locally advanced or metastatic breast cancer Repotrectinib A tyrosine kinase inhibitor used to treat locally active or metastatic non-small cell lung cancer Resmetirom A thyroid hormone receptor-beta agonist used to treat noncirrhotic nonalcoholic steatohepatitis (NASH) with moderate to advanced liver fibrosis in adults. Ceftobiprole A broad spectrum 5th-generation cephalosporin antibacterial indicated for certain kinds of pneumonia, bacteremia, and skin and skin structure infections, including those caused by MRSA. Ceftobiprole medocaril A broad spectrum 5th-generation cephalosporin antibacterial indicated for certain kinds of pneumonia, bacteremia, and skin and skin structure infections, including those caused by MRSA. Imetelstat A human telomerase inhibitor used to treat myelodysplastic syndromes in patients with transfusion-dependent anemia. - Drugs & Drug Targets