Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
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Drug Drug Description Aminophylline A bronchodilator consisting of theophylline that is used for the treatment of bronchospasm due to asthma, emphysema and chronic bronchitis. Amiodarone A class III antiarrhythmic indicated for the treatment of recurrent hemodynamically unstable ventricular tachycardia and recurrent ventricular fibrillation. Argatroban A synthetic direct thrombin inhibitor used for the prevention and treatment of thrombosis related to heparin use. Busulfan An alkylating agent used to treat chronic myelogenous leukemia. Carbamazepine An anticonvulsant used to treat various types of seizures and pain resulting from trigeminal neuralgia. 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. Digitoxin A cardiac glycoside used in the treatment and management of congestive cardiac insufficiency, arrhythmias and heart failure. Dofetilide A class III antiarrhythmic drug used for the maintenance of normal sinus rhythm and cardioversion in cases of atrial fibrillation and atrial flutter. Everolimus A mammalian target of rapamycin (mTOR) kinase inhibitor used to treat various types of malignancies. Fosphenytoin An antiepileptic agent used for the management of generalized convulsive status epilepticus and prevention and treatment of seizures occurring during neurosurgery. Phenprocoumon An anticoagulant drug used for the prevention of thrombosis. Pimozide An antipsychotic used to manage debilitating motor and phonic tics in patients with Tourette's Disorder. Quinidine A medication used to restore normal sinus rhythm, treat atrial fibrillation and flutter, and treat ventricular arrhythmias. Sirolimus An mTOR inhibitor immunosuppressant used to prevent organ transplant rejections, treat lymphangioleiomyomatosis, and treat adults with perivascular epithelioid cell tumors. Tacrolimus A calcineurin inhibitor used to prevent organ transplant rejection and to treat moderate to severe atopic dermatitis. Temsirolimus A antineoplastic agent used in the treatment of renal cell carcinoma (RCC) that works by inhibiting mTOR. Theophylline A xanthine used to manage the symptoms of asthma, COPD, and other lung conditions caused by reversible airflow obstruction. Tianeptine An atypical tricyclic antidepressant with antidepressant and anxiolytic effects primarily used to treat major depressive disorder. Warfarin A vitamin K antagonist used to treat venous thromboembolism, pulmonary embolism, thromboembolism with atrial fibrillation, thromboembolism with cardiac valve replacement, and thromboembolic events post myocardial infarction. Dronedarone An antiarrhythmic agent used in the reduce the risk of hospitalization in patients with paroxysmal or persistent atrial fibrillation. Dasatinib A tyrosine kinase inhibitor used for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia or chronic myeloid leukemia. Paclitaxel A taxoid chemotherapeutic agent used as first-line and subsequent therapy for the treatment of advanced carcinoma of the ovary, and other various cancers including breast and lung cancer. Acenocoumarol An anticoagulant drug used in the prevention of thromboembolic diseases in infarction and transient ischemic attacks, as well as management of deep vein thrombosis and myocardial infarction. 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. Zanubrutinib A kinase inhibitor used to treat mantle cell lymphoma, a type of B-cell non-Hodgkin lymphoma, in adults who previously received therapy. Vinorelbine A vinca alkaloid used in the treatment of metastatic non-small cell lung carcinoma (NSLC) and in conjunction with other drugs in locally advanced NSCLC. Acalabrutinib A Bruton tyrosine kinase inhibitor used to treat mantle cell lymphoma, chronic lymphocytic leukemia, and small lymphocytic lymphoma. Vinflunine A vinca alkaloid used to treat advanced or metastatic transitional cell carcinoma of the urothelial tract after a platinum containing treatment has failed. Cytarabine A pyrimidine nucleoside analogue used to treat acute non-lymphocytic leukemia, lymphocytic leukemia, and the blast phase of chronic myelocytic leukemia. Vincristine A vinca alkaloid used to treat acute leukemia, malignant lymphoma, Hodgkin's disease, acute erythraemia, and acute panmyelosis. 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. Alectinib A kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Venetoclax A BCL-2 inhibitor used to treat chronic lymphocytic leukemia, small lymphocytic lymphoma, or acute myeloid leukemia. 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. Vandetanib An antineoplastic kinase inhibitor used to treat symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. 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... Daunorubicin An anthracycline aminoglycoside used to induce remission of nonlymphocytic leukemia and acute lymphocytic leukemia. 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. Doxorubicin A medication used to treat various cancers, including AIDS-associated Kaposi's Sarcoma and metastatic cancers. Trabectedin An alkylating agent approved for the treatment of unresectable or metastatic soft tissue sarcoma (liposarcoma or leiomyosarcoma). Thiotepa An alkylating agent used to prevent graft rejection in stem cell transplantation and to treat a variety of malignancies including certain types of adenocarcinoma and superficial bladder carcinomas. Enasidenib An isocitrate dehydrogenase-2 inhibitor used to treat relapsed or refractory acute myeloid leukemia with an isocitrate dehydrogenase-2 mutation. Entrectinib Entrectinib is indicated for the treatment of metastatic ROS1-positive non-small cell lung cancer in adults. Entrectinib is also indicated in adults and children over 12 years old for the treatment... Erlotinib An EGFR tyrosine kinase inhibitor used to treat certain small cell lung cancers or advanced metastatic pancreatic cancers. Axitinib An oral VEGFR and kinase inhibitor used for the treatment of advanced renal cell carcinoma after failure of one prior systemic therapy. Belinostat A histone deacetylase (HDAC) inhibitor used for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). Etoposide A podophyllotoxin derivative used to treat testicular and small cell lung tumors. Teniposide A cytotoxic drug used as an adjunct for chemotherapy induction in the treatment of refractory childhood acute lymphoblastic leukemia. Ixabepilone A microtubule inhibitor administered in combination with capecitabine or alone in the treatment of metastatic or locally advanced breast cancer that has shown inadequate response to taxanes and anthracyclines. 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). Ifosfamide An alkylating and immunosuppressive agent used in chemotherapy for the treatment of cancers, including testicular cancer, ovarian cancer, cervical cancer, osteocarcinoma, bladder cancer, small cell lung cancer, and non-Hodgkin's lymphoma. Ixazomib A monoclonal antibody used with other medications to treat multiple myeloma in patients who have received one other therapy already. Midostaurin An antineoplastic agent used to treat high-risk acute myeloid leukemia (AML) with specific mutations, aggressive systemic mastocytosis (ASM), systemic mastocytosis with associated hematologic neoplasm (SM-AHN), or mast cell leukemia (MCL). Bortezomib A proteasome inhibitor used to treat multiple myeloma in patients who have not been successfully treated with at least two previous therapies. 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. Bosutinib An antineoplastic agent used for the treatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) in adults with inadequate clinical response to other treatments. Olaparib A poly (ADP-ribose) polymerase (PARP) inhibitor used to treat ovarian cancer, breast cancer, pancreatic cancer, and prostate cancer. Brentuximab vedotin A CD30-directed antibody-drug conjugate used to treat various types of lymphoma. Brigatinib An anaplastic lymphoma kinase inhibitor used to treat anaplastic lymphoma kinase positive metastatic non small cell lung cancer. Neratinib A protein kinase inhibitor used to treat breast cancer that over expresses the HER2 receptor. 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). 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. 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. Panobinostat A non-selective histone deacetylase inhibitor used to treat multiple myeloma in combination with other antineoplastic agents. Cabergoline A dopamine receptor agonist used for the treatment of hyperprolactinemic conditions due to various causes. Pazopanib An antineoplastic agent used in the treatment of advanced renal cell cancer and advanced soft tissue sarcoma in patients with prior chemotherapy. Cabozantinib A tyrosine kinase inhibitor used to treat advanced renal cell carcinoma, hepatocellular carcinoma, and medullary thyroid cancer. 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. Sorafenib A kinase inhibitor used to treat unresectable liver carcinoma, advanced renal carcinoma, and differentiated thyroid carcinoma. Sonidegib An antineoplastic agent used for the treatment of locally advanced recurrent basal cell carcinoma (BCC) following surgery and radiation therapy, or in cases where surgery or radiation therapy are not appropriate. Ponatinib A kinase inhibitor used to treat patients with various types of chronic myeloid leukemia (CML). Ruxolitinib A kinase inhibitor used to treat various types of myelofibrosis, polycythemia vera in patients who have not responded to or cannot tolerate hydroxyurea, and to treat graft-versus-host disease in cases that are refractory to steroid treatment. Ceritinib An antineoplastic kinase inhibitor used to treat anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) in patients with inadequate clinical response or intolerance to crizotinib. Vindesine A vinca alkaloid derived from vinblastine used for various types of malignancies, but mainly acute lymphocytic leukemia (ALL). Romidepsin A histone deacetylase (HDAC) inhibitor used to treat cutaneous T-cell lymphoma. Cobimetinib An antineoplastic agent and selective inhibitor of the mitogen-activated extracellular kinase (MEK) pathway used to treat unresectable or metastatic melanoma. Rucaparib A poly (ADP-ribose) polymerase (PARP) inhibitor used to treat recurrent ovarian and prostate cancers in previously treated adults. Ribociclib A kinase inhibitor used to treat HR+, HER2- advanced or metastatic breast cancer. Dabrafenib A kinase inhibitor used to treat patients with specific types of melanoma, non-small cell lung cancer, and thyroid cancer. Copanlisib A medication used to treat relapsed follicular lymphoma who have attempted at least two other treatments. Dacomitinib A medication used to treat non small cell lung cancer with EGFR exon 19 deletion of exon 21 L858R substitution. Crizotinib A receptor tyrosine kinase inhibitor used to treat metastatic non-small cell lung cancer (NSCLC) where the tumors have been confirmed to be anaplastic lymphoma kinase (ALK), or ROS1-positive. Erdafitinib A fibroblast growth factor receptor tyrosine kinase inhibitor used to treat locally advanced or metastatic urothelial carcinoma. Ivosidenib An isocitrate dehydrogenase-1 inhibitor used to treat acute myeloid leukemia and cholangiocarcinoma in adults with a susceptible IDH1 mutation. Regorafenib A kinase inhibitor used to treat patients with metastatic colorectal cancer, unresectable, locally advanced, or metastatic gastrointestinal stromal tumors, and hepatocellular carcinoma. Dihydroergotamine An ergot alkaloid used in the acute treatment of migraine headache and cluster headache. Astemizole A second generation antihistamine used to treat allergy symptoms. Ergotamine An alpha-1 selective adrenergic agonist vasoconstrictor used to treat migraines with or without aura and cluster headaches. Irinotecan An antineoplastic enzyme inhibitor used to treat metastatic carcinoma of the colon or rectum. Conivaptan An antidiuretic hormone inhibitor used to raise serum sodium levels. Levacetylmethadol For the treatment and management of opiate dependence. It is sometimes used to treat severe pain in terminal patients. Amitriptyline A tricyclic antidepressant indicated in the treatment of depressive illness, either endogenous or psychotic, and to relieve depression associated anxiety. Nortriptyline A tricyclic antidepressant used in the treatment of depression. Cyclophosphamide A nitrogen mustard used to treat lymphomas, myelomas, leukemia, mycosis fungoides, neuroblastoma, ovarian adenocarcinoma, retinoblastoma, and breast carcinoma. Tolvaptan A selective vasopressin V2-receptor antagonist to slow kidney function decline in patients at risk for rapidly progressing autosomal dominant polycystic kidney disease (ADPKD). Also used to treat hypervolemic and euvolemic hyponatremia. Phenytoin An anticonvulsant drug used in the prophylaxis and control of various types of seizures. Bicalutamide An androgen receptor inhibitor used to treat Stage D2 metastatic carcinoma of the prostate. Clomipramine A tricyclic antidepressant used in the treatment of obsessive-compulsive disorder and disorders with an obsessive-compulsive component, such as depression, schizophrenia, and Tourette’s disorder. Imipramine A tricyclic antidepressant indicated for the treatment of depression and to reduce childhood enuresis. 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. Clonidine An alpha-2 adrenergic agonist used to treat hypertension and severe cancer pain, among other conditions, and to treat withdrawal symptoms from various substances. It is also used to aid in the diagnosis of pheochromocytoma and to prevent migraines. Lomitapide A microsomal triglyceride transfer protein inhibitor used to lower cholesterol associated with homozygous familial hypercholesterolemia (HoFH), reducing risk of cardiovascular events such as myocardial infarction and stroke. Pomalidomide A thalidomide analogue used in combination with dexamethasone to treat patients with multiple myeloma. Trastuzumab emtansine An antineoplastic agent and antibody-drug conjugate used to treat HER2-overexpressing breast cancer. Osimertinib A tyrosine kinase inhibitor used in the treatment of certain types of non-small cell lung carcinoma. Abemaciclib A medication used to treat HR+ HER2- advanced or metastatic breast cancer. Baricitinib A Janus kinase inhibitor used to treat moderate to severe rheumatoid arthritis that has responded poorly to at least one TNF antagonist. Siponimod A medication used to treat relapsing multiple sclerosis. Mycophenolic acid An immunosuppressant used to prevent organ transplant rejections. Trametinib A kinase inhibitor used alone or in combination with dabrafenib to treat patients with cancers with specific BRAF mutations, such as melanoma and non-small cell lung cancer.
- Drugs & Drug Targets